Escitalopram


Description

Escitalopram is a selective serotonin re-uptake inhibitor (SSRI) and the S-enantiomer of racemic [Citalopram].[

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Pharmacology

Indication

Escitalopram is indicated for both acute and maintenance treatment of major depressive disorder (MDD... Read more

Pharmacodynamic

Escitalopram belongs to a class of medications called selective serotonin re-uptake inhibitors (SSRI... Read more

Mechanism of action

Escitalopram, like other selective serotonin re-uptake inhibitors, enhances serotonergic activity by... Read more

Absorption

Absorption of escitalopram following oral administration is expected to be almost complete, with an... Read more

Protein binding

Escitalopram exhibits relatively low protein binding at approximately 55-56%.[ Read more

Volume of distribution

Escitalopram appears to distribute extensively into tissues, with an apparent volume of distribution... Read more

Clearance

The oral plasma clearance of escitalopram is 600 mL/min, of which approximately 7% is due to renal c... Read more

Half life

The elimination half-life of escitalopram is 27-32 hours, though this is increased by approximately... Read more

Route of elimination

After oral administration of escitalopram, approximately 8% of the total dose is eliminated in the u... Read more

Toxicity

Symptoms of overdose may include CNS effects (dizziness, convulsions, coma, somnolence), gastrointes... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 24%
  • Kind: placebo
    • Percent: 17%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 18%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Ejaculation disorder US
  • Kind: experimental
    • Percent: 14%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Ejaculation disorder US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Libido decreased US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Anorgasmia US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Influenza-like symptoms US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Sweating increased US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Influenza-like symptoms US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Sweating increased US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Indigestion US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Shoulder Pain US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dreaming Abnormal US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Appetite decreased US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Lethargy US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Neck Pain US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Indigestion US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Libido decreased US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Appetite decreased US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Yawning US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Menstrual disorder US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Toothache US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Anorgasmia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Sinus Congestion US
    Clinical Trial
    Nasal Congestion US
    Clinical Trial
    Coughing US
    Clinical Trial
    Bronchitis US
    Clinical Trial
    Tinnitus US
    Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Regions: Canada
    • Patient Conditions:
        • Name: Congenital long QT syndrome
        • Drugbank Id: DBCOND0107917
    • Route:
      • Oral
    • Regions: Canada
    • Patient Conditions:
        • Name: QT Interval Prolongation
        • Drugbank Id: DBCOND0058707
    • Route:
      • Oral
    • Hypersensitivity:
      • true
    • Regions: US
    • Route:
      • Oral
    • Regions: US
    • With Drugs Coadmin:
        • Name: Pimozide
        • Drugbank Id: DB01100
    • Route:
      • Oral
    • Time Period: Do not use within 14 days of each other
    • Regions: US
    • With Categories Coadmin:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996

    Food Interactions

    • Take without regard to meals.

    Interactions

    Type in a drug name to check for interaction with Escitalopram

    The risk or severity of bleeding can be increased when Escitalopram is combined with (R)-warfarin.
    The risk or severity of bleeding can be increased when Escitalopram is combined with (S)-Warfarin.
    The metabolism of Escitalopram can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
    The therapeutic efficacy of Escitalopram can be decreased when used in combination with 1,10-Phenanthroline.
    The risk or severity of hypoglycemia can be increased when Escitalopram is combined with 2,4-thiazolidinedione.
    The risk or severity of serotonin syndrome can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Escitalopram.
    The risk or severity of serotonin syndrome can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Escitalopram.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Escitalopram.
    The therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Escitalopram.
    The risk or severity of serotonin syndrome can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Escitalopram.
    The risk or severity of bleeding can be increased when Escitalopram is combined with 4-hydroxycoumarin.
    The serum concentration of 4-Methoxyamphetamine can be increased when it is combined with Escitalopram.
    The metabolism of 5-androstenedione can be decreased when combined with Escitalopram.
    The risk or severity of serotonin syndrome can be increased when 5-methoxy-N,N-dimethyltryptamine is combined with Escitalopram.
    The metabolism of Escitalopram can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Escitalopram.
    The metabolism of Escitalopram can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Escitalopram is combined with 7-Nitroindazole.
    The risk or severity of serotonin syndrome can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Escitalopram.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Escitalopram.

    References

    • 1 . Moore N, Verdoux H, Fantino B: Prospective, multicentre, randomized, double-blind study of the efficacy of escitalopram versus citalopram in outpatient treatment of major depressive disorder. Int Clin Psychopharmacol. 2005 May;20(3):131-7. [PubMed: 15812262]
    • 2 . Boulenger JP, Huusom AK, Florea I, Baekdal T, Sarchiapone M: A comparative study of the efficacy of long-term treatment with escitalopram and paroxetine in severely depressed patients. Curr Med Res Opin. 2006 Jul;22(7):1331-41. [PubMed: 16834832]
    • 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 . Nierenberg AA, Greist JH, Mallinckrodt CH, Prakash A, Sambunaris A, Tollefson GD, Wohlreich MM: Duloxetine versus escitalopram and placebo in the treatment of patients with major depressive disorder: onset of antidepressant action, a non-inferiority study. Curr Med Res Opin. 2007 Feb;23(2):401-16. [PubMed: 17288694]
    • 5 . Chen F, Larsen MB, Sanchez C, Wiborg O: The S-enantiomer of R,S-citalopram, increases inhibitor binding to the human serotonin transporter by an allosteric mechanism. Comparison with other serotonin transporter inhibitors. Eur Neuropsychopharmacol. 2005 Mar;15(2):193-8. [PubMed: 15695064]
    • 6 . Rao N: The clinical pharmacokinetics of escitalopram. Clin Pharmacokinet. 2007;46(4):281-90. doi: 10.2165/00003088-200746040-00002. [PubMed: 17375980]
    • 7 . von Moltke LL, Greenblatt DJ, Giancarlo GM, Granda BW, Harmatz JS, Shader RI: Escitalopram (S-citalopram) and its metabolites in vitro: cytochromes mediating biotransformation, inhibitory effects, and comparison to R-citalopram. Drug Metab Dispos. 2001 Aug;29(8):1102-9. [PubMed: 11454728]
    • 8 . Rudberg I, Reubsaet JL, Hermann M, Refsum H, Molden E: Identification of a novel CYP2C19-mediated metabolic pathway of S-citalopram in vitro. Drug Metab Dispos. 2009 Dec;37(12):2340-8. doi: 10.1124/dmd.109.029355. Epub 2009 Sep 22. [PubMed: 19773541]
    • 9 . Nikisch G, Eap CB, Baumann P: Citalopram enantiomers in plasma and cerebrospinal fluid of ABCB1 genotyped depressive patients and clinical response: a pilot study. Pharmacol Res. 2008 Nov-Dec;58(5-6):344-7. doi: 10.1016/j.phrs.2008.09.010. Epub 2008 Sep 30. [PubMed: 18940259]
    • 10 . Fisar Z: Drugs related to monoamine oxidase activity. Prog Neuropsychopharmacol Biol Psychiatry. 2016 Aug 1;69:112-24. doi: 10.1016/j.pnpbp.2016.02.012. Epub 2016 Mar 2. [PubMed: 26944656]
    • 11 . Pastoor D, Gobburu J: Clinical pharmacology review of escitalopram for the treatment of depression. Expert Opin Drug Metab Toxicol. 2014 Jan;10(1):121-8. doi: 10.1517/17425255.2014.863873. Epub 2013 Nov 30. [PubMed: 24289655]
    • 12 . Bartlett D: Drug-Induced Serotonin Syndrome. Crit Care Nurse. 2017 Feb;37(1):49-54. doi: 10.4037/ccn2017169. [PubMed: 28148614]
    • 13 . Sanchez C, Reines EH, Montgomery SA: A comparative review of escitalopram, paroxetine, and sertraline: Are they all alike? Int Clin Psychopharmacol. 2014 Jul;29(4):185-96. doi: 10.1097/YIC.0000000000000023. [PubMed: 24424469]
    • 14 . Sanchez C: The pharmacology of citalopram enantiomers: the antagonism by R-citalopram on the effect of S-citalopram. Basic Clin Pharmacol Toxicol. 2006 Aug;99(2):91-5. doi: 10.1111/j.1742-7843.2006.pto_295.x. [PubMed: 16918708]
    • 15 . Kasper S, Spadone C, Verpillat P, Angst J: Onset of action of escitalopram compared with other antidepressants: results of a pooled analysis. Int Clin Psychopharmacol. 2006 Mar;21(2):105-10. [PubMed: 16421462]
    • 16 . Zhong H, Haddjeri N, Sanchez C: Escitalopram, an antidepressant with an allosteric effect at the serotonin transporter--a review of current understanding of its mechanism of action. Psychopharmacology (Berl). 2012 Jan;219(1):1-13. doi: 10.1007/s00213-011-2463-5. Epub 2011 Sep 8. [PubMed: 21901317]
    • 17 . Gray NA, Milak MS, DeLorenzo C, Ogden RT, Huang YY, Mann JJ, Parsey RV: Antidepressant treatment reduces serotonin-1A autoreceptor binding in major depressive disorder. Biol Psychiatry. 2013 Jul 1;74(1):26-31. doi: 10.1016/j.biopsych.2012.11.012. Epub 2013 Jan 29. [PubMed: 23374637]
    • 18 . FDA Approved Drugs: Escitalopram [Link]
    • 19 . DPD Approved Drugs: Escitalopram [Link]
    • 20 . Medsafe NZ: Escitalopram [Link]
    • 21 . CaymenChem: Escitalopram MSDS [Link]

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