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Appendix XII: Drug Interactions Between ARV Agents and Recreational Drugs

Updated February 2009

Table 1: Drug Interactions With ARV Agents and Recreational Drugs
Substance Route of Elimination Effect when Combined with ARV Therapy Agents
Alcohol Metabolized by alcohol dehydrogenase ↑ ABC AUC 41% – Clinical significance likely minimal
Amphetamines Metabolized by CYP2D6 Toxicity may be potentiated by ritonavir (low- or full-dose)
Barbiturates Several are metabolized by CYP3A4 and induce CYP3A4 May ↓ PIs, NNRTIs, MVC, and RAL. Avoid co-administration or use with close monitoring.
Benzodiazepines Several are metabolized by CYP3A4 (midazolam,
triazolam)		 Oral midazolam and
triazolam are contraindicated with PIs, EFV, and DLV. IV midazolam may be
co-administered with very close monitoring. Consider alternative benzodiazepines (lorazepam, oxazepam, or temazepam) with ARV therapy co-administration.
Cocaine Minor metabolism by CYP3A4 to hepatotoxic metabolite None known
Gamma hydroxybutyrate
(GHB)		 Metabolized by CYP2D6
Eliminated via first pass metabolism		 RTV and other boosted PIs may precipitate life-threatening toxicity when GHB used concurrently
Heroin Metabolized to morphine, then to morphine-6-glucuronide via glucuronidation None known
Ketamine Metabolized via CYP2B6, 3A4, and 2C9 PIs, DLV, and ETR may
significantly ↑ ketamine serum concentrations
Marijuana Metabolized via hydroxylation, some involvement of CYP3A4, 2C9, and 2C6 Effect of smoked marijuana and oral tablets on IDV or NFV concentrations not clinically significant
Meperidine Metabolized via hydroxylation and CYP450, CYP2D6, and CYP1A2 Ritonavir associated with ↓ meperidine AUC by 67% and ↑ normeperidine AUC by 47%. Avoid co-administration with any boosted PI.
Methylenedioxy-methamphetamine (MDMA) Metabolized via CYP2D6 RTV and other boosted PIs may precipitate life-threatening toxicity when MDMA used concurrently
Morphine Metabolism via glucuronidation None known
Oxycodone Metabolized via CYP2D6 to oxymorphone CYP3A4 to noroxycodone ketoreductase None known
PCP Metabolized via CYP3A, 2C11; inhibits CYP2B1 PIs and DLV may significantly ↑ PCP serum concentrations
ABC, abacavir; DLV, delavirdine; EFV, efavirenz; ETR, etravirine; IDV, indinavir; MVC, maraviroc; NFV, nelfinavir; NNRTI, Non-nucleoside Reverse Transcriptase Inhibitor; PI, Protease Inhibitor; RAL, raltegravir; RTV, ritonavir.