Table 1.
Enzymes and HAART Agents.
| Drugs | Class | Substrate | Inhibit | Induce | References |
|---|---|---|---|---|---|
| Abacavir (Ziagen) | NRTI | ALDH | 11,12 | ||
| Amprenavir (Agenerase) | PI | CYP3A4 | CYP3A4 | 13-15 | |
| Atazanavir (Reyataz) | PI | CYP3A4 | CYP3A4, UGT1A1, CYP2C8 | 16-19 | |
| Delavirdine (Rescriptor) | NNRTI | CYP3A4 CYP2D6 |
CYP3A4 CYP2C9 CYP2C19 CYP2D6 |
20 | |
| Didanosine (Videx) | NRTI | 21,22 | |||
| Efavirenz (Sustiva) | NNRTI | CYP2B6 | CYP2B6 | CYP3A4 | 23-26 |
| Indinavir (Crixivan) | PI | CYP3A4 | CYP3A4 UGT1A1 |
15,17, 27-29 | |
| Lamivudine (Epivir) | NRTI | 30,31 | |||
| Lopinavir | PI | CYP3A4 | 32-34 | ||
| Maraviroc (Selzentry) | C5I | CYP3A4 | CYP2D6 | 35,36 | |
| Nelfinavir (Viracept) | PI | CYP3A4, CYP2C19 | CYP3A4 CYP2B6 |
15,37,38 | |
| Nevirapine (Viramune) | NNRTI | CYP3A4 CYP2B6 |
CYP3A4 CYP2B6 |
39,40 | |
| Raltegravir (Isentress) | IGI | UGT1A1 | 41-43 | ||
| Ritonavir (Norvir) | PI | CYP3A4 CYP2D6 |
CYP3A4 CYP2D6 CYP2B6 |
CYP2C9 | 28,44,45 |
| Saquinavir (Invirase) | PI | CYP3A4 | CYP3A4 | 15, 46-48 | |
| Stavudine (Zerit) | NRTI | 49 | |||
| Tenofovir (Viread) | NtRTI | CYP3A4 | 50,51 | ||
| Tipranavir (Aptivus) | PI | CYP3A4 | CYP1A2 CYP2C9, CYP2C19, CYP2D6 |
52,53 | |
| Zalcitabine (ddC) | NRTI | 54 | |||
| Zidovudine (AZT) | NRTI | UGTB7 | 55-57 |
Enzymes that are known to metabolize commonly used HAART agents are listed, as well as enzymes that are inhibited or induced by each agent. If a HAART drug inhibits a metabolizing enzyme, then blood levels of other drugs that are substrates for that same enzyme may be increased. Likewise, if a HAART agent inducing the expression or function of an enzyme, than drugs that are substrates for that same enzyme will be more rapidly metabolized and eliminated.
Abbreviations : NNRTI - non-nucleoside reverse transcriptase inhibitor; NRTI - nucloeside reverse transcriptase inhibitor; PI - protease inhibitor; IGI - integrase inhibitor; C5I - CCR5 nhibitor; ALDH - Alcohol dehydrogenase.