Brown Medical School

HIV 101: Summary of Antiretroviral Agents Dosing and Administration Recommendations

By HEPP News Staff

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.

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
	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)	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	None	None	None	None Alcohol ABC levels 41%	Should be taken with a meal
Major Toxicity Class Toxicity	Bone marrow suppression: anemia and/or neutropenia Advertisement Subjective complaints: GI intolerance, headache, insomnia, asthenia	Pancreatitis Peripheral neuropathy GI intolerance, nausea, diarrhea	Peripheral neuropathy Stomatitis	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)
	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*	Methadone AUC decreased 60% titrate methadone dose Not recommended: Ketoconazole and rifampin Caution: anticonvulsant	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
Major Toxicity Class Toxicity	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 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)

Protease Inhibitors (PIs)
	Indinavir** (Crixivan)	Ritonavir (Norvir)	Saquinavir**		Amprenavir (Agenerase)	Nelfinavir (Viracept)	Lopinavir + Ritonavir (Kaletra)
	Indinavir** (Crixivan)	Ritonavir (Norvir)	(Invirase)	(Fortovase)	Amprenavir (Agenerase)	Nelfinavir (Viracept)	Lopinavir + Ritonavir (Kaletra)
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).

Back to the HEPP News November 2001 contents page.

This article was provided by Brown Medical School. It is a part of the publication HEPP News.

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