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 commonly 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.[6,10,19]

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 neuronal membrane, thereby increasing serotonergic activity. This results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonerg... Read more

Absorption

Following once-daily administration of 50 to 200 mg for two weeks, the mean peak plasma concentrations (Cmax) of sertraline occurred between 4.5 to 8.4 hours after administration, and measured at 20 to 55 μg/L.[ Read more

Protein binding

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

Volume of distribution

Sertraline is widely distributed, and its volume of distribution is estimated to be more than 20L/kg.[ Read more

Clearance

In pharmacokinetic studies, the clearance of a 200mg dose of sertraline in studies of both young and elderly patients ranged between 1.09 ± 0.38 L/h/kg - 1.35 ± 0.67 L/h/kg.[ Read more

Half life

The elimination half-life of sertraline is approximately 26 hours.[ Read more

Route of elimination

Since sertraline is extensively metabolized, excretion of unchanged drug in the urine is a minor route of elimination, with 12-14% of unchanged sertraline excreted in the feces.[ Read more

Toxicity

The LD50 of sertraline is >2000 mg/kg in rats according to the FDA label.[25] One other references indicates an oral LD50 of in mice and rats of 419 - 548 mg/kg and 1327 - 1591mg/kg, respectively.[MSDS]

The most c... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • adult
  • Kind: experimental
    • Percent: 30%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 29%
  • Kind: placebo
    • Percent: 18%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 12%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 25%
  • Kind: placebo
    • Percent: 18%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 25%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Loose stools US
    • adult
  • Kind: experimental
    • Percent: 24%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 24%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 24%
  • Kind: placebo
    • Percent: 15%
  • Clinical Trial
    Loose stools US
    • adult
  • Kind: experimental
    • Percent: 24%
  • Kind: placebo
    • Percent: 15%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 13-23%
  • Kind: placebo
    • Percent: 3-9%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 22%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 21%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Loose stools US
    • adult
  • Kind: experimental
    • Percent: 21%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 21%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 20%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Ejaculation disorder US
    • adult
  • Kind: experimental
    • Percent: 19%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Loose stools US
    • adult
  • Kind: experimental
    • Percent: 18%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 17%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Ejaculation failure US
    • adult
  • Kind: experimental
    • Percent: 17%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 12-17%
  • Kind: placebo
    • Percent: 10-11%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 16%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Mouth dry US
    • adult
  • Kind: experimental
    • Percent: 16%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Fatigue US
    • adult
  • Kind: experimental
    • Percent: 10-16%
  • Kind: placebo
    • Percent: 0-7%
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Mouth dry US
    • adult
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: 15%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Malaise US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 14%
  • Clinical Trial
    Fatigue US
    • adult
  • Kind: experimental
    • Percent: 14%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial
    Mouth dry US
    • adult
  • Kind: experimental
    • Percent: 14%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Ejaculation failure US
    • adult
  • Kind: experimental
    • Percent: 14%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 14%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 3-7%
  • Clinical Trial
    Loose stools US
    • adult
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 3-7%
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Dyspepsia US
    • adult
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Mouth dry US
    • adult
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Fatigue US
    • adult
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Fatigue US
    • adult
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Libido decreased US
    • adult
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Anorexia US
    • adult
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Fatigue US
    • adult
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 8%
  • Clinical Trial
    Tremor US
    • adult
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Libido decreased US
    • adult
  • Kind: experimental
    • Percent: 4-11%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Sweating increased US
    • adult
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Mouth dry US
    • adult
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Ejaculation failure US
    • adult
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 10%
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Recommended Actions:
      • Avoid use with intravenous methylene blue.
    • Regions: US
    • With Drugs:
        • Name: Methylene blue
        • Drugbank Id: DB09241
    • Route:
      • Oral
    • Regions: US
    • With Drugs:
        • Name: Pimozide
        • Drugbank Id: DB01100
    • Route:
      • Oral
    • Recommended Actions:
      • Do not use with or within 14 days of stopping of MAOIs.
    • Regions: US
    • With Categories:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Route:
      • Oral
    • Hypersensitivity:
      • true
    • Regions: US
    • Route:
      • Oral
    • Dose Form:
      • Solution
    • Recommended Actions:
      • This contraindication applies to the oral solution only. Seek other preparations if disulfiram is given.
    • Regions: US
    • With Drugs:
        • Name: Disulfiram
        • Drugbank Id: DB00822

    Food Interactions

    Avoid St. John's Wort.

    Take with or without food.