HIV 101: Summary of Antiretroviral Agents Dosing and Administration Recommendations
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.
|Nucleoside Reverse Transcriptase Inhibitors (NRTIs)|
(AZT, ZDV, Retrovir)
(ddl, Videx, Videx EC)
|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)
||0.75 mg tid||>60kg: 40 mg bid|
<60kg: 30 mg bid
|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
Alcohol ABC levels 41%
|Should be taken with a meal|
|Bone marrow suppression: anemia and/or neutropeniaAdvertisementSubjective complaints: GI intolerance, headache, insomnia, asthenia
GI intolerance, nausea, diarrhea
|Peripheral neuropathy||(Minimal toxicity)||Hypersensitivity (2-5%), fever, nausea, vomiting, anorexia, cough, dyspena, malaise, morbilliform rash. May be life-threatening with rechallenge.
||Bone (in animals)|
Renal (in animals)
Mild to moderate gastrointestinal: nausea, vomiting, diarrhea, flatulence
|Drug Interaction||Ribavirin may reduce AZT activity||Methadone ddI levels 41%, consider ddI dose increase
||Methadone ddI levels 27%. No dose adjustment
||None||None||None||Take two hours before or one hour after didanosine (if applicable)
|Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)|
|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*
|Methadone AUC decreased 60% titrate methadone dose|
Not recommended: Ketoconazole and rifampin
|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
|Rash (15-30%) may require hospitalization; rare cases of Stevens-Johnson syndrome; hepatitis||Rash; headaches|
Increased transaminase levels
|Dizziness, "disconnectedness," somnolence, insomnia, bad dreams, confusion, amnesia, agitation, hallucinations, poor concentration |
40% usually resolves after 2 weeks
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)
|Protease Inhibitors (PIs)|
|Lopinavir + Ritonavir|
|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*||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*||GI intolerance (10-20%); increase Class side effects*||GI intolerance (20-30%); headache; hypoglycemia; transaminase increase Class side effects*||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*||Diarrhea (10-30%) Class side effects*||GI intolerance: nausea, vomiting, diarrhea Elevated Lipids Asthenia Class side effects*|
* 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).
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