Venlafaxine
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| Trade names | Effexor XR, Effexor, Trevilor, Lanvexin |
| AHFS/Drugs.com | Monograph |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | 42±15% |
| Protein binding | 27±2% (parent compound), 30±12% (active metabolite, desvenlafaxine) |
| Metabolism | Hepatic (~50% of the parent compound is metabolised on first pass through the liver) |
| Biological half-life | 5±2 h (parent compound for immediate release preparations), 15±6 h (parent compound for extended release preparations), 11±2 h (active metabolite) |
| Excretion | Renal (87%; 5% as unchanged drug; 29% as desvenlafaxine and 53% as other metabolites) |
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| ECHA InfoCard | 100.122.418 |
| Chemical and physical data | |
| Formula | C17H27NO2 |
| Molar mass | 277.402 g/mol |
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| Chirality | Racemic mixture |
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Venlafaxine — brand names: Effexor, Effexor XR, Lanvexin, Viepax and Trevilor — is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. This means it increases the concentrations of the neurotransmitters serotonin and norepinephrine in the body and the brain. First introduced by Wyeth in 1993, now marketed by Pfizer, it is licensed for the treatment of major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.
A comparative meta-analysis of 12 major antidepressants found that venlafaxine, mirtazapine, escitalopram, and sertraline were significantly more efficacious than duloxetine, fluoxetine, fluvoxamine, paroxetine, and reboxetine. A combination of venlafaxine and mirtazapine achieved remission rates (defined as a HAM-D score of 7 or less) of 58% in one controlled trial. In combination with an antipsychotic medicine aripiprazole, better results in treatment resistant depression in older adults have been demonstrated.
The rate of life-threatening or lethal outcomes for suicidal overdoses of venlafaxine is lower than for the TCAs, MAOIs, and bupropion but higher than all of the SSRIs, and equal to citalopram. It is metabolised in the body into another antidepressant drug called desvenlafaxine (O-desmethylvenlafaxine) which is also sold as an antidepressant, under the brand name Pristiq.
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