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Active substances

Sertraline

Author: Markus Falkenstätter, BScReviewed by Mag. pharm. Stefanie Brandauer (Pharmacist)
Contents
  1. Basics
  2. Pharmacology
  3. Toxicity

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Basics

Sertraline is an antidepressant in the selective serotonin reuptake inhibitor (SSRI) class. It is used to treat depressive disorders, obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, and social anxiety disorder. Sertraline is usually administered orally and is only available by prescription.

Pharmacology

Pharmacodynamics

Sertraline acts as a potent serotonin reuptake inhibitor (SSRI). By inhibiting the reuptake of serotonin, sertraline increases extracellular serotonin levels, thereby increasing serotonergic neurotransmission in the brain. This mechanism is responsible for the antidepressant effect.

Pharmacokinetics

Sertraline is slowly absorbed when taken orally and reaches its maximum concentration in plasma 4 to 6 hours after administration. In blood, it is 98.5% bound to plasma proteins and has a half-life of 25 to 26 hours. Sertraline is inactivated in the liver by demethylation. Sertraline is metabolized by several cytochrome 450 isoforms: CYP2D6, CYP2C9, CYP2B6, CYP2C19, and CYP3A4.

Toxicity

Side effects

Compared to other SSRIs, sertraline tends to be associated with higher rates of psychiatric side effects and diarrhea.

Common and very common side effects:

  • Insomnia
  • Drowsiness
  • Headache
  • Dizziness
  • Gastrointestinal disorders
  • Nausea
  • Diarrhea
  • Dry mouth
  • Ejaculation disorders
  • nervousness
  • Sweating
  • tremor
  • Skin rash
  • Vomiting
  • dyspepsia
  • sexual dysfunction
  • hot flushes
  • micturition disorders
  • palpitations
  • chest pain

Toxicological data

LD50 (rat,oral): 840 mg-kg-1

Markus Falkenstätter, BSc

Author

Markus Falkenstätter, BSc

Pharmacy student

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Brandauer

Reviewer

Mag. pharm. Stefanie Brandauer

Pharmacist

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.


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