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خرید پکیج
تعداد آیتم قابل مشاهده باقیمانده : -7 مورد

Atypical antidepressants: Pharmacokinetics

Atypical antidepressants: Pharmacokinetics
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
These classifications are based upon US Food and Drug Administration (FDA) guidance.[1,2] Other sources may use a different classification system resulting in some agents being classified differently.

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.

References:
  1. Clinical drug interaction studies — Cytochrome P450 enzyme- and transporter-mediated drug interactions: Final guidance for industry. US Food & Drug Administration. https://www.fda.gov/media/135586/download (Accessed on May 26, 2020).
  2. Drug development and drug interactions: Table of substrates, inhibitors and inducers. US Food & Drug Administration. https://www.fda.gov/drugs/drug-interactions-labeling/drug-development-and-drug-interactions-table-substrates-inhibitors-and-inducers (Accessed on October 9, 2019).

Data from: UpToDate Lexidrug. More information available at https://online.lexi.com/.

Additional 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.
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