Drug | Bioavailability (%) | Time to peak plasma concentration (hours) | Primary metabolism* | Active metabolite(s) | Elimination half-life (hours) | Effect on drug metabolism (significant)* | Clearance |
Agomelatine¶ | <5 Wide inter-individual variation; unaffected by food | 1 to 2 | CYP1A2 Avoid use with moderate or strong inhibitors of CYP1A2 | No | 1 to 2 | None | Hepatic; avoid use in setting of hepatic impairment or active liver disease |
Bupropion | Not available; modestly increased by food | Immediate release: 2 Sustained release: 3 Extended release: 5 | CYP2B6 UGT glucuronidation | Yes (hydroxybupropion and others) | 14 (parent, immediate release) 20 (parent, extended release) 21-51 (active metabolites) | Inhibits CYP2D6 (strong) | Hepatic and renal; dose adjustment may be needed in setting of renal or hepatic insufficiency |
Mirtazapine | 50 Unaffected by food | 2 | CYP1A2 CYP2D6 CYP3A4 | Yes (N-desmethyl mirtazapine) | 20 to 40 (parent) 25 (active metabolite) T ½ and serum concentrations are increased in female and older subjects | None | Hepatic and renal; dose adjustment may be needed in setting of renal or hepatic insufficiency |
CYP: cytochrome P450; UGT: uridine diphosphate glucuronosyltransferase.
* Drug interactions and management suggestions may be determined by use of the drug interactions program included within UpToDate.
¶ Not available in the United States.
Data from: UpToDate Lexidrug. More information available at https://online.lexi.com/.
Additional data from: