Description

Simple

An antidepressant used to treat depression, anxiety and a variety of other psychiatric disorders.

Clinical

A selective serotonin reuptake inhibitor (SSRI) indicated to treat major depressive disorder, social anxiety disorder and many other psychiatric conditions.

Overview

Sertraline is a popular antidepressant medication known as a selective serotonin reuptake inhibitor (SSRI), and is similar to drugs such as [Citalopram] and [Fluoxetine]. Despite marked structural differences between compounds in this drug class, SSRIs exert similar pharmacological effects. Several weeks of therapy with sertraline may be required before beneficial effects are noticed. Sertraline displays enhanced safety or tolerability than other classes of antidepressants, which frequently cause high levels of drowsiness, dizziness, blurred vision, and other undesirable effects.[6,10,17]

Pharmacology

Indication

Sertraline is indicated for the management of major depressive disorder (MDD), post-traumatic stress disorder (PTSD), obsessive-compulsive disorder (OCD), panic disorder (PD), premenstrual dysphoric disorder (PMDD), and social anxiety disorder (SAD).[ Read more

Pharmacodynamic

Sertraline improves or relieves the symptoms of depression, OCD, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, and premenstrual dysphoric disorder via the inhibition of serotonin reuptake.[ Read more

Mechanism of action

Sertraline selectively inhibits the reuptake of serotonin (5-HT) 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.[ Read more

Absorption

Following once-daily administration over the range of 50 to 200 mg for 14 days, mean peak plasma concentrations (Cmax) of sertraline occurred between 4.5 to 8.4 hours post-administration.[19] The steady-state concentration... Read more

Protein binding

Sertraline is highly bound to serum proteins, at about 98%-99%[ Read more

Volume of distribution

Sertraline has a volume of distribution of 201 kg^(-1)[ Read more

Clearance

Information currently not available.

Half life

The elimination half-life of sertraline is approximately 25-26 hours. The elimination half-life of desmethylsertraline is approximately 62-104 hours.[19]

Route of elimination

Sertraline is extensively metabolized and excretion of unchanged drug in urine is a minor route of elimination.[19] Sertraline metabolites are also eliminated in the faeces. In a study of radiolabeled sertraline involving... Read more

Toxicity

The LD50 of sertraline is >2000 mg/kg in rats.[23]

The most common signs and symptoms associated with non-fatal sertraline overdosage were somnolence, vomiting, tachycardia, nausea, dizziness, agitation and tremor... Read more

Adverse Effects

Contraindications

  • Regions: US
  • With Categories Coadmin:
      • Name: Monoamine Oxidase Inhibitors
      • Drugbank Id: DBCAT001004
      • Mesh Id: D008996
  • Regions: US
  • With Drugs Coadmin:
      • Name: Methylene blue
      • Drugbank Id: DB09241
  • Regions: US
  • With Drugs Coadmin:
      • Name: Linezolid
      • Drugbank Id: DB00601
  • Hypersensitivity:
    • disulfiram
  • Regions: US
  • Regions: US
  • With Drugs Coadmin:
      • Name: Pimozide
      • Drugbank Id: DB01100

Food Interactions

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

Interactions

Type in a drug name to check for interaction with Sertraline
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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 serum concentration of (R)-warfarin can be increased when it is combined with Sertraline.
(S)-Warfarin
The serum concentration of (S)-Warfarin can be increased when it is combined with Sertraline.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Sertraline can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Sertraline is combined with 2,4-thiazolidinedione.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when Sertraline is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when 2,5-Dimethoxy-4-ethylthioamphetamine is combined with Sertraline.
3,5-Diiodotyrosine
The therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Sertraline.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Sertraline is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
The risk or severity of hemorrhage can be increased when Sertraline is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Sertraline is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when 5-methoxy-N,N-dimethyltryptamine is combined with Sertraline.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Sertraline is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the serotonergic activities of Sertraline.
9-aminocamptothecin
The metabolism of 9-aminocamptothecin can be decreased when combined with Sertraline.
Abaloparatide
The therapeutic efficacy of Abaloparatide can be decreased when used in combination with Sertraline.
Abatacept
The metabolism of Sertraline can be increased when combined with Abatacept.
Abciximab
The risk or severity of hemorrhage can be increased when Sertraline is combined with Abciximab.
Abemaciclib
The serum concentration of Abemaciclib can be increased when it is combined with Sertraline.
Abexinostat
The risk or severity of QTc prolongation can be increased when Sertraline is combined with Abexinostat.
Abiraterone
The metabolism of Sertraline can be decreased when combined with Abiraterone.
24 References
  1. 1 . Fabre LF, Abuzzahab FS, Amin M, Claghorn JL, Mendels J, Petrie WM, Dube S, Small JG: Sertraline safety and efficacy in major depression: a double-blind fixed-dose comparison with placebo. Biol Psychiatry. 1995 Nov 1;38(9):592-602.PubMed: 8573661
  2. 2 . Kronig MH, Apter J, Asnis G, Bystritsky A, Curtis G, Ferguson J, Landbloom R, Munjack D, Riesenberg R, Robinson D, Roy-Byrne P, Phillips K, Du Pont IJ: Placebo-controlled, multicenter study of sertraline treatment for obsessive-compulsive disorder. J Clin Psychopharmacol. 1999 Apr;19(2):172-6.PubMed: 10211919
  3. 3 . Brady K, Pearlstein T, Asnis GM, Baker D, Rothbaum B, Sikes CR, Farfel GM: Efficacy and safety of sertraline treatment of posttraumatic stress disorder: a randomized controlled trial. JAMA. 2000 Apr 12;283(14):1837-44.PubMed: 10770145
  4. 4 . Yonkers KA, Halbreich U, Freeman E, Brown C, Endicott J, Frank E, Parry B, Pearlstein T, Severino S, Stout A, Stone A, Harrison W: Symptomatic improvement of premenstrual dysphoric disorder with sertraline treatment. A randomized controlled trial. Sertraline Premenstrual Dysphoric Collaborative Study Group. JAMA. 1997 Sep 24;278(12):983-8.PubMed: 9307345
  5. 5 . Shelton RC: The role of sertraline in the management of depression. Clin Ther. 1994 Sep-Oct;16(5):768-82; discussion 767.PubMed: 7859236
  6. 6 . Murdoch D, McTavish D: Sertraline. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depression and obsessive-compulsive disorder. Drugs. 1992 Oct;44(4):604-24.PubMed: 1281075
  7. 7 . DeVane CL, Liston HL, Markowitz JS: Clinical pharmacokinetics of sertraline. Clin Pharmacokinet. 2002;41(15):1247-66. doi: 10.2165/00003088-200241150-00002.PubMed: 12452737
  8. 8 . Cooper JM, Duffull SB, Saiao AS, Isbister GK: The pharmacokinetics of sertraline in overdose and the effect of activated charcoal. Br J Clin Pharmacol. 2015 Feb;79(2):307-15. doi: 10.1111/bcp.12500.PubMed: 25155462
  9. 9 . Lau GT, Horowitz BZ: Sertraline overdose. Acad Emerg Med. 1996 Feb;3(2):132-6. doi: 10.1111/j.1553-2712.1996.tb03400.x.PubMed: 8808373
  10. 10 . Cipriani A, La Ferla T, Furukawa TA, Signoretti A, Nakagawa A, Churchill R, McGuire H, Barbui C: Sertraline versus other antidepressive agents for depression. Cochrane Database Syst Rev. 2010 Jan 20;(1):CD006117. doi: http://dx.doi.org/10.1002/14651858.CD006117.PubMed: 20091586
  11. 11 . Feng R, Wang P, Gao C, Yang J, Chen Z, Yang Y, Jiao J, Li M, Fu B, Li L, Zhang Z, Wang S: Effect of sertraline in the treatment and prevention of poststroke depression: A meta-analysis. Medicine (Baltimore). 2018 Dec;97(49):e13453. doi: 10.1097/MD.0000000000013453.PubMed: 30544429
  12. 12 . Narita N, Hashimoto K, Tomitaka S, Minabe Y: Interactions of selective serotonin reuptake inhibitors with subtypes of sigma receptors in rat brain. Eur J Pharmacol. 1996 Jun 20;307(1):117-9.PubMed: 8831113
  13. 13 . Hashimoto K: Sigma-1 receptors and selective serotonin reuptake inhibitors: clinical implications of their relationship. Cent Nerv Syst Agents Med Chem. 2009 Sep;9(3):197-204.PubMed: 20021354
  14. 14 . Doogan DP, Caillard V: Sertraline: a new antidepressant. J Clin Psychiatry. 1988 Aug;49 Suppl:46-51.PubMed: 2842321
  15. 15 . Kristensen JH, Ilett KF, Dusci LJ, Hackett LP, Yapp P, Wojnar-Horton RE, Roberts MJ, Paech M: Distribution and excretion of sertraline and N-desmethylsertraline in human milk. Br J Clin Pharmacol. 1998 May;45(5):453-7. doi: 10.1046/j.1365-2125.1998.00705.x.PubMed: 9643617
  16. 16 . Pittenger C, Bloch MH, Williams K: Glutamate abnormalities in obsessive compulsive disorder: neurobiology, pathophysiology, and treatment. Pharmacol Ther. 2011 Dec;132(3):314-32. doi: 10.1016/j.pharmthera.2011.09.006. Epub 2011 Sep 22.PubMed: 21963369
  17. 17 . 46. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 573-574). Edinburgh: Elsevier/Churchill Livingstone.
  18. 18 . EMA Label: Zoloft; INN: sertraline Link
  19. 19 . Zoloft FDA label Link
  20. 20 . Zoloft, PDR Link
  21. 21 . AAFP: Off-label Applications for SSRIs Link
  22. 22 . Sertraline, pubchem Link
  23. 23 . Sertraline, Pfizer SDS Link
  24. 24 . Sertraline pathway Link