HIV 101: Summary of Antiretroviral Agents Dosing and Administration Recommendations
By HEPP News Staff
From Brown Medical School
November 2001
Adapted from Bartlett J.G. and Gallant J.E. 2001-2002 Medical Management of HIV Infection. Johns Hopkins University, Baltimore, MD. 2001. Additional information from http://www.gilead.com/pdf/viread_pi.pdf.
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Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
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Zidovudine
(AZT, ZDV, Retrovir) |
Didanosine
(ddl, Videx, Videx EC) |
Zalcitabine
(ddC, Hivid) |
Stavudine
(d4T, Zerit) |
Lamivudine
(3TC, Epivir) |
Abacavir
(ABC, Ziagen) |
Tenofovir
(Viread) |
| Recommended Dose |
300 mg bid (or with 3TC as Combivir 1 tab bid) |
Tablets or oral solution >60kg: 400 mg qd (EC) or 200 mg bid (tabs) or 250 mg bid (powder) <60kg: 250 mg qd or 125 mg bid (tabs) or 167 mg bid (powder)
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0.75 mg tid |
>60kg: 40 mg bid <60kg: 30 mg bid
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150 mg bid or with AZT as Combivir (1 tab bid) <50kg: 2 mg/kg bid) |
300 mg bid |
(Nucleotide analog) 300 mg once daily |
| Food Effect |
None |
Levels  55% Take 1 hr before or 1 hr after meal
|
None |
None |
None |
NoneAdvertisementAlcohol  ABC levels 41%
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Should be taken with a meal |
Major Toxicity
Class Toxicity |
Bone marrow suppression: anemia and/or neutropenia Subjective complaints: GI intolerance, headache, insomnia, asthenia
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Pancreatitis Peripheral neuropathy
GI intolerance, nausea, diarrhea
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Peripheral neuropathy Stomatitis
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Peripheral neuropathy |
(Minimal toxicity) |
Hypersensitivity (2-5%), fever, nausea, vomiting, anorexia, cough, dyspena, malaise, morbilliform rash. May be life-threatening with rechallenge.
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Bone (in animals) Renal (in animals)
Mild to moderate gastrointestinal: nausea, vomiting, diarrhea, flatulence
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| Drug Interaction |
Ribavirin may reduce AZT activity |
Methadone ddI levels 41%, consider ddI dose increase
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Methadone ddI levels 27%. No dose adjustment
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None |
None |
None |
Take two hours before or one hour after didanosine (if applicable)
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Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
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Nevirapine
(Viramune) |
Delavirdine
(Rescriptor) |
Efavirenz
(Sustiva) |
| Recommended Dose |
200 mg po qd x 14 days, then 200 mg po bid |
400 mg po tid |
600 mg po qd at hs |
| Food Effect |
None |
None |
-50% with high fat meal; avoid after high fat meal |
| Drug Interaction |
Induces cytochrome P450 enzymes PI interactions see Table 4-16 in Bartlett Guide*
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Methadone AUC decreased 60% titrate methadone dose Not recommended: Ketoconazole and rifampin
Caution: anticonvulsant
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Inhibits and induces cytochrome P450 3A4 enzymes Contraindicated drugs: astemizole, midazolam, triazolam, cisapride, ergot alkaloids, tergenadine
PI interactions: generally dose when given with PIs (like Kaletra) and see Table 4-16 in Bartlett Guide*
Possibly important drug interactions: see Chapter 4 in Bartlett Guide*
Methadone AUC decreased 60% titrate methadone dose
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Major Toxicity
Class Toxicity |
Rash (15-30%) may require hospitalization; rare cases of Stevens-Johnson syndrome; hepatitis |
Rash; headaches Increased transaminase levels
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Dizziness, "disconnectedness," somnolence, insomnia, bad dreams, confusion, amnesia, agitation, hallucinations, poor concentration 40% usually resolves after 2 weeks
Take hs.
Rash -- severe in 5%; rare reports of Stevens-Johnson syndrome.
Teratogenic in cynomalgus monkeys
Avoid in pregnancy, and women and men should use adequate contraception methods.
False positive drug screening test for cannabinoids (marijuana)
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Protease Inhibitors (PIs)
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Indinavir**
(Crixivan) |
Ritonavir
(Norvir) |
Saquinavir** |
Amprenavir
(Agenerase) |
Nelfinavir
(Viracept) |
Lopinavir + Ritonavir
(Kaletra) |
| (Invirase) |
(Fortovase) |
| Recommended Dose |
800 mg q 8h
Separated ddI dose by 1 hr |
600 mg bid
Separate ddI dose by 2 hr |
Not recommended as single PI 400 mg bid with RTV |
1,200 mg tid |
1,200 mg bid (caps)
1400 mg bid (oral solution) |
1,250 mg bid or 750 mg tid |
3 caps or 0.5mL twice daily
4 caps bid when used with efavirenz or nevirapine |
| Food Effect |
77%; take 1 hr before or 2 hours after meals; may take with low fat snack or skim milk |
15%; take with food if possible to improve tolerability |
No food effect when taken with RTV |
6x; take with large meal unless taken with RTV |
High fat meal decreases AUC 20%; can be taken with or without food, but high fat meal should be avoided |
2-3x; take with meal or snack |
Fat increases AUC 50% to 80%; should be taken with food |
| Side Effects* |
GI intolerance (10-15%); nephrolithiasis or nephrotoxicity (10-15%); headache; asthenia; dizziness; rash; metallic taste; ITP; alopecia; lab: increase indirect bilirubinemia (inconsequential) Class side effects*
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GI intolerance (20-40%); paresthesias-circum-oral and extremities (10%); taste perversion (10%); lab: triglycerides increase in 60% and transaminase increase in 10-15%, CPK and uric acid increase Class side effects*
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GI intolerance (10-20%); increase Class side effects*
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GI intolerance (20-30%); headache; hypoglycemia; transaminase increase Class side effects*
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GI intolerance (10-30%); rash (20-25% -- usually at 1-10 wks), Stevens-Johnson syndrome (1%); paresthesias (10-30% -- perioral or peripheral) Increase in liver function tests. Class side effects*
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Diarrhea (10-30%) Class side effects*
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GI intolerance: nausea, vomiting, diarrhea Elevated Lipids Asthenia Class side effects*
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* For full information on toxicity and drug interactions for PIs and class side effects, see Chapter 4 of Bartlett J.G. and Gallant J.E. 2001-2002 Medical Management of HIV Infection. Johns Hopkins University, Baltimore, MD. 2001. For information on tenofovir, see www.gilead.com/pdf/viread_pi.pdf.
** These two drugs usually used in combination with ritonavir (see HEPP News, February 2001).
Back to the HEPP News November 2001 contents page.
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