CIPLADOC - AIDS Update - DRUGS THAT SHOULD NOT BE USED WITH ANTIRETROVIRALS

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DRUG INTERACTIONS IN HIV THERAPY
A Clinician's Guide

DRUGS THAT SHOULD NOT BE USED WITH ANTIRETROVIRALS

a) Protease inhibitors

ü= may be used; x = not to be used

Drug Category	Indinavir	Ritonavir**	Saquinavir	Nelfinavir	Amprenavir	Lopinavir + Ritonavir
Ca++ channel blocker	ü	xBepridil	ü	ü	xBepridil	(none)
Cardiac	ü	xAmiodarone, flecainide, propafenone, quinidine	ü	ü	ü	Flecainide propafenone
Lipid Lowering Agents	xSimvastatin, lovastatin	xSimvastatin, lovastatin	xSimvastatin, lovastatin	xSimvastatin, lovastatin	xSimvastatin, lovastatin	xSimvastatin, lovastatin
Anti- Mycobacterial	xRifampin	ü	xRifampin rifabutin	xRifampin	xRifampin	xRifampin
Antihistamine	xAstemizole, terfenadine	xAstemizole, terfenadine	xAstemizole, terfenadine	xAstemizole, terfenadine	xAstemizole, terfenadine	xAstemizole, terfenadine
Gastrointestinal Drugs	XCisapride***	XCisapride***	XCisapride***	XCisapride***	XCisapride***	XCisapride***
Neuroleptic	ü	XClozapine, pimozide	ü	ü	ü	xPimozide
Psychotropic	xMidazolam, triazolam	xMidazolam, triazolam	xMidazolam, triazolam	xMidazolam, triazolam	xMidazolam, triazolam	xMidazolam, triazolam
Ergot Alkaloids (vasoconstrictor)	xDihydroergo -tamine (D.H.E.45), ergotamine* (various forms)	xDihydroergo -tamine (D.H.E.45), ergotamine* (various forms)	xDihydroergo -tamine (D.H.E.45), ergotamine* (various forms)	xDihydroergo -tamine (D.H.E.45), ergotamine* (various forms)	xDihydroergo -tamine (D.H.E.45), ergotamine* (various forms)	xDihydroergo -tamine (D.H.E.45), ergotamine* (various forms)

**     Some of the contraindicated drugs listed are based on theoretical considerations. Thus, drugs         with low therapeutic indices yet with suspected major metabolic contribution from cytochrome         P450 3A, CYP2D6, or unknown pathways are included in this table. Actual interactions may or         may not occur in patients.
*     This is likely to be a class effect.
***   Cisapride has been withdrawn from the market by the US FDA.

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b) Non-nucleoside reverse transcriptase inhibitors

ü= may be used; x = not to be used

Drug Category	Nevirapine	Delavirdine	Efavirenz
Ca++ channel blocker	ü	ü	ü
Cardiac	ü	ü	ü
Lipid Lowering Agents	ü	xSimvastatin, lovastatin	ü
Anti-Mycobacterial	Insufficient data	xRifampin, rifabutin	ü
Antihistamine	ü	xAstemizole, terfenadine	xAstemizole, terfenadine
Gastrointestinal Drugs	ü	XCisapride H2 blockers, Proton pump inhibitors	XCisapride*
Neuroleptic Psychotropic	ü ü	ü xMidazolam, triazolam	ü xMidazolam, triazolam
Ergot Alkaloids (Vasoconstrictor)	ü	xDihydroergotamine (D.H.E.45), ergotamine* (various forms)	xDihydroergotamine (D.H.E.45), ergotamine* (various forms)

* This is likely a class effect

Suggested Alternatives

Simvastatin, lovastatin: atorvastatin, pravastatin, fluvastatin, cerivastatin (alternatives should be used with caution).
Rifabutin: clarithromycin, azithromycin (MAI prophylaxis); clarithromycin, ethambutol (MAI treatment).
Astemizole, terfenadine: loratidine, fexofenadine, cetirizine
Midazolam, triazolam: temazepam, lorazepam

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