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©2013 UpToDate ® Print Email Atypical antidepressants - Pharmacokinetics Drug Bioavailability (percent) 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 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 Lexi-Interact, the drug interactions program included with UpToDate. • Not available in the United States. Data from: Spina E, Trifirò G, Caraci F. Clinically significant drug interactions with newer antidepressants. CNS Drugs 2012; 26:39. Jefferson JW, Pradko JF, Muir KT. Bupropion for major depressive disorder: Pharmacokinetic and formulation considerations. Clin Ther 2005; 27:1685. McAllister-Williams RH, Baldwin DS, Haddad PM, Bazire S. The use of antidepressants in clinical practice: focus on agomelatine. Hum Psychopharmacol 2010; 25:95. Croom KF, Perry CM, Plosker GL. Mirtazapine: a review of its use in major depression and other psychiatric disorders. CNS Drugs 2009; 23:427.