Effect of Food on Antiretroviral Pharmacokinetics

Patrick Smith, Pharm.D.

Clinical Assistant Professor, Department of Pharmacy Practice
School of Pharmacy and Pharmaceutical Sciences
University at Buffalo
E-mail: pfsmith@buffalo.edu

Protease Inhibitors

Drug	Recommendation	Tmax	Cmax	AUC
Amprenavir	with or without food, but not a high-fat meal	0.5h (44%)	36%	21%
Indinavir	1 h before or 2 h after a meal		84%	77%
Nelfinavir	with a meal or light snack		2-3 fold	2-3 fold
Ritonavir	with a meal			15%
Saquinavira	with a meal or up to 2 h after a meal			670%

Abbreviations: increases with food; decreases with food; h, hour; min, minutes.
^a Both formulations: Fortovase and Invirase.

Nucleoside Reverse Transcriptase Inhibitors

Drug	Recommendation	Tmax	Cmax	AUC
Abacavir
Didanosine	empty stomach, 30 min before or 2 h after a meal		55% (tab); 46% (EC cap)	55% (tab); 19% (EC cap)
Lamivudine	with or without food	2.3h (255%)	40%	no significant difference
Stavudine
Zalcitabine	empty stomach	2-fold	39%	14%
Zidovudine	30 min before or 1 h after a meal		>50%

Abbreviations: increases with food; decreases with food; h, hour; min, minutes; tab, tablet; EC cap, enteric coated capsule.

Non-Nucleoside Reverse Transcriptase Inhibitors

Drug	Recommendation	Tmax	Cmax	AUC
Delavirdine	with or without food
Efavirenz	with or without food, avoid high-fat meal			50% with a high-fat meal
Nevirapine	with or without food			Comparable to fasting

Abbreviations: increases with food; decreases with food