Medications that affect people psychologically are called psychoactive drugs. They are often helpful in treating depression, anxiety, insomnia, and other psychological complications that may accompany HIV infection. Psychoactive drugs don't affect the underlying causes of these disorders, but they can provide symptomatic relief to allow people to live more normal lives.
Most of the drugs covered in this section have numerous effects on the nervous system, but each is usually reserved to treat one of the following conditions: anxiety, depression, insomnia, psychosis, or mania.
Anxiety can be defined as persistent nervousness, tension, or panic caused by stress or other psychological causes. Antianxiety drugs (also known as minor tranquilizers) are used to promote relaxation or reduce the physical symptoms of anxiety. Benzodiazepines are a class of psychoactive drugs used to treat anxiety and insomnia. They depress the central nervous system, causing relaxation and sedation. A class of drugs called beta-blockers reduce the shaking or palpitations that may occur when people panic in highly stressful situations, such as job interviews or speaking in public. Other drugs used to treat anxiety include buspirone, some antidepressants, and in special cases, barbiturates.
Everyone feels depressed at times, but when it is prolonged and starts interfering with daily life, support, professional help, and/or psychoactive medications may be appropriate.
Depression is thought to be caused by a reduction in the level of certain chemicals, called neurotransmitters, in the brain. Antidepressants increase the levels of these chemicals in the spaces (called synapses) between nerve cells in the brain. Tricyclic antidepressants (e.g., amoxapine) and serotonin reuptake inhibitors (e.g., fluoxetine or sertraline) prevent cells from absorbing certain neurotransmitters, which increases their levels in the synapses. Monoamine oxidase (MAO) inhibitors increase neurotransmitter levels by interfering with the enzymes that break them down. It takes some time before antidepressants are effective. Ten to fourteen days may elapse after the initial dose before an effect is observable, and it may be six to eight weeks before they are fully effective.
Antidepressants often have severe side effects. MAO inhibitors in particular must be used with caution because they deactivate enzymes in the body that break down chemicals found in many foods, such as meat, cheese, yeast extracts, and red wine. Eating these foods while taking an MAO inhibitor can cause a dramatic rise in blood pressure.
Insomnia has many causes, including anxiety and depression. When the cause is known and can be treated, sleep patterns generally return to normal. When the insomnia is persistent, sleeping drugs may be appropriate.
Most sleeping pills cause sedation by depressing the central nervous system. The most commonly used sleeping medications are the benzodiazepines, but barbiturates and some sedating antihistamines or antidepressant drugs are used as well.
The sleep induced by drugs is not the same as natural sleep. The drugs suppress brain activity and dreaming, and many have a "hangover" effect the next day. Because the drugs are often habit-forming and can cause withdrawal symptoms, they are usually recommended for short-term use only.
Psychosis is a condition in which a person may not be able to think clearly, recognize reality, or act rationally. The precise cause is often unknown, but stress, drug use, heredity, brain injury, or neurological disease may be involved. Drug treatment is usually reserved for when the psychosis is prolonged and interferes with normal life.
Most antipsychosis drugs, including a commonly used class called phenothiazines, work by inhibiting the activity of a neurotransmitter called dopamine. Dopamine is released in excess concentrations in psychosis. Antipsychotics reduce the effect of dopamine by blocking the nerve cell receptors that respond to the chemical.
Antipsychotics also interfere with the activity of another neurotransmitter, called acetylcholine, and after long-term use can cause involuntary muscle movements of the face and hands and other symptoms that resemble Parkinson's disease. These side effects may not be reversible when the drug is stopped.
Mania (exaggerated euphoria or elation) is a type of psychosis that can be caused by a number of medical problems or as a side effects of certain drugs, such as the amphetamines, cocaine, and steroids. The most effective treatment is to remove the cause, if possible. Where the cause is unknown, drug treatment may be appropriate. Rapid or wild mood swings, with peaks of mania and troughs of depression, are usually treated with lithium, a drug that reduces the intensity of the mania and reduces the frequency of mood swings. Acute mania may be treated with haloperidol or phenothiazine drugs including thioridazine, fluphenazine, perphenazine, and trifluoperazine.
The following drugs, listed by class, are profiled in this section:
Alprazolam
Brand Name (Manufacturer)
Xanax (Upjohn)
Type of Drug
Psychoactive-antianxiety agent
Used For
Alprazolam is used primarily for short-term relief of anxiety. It is also effective for treating anxiety associated with depression and for the treatment of panic disorders.
General Information
Alprazolam belongs to a class of psychoactive drugs called benzodiazepines. Benzodiazepines are the most commonly used antianxiety drugs because they are fairly safe; they rapidly reduce the symptoms of anxiety, and they don't have to be taken on an ongoing basis in order to be effective. All benzodiazepines cause dose-related suppression of the central nervous system, varying from slight impairment to hypnosis.
Alprazolam is available in tablets for oral administration.
Treatment
In general, the minimum effective dose of the drug should be used. For treatment of symptoms of anxiety, 0.25 to 0.5 mg taken three to four times a day is the usual starting dosage. The dose may be increased, if necessary, at intervals of three to four days. The maximum daily dose is 4 mg.
When discontinuing the drug, it is recommended that the daily dose be decreased by no more than 0.5 mg every three days to avoid withdrawal symptoms. Some people may require an even slower dose reduction.
Treatment of panic is usually started at 0.5 mg taken three times a day, but may require more than 4 mg per day. In clinical studies, participants have used dosages up to 10 mg per day, but the appropriate dose must be determined for each individual by starting at a low dose and slowly increasing until the desired effect is observed (as long as the drug is tolerated without serious side effects). After a period free of attacks, a carefully controlled dosage reduction and weaning may be attempted.
Cautions and Warnings
Alprazolam should not be used by people with a known allergy to it or people who have glaucoma. The drug depresses the central nervous system, so it may not be appropriate to operate heavy machinery or drive a motor vehicle when taking it.
Like other benzodiazepines, alprazolam can be dangerous when taken with alcohol. Alcohol intensifies the depressive effect of benzodiazepines.
All benzodiazepines are habit-forming, and alprazolam is particularly likely to be addictive, even after relatively short-term use at the recommended doses. This usually means that, over time, increasing doses are needed to achieve the same effect. This differs from person to person, but in general, after several months of use, addiction is common. The risk of dependency seems to be higher in people treated with relatively high doses (greater than 4 mg per day) and in those treated for more than eight to twelve weeks. Because treatment of panic disorder often requires doses over 4 mg per day, the risk of dependence among these people is greater than that for those treated for anxiety. Withdrawal reactions may occur when dosages of the drug are reduced for any reason.
Early-morning anxiety, a type of withdrawal reaction that occurs in between doses, has been observed in people with panic disorder taking prescribed amounts of the drug.
Side Effects
Side effects of the drug usually appear at the beginning of therapy and usually disappear upon continued medication. Most often the side effects include drowsiness, light-headedness, or dizziness. More serious side effects, although reported rarely, are seizures, hallucinations, taste alteration, double vision, liver toxicity, and jaundice.
Withdrawal symptoms include insomnia, headache, anxiety, fatigue, irritability, difficulty thinking or remembering, nausea, vomiting, diarrhea, weight loss, sweating, and rapid heartbeat.
Pregnancy/Breast-Feeding
Benzodiazepines, including alprazolam, can cause birth defects when taken during pregnancy. Taken late in pregnancy, they may increase the risk that the baby will be born dependent on the drug. Pregnant women should avoid using alprazolam.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Benzodiazepines are excreted in human milk and can cause serious effects in infants. Because of the potential toxicity of the drug, women should consider alternatives to breast-feeding while taking the drug.
Use In Children
The safety and effectiveness of alprazolam in children under eighteen have not been studied.
Use in the Elderly
Elderly or debilitated people may be particularly susceptible to side effects of alprazolam. The starting dose for them is usually 0.25 mg two or three times a day. The dose may be gradually increased if needed and tolerated.
Drug Interactions
Oral contraceptives and cimetidine may increase the concentration of alprazolam in the blood and potentially increase the risk of side effects. Benzodiazepines intensify the central nervous system depression caused by other psychoactive medications, anticonvulsants, antihistamines, and alcohol.
Alprazolam increases levels of imipramine and desipramine in the body, potentially increasing the risk of side effects.
Food Interactions
Alprazolam is absorbed into the body most effectively when taken on an empty stomach, but it can be taken with food if necessary.
Other drugs used for similar conditions
Many different benzodiazepines are available by prescription. They include lorazepam, diazepam, chlordiazepoxide, oxazepam, temazepam, flurazepam, and triazolam. The drugs differ somewhat in the side effects they produce, their potencies, the time it takes for them to work, and the tendency for them to cause withdrawal symptoms.
Buspirone is an antianxiety medication that is not part of the benzodiazepine class. It is not addictive or sedating and has less tendency to slow down mental and physical reactions. On the other hand, it is not effective for many people.
Benztropine
Brand Name (Manufacturer)
Cogentin (Merck)
Type of Drug
Psychoactive-muscle relaxant
Used For
Benztropine is used for the treatment of the symptoms of Parkinson's disease. It is also used to prevent or treat the muscle spasms caused by certain drugs used to treat psychosis.
Parkinson's disease is an uncommon manifestation of toxoplasmosis encephalitis in people infected with HIV, and in these cases, the symptoms may be treated with benztropine.
General Information
Benztropine is classified as an anticholinergic drug because it blocks the activity of a nerve-impulse transmitter called acetylcholine. Muscle rigidity is one of the primary symptoms of Parkinson's disease. Benztropine blocks the nerve signals that cause the rigidity, allowing the muscles to relax. By a similar mechanism, benztropine can prevent or counteract the muscle spasms that occur as a side effect of some psychoactive drugs.
Benztropine is available as a solution for injection and as tablets for oral administration. The injectable drug is used where rapid action is necessary and in cases where the muscle rigidity makes taking the tablets difficult or impossible.
Treatment
As with all psychoactive drugs, the minimum effective dosage should be used. Therapy usually starts at a low dose and is increased gradually at five- or six-day intervals as necessary and tolerated. For Parkinson's disease, the effective dosage ranges from 0.5 to 6.0 mg per day, with most adults using 1 to 2 mg per day. For treatment of muscle spasms caused by psychoactive drugs, benztropine is used at a dosage of 1 to 4 mg, once or twice a day, adjusted for the individual.
Cautions and Warnings
Benztropine should not be used by anyone with a known allergy to it. It may impair the mental or physical abilities needed to operate dangerous machinery or drive an automobile.
Because benztropine may prevent sweating and interfere with the body's internal heat control, it should be used with caution by people with chronic illness, a history of alcoholism, central nervous system disease, and people with inability to sweat. Benztropine should also be used with caution by people doing manual labor in a hot environment. In these cases the drug can cause heatstroke, which on occasion has been fatal.
Benztropine should be used with caution in people with heart disease, prostate disorders, difficulty urinating, or glaucoma. Although the drug does not appear to affect simple glaucoma, it may worsen angle-closure glaucoma and should not be used by people with this condition.
Side Effects
The most common side effects of benztropine include constipation, vomiting, nausea, dry mouth, and difficulty urinating. These can usually be eliminated or reduced in severity by lowering the dose of the drug.
Other side effects of benztropine include irregular heartbeat, confusion, disorientation, mental impairment, hallucinations, nervousness, depression, listlessness, numbness in the fingers, heatstroke, fever, and blurred vision. Occasionally, an allergic reaction such as a skin rash develops in people taking the drug.
Pregnancy/Breast-Feeding
Benztropine has not been formally studied in pregnant women or animals, but in clinical practice, there has been no evidence that the drug causes fetal harm. Pregnant women are encouraged to discuss the benefits and potential risks of benztropine with their physician before deciding to take the drug.
HIV may be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Benztropine may reduce the amount of milk a woman can produce. In addition, infants are highly susceptible to the side effects of the drug. Women who must take the drug should discontinue breast-feeding.
Use In Children
Because children are more sensitive to the side effects of benztropine than adults, the drug is not recommended for anyone under the age of three years. Older children who use the drug should be carefully monitored for side effects.
Use in the Elderly
Older adults may be more susceptible to the side effects of the drug and may require reduced doses.
Drug Interactions
When benztropine is used with other psychoactive drugs, including phenothiazines (e.g., chlorpromazine), haloperidol, tricyclic antidepressants (e.g., amoxapine, amitriptyline, nortriptyline), or other anticholinergics (e.g., atropine), the risk of side effects is increased. In some cases, these combinations have been fatal.
Food Interactions
Oral benztropine is absorbed into the body most effectively when taken on an empty stomach, but it may be taken with food if it causes stomach upset.
Other drugs used for similar conditions
Other drugs used to treat the symptoms of Parkinson's disease include diphenhydramine, levodopa, bromocriptine, and carbidopa. The choice of drug generally depends on the severity of the condition, the health of the individual, and other drugs being concurrently used. In many cases, combinations of these drugs are more effective than using individual drugs alone.
Bupropion
Brand Name (Manufacturer)
Wellbutrin (Burroughs Wellcome)
Type of drug
Psychoactive-antidepressant
Used For
Bupropion is used to treat depression in people who cannot take other medications.
General Information
Bupropion belongs to a class of drugs known as aminoketone antidepressants. It is chemically unrelated to tricyclic, tetracyclic, or other known classes of antidepressants. It is not known how bupropion works. It does not affect the cellular enzyme monoamine oxidase (MAO), which is the target of a class of antidepressants called MAO inhibitors. It raises brain levels of the neuro- transmitters serotonin and norepinephrine only weakly, which is the mechanism of action of another class of antidepressants that includes fluoxetine (Prozac).
Bupropion is generally used only after other drugs have failed, because people taking it have a higher risk of seizures than those taking other antidepressants.
Antidepressant medications are usually taken over long periods. It may take three to four weeks for antidepressants, including bupropion, to have an effect on depression. Bupropion accumulates in the body's tissues with prolonged use, and after it is discontinued, the drug takes about two weeks to get completely out of the body.
Bupropion is available as tablets for oral administration.
Treatment
Bupropion is usually taken at a dosage of 300 to 400 mg per day, divided into three or four doses. The total dose is divided into these small amounts to reduce the risk of seizures.
Cautions and Warnings
Bupropion should not be used by anyone with a known allergy to it or people who have a history of seizures or eating disorders. The drug should also not be taken when taking MAO inhibitors. At least fourteen days should elapse between discontinuing a MAO inhibitor and using bupropion.
In contrast to most other antidepressants, bupropion may cause weight loss. HIV-positive people who are already experiencing weight loss should consider using a different antidepressant.
Suddenly stopping bupropion may cause withdrawal symptoms or side effects.
Side Effects
The most serious side effect of bupropion is seizures. Approximately four out of every thousand people taking the drug experience seizures. The risk may be reduced if the total daily dose does not exceed 450 mg and if the drug is taken, as directed, in divided doses to reduce the maximum blood levels.
Other side effects of the drug include restlessness, agitation, anxiety, insomnia, confusion, hyperactivity, feelings of elation, delusions, hallucinations, or impaired mental function.
More than 28% of people treated with bupropion in clinical trials had loss of appetite and/or weight loss of more than five pounds.
Pregnancy/Breast-Feeding
Bupropion has not been formally studied in pregnant women. In animal studies it did not cause fetal harm, but it is not known whether the same would be true for humans. Pregnant women are encouraged to discuss the benefits and potential risks of bupropion with their physician before deciding whether or not to use the drug.
HIV may be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Bupropion may pass through human milk and cause serious side effects in nursing children. Because of the potential toxicity of the drug, women should consider alternatives to breast-feeding while taking it.
Use In Children
The safety and effectiveness of bupropion in people under eighteen have not been formally studied.
Use in the Elderly
Older adults may be more susceptible to the side effects of the drug and may require reduced doses.
Drug Interactions
Bupropion is metabolized by the liver. Caution should be used when taking other drugs that affect the liver, including carbamazepine, cimetidine, phenobarbital, and phenytoin. There is some evidence of increased side effects when bupropion and L-dopa are used together.
Alcohol, tranquilizers, or other central nervous system depressants may intensify the effect of bupropion. Alcohol use also increases the risk of seizures caused by bupropion.
Food Interactions
Bupropion may be taken with or without food.
Other drugs used for similar conditions
For treatment of depression, there are many options, including tricyclic antidepressants (desipramine, nortriptyline, protriptyline, amoxapine, maprotiline, imipramine, trimipramine, doxepin), MAO inhibitors (tranylcypromine, phenelzine, isocarboxazid), serotonin reuptake inhibitors (fluoxetine, paroxetine, and sertraline), and stimulants such as methylphenidate. The appropriate choice varies from person to person and depends on age, physical health and condition, and other drugs being concurrently used.
Buspirone
Brand Name (Manufacturer)
BuSpar (Bristol-Myers Squibb)
Type of Drug
Psychoactive-antianxiety drug
Used For
Buspirone is used primarily for the short-term relief of anxiety. It is also occasionally used to treat the pain, fatigue, and cramps of premenstrual syndrome (PMS).
General Information
Buspirone is an antianxiety drug that is chemically different from and works by a completely different mechanism than most other antianxiety drugs. Buspirone is less sedating than a majority of antianxiety drugs and has no potential for addiction. It is also less likely to slow down the mental and physical reactions in the people who take it. It may be an appropriate choice for people who need to remain alert and for those with a potential for substance abuse.
Buspirone is available in tablets for oral administration.
Treatment
As with all psychoactive drugs, the lowest effective dosage of buspirone should be used. The recommended initial dose is 5 mg taken three times a day. The dose is usually increased gradually as necessary and as long as it is tolerated. Total daily doses of 20 to 30 mg are common after the condition has stabilized.
Cautions and Warnings
Buspirone should not be used by anyone with a known allergy to it. It is not recommended for people who are taking antidepressants of the monoamine oxidase (MAO) inhibitor class, because of the potential for serious side effects.
People who are taking benzodiazepine antianxiety drugs (alprazolam, diazepam, chlordiazepoxide, for example) and want to switch to buspirone should gradually reduce their dose under a doctor's supervision and stop taking the benzodiazepine before starting buspirone. This strategy reduces the risk of withdrawal symptoms from the benzodiazepines.
Although buspirone is less sedating than other antianxiety medications, drowsiness is still one of its side effects, and it is not possible to predict how an individual will react to the drug. People taking buspirone should be cautious about operating dangerous machinery or driving an automobile while on the drug.
Side Effects
Dizziness, nausea, headache, and nervousness were reported by 5% to 10% of people taking the drug in clinical trials. Light-headedness and excitability were reported by approximately 2% of people in clinical trials.
Other side effects that occur in more than 1% of people who use buspirone include chest pain, dream disturbances, ringing in the ears, sore throat, and nasal congestion. In fewer than 1% of people taking the drug, changes in blood pressure, redness and itching of the eyes, altered taste, altered smell, gas, changes in appetite, rectal bleeding, changes in urination patterns, menstrual irregularity, muscle cramps, muscle spasms, shortness of breath, changes in sex drive, allergic reactions, dry skin, weight changes (both gains and losses), and malaise were reported.
Pregnancy/Breast-Feeding
Buspirone has not been formally studied in pregnant women. In animal studies, the drug did not cause fetal harm, but it is not known whether this would be true for humans. Pregnant women are encouraged to discuss the benefits and potential risks of buspirone with their physician before deciding to take the drug.
HIV may be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. It is not known whether buspirone is excreted in human milk. It was, however, excreted in the milk of laboratory animals during testing. Because of the potential toxicity of the drug to their infants, women should consider alternatives to breast-feeding while taking it.
Use In Children
The safety and effectiveness of buspirone for children under the age of eighteen have not been formally studied in clinical trials.
Use in the Elderly
Although buspirone has not been formally studied in the elderly, several hundred people over the age of sixty-five participated in studies of buspirone for the general population, and no unusual, age-related increase in side effects was identified.
Drug Interactions
When used with MAO inhibitors (e.g., phenelzine or tranylcypromine), buspirone may increase the risk of serious elevations in blood pressure. Buspirone may increase haloperidol levels in the blood, potentially increasing the risk of side effects. The combination of buspirone and trazodone may cause liver toxicity.
Food Interactions
Food slows down the rate at which buspirone is absorbed into the body, but increases the total amount absorbed. Buspirone may be taken with or without food.
Other drugs used for similar conditions
The benzodiazepines (e.g., alprazolam, diazepam, chlordiazepoxide) are the most frequently used antianxiety medications. They are fairly safe, they work rapidly, and they don't have to be taken on an ongoing basis to be effective. The drugs in the class differ somewhat in the side effects they produce, their potencies, the time it takes for them to work, and the tendency for them to be addictive or cause withdrawal symptoms.
Buspirone is not addictive and is less likely to be sedating. On the other hand, it is not effective for many people, and in others it must be taken several times a day in order to be effective.
Chlordiazepoxide
Brand Names (Manufacturers)
Libritabs (Roche); Librax (Roche); Librium (Roche)
Type of drug
Psychoactive-antianxiety agent
Used For
Chlordiazepoxide is used for the short-term relief of anxiety. It is also used to treat withdrawal symptoms of alcoholism and to prevent apprehension and anxiety.
General Information
Chlordiazepoxide was the first of a class of psychoactive drugs called benzodiazepines. Benzodiazepines are the most commonly used antianxiety drugs because they are fairly safe, they rapidly reduce symptoms of anxiety, and they don't have to be taken on an ongoing basis to be effective.
Chlordiazepoxide or other benzodiazepines are appropriate for short-term use in people experiencing extreme stress or anxiety.
Chlordiazepoxide is available as tablets for oral administration.
Treatment
The optimum dosage of chlordiazepoxide is determined by the diagnosis and the age and condition of the individual. For anxiety, the oral drug is generally used at 5 to 25 mg three or four times daily. The upper range is usually reserved for relief of severe anxiety disorders. Elderly people and children generally take lower doses: an initial dose of 10 mg or less per day is common.
The injectable form of the drug is preferred for treating withdrawal symptoms of acute alcoholism. The adult dosage is 50 to 100 mg injected into a muscle or given intravenously, repeated in two to four hours as necessary. When used for simple anxiety, the initial dose of the injectable is 50 to 100 mg initially, then reduced to 25 to 50 mg three or four times daily if necessary. Dose reductions are usually required for children and for elderly and/or debilitated people.
Cautions and Warnings
Chlordiazepoxide should not be used by anyone with a known allergy to it. The drug depresses the central nervous system, so it may not be appropriate to operate heavy machinery or drive a motor vehicle when taking it.
Like other benzodiazepines, chlordiazepoxide can be dangerous when taken with alcohol, because alcohol intensifies the depressive effect of benzodiazepines.
Taking chlordiazepoxide can be habit-forming. It appears that physical or psychological dependency may require several months of daily use, but dependency can sometimes occur much sooner. Rapid withdrawal after long-term use can lead to increased anxiety, insomnia, tremors, and in severe cases, seizures.
Side Effects
The most common side effects of chlordiazepoxide include drowsiness, confusion, and loss of balance, especially among elderly or debilitated people. Less commonly, people experience constipation, depression, headache, low blood pressure, incontinence, jaundice, changes in sex drive, nausea, changes in salivation, skin rash, and in women, menstrual irregularities.
For people who use the drug routinely, periodic blood counts and liver function tests are recommended because both an increase or decrease in white blood cell count may occur after use of the drug.
Pregnancy/Breast-Feeding
Chlordiazepoxide has not been formally studied in pregnant women. There is some evidence that it increases the risk of fetal deformities when used during the first trimester of pregnancy. Taken later in pregnancy, it may increase the risk that the baby will become addicted to it. Pregnant women are encouraged to discuss the benefits and potential risks of using chlordiazepoxide with their physician before deciding whether or not to use the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Chlordiazepoxide is excreted in human milk and can cause serious side effects in infants. Because of the potential toxicity of the drug, women should consider alternatives to breast-feeding while taking it.
Use In Children
Because there is little information about the safety and effectiveness of the drug for them, the oral form of the drug is not recommended in children under six years of age, and the injectable is not recommended for children under twelve.
Use in the Elderly
Elderly or debilitated people should receive the smallest effective dosage. Ten milligrams or less per day is recommended for initial treatment, only to be increased gradually as needed and tolerated.
Drug Interactions
Chlordiazepoxide may decrease the effectiveness of carbamazepine, levodopa, and oral anticoagulants such as warfarin. It may increase the effects of phenytoin. Disulfiram, oral contraceptives, isoniazid, and cimetidine can increase the blood levels of chlordiazepoxide, potentially increasing the risk of side effects. Rifampin may decrease the effectiveness of chlordiazepoxide.
Food Interactions
Chlordiazepoxide is absorbed most effectively into the body when taken on an empty stomach, but if necessary, it can be taken with food to minimize stomach upset.
Other drugs used for similar conditions
Many different benzodiazepines are available for prescription use. They include lorazepam, diazepam, alprazolam, oxazepam, temazepam, flurazepam, and triazolam. The drugs differ somewhat in the side effects they produce, their potencies, the time it takes for them to work, their duration of action, and the tendency for them to cause withdrawal symptoms.
Buspirone is an antianxiety medication that is not part of the benzodiazepine class. It is not addictive or sedating and has less tendency to slow down mental and physical reactions in people who take it. On the other hand, it is not effective for many people.
To treat anxiety accompanied by depression, a number of manufacturers market chlordiazepoxide/amitriptyline combinations.
Diazepam
Brand Names (Manufacturers)
Valium (Roche); Valrelease (Roche)
Type of Drug
Psychoactive-antianxiety agent
Used For
Diazepam is primarily used for the treatment of anxiety. It is also sometimes used to relax muscles, treat seizures, or to reduce the symptoms of acute alcohol withdrawal. Diazepam is also used to reduce anxiety before surgical procedures.
General Information
Diazepam belongs to a class of psychoactive drugs called benzodiazepines. Benzodiazepines are the most commonly used antianxiety drugs because they are fairly safe, they rapidly reduce the symptoms of anxiety, and they don't have to be taken on an ongoing basis to be effective.
Diazepam is available as tablets, capsules, and solution for oral administration as well as a solution for intravenous administration.
Treatment
The usual dosage of diazepam for adults is 2 to 10 mg two to four times a day, depending on the severity of symptoms and the diagnosis.
Elderly people usually take reduced doses, starting at 2 to 2.5 mg once or twice a day, increasing the dosage as tolerated and only when necessary.
Diazepam is not for use in children under six years of age. Older children may receive 1 to 2.5 mg three to four times a day initially, increased gradually as needed and tolerated.
Cautions and Warnings
Diazepam should not be used by people who are allergic to the drug or people who have glaucoma unless they are receiving appropriate antiglaucoma therapy. The drug depresses the central nervous system, so it may not be appropriate to operate heavy machinery or drive a motor vehicle when taking diazepam.
Like other benzodiazepines, diazepam can be dangerous when taken with alcohol. Alcohol intensifies the depressive effect of benzodiazepines.
Taking diazepam can be habit-forming. It appears that physical or psychological dependency may require several months of daily use, but dependency can sometimes occur much sooner. Rapid withdrawal after long-term use can lead to increased anxiety, insomnia, tremors, and in severe cases, seizures.
Abrupt withdrawal of diazepam when used with anticonvulsants may also cause a temporary increase in the frequency and/or severity of seizures.
Side Effects
The most common side effects of diazepam include drowsiness, fatigue, and loss of balance. Less commonly, people taking the drug experience confusion, constipation, depression, headache, low blood pressure, incontinence, jaundice, changes in sex drive, nausea, changes in salivation, skin rash, slurred speech, tremor, difficulty urinating, vertigo, and blurred vision.
On rare occasion, individuals have experienced a deficiency in certain white blood cells called neutrophils after taking diazepam. For this reason, periodic blood counts and liver-function tests are recommended for people who use diazepam routinely.
Pregnancy/Breast-Feeding
Diazepam may cause an increased risk for fetal deformities when used during the first trimester of pregnancy. Diazepam taken later in pregnancy may increase the risk that the baby will become dependent on it. Pregnant women should discontinue using the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Diazepam is excreted in human milk and can cause serious side effects in infants. Because of the potential toxicity of the drug, women should consider alternatives to breast-feeding while taking it.
Use In Children
Newborn infants have immature kidney and liver function and are often unable to metabolize drugs and excrete them from their bodies. In infants under thirty days of age, diazepam has caused prolonged central nervous system depression, possibly caused by the immature kidney function. The drug is not recommended for children under six months of age.
For older children, diazepam may effectively be used at lower doses than those given to adults. In general, the dose is started at 1 to 2.5 mg, taken three or four times daily, gradually increased as needed and tolerated.
Use in the Elderly
Older adults may be more susceptible to the side effects of the drug and may require reduced doses.
Drug Interactions
Phenothiazines, cimetidine, oral contraceptives, narcotics, barbiturates, alcohol, monoamine oxidase inhibitors, and other antidepressants may intensify the effect of diazepam and increase the risk of serious side effects.
Diazepam may decrease the effectiveness of carbamazepine, levodopa, and blood thinners and may increase the effects of phenytoin.
Concurrent use with rifampin may decrease the effectiveness of diazepam.
Food Interactions
Diazepam is absorbed most rapidly into the body when taken on an empty stomach, but it may be taken with food if it causes stomach upset.
Other drugs used for similar conditions
Many different benzodiazepines are available for prescription use. They include lorazepam, chlordiazepoxide, alprazolam, oxazepam, temazepam, flurazepam, and triazolam, among others.
The drugs differ somewhat in their side effects, potencies, the time it takes for them to work, and their tendency to cause withdrawal symptoms.
Buspirone is an antianxiety medication that is not part of the benzodiazepine class. It is not addictive or sedating and has less tendency to slow down mental and physical reactions in the people who take it. On the other hand, it is not effective for many people.
Fluoxetine
Brand Name (Manufacturer)
Prozac (Dista)
Type of Drug
Psychoactive-antidepressant
Used For
Fluoxetine is widely used to treat the symptoms of mental depression. It is less frequently used to treat obsessive-compulsive disorder, classic panic disorder, the eating disorder bulimia, and as an appetite suppressant.
General Information
Fluoxetine is an antidepressant that belongs to a class known as serotonin reuptake inhibitors. It is chemically unrelated to tricyclic, tetracyclic, or other known classes of antidepressants. It has become widely used because it is effective and tends to have fewer side effects than older antidepressants (such as the monoamine oxidase inhibitors, for example). It does not cause sedation, weight gain, dry mouth, or constipation.
Antidepressant medications are usually taken over long periods. It takes four weeks or more before steady levels are built up in the blood, and it may take as long for the drug to have an effect on depression. Fluoxetine accumulates in the body's tissues with prolonged use, and the drug may stay in the body for weeks or months after discontinuing therapy. It is especially important that at least five weeks pass after stopping the drug before starting another drug that may interact with fluoxetine.
Fluoxetine has been studied in a number of small clinical trials in people with HIV infection. It general, it has been highly effective in reducing the symptoms of depression. People with low CD4+ counts (under 200) did as well on the drug as people with higher counts.
Fluoxetine is available as capsules for oral administration.
Treatment
For depression, the recommended dose is 20 to 80 mg per day. As with all antidepressants, it is recommended that the lower dose be initially used and increased after several weeks as necessary if the person is not experiencing serious side effects. It may take up to four weeks to notice an effect. The dose may need to be reduced for people with poor liver or kidney function.
For obsessive-compulsive disorder, the recommended treatment is 20 mg per day taken in the morning. Full therapeutic effect may take five weeks or longer. A dose increase may be considered after several weeks if no improvement is seen, but the dose should not exceed 80 mg per day.
Cautions and Warnings
Fluoxetine should not be used by anyone with a known allergy to it. It should not be used by people taking monoamine oxidase (MAO) inhibitor antidepressants. Because fluoxetine and MAO inhibitors remain in the body for a time after stopping therapy, fluoxetine should not be started within fourteen days of receiving a MAO inhibitor. MAO inhibitors should not be started within at least five weeks, and perhaps longer, after stopping fluoxetine.
People with diabetes should use fluoxetine with caution. The drug may alter control of sugar metabolism in the body.
Side Effects
Fluoxetine is relatively well-tolerated. Its most common side effects (which were observed in more than 5% of people taking the drug in clinical trials) include anxiety, nervousness, insomnia, fatigue, tremors, sweating, changes in appetite, reduced sex drive, nausea, diarrhea, dizziness, or light-headedness.
Pregnancy/Breast-Feeding
There was no harm to the fetus when fluoxetine was given to pregnant laboratory animals, but there have been no studies of fluoxetine in pregnant women. Pregnant women are encouraged to discuss the benefits and potential risks of fluoxetine with their physician before deciding to use the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Fluoxetine is excreted in human milk. Because of the potential toxicity of the drug, women should consider alternatives to breast-feeding while taking it.
Use In Children
The safety and effective of fluoxetine for children has not been formally studied in clinical trials.
Use in the Elderly
It is not known if fluoxetine is metabolized differently in elderly people than in younger people. No unexpected side effects have been seen in elderly people taking 20 mg daily.
Drug Interactions
Extreme drowsiness may occur when fluoxetine is taken with alcohol or other central nervous system depressants such as barbiturates, muscle relaxants, sleeping pills, antihistamines, or tranquilizers.
Fluoxetine increases the blood-thinning effect of warfarin, which may require adjustment of warfarin dose. Similarly, fluoxetine may increase the effect of heart medicine such as digitoxin.
Serious side effects may occur when fluoxetine is taken with MAO inhibitors or when taken by people with residual levels of MAO inhibitors in their blood.
Fluoxetine can increase the levels of tryptophan and increase the chance of tryptophan-related side effects, including anxiety, agitation, restlessness, and stomach irritation.
Food Interactions
None reported.
Other drugs used for similar conditions
For treatment of depression, there are many options, including tricyclic antidepressants (desipramine, nortriptyline, protriptyline, amoxapine, maprotiline, imipramine, trimipramine, doxepin), MAO inhibitors (tranylcypromine, phenelzine, isocarboxazid), other serotonin reuptake inhibitors (paroxetine and sertraline), and stimulants such as methylphenidate. The appropriate drug varies from person to person and depends on age, physical health and condition, and other drugs being concurrently used.
Fluphenazine
Brand Name (Manufacturer)
Prolixin (Apothecon)
Type of Drug
Psychoactive-antipsychotic tranquilizer
Used For
Fluphenazine is used for the management of psychosis, a mental disorder characterized by difficulty thinking, recognizing reality, and acting rationally.
General Information
Fluphenazine belongs to a class of psychoactive drugs called phenothiazines. Although the mechanism by which they work is unknown, they have potent effects on the central nervous system and other organs. In addition to their effects on mental disorders, they also prolong the effects of anesthetics and other central nervous system depressants. They can reduce blood pressure, stop seizures, and prevent vomiting. Fluphenazine is more potent than most of the other phenothiazines and it is less likely to cause serious side effects.
Fluphenazine is available in a number of different chemical forms, which differ primarily in the duration of their action. The drug is available in tablets, as a solution for injection, and as an oral concentrate.
Treatment
As with all psychoactive drugs, the minimum effective dosage should be taken. The oral forms of fluphenazine are usually initially used at a range of 2.5 to 10 mg per day, divided into equal doses given at six- to eight-hour intervals. Treatment usually starts at low initial dosages and is gradually increased as necessary and tolerated. Treatment is effective for most people with doses under 20 mg daily, but some people with severe disease may require up to 40 mg per day.
When the symptoms are controlled, the dosage can generally be reduced gradually to a daily maintenance dose of 1 to 5 mg, often given as a single daily dose. After stabilization on the short-acting forms of the drug, individuals may elect to switch to the longer-acting forms to make taking the drug easier. Once monthly intramuscular injections may be appropriate once control is achieved.
Cautions and Warnings
Fluphenazine should not be used by anyone with a known allergy to it. It should also not be used by people with brain damage, those receiving large doses of other psychoactive drugs, or those in comatose or severely depressed states. The drug should also not be used by people with severe liver damage or blood disorders.
People who are allergic to other phenothiazines may also be allergic to fluphenazine and should use the drug with caution. Similarly, people who are exposed to extreme heat or phosphorus pesticides and people with a history of seizures or heart disease should use the drug with caution because of their increased risk of side effects.
Although phenothiazines are in general not addictive, some people have experienced withdrawal symptoms (including nausea, vomiting, dizziness, and tremors) when stopping therapy after receiving high doses. These symptoms may be reduced by taking an anti-Parkinson's-disease drug like benztropine.
Fluphenazine may impair the mental and physical abilities necessary to operate dangerous machinery or to drive an automobile.
Side Effects
The side effects reported most frequently after using phenothiazines include loss of muscle coordination or tone, muscle rigidity, and other disorders of the nerve control of muscles. In general, the symptoms are reversible when treatment is stopped or benztropine is used, but in some cases they may persist.
Tardive dyskinesia is a special neuromuscular side effect of phenothiazines. It is characterized by potentially irreversible, involuntary muscle movements that usually involve the tongue, face, mouth, lips, jaw, torso, and extremities. Although the side effect occurs most frequently among the elderly (especially elderly women), it is not possible to predict whether an individual will develop the disorder. The risk of the side effect and the likelihood it will be irreversible are believed to be increased with increased duration of treatment and cumulative dose.
Antipsychotic drugs, including fluphenazine, can cause a potentially fatal side effect called neuroleptic malignant syndrome. The syndrome is characterized by high fever, muscle rigidity, altered mental status, irregular pulse or blood pressure, and abnormal heart rhythms. If these symptoms occur, the drug should be stopped and a physician contacted immediately.
Other side effects of fluphenazine include low blood pressure or fluctuations in blood pressure, weight change, swelling in the extremities, allergic reactions, and liver damage.
Pregnancy/Breast-Feeding
Fluphenazine has not been formally studied in pregnant women. Most evidence suggests, however, that phenothiazines have a low risk of causing birth defects or other fetal harm when used during pregnancy. Pregnant women are encouraged to discuss the benefits and potential risks of fluphenazine with their physician before deciding to use the drug.
HIV may be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. It is not known whether fluphenazine is excreted in human milk. Other phenothiazines have not had serious adverse effects on nursing infants, but whether this would be true for fluphenazine is not known.
Use In Children
Fluphenazine has not been formally studied in children, and there are no recommendations regarding its use for them.
Use in the Elderly
Older adults may be more susceptible to the side effects of the drug and may require reduced doses.
Drug Interactions
Fluphenazine may intensify the effects of alcohol, analgesics, narcotics, antihistamines, and barbiturates. Antacids may decrease absorption of fluphenazine. Phenobarbital or lithium may decrease the effect of fluphenazine. Guanethidine or methyldopa used with fluphenazine may cause increased blood pressure. Use of insulin with fluphenazine may result in increased blood-sugar levels. Use of orphenadrine with fluphenazine may result in lowered blood-sugar levels.
Food Interactions
None reported.
Other drugs used for similar conditions
A number of different drugs are available for treating psychosis. They include chlorpromazine, thioridazine, trifluoperazine, haloperidol, loxapine, and thiothixene. They differ in their duration of action, side effects, dosage, and administration. Because different people respond differently to each of the drugs, the choice of therapy usually comes down to finding through trial and error a drug that is both effective and tolerable. In comparison to the others, fluphenazine has relatively mild effects on alertness and blood pressure, but it has a relatively high risk of causing neuromuscular side effects.
Flurazepam
Brand Name (Manufacturer)
Dalmane (Roche)
Type of Drug
Psychoactive-sedative
Used For
Flurazepam is used for the short-term treatment of insomnia.
General Information
Anxiety, depression, and many medications can cause sleep problems in people with HIV infection. Flurazepam, one of the most widely used sleeping pills in the United States, is a member of a class of psychoactive drugs called benzodiazepines. All of these drugs reduce anxiety or cause drowsiness to some degree. They differ mostly in the degree of their effects and the duration of their action. Flurazepam is one of the longer-acting benzodiazepines, so it may be more likely to cause a "hangover" effect.
Like other benzodiazepines, flurazepam can cause dependency. Withdrawal symptoms may include convulsions, tremors, abdominal pain, muscle cramps, vomiting, sweating, restlessness, perceptual disturbances, and insomnia. The risk of addiction is increased in people with a history of alcoholism, drug use, or marked personality disorders.
Treatment
The dose should be adjusted for the age, condition, and health of the individual. The usual adult dosage is 30 mg taken at bedtime. For some people, especially those who are elderly or debilitated, 15 mg may be sufficient. It may take one or two days of consecutive use before flurazepam is fully effective, and after stopping the drug, it may take a few days for its effects to wear off.
Cautions and Warnings
Flurazepam should not be used by anyone with a known allergy to it.
Sleep disorders may be symptoms of other physical or psychiatric problems. Eliminating the underlying cause of sleeplessness, if it can be determined, may be a better long-term solution to the problem.
Flurazepam, like other benzodiazepines, may be habit-forming if taken for more than three or four days in a row. Consequently, it is possible for a person taking the drug to develop withdrawal symptoms if the drug is suddenly discontinued, including convulsions, tremors, muscle cramps, insomnia, agitation, diarrhea, vomiting, and sweating.
As with all psychoactive drugs, the minimum effective dosage should be used because some of the drug's side effects are dose-related. Elderly people are especially susceptible to the dose-related side effects of the drug.
Flurazepam depresses the central nervous system. People taking the drug should not drive an automobile or operate heavy machinery. Because flurazepam is a relatively long-acting benzodiazepine, its effects on alertness may continue into the day after taking the drug.
Side Effects
The most common side effects of the drug include dizziness, drowsiness, light-headedness, staggering, loss of muscle coordination, and falling.
Other less frequent side effects of the drug include headache, heartburn, upset stomach, nausea, vomiting, diarrhea, constipation, stomach pain, nervousness, talkativeness, apprehension, irritability, weakness, heart palpitations, body and joint pain, and difficulty urinating.
Severe sedation, lethargy, disorientation, and coma have been reported on rare occasions.
Pregnancy/Breast-Feeding
Flurazepam should not be used during pregnancy. Although flurazepam has not been formally studied in pregnant women, other benzodiazepines have caused birth defects when used during the first trimester of pregnancy. There have also been cases of severe side effects of flurazepam in infants whose mothers took the drug during pregnancy.
HIV may be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Flurazepam is excreted in breast milk and may cause serious side effects in newborn infants. Because of the potential toxicity of the drug, women should consider alternatives to breast-feeding while taking it.
Use In Children
The safety and effectiveness of flurazepam have not been studied in children under the age of fifteen, so there are no recommendations about its use for them.
Use in the Elderly
Older adults may be more susceptible to the side effects of the drug and may require reduced doses.
Drug Interactions
Flurazepam produces additive central nervous system depression when used with anticonvulsants, antihistamines, alcohol, and other drugs that produce central nervous system depression.
Oral contraceptives, cimetidine, disulfiram, probenecid, and isoniazid may increase the effects of flurazepam by increasing blood levels of the drug. Cigarette smoking, rifampin, and theophylline may reduce blood levels of flurazepam, potentially reducing the drug's effectiveness.
Flurazepam may increase the amount of phenytoin or digoxin in the blood, increasing the risk of side effects. Flurazepam used with clozapine has caused respiratory collapse in some people. Clozapine should not be used until at least one week after flurazepam is stopped.
Food interactions
None reported.
Other drugs used for similar conditions
A number of drugs are available for treatment of insomnia. Barbiturates such as secobarbital or phenobarbital are occasionally used. More commonly, sedatives such as lorazepam, diazepam, triazolam, or promethazine are used. There is no ideal treatment for insomnia. Choosing one depends primarily on which can be tolerated, which side effects a person is at risk for, and which proves to be the most effective for the individual.
Haloperidol
Brand Name (Manufacturer)
Haldol (McNeil)
Type of Drug
Psychoactive-tranquilizer
Used For
Haloperidol is used for the management of the symptoms of psychotic disorders in children and adults. In children this may include treatment of hyperactivity, severe behavioral problems, inability to sustain attention, and an abnormally low tolerance for frustration. In adults, the treated disorders may include Tourette's syndrome, chronic schizophrenia, and phencyclidine psychosis.
General Information
Haloperidol affects a part of the brain called the hypothalamus. This part of the brain affects some of the automatic functions of the body, including temperature, metabolism levels, alertness, muscle tone, and hormone balance. It is not known exactly how the drug works to alleviate the symptoms of psychosis.
Haloperidol is available as tablets, liquid concentrate, and solution for injection.
Treatment
Most adults and children use the tablet form unless they have difficulty swallowing it. The solution for injection is used for severely agitated people to achieve a rapid response. This formulation has not been tested in children.
The dose of haloperidol must be adjusted for a person's age, condition, severity of illness, previous response to other psychoactive drugs, and other medications taken at the same time. Children and elderly adults with impaired kidney function may require lower doses. The optimal response is usually obtained by starting with a low dose and gradually increasing it.
Haloperidol decanoate is a long-acting form of the drug and is administered by deep injection into a large muscle once a month. It is generally used only after an individual has stabilized while taking the shorter-acting oral drug.
Cautions and Warnings
Haloperidol should not be used by people in severe central nervous system depression comatose states. It should also not be used by those with Parkinson's disease or who have a known allergy to the drug.
Tardive dyskinesia, a syndrome consisting of potentially irreversible, involuntary movements, may develop in people treated with haloperidol. The risk is correlated with length of therapy and total dose, but it is not possible to predict whether any individual will experience the side effect.
As with other central nervous system depressants, haloperidol may affect the mental and physical capacity to operate heavy machinery or drive an automobile.
Haloperidol should be used with caution in people with heart conditions because of the risk of low blood pressure and in those with a history of seizures or receiving anticonvulsant medication because haloperidol may increase the risk of seizures.
Side Effects
The most common side effect to haloperidol is drowsiness. Less commonly, haloperidol can cause jaundice, fever, bone-marrow toxicity, alteration in blood pressure, abnormal heartbeat, heart attack, faintness, and dizziness.
Haloperidol can cause serious neurological side effects that include spasms of the neck muscles, severe stiffness of the back, rolling of the eyes, convulsions, difficulty swallowing, and symptoms associated with Parkinson's disease.
Haloperidol may cause an unusual increase in psychotic reactions, including paranoia, tiredness, lethargy, restlessness, confusion, bizarre dreams, insomnia, depression, or euphoria.
Pregnancy/Breast-Feeding
Haloperidol has not been formally studied in pregnant women. In animal studies, it did cause some evidence of fetal harm, but it is not known whether this would be true in humans. There have been reports of birth defects in women taking haloperidol with other drugs that have the potential to cause fetal harm, but it is not known whether haloperidol itself caused the birth defects. Pregnant women are encouraged to discuss the benefits and potential risks of haloperidol with their physician before deciding to use the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Haloperidol is excreted at high concentrations in human milk. It is not recommended for nursing women.
Use In Children
Haloperidol has been used effectively in children without unexpected side effects.
Use in the Elderly
Tardive dyskinesia is a haloperidol-related side effect that most commonly occurs in elderly people who take the drug, particularly elderly women.
Older adults may be more susceptible to the side effects of the drug and may require reduced doses.
Drug Interactions
Irreversible brain damage has occurred in a small number of people treated with lithium and haloperidol. It is not known, however, whether the drugs actually caused the side effect.
The use of haloperidol with alcohol, sleeping pills, barbiturates, anesthetics, or narcotics may cause severe central nervous system depression and low blood pressure.
Haloperidol may reduce the blood-pressure-lowering effect of guanethidine. Mixing haloperidol with propranolol may result in unusually low blood pressure. Blood concentrations of tricyclic antidepressants may be increased when they are used with haloperidol, increasing the risk of side effects.
Food Interactions
Haloperidol is absorbed most effectively when taken without food, but food may be used if the drug causes stomach upset.
Other drugs used for similar conditions
Other drugs with antipsychotic and tranquilizing activity include thorazine, fluphenazine, mesoridazine, thioridazine, and trifluoperazine. In general, they are equally effective when given in therapeutically equivalent doses. The major differences are in the type and severity of side effects, which may be different from person to person.
Lithium
Brand Names (Manufacturers)
Eskalith (Smithkline Beecham); Lithonate (Reid-Rowell); Lithotabs (Reid-Rowell)
Type of Drug
Psychoactive-antimanic agent
Used For
Lithium is used to treat or prevent the manic phases of manic depression, a mental disorder in which a person's mood swings wildly from elation to depression.
Lithium has also been used but not approved to reduce or counteract the bone-marrow toxicity of AZT in people with HIV, although there is little clinical evidence to support this use.
General Information
Lithium is the only available effective drug treatment for mania. When ingested and absorbed into the body, lithium alters the way nerve cells transmit their signals. This action effectively controls the symptoms of mania within one to three weeks after starting the drug.
Certain drugs commonly used by people infected with HIV, including AZT, can be toxic to bone marrow, often resulting in deficiencies in white blood cells. Because one side effect of lithium is an increase in white blood cells, the drug has been tested as a potential therapy to reverse the bone-marrow toxicity of AZT. Encouraging results in studies in animals prompted the start of clinical trials in humans. In one study, twenty volunteers were randomly chosen to receive AZT and either lithium at a dose of 300 mg twice a day or a placebo, for an average of twenty-four weeks. While the group receiving lithium had a transient increase in neutrophil counts six weeks after starting therapy, by the end of twenty-four weeks of treatment there was no difference in the counts of neutrophils or CD4+ cells between groups. This lack of long-term effect dampened the interest in lithium as a treatment for AZT toxicity.
In the meantime, other drugs that stimulate white blood cell production have become available. One, called G-CSF, is now widely used for the condition.
Lithium is available in capsules, controlled-release tablets, and syrup.
Treatment
Lithium is usually started with the immediate-release capsules and switched to the controlled-release tablets after the condition has stabilized. The immediate-release capsules are usually taken three or four times a day. The controlled-release tablets need to be taken only twice a day.
The optimal dose must be determined for each person, but most people take around 1,800 mg per day for acute episodes of mania. For long-term control after the condition has stabilized, the adult dose ranges from 600 to 1,200 mg per day.
When switching from the capsules to the tablets, it is important that the same total daily dose be given.
Cautions and Warnings
Lithium should not be used by anyone with a known allergy to it. In addition, it should generally not be used by people with significant kidney or heart disease, severe debilitation, or sodium deficiency because the risk of side effects is high in these people.
In most people, the effective dose of lithium is close to the dose that causes severe toxicities. In general, people taking the drug will be closely monitored by their physician to maintain appropriate levels of the drug in their blood.
People who experience diarrhea, nausea, vomiting, tremors, loss of coordination, drowsiness, or muscle weakness while taking lithium should contact their physicians as soon as possible. People with HIV may experience these symptoms as a result of their disease or other drugs being taken, but they may also be the early warning signs of lithium toxicity.
Side Effects
The side effects of lithium are generally dose-related, occurring more frequently and with greater severity when higher concentrations of lithium are in the blood. Hand tremors, frequent urination, mild nausea, general discomfort, and mild thirst may occur during initial therapy. These side effects usually subside with continued treatment or dose reductions. If they persist, the drug should be stopped.
Diarrhea, vomiting, drowsiness, muscle weakness, lack of coordination, giddiness, ringing in the ears, and blurred vision may occur at therapeutic levels of the drug. At dosages higher than recommended, severe side effects may occur.
Pregnancy/Breast-Feeding
Lithium can cause severe fetal harm and should not be taken during pregnancy, particularly during the first trimester. As many as 8% to 9% of babies exposed to lithium in the womb may develop heart defects. Other birth defects observed include brain and spine malformations. Women of childbearing age are encouraged to use effective contraception while taking the drug.
HIV may be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Lithium passes into breast milk. Because of the potential toxicity of the drug, women should consider alternatives to breast-feeding while using it.
Use In Children
Lithium has not been formally studied in children under the age of fifteen, so no recommendations regarding its use in them can be made.
Use in the Elderly
Older adults may be more susceptible to the side effects of the drug and may require reduced doses. Even when lithium blood levels are within the recommended range, elderly people are at higher risk of the drug's side effects than the general population.
Drug Interactions
Haloperidol may increase the blood levels of lithium. This combination has caused weakness, fatigue, and confusion in some people, rarely resulting in permanent damage.
Lithium may reduce chlorpromazine levels in the blood, potentially reducing its effectiveness. Chlorpromazine may increase lithium levels in the blood, potentially resulting in increased side effects.
Sodium bicarbonate, acetazolamide, urea, mannitol, and theophylline neutralize the effect of lithium. Verapamil may reduce both the blood levels and toxicity of lithium.
Methyldopa, fluoxetine, carbamazepine, thiazide and loop diuretics, metronidazole, enalapril, captopril, and some arthritis medications like indomethacin or piroxicam may increase the effects of lithium.
Lithium may increase the blood levels of tricyclic antidepressants such as amoxapine, amitriptyline, desipramine, or maprotiline.
Food Interactions
For best absorption, lithium should be taken immediately after food or milk. Because lithium can cause a reduction in body salt levels, it is important to maintain a well-balanced diet.
Other drugs used for similar conditions
Lithium is the only available drug treatment for mania. For AZT-induced white blood cell deficiencies, the colony-stimulating factor G-CSF is the drug of choice.
Lorazepam
Brand Name (Manufacturer)
Ativan (Wyeth-Ayerst)
Type of Drug
Psychoactive-tranquilizer
Used For
Lorazepam is used in adults for the treatment of anxiety. In addition, the injectable form of the drug is used as a sedative and as a presurgical medication for people who prefer not to remember the events of the day of their surgery.
General Information
Lorazepam belongs to a class of psychoactive drugs called benzodiazepines. Benzodiazepines are the most commonly used antianxiety drugs because they are fairly safe, rapidly reduce the symptoms of anxiety, and don't have to be taken on a ongoing basis to be effective. All benzodiazepines cause dose-related suppression of the central nervous system, varying from slight impairment to deep sedation. Lorazepam is one of the more sedating benzodiazepines.
Like other benzodiazepines, lorazepam can cause dependency. Withdrawal symptoms may include convulsions, tremors, abdominal pain, muscle cramps, vomiting, sweating, restlessness, perceptual disturbances, and insomnia. The risk of addiction is increased in people with a history of alcoholism, drug use, or marked personality disorders.
While lorazepam is available as tablets and a solution for intravenous injection, most people will use the tablets.
Treatment
The dose of lorazepam should be optimized for each individual. As with other psychoactive drugs, the minimum effective dosage should be used to minimize the risk of side effects. In general, treatment is started at a low dose and gradually increased as necessary and as tolerated. The usual dosage range for healthy adults is 2 to 6 mg per day given in divided doses. For anxiety, most people require an initial dosage of 2 to 3 mg per day, split into two or three doses.
Lower doses may be required for elderly people and people with kidney or liver impairment.
Cautions and Warnings
Lorazepam should not be used by anyone with a known allergy to it. It should also not be used by people with acute narrow-angle glaucoma.
Lorazepam is metabolized in the liver and excreted by the kidney. Consequently, it should be used with caution by people with kidney or liver impairment.
Lorazepam depresses the central nervous system. People taking the drug should not drive an automobile or operate dangerous machinery.
Side Effects
Side effects to the drug usually occur early in treatment and disappear as treatment continues. The most frequent side effects in clinical trials were sedation (reported by about 16% of people taking the drug), dizziness (7%), weakness (4%), and unsteadiness (3%). Less frequent side effects include disorientation, depression, nausea, change in appetite, headache, sleep disturbance, agitation, and skin reactions. Transient amnesia or memory impairment has been reported after the use of other benzodiazepines.
Pregnancy/Breast-Feeding
Although lorazepam has not been formally studied in pregnant women, use of other benzodiazepines (chlordiazepoxide, diazepam, and meprobamate) during the first trimester of pregnancy has sometimes resulted in fetal malformations.
HIV may be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Lorazepam is excreted in breast milk and it may accumulate in nursing infants. Because of the potential toxicity of the drug, women should consider alternatives to breast-feeding while taking it.
Use In Children
There is little clinical data regarding the use of lorazepam in children, therefore no recommendations about its use in this population can be made.
Use in the Elderly
People over the age of fifty may have deeper and more prolonged sedation when using lorazepam. In addition, elderly people may be at increased risk for the drug's other side effects, which include unsteadiness and disorientation. In general, elderly people will use a reduced dosage of the drug to obtain the same therapeutic effects.
Drug Interactions
Lorazepam produces additive central nervous system depression when used with anticonvulsants, antihistamines, alcohol, and other drugs that produce central nervous system depression.
Smoking may reduce the effectiveness of lorazepam by reducing blood levels of the drug. The effects of lorazepam may be prolonged when taken with cimetidine, oral contraceptives, disulfiram, fluoxetine, isoniazid, ketoconazole, metoprolol, probenecid, propoxyphene, propranolol, rifampin, or valproic acid.
Theophylline may reduce lorazepam's sedative effects.
Antacids or ddI should be taken two hours before or after lorazepam, because they interfere with the drug's absorption into the body.
Phenytoin and digoxin blood levels are increased when taken with lorazepam, potentially increasing the risk of side effects from these drugs. Lorazepam may reduce blood levels of levodopa, potentially reducing its effectiveness.
Food Interactions
Lorazepam is absorbed most effectively into the body when taken on an empty stomach, but it may be taken with food if it causes an upset stomach.
Other drugs used for similar conditions
Many different benzodiazepines are available for prescription use. They include alprazolam, diazepam, chlordiazepoxide, and flurazepam among others. The drugs in the class differ somewhat in the side effects they produce, their potencies, the time it takes for them to work, and the tendency for them to be addictive or cause withdrawal symptoms.
Buspirone is an antianxiety medication that is not part of the benzodiazepine class. It is not addictive and is less likely to be sedating. It also has less tendency to slow down mental and physical reactions in the people who take it. On the other hand, it is not effective for many people.
Methylphenidate
Brand Name (Manufacturer)
Ritalin (Ciba)
Type of Drug
Psychoactive-stimulant
Used For
Methylphenidate is a central nervous system stimulant used to treat attention-deficit disorders, primarily in children. It is also used in narcolepsy, a disorder involving uncontrollable sleep attacks or desire to sleep. It is also occasionally used to treat depression in people who do not respond to other medication.
Methylphenidate is also occasionally used without approval by people with HIV for the treatment of AIDS dementia complex.
Methylphenidate is available as tablets for oral administration.
General Information
Attention-deficit disorder, which occurs primarily in young boys, involves moderate-to-severe distractibility, short attention span, hyperactivity, wide emotional swings, and impulsivity. A total treatment program for the disorder typically includes psychological, educational, and social measures as well as drug therapy.
Methylphenidate is a psychostimulant. It has proven useful in people who are withdrawn or apathetic. It works more rapidly than drugs in other classes of antidepressants.
Treatment
The dosage must be adjusted for each person. The standard dose for adults and adolescents is 20 to 30 mg per day. Some people may require up to 60 mg per day. The drug is also available in a slow-release (SR) form. The SR tablets must be swallowed whole, never crushed or chewed. The SR tablets can replace standard tablets when eight-hour dosing is necessary.
Children are generally given small initial doses with gradual weekly increments as necessary, if they don't experience serious side effects. The recommended dose for children is 5 mg twice daily before breakfast and lunch, with gradual dose increments of 5 to 10 mg each week. A daily dose over 60 mg is not recommended for children.
In treatment of symptoms of AIDS dementia complex, doses of 5 to 10 mg per day are often sufficient to alleviate apathy and to increase energy, concentration, and appetite.
Cautions and Warnings
People with marked anxiety, tension, or agitation should not take the drug, since it may aggravate these symptoms. People who know they are allergic to it, have glaucoma, motor tics, or a family history of Tourette's syndrome should not take the drug.
There is some clinical evidence that suggests methylphenidate increases the likelihood of seizures in people with a prior history of seizures.
The drug should be used with caution in people with high blood pressure.
Chronic use of methylphenidate can cause dependency. Abuse can cause psychotic episodes.
Side Effects
Nervousness and insomnia are the most frequent side effects. Hypersensitivity, anorexia, nausea, dizziness, heart palpitations, headache, drowsiness, high blood pressure and pulse changes, rapid heartbeat, angina, irregular heart rhythm, abdominal pain, and weight loss during prolonged therapy have been observed. There have been rare reports of Tourette's syndrome and toxic psychosis.
Pregnancy/Breast-Feeding
Methylphenidate has not been formally studied in pregnant women. It passes through the placenta into the fetal blood circulation, but it has not been found to cause birth defects. Pregnant women are encouraged to discuss the benefits and potential risks of methylphenidate with their physician before deciding to use the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. It is not know if methylphenidate passes into human milk, but the drug has caused no significant problems among breast-fed infants.
Use In Children
Methylphenidate has not been studied in children under six. Children six and older are generally treated at the dosages listed above. The long-term effects in children have not been well established. Side effects in children may occur more frequently than in adults.
Use in the Elderly
No changes in dosage or administration are recommended for elderly people.
Drug Interactions
Methylphenidate may decrease the effectiveness of the blood-pressure medicine guanethidine. It may inhibit the metabolism of the blood-thinner warfarin, anticonvulsants (phenobarbital, diphenylhydantoin, primidone), phenylbutazone, and tricyclic antidepressants (imipramine, clomipramine, desipramine).
Food Interactions
Methylphenidate should be taken thirty to forty-five minutes before meals to maximize absorption of the drug into the body.
Other drugs used for similar conditions
To alleviate symptoms of depression, a number of antidepressants, such as fluoxetine, are available. For treatment of AIDS dementia complex, haloperidol may be used. Amphetamines are sometimes prescribed to increase energy and improve concentration.
Oxazepam
Brand Name (Manufacturer)
Serax (Wyeth-Ayerst)
Type of Drug
Psychoactive-tranquilizer
Used For
Oxazepam is used for the short-term relief of anxiety, including anxiety associated with depression. It is also used to treat withdrawal symptoms of alcoholism.
General Information
Oxazepam is a member of a class of psychoactive drugs called benzodiazepines. Benzodiazepines are the most commonly used antianxiety drugs because they are fairly safe, they rapidly reduce the symptoms of anxiety, and they do not have to be taken on an ongoing basis in order to be effective. All benzodiazepines cause dose-related suppression of the central nervous system, varying from slight impairment to deep sedation.
Oxazepam is a short-acting benzodiazepine, which means that the drug is rapidly eliminated from the body. This reduces the risk that the drug will cause a "hangover" effect the day after it is taken. It also reduces the risk the drug will accumulate in the body to high levels that may cause side effects.
Like other benzodiazepines, oxazepam can cause dependency. Withdrawal symptoms may include convulsions, tremors, abdominal pain, muscle cramps, vomiting, sweating, restlessness, perceptual disturbances, and insomnia. The risk of dependency is increased in people with a history of alcoholism, drug use, or marked personality disorder. However, clinical studies show that oxazepam is less likely to cause addiction than diazepam, lorazepam, alprazolam, or triazolam.
Oxazepam is available as tablets and capsules for oral administration.
Treatment
The dosage of oxazepam should be adjusted for each individual. As with other psychoactive drugs, the minimum effective dosage should be used to reduce the risk of side effects. The dosage is generally started low and increased as necessary and tolerated.
For treatment of mild-to-moderate anxiety, the usual adult dosage is 10 to 15 mg, taken three or four times a day. For severe cases, the dosage may be doubled. Older people generally receive 10 mg, three or four times a day, to be increased as necessary to 15 mg per day.
Cautions and Warnings
Oxazepam should not be used by people who know they are allergic to it. Oxazepam depresses the central nervous system. People taking the drug should not drive an automobile or operate dangerous machinery.
Because of their increased risk of side effects, people with a history of low blood pressure should take the drug with caution.
Side Effects
People rarely discontinue using oxazepam because of side effects. Transient mild drowsiness is common for the first few days of therapy. If it persists, the dosage of the drug should be reduced. In a few instances, dizziness, vertigo, headache, or rarely fainting has occurred after taking the drug. Occasionally, the drug may cause excitement or stimulation during the first two weeks of therapy. Rarely, allergic reactions, nausea, vomiting, lethargy, swelling, slurred speech, tremor, changes in sex drive, white blood cell deficiency, and liver toxicity occur.
Pregnancy/Breast-Feeding
Oxazepam has not been formally studied in pregnant women. However, other benzodiazepines have caused serious birth defects when taken by pregnant women. Pregnant women are encouraged to discuss the benefits and potential risks of oxazepam with their physician before deciding to use the drug.
HIV may be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Oxazepam is excreted in breast milk and causes sedation in infants. Because of the potential risk of the drug, women should consider alternatives to breast-feeding while taking it.
Use In Children
Children over twelve years of age can use the lowest adult dosage, to be increased as necessary and tolerated. Little data are available regarding the use of the drug for children under twelve. The drug is not recommended for children under the age of six years because it has not been formally studied in them.
Use in the Elderly
Elderly people are more susceptible to the dose-related side effects of the drug and should use the reduced dosages listed above.
Drug Interactions
Oxazepam can cause additive central nervous system depression when used with anticonvulsants, antihistamines, alcohol, and other drugs that produce central nervous system depression. Cimetidine, isoniazid, and valproic acid may increase oxazepam levels in the blood, potentially increasing the risk of side effects. Oxazepam may reduce the effectiveness of oral contraceptives and increase the risk of phenytoin toxicity. Concomitant use of oxazepam with lithium may cause serious reductions in body temperature.
Food Interactions
None reported.
Other drugs used for similar conditions
Many different benzodiazepines are available for prescription use. They include lorazepam, diazepam, chlordiazepoxide, temazepam, flurazepam, and triazolam, among others. The drugs differ somewhat in the side effects they produce, their potencies, the time it takes them to work, and the tendency for them to cause withdrawal symptoms. Generally, oxazepam is considered to be one of the safer benzodiazepines.
Buspirone is an antianxiety medication that is not part of the benzodiazepine class. It is not addictive and is less likely to be sedating or to impair mental and physical alertness in people who take it. On the other hand, it needs to be taken many times each day and it is not effective for many people.
Paroxetine
Brand Name (Manufacturer)
Paxil (Smithkline Beecham)
Type of Drug
Psychoactive-antidepressant
Used For
Paroxetine is primarily used for the treatment of mental depression. It is also used to treat obsessive-compulsive disorder.
General Information
Paroxetine, an antidepressant belonging to a class known as serotonin reuptake inhibitors, is chemically unrelated to tricyclic, tetracyclic, or other known classes of antidepressants. It has become widely used because it is effective and tends to have fewer side effects than older antidepressants. It is available in 20-mg and 30-mg tablets.
Antidepressant medications are usually taken over long periods. It generally takes ten days of treatment before steady levels of paroxetine are built up in the blood, and it may take that long for the drug to have an effect on depression. In some people, it may take considerably longer.
Paroxetine accumulates in the body's tissues with prolonged use, and the drug may stay in the body for weeks after discontinuing therapy. It is especially important to wait at least two weeks after stopping the drug before taking an antidepressant that is a monoamine oxidase (MAO) inhibitor (e.g., phenelzine or tranylcypromine). Similarly, paroxetine should not be taken for at least two weeks after a MAO inhibitor is used.
In prolonged use, tolerance to paroxetine may develop over time, and the drug may lose its effectiveness.
Treatment
The recommended initial dose is 20 mg taken once a day, usually in the morning. Some people who do not respond to this dose may respond to dose increases, in 10-mg-per-day increments, up to a maximum of 50 mg per day. The dose increases should occur no more often than once a week.
The recommended initial dose for the elderly, debilitated, and/or people with kidney or liver impairment is 10 mg per day. In these people, the daily dose may be increased as necessary but should not to exceed 40 mg.
Cautions and Warnings
Paroxetine should not be used by anyone with a known allergy to it. The drug is broken down by the liver and excreted by the kidneys. People with liver or kidney disease should take it with caution. In a small number of people who suffer from mania, paroxetine cause a reactivation of the condition. Paroxetine should be used with caution by people with a history of seizure disorders.
Side Effects
Twenty-one percent of volunteers in clinical trials of paroxetine quit using the drug because of side effects. The most common side effects include nausea, sleepiness, insomnia, increased sweating, tremors, anxiety, agitation, abnormal ejaculation, diarrhea, dry mouth, and vomiting. Less common side effects include flushing, increased salivation, cold or clammy skin, dizziness, blood pressure changes, swelling, coldness in the hands or feet, rapid heartbeat, weakness, loss of coordination, headaches, acne, hair loss, dry skin, difficulty swallowing, stomach gas, joint pains, muscle pains, cramps and weakness, abnormal thinking patterns, blurred vision, bleeding between periods, weight changes, and lymph swelling.
Pregnancy/Breast-Feeding
Paroxetine has not been formally studied in pregnant women. In animal studies, the drug did not cause fetal harm, but it is not known whether this would be true for humans. Pregnant women are encouraged to discuss the benefits and potential risks of paroxetine with their physician before deciding to use the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Paroxetine is excreted in human milk. Because of the potential toxicity of the drug, women are encouraged to consider alternatives to breast-feeding while using it.
Use In Children
Paroxetine is not recommended for children because its safety and effectiveness have not been formally studied or established for them.
Use in the Elderly
Paroxetine is metabolized more slowly in the elderly than in younger people, and their blood levels of the drug are higher for a given dosage. Consequently, elderly people often require lower doses of the drug.
Drug Interactions
Paroxetine combined with tryptophan may cause headache, nausea, sweating, and dizziness. It is recommended that the two drugs not be taken together. Serious and fatal reactions may occur if paroxetine and monoamine oxidase (MAO) inhibitors are taken together. Paroxetine may increasing the anticoagulant effect of warfarin. Cimetidine may increase paroxetine blood levels. Phenobarbital or phenytoin may decrease paroxetine blood levels.
Coadministration of paroxetine with nortriptyline, amitriptyline, imipramine, desipramine, fluoxetine, thioridazine, propafenone, flecainide, and encainide may require dose adjustments in either drug used in the combination. Paroxetine may decrease procyclidine blood levels.
Food Interactions
Paroxetine may be taken with or without food.
Other drugs used for similar conditions
A number of other drugs are available for the treatment of depression. Fluoxetine and sertraline are other serotonin reuptake inhibitors that are effective. Monoamine oxidase inhibitors that are useful as antidepressants are tranylcypromine, phenelzine, and isocarboxazid. Tricyclic antidepressants include amoxapine, desipramine, nortriptyline, amitriptyline, and doxepin.
Each person may react differently to different antidepressants. The choice of drug usually depends on the individual's response to the drug, the drug's effectiveness, and side effects. People who do not benefit from one type of antidepressant may respond to another.
Perphenazine
Brand Names (Manufacturers)
Trilafon (Schering)
Perphenazine + Amitriptyline: Etrafon (Schering); Triavil (Merck)
Type of Drug
Psychoactive-antinausea, antivomiting, antipsychosis drug
Used For
Perphenazine is used to treat severe nausea and vomiting. It is also used to treat the symptoms of psychosis.
General Information
Perphenazine belongs to a class of psychoactive drugs called phenothiazines. Although the mechanism by which they work is unknown, they have potent effects on the central nervous system and other organs. They can reduce blood pressure, stop seizures, control nausea and vomiting, and control the symptoms of psychosis, a mental disorder characterized by difficulty thinking, recognizing reality, and acting rationally.
Perphenazine is available as tablets, oral concentrate, and solution for injection. It is also available in a number of combination products with the tricyclic antidepressant amitriptyline.
Treatment
The dosage is individualized and adjusted for each person's response. As with all psychoactive drugs, the lowest effective dose should be used to reduce the risk of side effects. The drug is generally started at a low dosage and increased as necessary and as tolerated. Adults usually take 8 to 16 mg a day, in divided doses for the treatment of nausea and vomiting. Doses up to 24 mg per day may be necessary. As soon as possible, the dosage should be reduced. Higher doses are used for the treatment of psychosis.
The oral concentrate should not be mixed with beverages containing caffeine (coffee, cola, etc.), tannic acid (tea), or pectinates (apple juice). It may be diluted with water, saline, homogenized milk, carbonated orange or pineapple drinks, apricot, prune, orange, tomato, or grapefruit juices.
Cautions and Warnings
Perphenazine should not be used by anyone with a known allergy to it. It should also not be used by people in comas, those with fevers above 104F, suspected or established brain damage, liver damage, or suppressed bone-marrow activity (as may occur when using AZT, ganciclovir, alpha interferon, or other drugs).
Perphenazine may increase the risk of seizures and should be used with caution in people with a history of seizures and those experiencing alcohol withdrawal symptoms.
Perphenazine may impair the mental and physical abilities necessary to operate an automobile or dangerous machinery.
Phenothiazines elevate blood levels of prolactin, a hormone involved in the production of breast milk. Because many breast cancers are stimulated by prolactin, perphenazine may aggravate existing breast cancers, but there is no evidence that it increases the risk of developing breast cancer.
Perphenazine should be used with caution by people who are exposed to phosphorus insecticides or extreme heat, because of the risk of serious side effects.
Side Effects
Drowsiness, stuffy nose, dizziness, blurred vision, tremors, and constipation are common side effects of perphenazine.
Tardive dyskinesia is a special neuromuscular side effect of phenothiazines. It is characterized by potentially irreversible, involuntary muscle movements that usually involve the tongue, face, mouth, lips, jaw, torso, and extremities. Although the side effect occurs most frequently among the elderly (especially elderly women), it is not possible to predict whether an individual will develop the disorder. The risk of the side effect and the likelihood it will be irreversible are believed to be increased with increased duration of treatment and cumulative dose.
Other neuromuscular side effects of phenothiazines include agitation, insomnia, muscle spasm, difficulty swallowing, and shuffling gait, among others.
Antipsychotic drugs, including perphenazine, can cause a potentially fatal side effect called neuroleptic malignant syndrome. The syndrome is characterized by high fever, muscle rigidity, altered mental status, irregular pulse or blood pressure, and abnormal heart rhythms. If these symptoms occur, the drug should be stopped and a physician contacted immediately.
Other side effects of perphenazine include low blood pressure or fluctuations in blood pressure, weight change, swelling in the extremities, allergic reactions, high fever, darkening of the skin, impaired vision, muscle weakness, and liver damage. In some cases, the drug has caused deficiencies in white blood cell counts.
Pregnancy/Breast-Feeding
Perphenazine has not been formally studied in pregnant women. It is usually not prescribed during pregnancy because its effects on the fetus are uncertain. Pregnant women are encouraged to discuss the benefits and potential risks of perphenazine with their physician before deciding to use the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Perphenazine is excreted in human milk, but its effects on nursing infants are not well understood.
Use In Children
Perphenazine is not recommended for children under twelve, because its safety and effectiveness in this population have not been studied or established.
Use in the Elderly
Older adults may be more susceptible to the side effects of the drug and may require reduced doses.
Drug Interactions
Perphenazine and other central nervous system depressants (narcotic analgesics, alcohol, antihistamines, sleeping pills, tranquilizers, and some antidepressants) may enhance the depressing effect of each other.
The use of alcohol with perphenazine may result in severe low blood pressure.
Antacids (including those in ddI tablets or powder) may interfere with absorption of perphenazine into the body. Perphenazine should be taken one hour before or after taking an antacid.
Food Interactions
Perphenazine may be taken with or without food. Foods with caffeine may interfere with the effects of perphenazine and should be avoided while taking the drug.
Other drugs used for similar conditions
For treatment or prevention of nausea and vomiting, a number of different types of drugs are available. Drugs used include metoclopramide, antihistamines (e.g., dimenhydrinate, meclizine, and promethazine), phenothiazines (e.g., prochlorperazine or thiethylperazine), granisetron, or ondansetron. The different types of drugs differ significantly in their side effects, and the choice of therapy is often determined by the side effects for which an individual is at risk.
Propranolol
Brand Name (Manufacturer)
Inderal (Wyeth-Ayerst)
Propranolol + Hydrochlorothiazide: Inderide (Wyeth-Ayerst)
Type of Drug
Psychoactive-beta-blocker
Used For
Propranolol is used most often for the treatment of high blood pressure, angina, and abnormal heart rhythms. It is also used to treat the symptoms of anxiety and to prevent migraine headaches.
General Information
Propranolol was the first beta-blocker available in the United States. Beta-blockers are drugs that interfere with nerve signals transmitted by the chemical norepinephrine. They reduce the force and speed of the heartbeat and prevent dilation of certain blood vessels. These actions reduce the work load on the heart, relieve the muscle tremors that often accompany anxiety, and reduce the blood pressure in the brain to prevent migraines.
Propranolol is available as tablets, long-acting capsules, and solution for injection.
Treatment
The dosage of propranolol must be adjusted for the condition and each individual person. When used orally, common dosages range from 40 to 320 mg per day. Dosages in the lower end of the range are usually prescribed for anxiety or the prevention of migraines. Angina, hypertension, and irregular heart rhythms are generally treated with higher dosages.
Cautions and Warnings
Propranolol should not be used by anyone with a known allergy to it. It should also not be used by anyone with certain heart conditions such as congestive heart failure.
People with angina who abruptly stop propranolol may experience heart attacks or more severe angina. When discontinuing the drug, its dosage should be tapered off with the guidance of a physician.
In general, people with bronchial diseases such as bronchial asthma, chronic bronchitis, or emphysema should not use propranolol because the drug may cause severe difficulty in breathing.
Because propranolol affects the body's sugar metabolism, it should be used with caution in people with diabetes or hypoglycemia (low blood sugar). Propranolol may mask certain clinical signs of thyroid disease and interfere with thyroid-function tests. Similarly, propranolol may interfere with tests for glaucoma.
Because of the risk of side effects, propranolol should be used with caution in people with impaired kidney or liver function.
Side Effects
Lethargy and cold hands and feet are common side effects of propranolol. Less common side effects include irregular heartbeat or rhythm, heart failure, low blood pressure, light-headedness, insomnia, weakness, fatigue, mental depression, visual disturbances, hallucinations, nightmares/vivid dreams, disorientation, short-term memory loss, emotional swings, clouded senses, nausea, vomiting, stomach irritation, cramping, diarrhea, constipation, allergic reactions, difficulty breathing, bone-marrow toxicity, hair loss, dry eyes, and impotence.
Pregnancy/Breast-Feeding
Propranolol has not been formally studied in pregnant women. In animal studies, it caused spontaneous abortions when administered at ten times the maximum human dose. It is not known whether the drug causes birth defects in humans. Pregnant women are encouraged to discuss the benefits and potential risks of propranolol with their physician before deciding to use the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Propranolol passes into breast milk, but at normal doses, side effects in nursing babies are uncommon.
Use In Children
The oral forms of propranolol are used in children. The usual pediatric dosage range is 2 to 4 mg per kg of body weight per day, in two equally divided doses. Doses above 16 mg per kg per day should not be used in children.
Use in the Elderly
No changes in dosage or administration are required for older adults.
Drug Interactions
Propranolol may intensify the effects of reserpine, potentially causing severe side effects. Haloperidol used in combination with propranolol may cause low blood pressure and heart attack.
Propranolol may increase blood levels of chlorpromazine, antipyrine, lidocaine, and theophylline. Chlorpromazine and cimetidine may increase propranolol blood levels. Phenytoin, phenobarbitone, indomethacin, and rifampin may reduce blood levels of propranolol.
Aluminum hydroxide antacids and alcohol interfere with the absorption of propranolol into the body.
Food Interactions
To maintain the most consistent blood levels of propranolol, it should be taken the same time every day on an empty stomach.
Other drugs used for similar conditions
Other beta-blockers include sotalol, timolol, carteolol, and penbutolol. For treatment or prevention of nausea and vomiting, a number of different types of drugs are available. Drugs used include metoclopramide, antihistamines (e.g., dimenhydrinate, meclizine, and promethazine), phenothiazines (e.g., prochlorperazine or thiethylperazine), and serotonin uptake inhibitors (e.g., granisetron or ondansetron). The different types of drugs differ significantly in their side effects, and the choice of therapy is often determined by the side effects for which an individual is at risk.
Protriptyline
Brand Name (Manufacturer)
Vivactil (Merck)
Type of Drug
Psychoactive-tricyclic antidepressant
Used For
Protriptyline is used for the relief of symptoms of mental depression.
General Information
Protriptyline belongs to a class of drugs known as tricyclic antidepressants. It is chemically unrelated to other classes of antidepressants, including monoamine oxidase (MAO) inhibitors. It is thought to work by increasing the concentrations of neurotransmitters called serotonin and norepinephrine in the brain.
Tricyclic antidepressants are usually taken over long periods. It takes weeks for steady levels of protriptyline to build up in the blood, and it may take up to a month for the drug to have an effect on depression.
Protriptyline is available as tablets for oral administration.
Treatment
To prevent side effects, the dosage of the drug should initially be low and increased as necessary until improvement, as long as there are no serious side effects.
The recommended initial dosage for treatment of depression in adults is 15 to 40 mg a day, divided into three or four doses. When satisfactory improvement has been reached, the dosage should be reduced to the smallest amount that will maintain relief of the symptoms. Lower doses (15 mg per day to start) are recommended for elderly adults.
Cautions and Warnings
Protriptyline should not be used by anyone with a known allergy to it. It should also not be used by people recovering from heart attacks. Because of the risk of serious side effects, protriptyline should not be used in combination with antidepressants of the monoamine oxidase (MAO) inhibitor class.
When protriptyline replaces an MAO inhibitor for treatment of depression, a minimum of fourteen days should elapse after stopping the MAO inhibitor before starting therapy with protriptyline. Protriptyline should be started cautiously with a gradual increase in dose until a response is achieved.
Protriptyline should be used with caution in people with a history of seizures, difficulty urinating, or glaucoma. People with thyroid disease or those receiving thyroid medication should not use protriptyline because of the risk of heart toxicity.
Protriptyline may increase the hazards of concurrent electroshock therapy. Similarly, when possible, the drug should be discontinued several days before surgery.
Protriptyline may impair the mental and physical abilities necessary to drive an automobile or operate dangerous machinery.
Rapidly stopping protriptyline may cause withdrawal symptoms, including nausea, headache, and a sickly feeling.
Side Effects
The most common side effects of protriptyline include rapid heartbeat, fainting when getting up quickly, sedation, blurred vision, disorientation, confusion, hallucinations, muscle spasms, seizures, dry mouth, constipation, difficulty urinating, and sensitivity to bright light or sunlight.
Other potential side effects include heart attack, stroke, changes in blood pressure, palpitations, delusions, anxiety, restlessness, agitation, panic, nightmares, numbness, tingling or pain in the extremities, weakness, fatigue, headache, allergic reactions, bone-marrow toxicity, nausea, vomiting, loss of appetite, stomach upset, diarrhea, peculiar taste, blackened tongue, impotence, changes in sex drive, jaundice, hair loss, weight change, frequent urinating, altered blood-sugar levels, and increased perspiration.
Pregnancy/Breast-Feeding
Protriptyline has not been formally studied in pregnant women. Protriptyline crosses the placenta. There have been reports of birth defects when the drug was taken during the first three months of pregnancy and severe side effects in newborns whose mothers took the drug during delivery. Pregnant women are encouraged to discuss the benefits and potential risks of protriptyline with their physician before deciding to use the drug.
HIV can be passed from a woman to her child through breast milk. In areas where nutritional alternatives are readily available, breast-feeding is discouraged for HIV-positive women. Protriptyline is excreted in human milk. Because of the potential toxicity of the drug for newborns, women are encouraged to consider alternatives to breast-feeding while taking it.
Use In Children
Protriptyline is not recommended for children because its safety and efficacy has not been formally established for them in clinical trials.
Use in the Elderly
Older adults may be more susceptible to the side effects of protriptyline. If they use the drug, it is usually at reduced dosages, as described above.
Drug Interactions
Protriptyline may interfere with the effect of blood-pressure medications such as guanethidine or clonidine. Taking protriptyline and thyroid drugs together may intensify the effects of both drugs.
Oral contraceptives and cigarette smoking may decrease the effect of protriptyline. Estrogens can increase or decrease the effect of protriptyline.
Bicarbonate of soda, acetazolamide, quinidine, and procainamide may increase the effect of protriptyline. Methylphenidate, cimetidine, and phenothiazines (perphenazine, prochlorperazine, etc.) may increase blood levels of protriptyline, potentially increasing the risk of its side effects.
Protriptyline may increase the effect of other central nervous system depressants including alcohol, sleeping pills, narcotic pain relievers, tranquilizers, barbiturates, and antihistamines.
Food Interactions
Protriptyline may be taken with or without food.
Other drugs used for similar conditions
For treatment of depression, there are many options, including other tricyclic antidepressants (desipramine, amitriptyline, nortriptyline, amoxapine, maprotiline, imipramine, trimipramine, doxepin), MAO inhibitors (tranylcypromine, phenelzine, isocarboxazid), serotonin reuptake inhibitors (fluoxetine, paroxetine, and sertraline), and stimulants such as methylphenidate. The appropriate choice varies from person to person and depends on age, physical health and condition, and other drugs being concurrently used.
Desipramine is often the first choice among tricyclic antidepressants because it is effective and has relatively few side effects in most people. Protriptyline is more likely to cause abnormal heart rhythms or low blood pressure and to aggravate agitation and anxiety than other antidepressants.
