Description

Simple

A medication used to treat depression and anxiety.

Clinical

A selective serotonin re-uptake inhibitor used in the treatment of major depressive disorder (MDD), generalized anxiety disorder (GAD), and other select psychiatric disorders such as obsessive-compulsive disorder (OCD).

Overview

Escitalopram is a selective serotonin re-uptake inhibitor (SSRI) and the S-enantiomer of racemic [Citalopram].[11] It is used to restore serotonergic function in the treatment of depression and anxiety.[18,19,20] Escitalopram is approximately 150 times more potent than citalopram’s R-enantiomer and is responsible for the vast majority of citalopram’s clinical activity, with some evidence suggesting that the R-enantiomer of racemic citalopram actively dampens the activity of escitalopram rather than existing simply as an inactive enantiomer.[6,Read more

Pharmacology

Indication

Escitalopram is indicated for both acute and maintenance treatment of major depressive disorder (MDD) and for the acute treatment of generalized anxiety disorder (GAD).[18] It is additionally indicated for... Read more

Pharmacodynamic

Escitalopram belongs to a class of medications called selective serotonin re-uptake inhibitors (SSRIs). These agents cause an increase in serotonin levels in neuronal synapses by preventing the re-uptake of serotonin (5-HT) into the presynaptic terminals of serotonergic neurons.[ Read more

Mechanism of action

Escitalopram, like other selective serotonin re-uptake inhibitors, enhances serotonergic activity by binding to the orthosteric (i.e. primary) binding site on the serotonin transporter (SERT), the same site to which endogenous 5-HT binds, and thus prevents the re-uptake of serotonin into the presyna... Read more

Absorption

Absorption of escitalopram following oral administration is expected to be almost complete, with an estimated absolute bioavailability of approximately 80%. Tmax occurs after about 4-5 hours.[18,... Read more

Protein binding

Escitalopram exhibits relatively low protein binding at approximately 55-56%.[18,19, Read more

Volume of distribution

Escitalopram appears to distribute extensively into tissues, with an apparent volume of distribution of approximately 12-26 L/kg.[18, Read more

Clearance

The oral plasma clearance of escitalopram is 600 mL/min, of which approximately 7% is due to renal clearance.[18,19 Read more

Half life

The elimination half-life of escitalopram is 27-32 hours, though this is increased by approximately 50% in the elderly and doubled in patients with reduced hepatic function.[ Read more

Route of elimination

After oral administration of escitalopram, approximately 8% of the total dose is eliminated in the urine as unchanged escitalopram and 10% is eliminated in the urine as S-desmethylcitalopram.[18, Read more

Toxicity

Symptoms of overdose may include CNS effects (dizziness, convulsions, coma, somnolence), gastrointestinal distress (nausea, vomiting), and/or cardiac abnormalities (hypotension, tachycardia, ECG changes).[18 Read more

Adverse Effects

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
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of bleeding can be increased when Escitalopram is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of bleeding can be increased when Escitalopram is combined with (S)-Warfarin.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Escitalopram can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1,10-Phenanthroline
The therapeutic efficacy of Escitalopram can be decreased when used in combination with 1,10-Phenanthroline.
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Escitalopram is combined with 2,4-thiazolidinedione.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Escitalopram.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of serotonin syndrome can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Escitalopram.
3,5-Diiodotyrosine
The therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Escitalopram.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of serotonin syndrome can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Escitalopram.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when Escitalopram is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The serum concentration of 4-Methoxyamphetamine can be increased when it is combined with Escitalopram.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of serotonin syndrome can be increased when 5-methoxy-N,N-dimethyltryptamine is combined with Escitalopram.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Escitalopram is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of serotonin syndrome can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Escitalopram.
Abaloparatide
The therapeutic efficacy of Abaloparatide can be decreased when used in combination with Escitalopram.
Abatacept
The metabolism of Escitalopram can be increased when combined with Abatacept.
Abciximab
The risk or severity of bleeding can be increased when Escitalopram is combined with Abciximab.
Abexinostat
The risk or severity of QTc prolongation can be increased when Abexinostat is combined with Escitalopram.
Abiraterone
The metabolism of Escitalopram can be decreased when combined with Abiraterone.
Acarbose
The risk or severity of hypoglycemia can be increased when Escitalopram is combined with Acarbose.
21 References
  1. 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. 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. 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. 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. 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. 6 . Rao N: The clinical pharmacokinetics of escitalopram. Clin Pharmacokinet. 2007;46(4):281-90. doi: 10.2165/00003088-200746040-00002.PubMed: 17375980
  7. 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. 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. 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. 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. 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. 12 . Bartlett D: Drug-Induced Serotonin Syndrome. Crit Care Nurse. 2017 Feb;37(1):49-54. doi: 10.4037/ccn2017169.PubMed: 28148614
  13. 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. 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. 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. 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. 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. 18 . FDA Approved Drugs: Escitalopram Link
  19. 19 . DPD Approved Drugs: Escitalopram Link
  20. 20 . Medsafe NZ: Escitalopram Link
  21. 21 . CaymenChem: Escitalopram MSDS Link