Venlafaxine


Description

Venlafaxine (Effexor) is an antidepressant within the serotonin-norepinephrine reuptake inhibitor (SNRI) class of medications. It exerts its effects primarily by blocking the transporters involved in the reuptake of the neurotransmitters serotonin an...

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Pharmacology

Indication

Venlafaxine is indicated in the management of major depressive disorder (MDD), generalized anxiety d... Read more

Pharmacodynamic

The mechanism of venlafaxine's (and its metabolite, O-desmethylvenlafaxine (ODV)) antidepressant eff... Read more

Mechanism of action

The exact mechanism of action of venlafaxine is unknown, but appears to be associated with the poten... Read more

Absorption

Venlafaxine is well absorbed, with at least 92% of a single dose absorbed on the basis of mass balan... Read more

Protein binding

The degree of binding of venlafaxine to human plasma is 27% ± 2% at concentrations ranging from 2.5... Read more

Volume of distribution

7.5 ± 3.7 L/kg [venlafaxine]5.7 ± 1.8 L/kg [O-desmethylvenlafaxine(active metabolite)]

Clearance

Steady state plasma clearance, venlafaxine = 1.3 ± 0.6 L/h/kg;Steady state plasma clearance, ODV =... Read more

Half life

5 hours

Route of elimination

Renal elimination of venlafaxine and its metabolites is the primary route of excretion. Approximatel... Read more

Toxicity

Overdose of venlafaxine is typically associated with mild symptoms. However, severe toxicity is repo... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • Kind: experimental
    • Percent: 37%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 25%
  • Kind: placebo
    • Percent: 24%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 23%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 22%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 19%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 18%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Sweating US
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Abnormal ejaculation US
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Abnormal orgasm US
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Vasodilatation US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Abnormal dreams US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Chills US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Hypertonia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Yawn US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Urinary Frequency US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Trauma US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Hypertension US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Tachycardia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Libido decreased US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Thinking abnormal US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Tinnitus US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Mydriasis US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Taste perversion US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Orgasm disturbance US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Urination impaired US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Laryngitis US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Pneumonia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Akathisia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Voice Alteration US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Apathy US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial
    CNS stimulation US
  • Kind: experimental
    • Percent: 0.1-1%
  • Clinical Trial

    Contraindications

    • Time Period: The use of MAOIs within 7 days of stopping treatment with venlafaxine, or the use of venlafaxine within 14 days of stopping and MAOI is contraindicated.
    • Regions: US
    • With Categories:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996

    Food Interactions

    • Avoid alcohol.
    • Avoid St.John's Wort.
    • Take with food.

    Interactions

    Type in a drug name to check for interaction with Venlafaxine

    Venlafaxine may increase the antiplatelet activities of (R)-warfarin.
    Venlafaxine may increase the antiplatelet activities of (S)-Warfarin.
    The metabolism of Venlafaxine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
    The risk or severity of hypoglycemia can be increased when Venlafaxine is combined with 2,4-thiazolidinedione.
    The risk or severity of serotonin syndrome can be increased when Venlafaxine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
    The risk or severity of adverse effects can be increased when Venlafaxine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Venlafaxine.
    The risk or severity of adverse effects can be increased when Venlafaxine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    Venlafaxine may increase the tachycardic activities of 4-Bromo-2,5-dimethoxyphenethylamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Venlafaxine.
    The metabolism of 4-Methoxyamphetamine can be decreased when combined with Venlafaxine.
    The metabolism of 5-androstenedione can be decreased when combined with Venlafaxine.
    The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Venlafaxine.
    The metabolism of Venlafaxine can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Venlafaxine.
    The metabolism of Venlafaxine can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Venlafaxine is combined with 7-Nitroindazole.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the serotonergic activities of Venlafaxine.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Venlafaxine.
    Venlafaxine may decrease the excretion rate of Abacavir which could result in a higher serum level.

    References

    • 1 . Golden RN, Nicholas L: Antidepressant efficacy of venlafaxine. Depress Anxiety. 2000;12 Suppl 1:45-9. [PubMed: 11098413]
    • 2 . Thase ME, Clayton AH, Haight BR, Thompson AH, Modell JG, Johnston JA: A double-blind comparison between bupropion XL and venlafaxine XR: sexual functioning, antidepressant efficacy, and tolerability. J Clin Psychopharmacol. 2006 Oct;26(5):482-8. [PubMed: 16974189]
    • 3 . Bielski RJ, Ventura D, Chang CC: A double-blind comparison of escitalopram and venlafaxine extended release in the treatment of major depressive disorder. J Clin Psychiatry. 2004 Sep;65(9):1190-6. [PubMed: 15367045]
    • 4 . Rowbotham MC, Goli V, Kunz NR, Lei D: Venlafaxine extended release in the treatment of painful diabetic neuropathy: a double-blind, placebo-controlled study. Pain. 2004 Aug;110(3):697-706. [PubMed: 15288411]
    • 5 . Ozyalcin SN, Talu GK, Kiziltan E, Yucel B, Ertas M, Disci R: The efficacy and safety of venlafaxine in the prophylaxis of migraine. Headache. 2005 Feb;45(2):144-52. [PubMed: 15705120]
    • 6 . Whirl-Carrillo M, McDonagh EM, Hebert JM, Gong L, Sangkuhl K, Thorn CF, Altman RB, Klein TE: Pharmacogenomics knowledge for personalized medicine. Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96. [PubMed: 22992668]
    • 7 . Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed: 19515014]
    • 8 . Shelton RC: Serotonin and Norepinephrine Reuptake Inhibitors. Handb Exp Pharmacol. 2019 Mar 6. doi: 10.1007/164_2018_164. [PubMed: 30838456]
    • 9 . Kennedy SH, Lam RW, McIntyre RS, Tourjman SV, Bhat V, Blier P, Hasnain M, Jollant F, Levitt AJ, MacQueen GM, McInerney SJ, McIntosh D, Milev RV, Muller DJ, Parikh SV, Pearson NL, Ravindran AV, Uher R: Canadian Network for Mood and Anxiety Treatments (CANMAT) 2016 Clinical Guidelines for the Management of Adults with Major Depressive Disorder: Section 3. Pharmacological Treatments. Can J Psychiatry. 2016 Sep;61(9):540-60. doi: 10.1177/0706743716659417. Epub 2016 Aug 2. [PubMed: 27486148]
    • 10 . Pringsheim T, Davenport W, Mackie G, Worthington I, Aube M, Christie SN, Gladstone J, Becker WJ: Canadian Headache Society guideline for migraine prophylaxis. Can J Neurol Sci. 2012 Mar;39(2 Suppl 2):S1-59. [PubMed: 22683887]
    • 11 . Gallagher HC, Gallagher RM, Butler M, Buggy DJ, Henman MC: Venlafaxine for neuropathic pain in adults. Cochrane Database Syst Rev. 2015 Aug 23;(8):CD011091. doi: 10.1002/14651858.CD011091.pub2. [PubMed: 26298465]
    • 12 . Katzman MA, Bleau P, Blier P, Chokka P, Kjernisted K, Van Ameringen M, Antony MM, Bouchard S, Brunet A, Flament M, Grigoriadis S, Mendlowitz S, O'Connor K, Rabheru K, Richter PM, Robichaud M, Walker JR: Canadian clinical practice guidelines for the management of anxiety, posttraumatic stress and obsessive-compulsive disorders. BMC Psychiatry. 2014;14 Suppl 1:S1. doi: 10.1186/1471-244X-14-S1-S1. Epub 2014 Jul 2. [PubMed: 25081580]
    • 13 . Handley AP, Williams M: The efficacy and tolerability of SSRI/SNRIs in the treatment of vasomotor symptoms in menopausal women: a systematic review. J Am Assoc Nurse Pract. 2015 Jan;27(1):54-61. doi: 10.1002/2327-6924.12137. Epub 2014 Jun 19. [PubMed: 24944075]
    • 14 . Roxanas M, Hibbert E, Field M: Venlafaxine hyponatraemia: incidence, mechanism and management. Aust N Z J Psychiatry. 2007 May;41(5):411-8. doi: 10.1080/00048670701261202. [PubMed: 17464733]
    • 15 . Thase ME: Effects of venlafaxine on blood pressure: a meta-analysis of original data from 3744 depressed patients. J Clin Psychiatry. 1998 Oct;59(10):502-8. [PubMed: 9818630]
    • 16 . Bymaster FP, Dreshfield-Ahmad LJ, Threlkeld PG, Shaw JL, Thompson L, Nelson DL, Hemrick-Luecke SK, Wong DT: Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology. 2001 Dec;25(6):871-80. [PubMed: 11750180]

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