Drug/Small Molecule:
escitalopram

last updated 08/10/2011

Dutch Pharmacogenetics Working Group Guideline for escitalopram and CYP2C19

Summary

For CYP2C19 ultrarapid metabolizers, monitor escitalopram plasma concentration and titrate dose to a maximum of 150% in response to efficacy and adverse drug event, or select alternative drug.

Annotation

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group has evaluated therapeutic dose recommendations for escitalopram based on the CYP2C19 genotype [Article:21412232]. They conclude to monitor plasma concentration and titrate dose to a maximum of 150% in response to efficacy and adverse drug event or select alternative drug (e.g. fluoxetine, paroxetine) for the CYP2C19 UM phenotype.

Phenotype (Genotype) Therapeutic Dose Recommendation Level of Evidence Clinical Relevance
CYP2C19 PM (*2/*2, *2/*3, *3/*3) None Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints Minor clinical effect (statistically significant difference): QTc prolongation (<450 ms female, <470 ms male); international normalized ratio (INR) increase < 4.5
Kinetic effect (statistically significant difference)
CYP2C19 IM (*1/*2, *1/*3, *17/*2, *17/*3) None Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints Minor clinical effect (statistically significant difference): QTc prolongation (<450 ms female, <470 ms male); INR increase < 4.5
Kinetic effect (statistically significant difference)
CYP2C19 UM (*17/*17) Monitor plasma concentration and titrate dose to a maximum of 150% in response to efficacy and adverse drug event or select alternative drug (e.g. fluoxetine, paroxetine) Published controlled studies of good quality* relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints Minor clinical effect (statistically significant difference): QTc prolongation (<450 ms female, <470 ms male); INR increase < 4.5
Kinetic effect (statistically significant difference)

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with escitalopram that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105012

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA CYP2C19 *1 N/A N/A N/A
No VIP available CA VA CYP2C19 *2 N/A N/A N/A
No VIP available CA VA CYP2C19 *3 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *4 N/A N/A N/A
No VIP available CA VA CYP2C19 *17 N/A N/A N/A
No VIP available CA VA CYP2D6 *1 N/A N/A N/A
No VIP available CA No VIP available CYP2D6 *2 N/A N/A N/A
No VIP available CA VA CYP2D6 *3 N/A N/A N/A
No VIP available CA VA CYP2D6 *4 N/A N/A N/A
No VIP available CA VA CYP2D6 *5 N/A N/A N/A
No VIP available CA No VIP available CYP2D6 *6 N/A N/A N/A
No VIP available CA VA CYP2D6 *10 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *17 N/A N/A N/A
No VIP available CA VA CYP2D6 *41 N/A N/A N/A
No VIP available CA VA SLC6A4 HTTLPR long form (L allele) N/A N/A N/A
No VIP available CA VA SLC6A4 HTTLPR short form (S allele) N/A N/A N/A
No VIP available No Clinical Annotations available VA
CYP2C19 poor metabolizers N/A N/A N/A
No VIP available No Clinical Annotations available VA
CYP2C19 poor metabolizer N/A N/A N/A
No VIP available No Clinical Annotations available VA
CYP2C19 ultrarapid metabolizer phenotype N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1065852 100C>T, 21917263G>A, 42526694G>A, 5190C>T, CYP2D6:100C>T, Pro34Ser, part of CYP2D6*4 and CYP2D6*10
G > A
Missense
Pro34Ser
No VIP available No Clinical Annotations available VA
rs1074145 47486310G>A, 96681846G>A
G > A
Not Available
No VIP available No Clinical Annotations available VA
rs10975641 2053-537G>C, 6546839C>G, 6556839C>G, 93854G>C
C > G
Intronic
No VIP available No Clinical Annotations available VA
rs11144870 235-641G>A, 79004213C>T, 8168745C>T
C > T
Intronic
No VIP available CA VA
rs11188072 -3402, 1599C>T, 47323525C>T, 96519061C>T, CYP2C19:, CYP2C19: -3402C>T, part of CYP2C19*17
C > T
Not Available
No VIP available No Clinical Annotations available VA
rs1126757 246G>A, 28148090C>T, 55879872C>T, 9G>A, Ala3=, Ala82=
G > T
G > C
Synonymous
Ala3Ala
No VIP available No Clinical Annotations available VA
rs11568817 -262T>G, 16293216A>C, 78173382A>C
A > C
5' Flanking
No VIP available No Clinical Annotations available VA
rs12054895 27601431G>T, 27611431G>T
G > T
Not Available
No VIP available CA VA
rs12248560 -806C>A, -806C>T, 4195C>A, 4195C>T, 47326121C>A, 47326121C>T, 96521657C>A, 96521657C>T, CYP2C19*17, CYP2C19*17 CYP2C19: -806C>T, CYP2C19: -806C>T
C > T
C > A
5' Flanking
No VIP available CA VA
rs2069521 29085G>A, 3113A>G, 45829524G>A, 75038967G>A, CYP1A2:
G > A
Not Available
No VIP available CA VA
rs2069526 -10+103T>G, 31459T>G, 45831898T>G, 739T>G, 740T>G, 75041341T>G, CYP1A2*1E
T > G
Intronic
No VIP available No Clinical Annotations available VA
rs2470890 +, 1548C>T, 295T>C, 37544C>T, 45837983C>T, 75047426C>T, Asn516=, CYP1A2*1B, CYP1A2:1545T>C, CYP1A2:1548T>C, CYP1A2:5347T>C, CYP1A2:Asn516Asn, CYP1A2:Ex7
C > T
Synonymous
Asn516Asn
No VIP available No Clinical Annotations available VA
rs2472304 1042+43G>A, 34356G>A, 45834795G>A, 75044238G>A
G > A
Intronic
No VIP available CA VA
rs352428 16337038A>G, 28478892A>G
A > G
Not Available
No VIP available No Clinical Annotations available VA
rs3743484 1043-65G>C, 34518G>C, 45834957G>C, 75044400G>C
G > C
Intronic
No VIP available CA VA
rs3892097 21915516C>T, 353-1G>A, 42524947C>T, 506-1G>A, 6937G>A, CYP2D6*4, CYP2D6:1846G>A, part of CYP2D6*4
C > T
Acceptor
No VIP available CA VA
rs41271330 55579028G>A, 55639028G>A, 846C>T, Asn282=
G > A
Synonymous
Asn282Asn
No VIP available No Clinical Annotations available VA
rs4244285 24154G>A, 24154G>C, 47346080G>A, 47346080G>C, 681G>A, 681G>C, 96541616G>A, 96541616G>C, CYP2C19*2, CYP2C19:681G>A, CYP2C19:G681A, Pro227=
G > A
G > C
Synonymous
Pro227Pro
No VIP available CA VA
rs4646425 33399C>T, 45833838C>T, 75043281C>T, 832-249C>T
C > T
Intronic
No VIP available CA VA
rs4646427 1253+81T>C, 35810T>C, 45836249T>C, 75045692T>C
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs4986893 22948G>A, 47344874G>A, 636G>A, 96540410G>A, CYP2C19*3, CYP2C19:636G>A, CYP2C19:G636A, Trp212Ter
G > A
Stop Codon
Trp212null
No VIP available No Clinical Annotations available VA
rs5443 10501C>T, 47295C>T, 6894875C>T, 6954875C>T, 825C>T, GNB3:825C>T, GNB3:Ser275Ser, Ser275=
C > T
Synonymous
Ser275Ser
No VIP available No Clinical Annotations available VA
rs57098334 GGGTGGGCT, SLC6A4:
C > (CCCACCCGA)12
C > (CCCACCCGA)9
C > (CCCACCCGA)10
Not Available
No VIP available No Clinical Annotations available VA
rs6311 -1438, -510G>A, -998G>A, 28451478C>T, 4692G>A, 47471478C>T, G>A, HTR2A c.-1438G>A, HTR2A:, HTR2A: -1438G/A, HTR2A:-1438G>A
C > T
5' Flanking
No VIP available CA VA
rs6318 113965735G>C, 152185G>C, 398067G>C, 68G>C, Cys23Ser, HTR2C:23Ser, HTR2C:Cys23Ser
C > G
Missense
Cys23Ser
No VIP available No Clinical Annotations available VA
rs762551 -9-154C>A, 32035C>A, 45832474C>A, 75041917C>A, CYP1A2*1F, CYP1A2:734C>A
C > A
Intronic
No VIP available CA VA
rs915120 121190113T>C, 597+163T>C, 71994577T>C
T > C
Intronic
No VIP available CA VA
rs9316233 28413355C>G, 362-23581G>C, 42815G>C, 47433355C>G, 614-23581G>C
C > G
Intronic
No VIP available CA VA
rs9380524 112291G>T, 251-1019G>T, 35529070C>A, 35589070C>A
C > A
Intronic
No VIP available CA VA
rs962369 -22+6638A>C, -22+6638A>G, -22+6638A>T, -22+7473A>C, -22+7473A>G, -22+7473A>T, -22+7556A>C, -22+7556A>G, -22+7556A>T, -22+7771A>C, -22+7771A>G, -22+7771A>T, 14186A>C, 14186A>G, 14186A>T, 27674420T>A, 27674420T>C, 27674420T>G, 27734420T>A, 27734420T>C, 27734420T>G, 3+8539A>C, 3+8539A>G, 3+8539A>T
T > C
Intronic
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Cipralex
  • Escitalopram Oxalate
  • escitalopram
Trade Names
  • Lexapro
Brand Mixture Names

PharmGKB Accession Id:
PA10074

Description

Escitalopram, the S-enantiomer of citalopram, belongs to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). Despite distinct structural differences between compounds in this class, SSRIs possess similar pharmacological activity. As with other antidepressant agents, several weeks of therapy may be required before a clinical effect is seen. SSRIs are potent inhibitors of neuronal serotonin reuptake. They have little to no effect on norepinephrine or dopamine reuptake and do not antagonize alpha- or beta-adrenergic, dopamine D 2 or histamine H 1 receptors. During acute use, SSRIs block serotonin reuptake and increase serotonin stimulation of somatodendritic 5-HT 1A and terminal autoreceptors. Chronic use leads to desensitization of somatodendritic 5-HT 1A and terminal autoreceptors. The overall clinical effect of increased mood and decreased anxiety is thought to be due to adaptive changes in neuronal function that leads to enhanced serotonergic neurotransmission. Side effects include dry mouth, nausea, dizziness, drowsiness, sexual dysfunction and headache. Side effects generally occur within the first two weeks of therapy and are usually less severe and frequent than those observed with tricyclic antidepressants. Escitalopram may be used to treat major depressive disorder (MDD) and generalized anxiety disorder (GAD).

Source: Drug Bank

Indication

Labeled indications include major depressive disorder (MDD) and generalized anxiety disorder (GAD). Unlabeled indications include treatment of mild dementia-associated agitation in nonpsychotic patients.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The antidepressant, antiobsessive-compulsive, and antibulimic actions of escitalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. Escitalopram blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT 1A autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs.

Source: Drug Bank

Pharmacology

Escitalopram is one of a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-compulsive, and antibulimic actions of escitalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. In vitro studies show that escitalopram is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. Escitalopram has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT 1A, 5HT 1B, 5HT 2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of escitalopram was found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Escitalopram does not inhibit monoamine oxidase.

Source: Drug Bank

Food Interaction

Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Mainly hepatic. Escitalopram undergoes N-demethylation to S-demethylcitalopram (S-DCT) and S-didemethylcitalopram (S-DDCT). CYP3A4 and CYP2C19 are the enzymes responsible for this N-demethylation reaction.

Source: Drug Bank

Protein Binding

~56%

Source: Drug Bank

Absorption

The absolute bioavailability of citalopram is about 80% relative to an intravenous dose.

Source: Drug Bank

Half-Life

27-32 hours

Source: Drug Bank

Toxicity

Signs of overdose include convulsions, coma, dizziness, hypotension, insomnia, nausea, vomiting, sinus tachycardia, somnolence, and ECG changes (including QT prolongation).

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Following oral administrations of escitalopram, the fraction of drug recovered in the urine as escitalopram and S-demethylcitalopram (S-DCT) is about 8% and 10%, respectively. The oral clearance of escitalopram is 600 mL/min, with approximately 7% of that due to renal clearance. Escitalopram is metabolized to S-DCT and S-didemethylcitalopram (S-DDCT).

Source: Drug Bank

Volume of Distribution

  • 12 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C20H21FN2O

Source: Drug Bank

Isomeric SMILES

CN(C)CCC[C@@]1(c2ccc(cc2CO1)C#N)c3ccc(cc3)F

Source: OpenEye

Canonical SMILES

CN(C)CCC[C@]1(OCC2=C1C=CC(=C2)C#N)C1=CC=C(F)C=C1

Source: Drug Bank

Average Molecular Weight

324.3919

Source: Drug Bank

Monoisotopic Molecular Weight

324.163791509

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ADRA1A (source: Drug Bank)
CHRM1 (source: Drug Bank)
HRH1 (source: Drug Bank)
SLC6A2 (source: Drug Bank)
SLC6A3 (source: Drug Bank)
SLC6A4 (source: Drug Bank)

Drug Interactions

Drug Description
escitalopram Increased risk of CNS adverse effects (source: Drug Bank)
escitalopram Increased risk of CNS adverse effects (source: Drug Bank)
escitalopram The SSRI increases the effect of the beta-blocker (source: Drug Bank)
escitalopram The SSRI, escitalopram, may increase the bradycardic effect of the beta-blocker, carvedilol. (source: Drug Bank)
escitalopram Increased risk of CNS adverse effects (source: Drug Bank)
escitalopram Increased risk of CNS adverse effects (source: Drug Bank)
almotriptan Increased risk of CNS adverse effects (source: Drug Bank)
almotriptan Increased risk of CNS adverse effects (source: Drug Bank)
carvedilol The SSRI increases the effect of the beta-blocker (source: Drug Bank)
carvedilol The SSRI, escitalopram, may increase the bradycardic effect of the beta-blocker, carvedilol. (source: Drug Bank)
eletriptan Increased risk of CNS adverse effects (source: Drug Bank)
eletriptan Increased risk of CNS adverse effects (source: Drug Bank)
frovatriptan Increased risk of CNS adverse effects (source: Drug Bank)
isocarboxazid Possible severe adverse reaction with this combination (source: Drug Bank)
isocarboxazid Possible severe adverse reaction with this combination (source: Drug Bank)
linezolid Combination associated with possible serotoninergic syndrome (source: Drug Bank)
linezolid Combination associated with possible serotoninergic syndrome (source: Drug Bank)
metoprolol The SSRI increases the effect of the beta-blocker (source: Drug Bank)
metoprolol The SSRI, escitalopram, may increase the bradycardic effect of the beta-blocker, metoprolol. (source: Drug Bank)
naratriptan Increased risk of CNS adverse effects (source: Drug Bank)
naratriptan Increased risk of CNS adverse effects (source: Drug Bank)
oxycodone Increased risk of serotonin syndrome (source: Drug Bank)
oxycodone Increased risk of serotonin syndrome (source: Drug Bank)
phenelzine Possible severe adverse reaction with this combination (source: Drug Bank)
phenelzine Possible severe adverse reaction with this combination (source: Drug Bank)
pimozide The SSRI increases the effect of the beta-blocker (source: Drug Bank)
propranolol The SSRI increases the effect of the beta-blocker (source: Drug Bank)
propranolol The SSRI, escitalopram, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
rasagiline Possible severe adverse reaction with this combination (source: Drug Bank)
rizatriptan Increased risk of CNS adverse effects (source: Drug Bank)
rizatriptan Increased risk of CNS adverse effects (source: Drug Bank)
selegiline Possible severe adverse reaction with this combination (source: Drug Bank)
selegiline Possible severe adverse reaction with this combination (source: Drug Bank)
sibutramine Risk of serotoninergic syndrome (source: Drug Bank)
sibutramine Risk of serotoninergic syndrome (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
tramadol Increased risk of serotonin syndrome (source: Drug Bank)
tramadol Increased risk of serotonin syndrome (source: Drug Bank)
tranylcypromine Possible severe adverse reaction with this combination (source: Drug Bank)
tranylcypromine Possible severe adverse reaction with this combination (source: Drug Bank)
zolmitriptan Increased risk of CNS adverse effects (source: Drug Bank)
zolmitriptan Increased risk of CNS adverse effects (source: Drug Bank)
escitalopram Increased risk of CNS adverse effects (source: Drug Bank)
escitalopram Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided. (source: Drug Bank)
escitalopram Possible severe adverse reaction with this combination (source: Drug Bank)
escitalopram Possible severe adverse reaction with this combination (source: Drug Bank)
escitalopram Concomitant therapy may result in additive antiplatelet effects and increase the risk of bleeding. Monitor for increased risk of bleeding during concomitant therapy. (source: Drug Bank)
escitalopram Combination associated with possible serotoninergic syndrome (source: Drug Bank)
escitalopram Combination associated with possible serotoninergic syndrome (source: Drug Bank)
escitalopram The SSRI increases the effect of the beta-blocker (source: Drug Bank)
escitalopram The SSRI increases the effect of the beta-blocker (source: Drug Bank)
escitalopram Increased risk of CNS adverse effects (source: Drug Bank)
escitalopram Increased risk of CNS adverse effects (source: Drug Bank)
escitalopram Increased risk of serotonin syndrome (source: Drug Bank)
escitalopram Increased risk of serotonin syndrome (source: Drug Bank)
escitalopram Possible severe adverse reaction with this combination (source: Drug Bank)
escitalopram Possible severe adverse reaction with this combination (source: Drug Bank)
escitalopram The SSRI increases the effect and toxicity of pimozide (source: Drug Bank)
escitalopram The SSRI, escitalopram, increases the effect and toxicity of pimozide. (source: Drug Bank)
escitalopram The SSRI increases the effect of the beta-blocker (source: Drug Bank)
escitalopram The SSRI, escitalopram, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
escitalopram Possible severe adverse reaction with this combination (source: Drug Bank)
escitalopram Telithromycin may reduce clearance of Escitalopram. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Escitalopram if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
escitalopram Additive antiplatelet effects increase the risk of bleeding. Consider alternate therapy or monitor for increased bleeding. (source: Drug Bank)
escitalopram Ticlopidine may decrease the metabolism and clearance of Escitalopram. Consider alternate therapy or monitor for adverse/toxic effects of Ambrisentan if Escitalopram is initiated, discontinued or dose changed. (source: Drug Bank)
escitalopram Increased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy. (source: Drug Bank)
escitalopram Tramadol increases the risk of serotonin syndrome and seizures. (source: Drug Bank)
escitalopram Increased risk of serotonin syndrome. Concomitant therapy should be avoided. A significant washout period, dependent on the half-lives of the agents, should be employed between therapies. (source: Drug Bank)
escitalopram Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
escitalopram Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
escitalopram The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Escitalopram. Monitor for increased bleeding during concomitant thearpy. (source: Drug Bank)
escitalopram The SSRI, Escitalopram, may decrease the metabolism and clearance of Trimipramine. Increased risk of serotonin syndrome. Monitor for changes in Trimipramine efficacy and toxicity if Escitalopram is initiated, discontinued or dose changed. (source: Drug Bank)
escitalopram The CNS depressants, Triprolidine and Escitalopram, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
escitalopram The CNS depressants, Triprolidine and Escitalopram, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
escitalopram Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
escitalopram Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of escitalopram by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of escitalopram if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)
escitalopram Additive QTc-prolongation may occur increasing the risk of life-threatening ventricular arrhythmias and torsade de pointes. Concomitant therapy should be avoided. (source: Drug Bank)
escitalopram Use of two serotonin modulators, such as zolmitriptan and escitalopram, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy. (source: Drug Bank)
escitalopram Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to escitalopram: 63

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Impact of Cytochrome P450 2C19 Polymorphisms on Citalopram/Escitalopram Exposure: A Systematic Review and Meta-Analysis. Clinical pharmacokinetics. 2014. Chang Ming, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of age on serum concentrations of venlafaxine and escitalopram in different CYP2D6 and CYP2C19 genotype subgroups. European journal of clinical pharmacology. 2014. Waade Ragnhild Birkeland, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
CYP2C19 variation, not citalopram dose nor serum level, is associated with QTc prolongation. Journal of psychopharmacology (Oxford, England). 2014. Kumar Yingying, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Treatment Outcomes of Depression: The Pharmacogenomic Research Network Antidepressant Medication Pharmacogenomic Study. Journal of clinical psychopharmacology. 2014. Mrazek David A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Citalopram and Escitalopram Plasma Drug and Metabolite Concentrations: Genome-Wide Associations. British journal of clinical pharmacology. 2014. Ji Yuan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genetic differences in cytochrome P450 enzymes and antidepressant treatment response. Journal of psychopharmacology (Oxford, England). 2013. Hodgson Karen, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Whole-exome sequencing identifies a polymorphism in the BMP5 gene associated with SSRI treatment response in major depression. Journal of psychopharmacology (Oxford, England). 2013. Tammiste Anu, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Tumor necrosis factor and its targets in the inflammatory cytokine pathway are identified as putative transcriptomic biomarkers for escitalopram response. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 2013. Powell Timothy R, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenetic polymorphisms and response to escitalopram and venlafaxine over 8 weeks in major depression. Human psychopharmacology. 2013. Ng Chee, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
CYP2D6 P34S Polymorphism and Outcomes of Escitalopram Treatment in Koreans with Major Depression. Psychiatry investigation. 2013. Han Kyu-Man, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Estimation of CYP2D6*10 genotypes on citalopram disposition in Chinese subjects by population pharmacokinetic assay. Journal of clinical pharmacy and therapeutics. 2013. Chen B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Prevention of depression with escitalopram in patients undergoing treatment for head and neck cancer: randomized, double-blind, placebo-controlled clinical trial. JAMA otolaryngology-- head & neck surgery. 2013. Lydiatt William M, et al. PubMed
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CYP1A2 genetic polymorphisms are associated with early antidepressant escitalopram metabolism and adverse reactions. Pharmacogenomics. 2013. Kuo Hsiang-Wei, et al. PubMed
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Influence of CYP2D6 and CYP2C19 gene variants on antidepressant response in obsessive-compulsive disorder. The pharmacogenomics journal. 2013. Brandl E J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Escitalopram reduces attentional performance in anxious older adults with high-expression genetic variants at serotonin 2A and 1B receptors. The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP). 2013. Lenze Eric J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Common genetic variation and antidepressant efficacy in major depressive disorder: a meta-analysis of three genome-wide pharmacogenetic studies. The American journal of psychiatry. 2013. GENDEP Investigators, et al. PubMed
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FKBP5 genetic variation: association with selective serotonin reuptake inhibitor treatment outcomes in major depressive disorder. Pharmacogenetics and genomics. 2013. Ellsworth Katarzyna A, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
The AmpliChip® CYP450 test and response to treatment in schizophrenia and obsessive compulsive disorder: a pilot study and focus on cases with abnormal CYP2D6 drug metabolism. Genetic testing and molecular biomarkers. 2012. Müller Daniel J, et al. PubMed
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Pharmacogenomics of selective serotonin reuptake inhibitor treatment for major depressive disorder: genome-wide associations and functional genomics. The pharmacogenomics journal. 2012. Ji Y, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of glutamate system genes and SSRI-associated sexual dysfunction. Psychiatry research. 2012. Bishop Jeffrey R, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
CYP2C19 genotype predicts steady state escitalopram concentration in GENDEP. Journal of psychopharmacology (Oxford, England). 2012. Huezo-Diaz Patricia, et al. PubMed
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Association between serotonin transporter-linked polymorphic region and escitalopram antidepressant treatment response in Korean patients with major depressive disorder. Neuropsychobiology. 2012. Won Eun-Soo, et al. PubMed
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A candidate gene study of serotonergic pathway genes and pain relief during treatment with escitalopram in patients with neuropathic pain shows significant association to serotonin receptor2C (HTR2C). European journal of clinical pharmacology. 2011. Brasch-Andersen Charlotte, et al. PubMed
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Sexual dysfunction during treatment with serotonergic and noradrenergic antidepressants: clinical description and the role of the 5-HTTLPR. The world journal of biological psychiatry : the official journal of the World Federation of Societies of Biological Psychiatry. 2011. Strohmaier Jana, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Variation in GNB3 predicts response and adverse reactions to antidepressants. Journal of psychopharmacology (Oxford, England). 2011. Keers Robert, et al. PubMed
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ABCB1 gene polymorphisms are associated with the severity of major depressive disorder and its response to escitalopram treatment. Pharmacogenetics and genomics. 2011. Lin Keh-Ming, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Convergent animal and human evidence suggests a role of PPM1A gene in response to antidepressants. Biological psychiatry. 2011. Malki Karim, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Glycine and a glycine dehydrogenase (GLDC) SNP as citalopram/escitalopram response biomarkers in depression: pharmacometabolomics-informed pharmacogenomics. Clinical pharmacology and therapeutics. 2011. Ji Y, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
CYP2C19 variation and citalopram response. Pharmacogenetics and genomics. 2011. Mrazek David A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Catechol O-methyltransferase pharmacogenomics and selective serotonin reuptake inhibitor response. The pharmacogenomics journal. 2010. Ji Y, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genome-wide association study of increasing suicidal ideation during antidepressant treatment in the GENDEP project. The pharmacogenomics journal. 2010. Perroud N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Antiplatelet effects of antidepressant treatment: a randomized comparison between escitalopram and nortriptyline. Thrombosis research. 2010. Flöck Anne, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Coprescription of tamoxifen and medications that inhibit CYP2D6. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Sideras Kostandinos, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Association between CYP2C19*17 and metabolism of amitriptyline, citalopram and clomipramine in Dutch hospitalized patients. The pharmacogenomics journal. 2010. de Vos A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of CYP2C19: functional and clinical implications of a new variant CYP2C19*17. British journal of clinical pharmacology. 2010. Li-Wan-Po Alain, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Evaluation of the influence of sex and CYP2C19 and CYP2D6 polymorphisms in the disposition of citalopram. European journal of pharmacology. 2010. Fudio Salvador, et al. PubMed
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Effect of age, weight, and CYP2C19 genotype on escitalopram exposure. Journal of clinical pharmacology. 2010. Jin Yuyan, et al. PubMed
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Nationwide drug-dispensing data reveal important differences in adherence to drug label recommendations on CYP2D6-dependent drug interactions. British journal of clinical pharmacology. 2010. Mannheimer Buster, et al. PubMed
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Genetic polymorphisms of cytochrome P450 enzymes influence metabolism of the antidepressant escitalopram and treatment response. Pharmacogenomics. 2010. Tsai Ming-Hsien, et al. PubMed
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Interaction between serotonin transporter gene variants and life events predicts response to antidepressants in the GENDEP project. The pharmacogenomics journal. 2010. Keers R, et al. PubMed
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Escitalopram is a weak inhibitor of the CYP2D6-catalyzed O-demethylation of (+)-tramadol but does not reduce the hypoalgesic effect in experimental pain. Clinical pharmacology and therapeutics. 2009. Noehr-Jensen L, et al. PubMed
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Identification of a novel CYP2C19-mediated metabolic pathway of S-citalopram in vitro. Drug metabolism and disposition: the biological fate of chemicals. 2009. Rudberg I, et al. PubMed
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Impact of CYP2C19 phenotypes on escitalopram metabolism and an evaluation of pupillometry as a serotonergic biomarker. European journal of clinical pharmacology. 2009. Noehr-Jensen L, et al. PubMed
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Serotonin transporter promoter region polymorphisms do not influence treatment response to escitalopram in patients with major depression. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 2009. Maron Eduard, et al. PubMed
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Serotonin transporter polymorphisms, microstructural white matter abnormalities and remission of geriatric depression. Journal of affective disorders. 2009. Alexopoulos George S, et al. PubMed
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Genetic predictors of increase in suicidal ideation during antidepressant treatment in the GENDEP project. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2009. Perroud Nader, et al. PubMed
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Moderation of antidepressant response by the serotonin transporter gene. The British journal of psychiatry : the journal of mental science. 2009. Huezo-Diaz Patricia, et al. PubMed
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Genetic predictors of response to antidepressants in the GENDEP project. The pharmacogenomics journal. 2009. Uher Rudolf, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
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Impact of the ultrarapid CYP2C19*17 allele on serum concentration of escitalopram in psychiatric patients. Clinical pharmacology and therapeutics. 2008. Rudberg I, et al. PubMed
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Kinetics of omeprazole and escitalopram in relation to the CYP2C19*17 allele in healthy subjects. European journal of clinical pharmacology. 2008. Ohlsson Rosenborg Staffan, et al. PubMed
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Influence of the CYP2D6*4 polymorphism on dose, switching and discontinuation of antidepressants. British journal of clinical pharmacology. 2008. Bijl Monique J, et al. PubMed
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Pharmacokinetic genes do not influence response or tolerance to citalopram in the STAR*D sample. PloS one. 2008. Peters Eric J, et al. PubMed
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Clinical response and risk for reported suicidal ideation and suicide attempts in pediatric antidepressant treatment: a meta-analysis of randomized controlled trials. JAMA : the journal of the American Medical Association. 2007. Bridge Jeffrey A, et al. PubMed
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Comparison of duloxetine, escitalopram, and sertraline effects on cytochrome P450 2D6 function in healthy volunteers. Journal of clinical psychopharmacology. 2007. Preskorn Sheldon H, et al. PubMed
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A common novel CYP2C19 gene variant causes ultrarapid drug metabolism relevant for the drug response to proton pump inhibitors and antidepressants. Clinical pharmacology and therapeutics. 2006. Sim Sarah C, et al. PubMed
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Serotonin transporter polymorphisms and side effects in antidepressant therapy--a pilot study. Pharmacogenomics. 2006. Popp Johannes, et al. PubMed
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Heterozygous mutation in CYP2C19 significantly increases the concentration/dose ratio of racemic citalopram and escitalopram (S-citalopram). Therapeutic drug monitoring. 2006. Rudberg Ida, et al. PubMed
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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. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 2005. Chen Fenghua, et al. PubMed
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Metabolism of citalopram enantiomers in CYP2C19/CYP2D6 phenotyped panels of healthy Swedes. British journal of clinical pharmacology. 2003. Herrlin Karin, et al. PubMed
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Enantioselective analysis of citalopram and metabolites in adolescents. Therapeutic drug monitoring. 2001. Carlsson B, et al. PubMed
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A double-blind, placebo-controlled study of citalopram with and without lithium in the treatment of therapy-resistant depressive patients: a clinical, pharmacokinetic, and pharmacogenetic investigation. Journal of clinical psychopharmacology. 1996. Baumann P, et al. PubMed
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Pharmacokinetics of citalopram in relation to the sparteine and the mephenytoin oxidation polymorphisms. Therapeutic drug monitoring. 1993. Sindrup S H, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0456-2005-01
DrugBank:
DB01175
ChEBI:
36791
PubChem Compound:
146570
PubChem Substance:
46507040
724297
Drugs Product Database (DPD):
2263238
ChemSpider:
129277
Therapeutic Targets Database:
DAP000741
FDA Drug Label at DailyMed:
13bb8267-1cab-43e5-acae-55a4d957630a

Clinical Trials

These are trials that mention escitalopram and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.