Drug/Small Molecule:
sertraline

last updated 08/10/2011

Dutch Pharmacogenetics Working Group Guideline for sertraline and CYP2C19

Summary

Reduce sertraline dose by 50% for patients with CYP2C19 poor metabolizer genotypes (PM), and be extra alert to adverse drug events in patients with CYP2C19 intermediate metabolizer genotypes (IM).

Annotation

The Royal Dutch Pharmacists Association - Pharmacogenetics Working Group has evaluated therapeutic dose recommendations for sertraline based on CYP2C19 genotype [Article:21412232].

Phenotype (Genotype) Therapeutic Dose Recommendation Level of Evidence Clinical Relevance
CYP2C19 PM (*2/*2, *2/*3, *3/*3) Reduce dose by 50%. Published controlled studies of moderate quality relating to phenotyped and/or genotyped patients or healthy volunteers, and having relevant pharmacokinetic or clinical endpoints Clinical effect (statistically significant difference): long-standing discomfort (48-168 hr) without permanent injury e.g. failure of therapy with tricyclic antidepressants, atypical antipsychotic drugs; extrapyramidal side effects; parkinsonism; adverse drug events resulting from increased bioavailability of tricyclic antidepressants, metoprolol, propafenone (central effects e.g. dizziness); international normalized ratio 4.5-6.0; neutropenia 1.0-1.5x109/l; leucopenia 2.0-3.0x109/l; thrombocytopenia 50-75x109/l
CYP2C19 IM (*1/*2, *1/*3, *17/*2, *17/*3) Insufficient data to allow calculation of dose adjustment. Be extra alert to adverse drug events (e.g., nausea, vomiting, diarrhea). Published controlled studies of moderate 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 increase < 4.5
Kinetic effect (statistically significant difference)
CYP2C19 UM (*17/*17) None no data was retrieved with the literature search no data was retrieved with the literature search

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 sertraline that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105245

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 No VIP available VA CYP2C19 *1A N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *1B N/A N/A N/A
No VIP available CA VA CYP2C19 *2 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *2B N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *2C 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 *8 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *9 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *10 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *11 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *13 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *14 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *15 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *16 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *17 N/A N/A N/A
No VIP available No VIP available VA CYP2C19 *19 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *1 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *2 N/A N/A N/A
No VIP available No VIP available VA CYP2C9 *3 N/A N/A N/A
No VIP available CA VA CYP2D6 *1 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *1XN N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *2 N/A N/A N/A
No VIP available No VIP available 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 No VIP available VA CYP2D6 *5 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *6 N/A N/A N/A
No VIP available No VIP available 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 No VIP available 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
rs1109866 117G>A, 220083279C>T, 5434G>A, 70292697C>T, Leu39=
C > T
Synonymous
Leu39Leu
No VIP available No Clinical Annotations available VA
rs1109867 -58C>A, 220083453G>T, 5260C>A, 70292871G>T
G > T
5' UTR
No VIP available CA VA
rs13432159 46795774T>G, 67973887T>G
T > G
Not Available
No VIP available CA VA
rs153549 112236297A>G, 20550169A>G, 351+1780T>C
A > G
Intronic
No VIP available CA VA
rs153560 112254377G>A, 20568249G>A, 212+2483C>T
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs182694 43698815A>G, 522+1760A>G, 579+1760A>G, 588+1760A>G, 594+1760A>G, 621+1760A>G, 693256A>G
A > G
Intronic
No VIP available CA VA
rs2032583 187004T>C, 25193404A>G, 2685+49T>C, 87160561A>G
A > G
Intronic
No VIP available CA VA
rs2235040 181815G>A, 2481+24G>A, 25198593C>T, 87165750C>T
C > T
Intronic
No VIP available CA VA
rs28401781 199237G>A, 25181171C>T, 2927+314G>A, 87148328C>T
C > T
Intronic
No VIP available No Clinical Annotations available VA
rs3731885 *700C>T, -1074C>T, 220084469G>A, 4244C>T, 70293887G>A
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs3747802 -440T>C, 25375429A>G, 458+2615A>G, 4979T>C, 509+2615A>G, 87342586A>G
A > G
5' UTR
No VIP available No Clinical Annotations available VA
rs3755047 *305C>T, -1469C>T, 220084864G>A, 3849C>T, 70294282G>A
G > A
5' Flanking
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
rs4148739 186516A>G, 2482-236A>G, 25193892T>C, 87161049T>C
T > C
Intronic
VIP No Clinical Annotations available No Variant Annotations available
rs4680 1-5G>A, 19951271G>A, 27009G>A, 3103421G>A, 322G>A, 472G>A, COMP: Val158Met, COMT:Val108Met, Val108Met, Val158Met
G > A
5' Flanking
Val158Met
No VIP available CA VA
rs495794 112201094A>G, 20514966A>G, 225+665A>G, 229+665A>G, 301+665A>G
A > G
Intronic
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
rs6265 196G>A, 220G>A, 241G>A, 27619916C>T, 27679916C>T, 283G>A, 434C>T, 442G>A, 503C>T, 68690G>A, BDNF:Val66Met, Val148Met, Val66Met, Val74Met, Val81Met, Val95Met
C > T
Missense
Val66Met
No VIP available CA VA
rs6295 1-1019C>G, 1-1019G>C, 13852924C>C, 13852924C>G, 4555G>C, 4555G>G, 63258565C>C, 63258565C>G, HTR1A: -1019C/G
C > G
5' Flanking
No VIP available No Clinical Annotations available VA
rs6946119 25161708T>C, 87128865T>C
T > C
Not Available
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Sertralina [Spanish]
  • Sertraline Hydrochloride
  • Sertralinum [Latin]
  • Sultamicillin Tosylate
Trade Names
  • Apo-Sertraline
  • Lustral
  • Zoloft
Brand Mixture Names

PharmGKB Accession Id:
PA451333

Description

Sertraline hydrochloride 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 (see Toxicity section below for a more detailed listing of side effects). Compared to other agents in this class, sertraline may cause greater diarrheal and male sexual dysfunction effects. Side effects generally occur within the first two weeks of therapy and are usually less severe and frequent than those observed with tricyclic antidepressants. Sertraline may be used to treat major depressive disorder, obsessive-compulsive disorder (OCD), panic disorder, post-traumatic stress disorder (PTSD), premenstrual dysphoric disorder (PMDD) and social anxiety disorder (social phobia).

Source: Drug Bank

Indication

For the management of major depressive disorder, posttraumatic stress disorder, obsessive-compulsive disorder, panic disorder with or without agoraphobia, premenstrual dysphoric disorder, social phobia, premature ejaculation, and vascular headaches.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The exact mechanism of action sertraline is not fully known, but the drug appears to selectively inhibit the reuptake of serotonin at the presynaptic membrane. This results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission. It is suggested that these modifications are responsible for the antidepressant action observed during long term administration of antidepressants. It has also been hypothesized that obsessive-compulsive disorder is caused by the dysregulation of serotonin, as it is treated by sertraline, and the drug corrects this imbalance.

Source: Drug Bank

Pharmacology

Sertraline, an antidepressant drug similar to citalopram, fluoxetine, and paroxetine, is of the selective serotonin reuptake inhibitor (SSRI) type. Sertraline has one active metabolite and, like the other SSRIs, have less sedative, anticholinergic, and cardiovascular effects than the tricyclic antidepressant drugs because it does not have clinically important anticholinergic, antihistamine, or adrenergic blocking activity.

Source: Drug Bank

Food Interaction

Avoid St.John's Wort.|Avoid alcohol.|Avoid taking with grapefruit juice.|Take with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Extensively metabolized in the liver. Sertraline metabolism involves N-demethylation, N-hydroxylation, oxidative deamination, and glucuronidation of sertraline carbamic acid. Sertraline undergoes N-demethylation primarily catalyzed by cytochrome P450 (CYP) 2B6, with CYP2C19, CYP3A4 and CYP2D6 contributing to a lesser extent. Deamination occurs via CYP3A4 and CYP2C19. In vitro studies have shown that monoamine oxidase A and B may also catalyze sertraline deamination. Sertraline N-carbamoyl glucuronidation has also been observed in human liver microsomes.

Source: Drug Bank

Protein Binding

98% bound to serum proteins, principally to albumin and alpha 1-acid glycoprotein

Source: Drug Bank

Absorption

The effects of food on the bioavailability of the sertraline tablet and oral concentrate were studied in subjects administered a single dose with and without food. For the tablet, AUC was slightly increased when drug was administered with food but the Cmax was 25% greater, while the time to reach peak plasma concentration (Tmax) decreased from 8 hours post-dosing to 5.5 hours. For the oral concentrate, Tmax was slightly prolonged from 5.9 hours to 7.0 hours with food.

Source: Drug Bank

Half-Life

The elimination half-life of sertraline is approximately 25-26 hours. The elimination half-life of desmethylsertraline is approximately 62-104 hours.

Source: Drug Bank

Toxicity

Symptoms of toxicity include alopecia, decreased libido, diarrhea, ejaculation disorder, fatigue, insomnia, somnolence and serotonin syndrome. The most frequently observed side effects include: GI effects such as nausea, diarrhea or loose stools, dyspepsia, and dry mouth; nervous system effects such as somnolence, dizziness, insomnia, and tremor; sexual dysfunction in males (principally ejaculatory delay); and sweating.

Source: Drug Bank

Route of Elimination

Sertraline is extensively metabolized and excretion of unchanged drug in urine is a minor route of elimination.

Source: Drug Bank

Chemical Properties

Chemical Formula

C17H17Cl2N

Source: Drug Bank

Isomeric SMILES

CN[C@H]1CC[C@H](c2c1cccc2)c3ccc(c(c3)Cl)Cl

Source: OpenEye

Canonical SMILES

CN[C@H]1CC[C@@H]

Source: Drug Bank

Average Molecular Weight

306.23

Source: Drug Bank

Monoisotopic Molecular Weight

305.073804963

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Selective Serotonin Reuptake Inhibitor Pathway, Pharmacodynamics
    Genes involved in serotonin synthesis, release, reuptake, and in mediation of the antidepressant effect of selective serotonin reuptake inhibitors (SSRI) in human brain.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

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
HTR1A (source: Drug Bank)
SLC6A3 (source: Drug Bank)
SLC6A4 (source: Drug Bank)

Drug Interactions

Drug Description
sertraline Increased risk of CNS adverse effects (source: Drug Bank)
sertraline Increased risk of CNS adverse effects (source: Drug Bank)
sertraline Sertraline increases the effect of carbamazepine (source: Drug Bank)
sertraline Sertraline increases the effect of carbamazepine (source: Drug Bank)
sertraline The SSRI increases the effect of the beta-blocker (source: Drug Bank)
sertraline The SSRI, sertraline, may increase the bradycardic effect of the beta-blocker, carvedilol. (source: Drug Bank)
sertraline Sertraline increases the effect of cilostazol (source: Drug Bank)
sertraline Possible serotoninergic syndrome with this combination (source: Drug Bank)
sertraline Possible serotoninergic syndrome with this combination (source: Drug Bank)
sertraline The antidepressant increases the effect of clozapine (source: Drug Bank)
sertraline The antidepressant increases the effect of clozapine (source: Drug Bank)
sertraline Possible antagonism of action (source: Drug Bank)
sertraline Possible antagonism of action (source: Drug Bank)
sertraline Increased risk of CNS adverse effects (source: Drug Bank)
sertraline Increased risk of CNS adverse effects (source: Drug Bank)
sertraline Possible serotoninergic syndrome with this combination (source: Drug Bank)
sertraline Possible serotoninergic syndrome with this combination (source: Drug Bank)
sertraline Sertraline increases the effect of hydantoin (source: Drug Bank)
sertraline Increased risk of CNS adverse effects (source: Drug Bank)
sertraline Possible antagonism of action (source: Drug Bank)
sertraline Possible antagonism of action (source: Drug Bank)
sertraline Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided. (source: Drug Bank)
sertraline Possible severe adverse reaction with this combination (source: Drug Bank)
sertraline Possible severe adverse reaction with this combination (source: Drug Bank)
sertraline 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)
sertraline Combination associated with possible serotoninergic syndrome (source: Drug Bank)
sertraline Combination associated with possible serotoninergic syndrome (source: Drug Bank)
sertraline The SSRI increases the effect of the beta-blocker (source: Drug Bank)
sertraline The SSRI increases the effect of the beta-blocker (source: Drug Bank)
sertraline Possible severe adverse reaction with this combination (source: Drug Bank)
sertraline Possible severe adverse reaction with this combination (source: Drug Bank)
sertraline Increased risk of CNS adverse effects (source: Drug Bank)
sertraline Increased risk of CNS adverse effects (source: Drug Bank)
sertraline Increased risk of serotonin syndrome (source: Drug Bank)
sertraline Increased risk of serotonin syndrome (source: Drug Bank)
sertraline Possible severe adverse reaction with this combination (source: Drug Bank)
sertraline Possible severe adverse reaction with this combination (source: Drug Bank)
sertraline Sertraline increases the effect of hydantoin (source: Drug Bank)
sertraline Sertraline increases the effect of hydantoin (source: Drug Bank)
sertraline The SSRI increases the effect and toxicity of pimozide (source: Drug Bank)
sertraline The SSRI, sertraline, increases the effect and toxicity of pimozide. (source: Drug Bank)
sertraline Fluoxetine increases the effect and toxicity of propafenone (source: Drug Bank)
sertraline Fluoxetine increases the effect and toxicity of propafenone (source: Drug Bank)
sertraline The SSRI increases the effect of the beta-blocker (source: Drug Bank)
sertraline The SSRI, sertraline, may increase the bradycardic effect of the beta-blocker, propranolol. (source: Drug Bank)
sertraline Possible severe adverse reaction with this combination (source: Drug Bank)
sertraline Sertraline may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
sertraline Sertraline may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
sertraline Sertraline, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Sertraline is initiated, discontinued, or dose changed. (source: Drug Bank)
sertraline Sertraline, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Sertraline is initiated, discontinued, or dose changed. (source: Drug Bank)
sertraline Terbinafine may reduce the metabolism and clearance of Sertraline. Consider alternate therapy or monitor for therapeutic/adverse effects of Sertraline if Terbinafine is initiated, discontinued or dose changed. (source: Drug Bank)
sertraline Additive antiplatelet effects increase the risk of bleeding. Consider alternate therapy or monitor for increased bleeding. (source: Drug Bank)
sertraline Tipranavir increases the concentration of Sertraline. The Sertraline dose may require an adjustment. (source: Drug Bank)
sertraline 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)
sertraline Sertraline may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
sertraline Sertraline may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
sertraline Tramadol increases the risk of serotonin syndrome and seizures. Sertraline may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Sertraline may decrease the effect of Tramadol by decreasing active metabolite production. (source: Drug Bank)
sertraline 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)
sertraline Increased risk of serotonin syndrome. The CYP3A4 inhibitor, Sertraline, may also increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. The 2D6 inhibitor, Trazodone, may increase the efficacy of Sertraline by decreasing Sertraline metabolism and clearance. Monitor for symptoms of serotonin syndrome and changes in Trazodone and Sertraline efficacy/toxicity if either agent is initiated, discontinued or dose changed. (source: Drug Bank)
sertraline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
sertraline The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Sertraline. Monitor for increased bleeding during concomitant thearpy. (source: Drug Bank)
sertraline The SSRI, Sertraline, may decrease the metabolism and clearance of Trimipramine. Increased risk of serotonin syndrome. Monitor for changes in Trimipramine efficacy and toxicity if Sertraline is initiated, discontinued or dose changed. (source: Drug Bank)
sertraline The CNS depressants, Triprolidine and Sertraline, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
sertraline The CNS depressants, Triprolidine and Sertraline, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
sertraline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
sertraline Use of two serotonin modulators, such as zolmitriptan and sertraline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy. (source: Drug Bank)

Curated Information ?

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

May Treat
Contraindicated With

Publications related to sertraline: 77

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Resolution of a clinical AmpliChip CYP450 Test™ no call: discovery and characterization of novel CYP2D6*1 haplotypes. Pharmacogenomics. 2014. Gaedigk Andrea, 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
The genetics of pro-arrhythmic adverse drug reactions. British journal of clinical pharmacology. 2014. Petropoulou Evmorfia, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
ABCB6, ABCB1 and ABCG1 genetic polymorphisms and antidepressant response of SSRIs in Chinese depressive patients. Pharmacogenomics. 2013. Huang Xiaoye, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Pharmacogenetics in major depression: a comprehensive meta-analysis. Progress in neuro-psychopharmacology & biological psychiatry. 2013. Niitsu Tomihisa, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
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 CA VA No VIP available No VIP available
Serotonin transporter genotype and function in relation to antidepressant response in Koreans. Psychopharmacology. 2013. Myung Woojae, 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
Cytochrome P450-mediated drug metabolism in the brain. Journal of psychiatry & neuroscience : JPN. 2012. Miksys Sharon, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of APC and REEP5 gene polymorphisms with major depression disorder and treatment response to antidepressants in a Han Chinese population. General hospital psychiatry. 2012. Yang Zhenxing, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA 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
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenomic study of side-effects for antidepressant treatment options in STAR*D. Psychological medicine. 2012. Clark S L, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
ABCB1 gene variants influence tolerance to selective serotonin reuptake inhibitors in a large sample of Dutch cases with major depressive disorder. The pharmacogenomics journal. 2012. de Klerk O L, 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
Association between serotonin transporter gene promoter-region polymorphism and 4- and 12-week treatment response to sertraline in posttraumatic stress disorder. Journal of affective disorders. 2012. Mushtaq Dhuha, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Determinants of pharmacodynamic trajectory of the therapeutic response to paroxetine in Japanese patients with panic disorder. European journal of clinical pharmacology. 2011. Ishiguro Shin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Evaluation of the effects of 18 non-synonymous single-nucleotide polymorphisms of CYP450 2C19 on in vitro drug inhibition potential by a fluorescence-based high-throughput assay. Xenobiotica; the fate of foreign compounds in biological systems. 2011. Wang Huijuan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
The brain-derived neurotrophic factor (BDNF) polymorphism Val66Met is associated with neither serum BDNF level nor response to selective serotonin reuptake inhibitors in depressed Japanese patients. Progress in neuro-psychopharmacology & biological psychiatry. 2011. Yoshimura Reiji, 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: From Bench to Byte- An Update of Guidelines. Clinical pharmacology and therapeutics. 2011. Swen J J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Predictive factors for responding to sertraline treatment: views from plasma catecholamine metabolites and serotonin transporter polymorphism. Journal of psychopharmacology (Oxford, England). 2010. Umene-Nakano Wakako, 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
Identifying genomic and developmental causes of adverse drug reactions in children. Pharmacogenomics. 2010. Becker Mara L, 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
HTR2A is associated with SSRI response in Major Depressive Disorder in a Japanese cohort. Neuromolecular medicine. 2010. Kishi Taro, et al. PubMed
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Early response to selective serotonin reuptake inhibitors in panic disorder is associated with a functional 5-HT1A receptor gene polymorphism. Journal of affective disorders. 2010. Yevtushenko Olga O, 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 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
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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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Composite functional genetic and comedication CYP2D6 activity score in predicting tamoxifen drug exposure among breast cancer patients. Journal of clinical pharmacology. 2010. Borges Silvana, et al. PubMed
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Selective serotonin reuptake inhibitors and breast cancer mortality in women receiving tamoxifen: a population based cohort study. BMJ (Clinical research ed.). 2010. Kelly Catherine M, et al. PubMed
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Effects of selective serotonin reuptake inhibitor therapy on endothelial function and inflammatory markers in patients with coronary heart disease. Clinical pharmacology and therapeutics. 2009. Pizzi C, 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
Warfarin interactions with substances listed in drug information compendia and in the FDA-approved label for warfarin sodium. Clinical pharmacology and therapeutics. 2009. Anthony M, et al. PubMed
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Sertraline hepatotoxicity: report of a case and review of the literature. Digestive diseases and sciences. 2009. Tabak Fehmi, et al. PubMed
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Pharmacogenetics of selective serotonin reuptake inhibitors and associated adverse drug reactions. Pharmacotherapy. 2009. Thomas Kelan L H, et al. PubMed
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Histone deacetylase inhibitors induce a very broad, pleiotropic anticancer drug resistance phenotype in acute myeloid leukemia cells by modulation of multiple ABC transporter genes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2009. Hauswald Stefanie, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
5-HTR1A, 5-HTR2A, 5-HTR6, TPH1 and TPH2 polymorphisms and major depression. Neuroreport. 2009. Illi Ari, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Genetic determinants of response to clopidogrel and cardiovascular events. The New England journal of medicine. 2009. Simon Tabassome, 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
Decreased susceptibility of the cytochrome P450 2B6 variant K262R to inhibition by several clinically important drugs. Drug metabolism and disposition: the biological fate of chemicals. 2009. Talakad Jyothi C, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Effect of 5-HT1A gene polymorphisms on antidepressant response in major depressive disorder. American journal of medical genetics. Part B, Neuropsychiatric genetics : the official publication of the International Society of Psychiatric Genetics. 2009. Kato Masaki, et al. PubMed
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Redox regulation of multidrug resistance in cancer chemotherapy: molecular mechanisms and therapeutic opportunities. Antioxidants & redox signaling. 2009. Kuo Macus Tien. PubMed
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Serum concentrations of sertraline and N-desmethyl sertraline in relation to CYP2C19 genotype in psychiatric patients. European journal of clinical pharmacology. 2008. Rudberg I, et al. PubMed
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Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008. Luna-Tortós Carlos, et al. PubMed
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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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5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies. The international journal of neuropsychopharmacology / official scientific journal of the Collegium Internationale Neuropsychopharmacologicum (CINP). 2008. Drago Antonio, et al. PubMed
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Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
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Serotonin transporter gene polymorphisms and sertraline response in major depression patients. Genetic testing. 2008. Dogan Ozlem, et al. PubMed
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Serotonin receptor 1A-1019C/G variant: impact on antidepressant pharmacoresponse in melancholic depression?. Neuroscience letters. 2008. Baune B T, 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
Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression. Neuron. 2008. Uhr Manfred, et al. PubMed
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Citalopram enantiomers in plasma and cerebrospinal fluid of ABCB1 genotyped depressive patients and clinical response: a pilot study. Pharmacological research : the official journal of the Italian Pharmacological Society. 2008. Nikisch Georg, et al. PubMed
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Stevens-Johnson syndrome and toxic epidermal necrolysis: assessment of medication risks with emphasis on recently marketed drugs. The EuroSCAR-study. The Journal of investigative dermatology. 2008. Mockenhaupt Maja, et al. PubMed
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Influence of cytochrome P450 polymorphisms on drug therapies: pharmacogenetic, pharmacoepigenetic and clinical aspects. Pharmacology & therapeutics. 2007. Ingelman-Sundberg Magnus, et al. PubMed
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Tricyclic antidepressant pharmacology and therapeutic drug interactions updated. British journal of pharmacology. 2007. Gillman P K. 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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Cobalamin potentiates vinblastine cytotoxicity through downregulation of mdr-1 gene expression in HepG2 cells. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2007. Marguerite Véronique, et al. PubMed
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Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Molecular pharmaceutics. 2007. Collnot Eva-Maria, et al. PubMed
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Monoamine transporter gene polymorphisms and antidepressant response in koreans with late-life depression. JAMA : the journal of the American Medical Association. 2006. Kim Hyeran, et al. PubMed
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Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer research. 2006. Leggas Markos, et al. PubMed
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Impact of P-glycoprotein on clopidogrel absorption. Clinical pharmacology and therapeutics. 2006. Taubert Dirk, 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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Single nucleotide polymorphisms in human P-glycoprotein: its impact on drug delivery and disposition. Expert opinion on drug delivery. 2006. Dey Surajit. PubMed
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Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study. Drug metabolism and disposition: the biological fate of chemicals. 2005. Obach R Scott, et al. PubMed
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The serotonin transporter polymorphism, 5HTTLPR, is associated with a faster response time to sertraline in an elderly population with major depressive disorder. Psychopharmacology. 2004. Durham L Kathryn, et al. PubMed
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Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical pharmacology. 2004. Ehrhardt Manuela, et al. PubMed
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Impact of polymorphisms of cytochrome-P450 isoenzymes 2C9, 2C19 and 2D6 on plasma concentrations and clinical effects of antidepressants in a naturalistic clinical setting. European journal of clinical pharmacology. 2004. Grasmäder Katja, et al. PubMed
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Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, et al. PubMed
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Breastfeeding during maternal antidepressant treatment with serotonin reuptake inhibitors: infant exposure, clinical symptoms, and cytochrome p450 genotypes. The Journal of clinical psychiatry. 2004. Berle Jan Øystein, et al. PubMed
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Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, et al. PubMed
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Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
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Pharmacokinetics of sertraline in relation to genetic polymorphism of CYP2C19. Clinical pharmacology and therapeutics. 2001. Wang J H, et al. PubMed
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Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus C, et al. PubMed
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CYP2B6 mediates the in vitro hydroxylation of bupropion: potential drug interactions with other antidepressants. Drug metabolism and disposition: the biological fate of chemicals. 2000. Hesse L M, et al. PubMed
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The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
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Evidence for involvement of polymorphic CYP2C19 and 2C9 in the N-demethylation of sertraline in human liver microsomes. British journal of clinical pharmacology. 1999. Xu Z H, et al. PubMed
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Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual review of pharmacology and toxicology. 1999. Ambudkar S V, et al. PubMed
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Competitive, non-competitive and cooperative interactions between substrates of P-glycoprotein as measured by its ATPase activity. Biochimica et biophysica acta. 1997. Litman T, et al. PubMed
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The disposition of fluoxetine but not sertraline is altered in poor metabolizers of debrisoquin. Clinical pharmacology and therapeutics. 1996. Hamelin B A, et al. PubMed
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Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clinical pharmacokinetics. 1996. Baumann P. PubMed
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P-glycoprotein structure and evolutionary homologies. Cytotechnology. 1993. Croop J M. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0049-4960-30
DrugBank:
DB01104
ChEBI:
9123
KEGG Compound:
C07246
KEGG Drug:
D02360
PubChem Compound:
68617
PubChem Substance:
210738
46505341
Drugs Product Database (DPD):
2245749
ChemSpider:
61881
Therapeutic Targets Database:
DAP000051
FDA Drug Label at DailyMed:
fe9e8b7d-61ea-409d-84aa-3ebd79a046b5

Clinical Trials

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

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