What is Sertraline (Selective Serotonin Reuptake Inhibitor - SSRI)?

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From the Guidelines

Sertraline is a selective serotonin reuptake inhibitor (SSRI) that is commonly prescribed for various mental health conditions, including depression, anxiety disorders, and obsessive-compulsive disorder, with an initial dose of 50mg once daily, which can be gradually increased to a maximum of 200mg daily based on response and tolerability.

Key Points

  • Sertraline works by increasing serotonin levels in the brain, a neurotransmitter that helps regulate mood, anxiety, and other psychological functions 1.
  • Patients should take sertraline at the same time each day, with or without food, and should continue treatment even after feeling better, as stopping abruptly can cause withdrawal symptoms 1.
  • Common side effects include nausea, diarrhea, insomnia, sexual dysfunction, and increased sweating, which often improve over time 1.
  • It typically takes 2-4 weeks to begin noticing improvement in symptoms, with full benefits sometimes taking 8-12 weeks 1.
  • Patients should inform their doctor about all other medications they're taking, as sertraline can interact with certain drugs, particularly MAOIs, which should never be taken concurrently due to risk of serotonin syndrome 1.

Important Considerations

  • Sertraline has a boxed warning for suicidal thinking and behavior in children and adolescents, and close monitoring is recommended, especially in the first months of treatment and following dosage adjustments 1.
  • The medication can also cause behavioral activation/agitation, mania/hypomania, and sexual dysfunction, and patients should be educated about these potential side effects 1.
  • Sertraline can interact with other medications, including opioids, stimulants, and cough/cold/allergy medications, and caution should be exercised when combining these medications 1.

From the FDA Drug Label

Sertraline hydrochloride is a selective serotonin reuptake inhibitor (SSRI) for oral administration. The mechanism of action of sertraline is presumed to be linked to its inhibition of CNS neuronal uptake of serotonin (5HT).

Sertraline is a Selective Serotonin Reuptake Inhibitor (SSRI), which means it works by inhibiting the reuptake of serotonin in the central nervous system. This action is believed to be responsible for its therapeutic effects. 2, 2, 2

From the Research

Definition and Mechanism of Action

  • Sertraline is a naphthalenamine derivative with the predominant pharmacological action of inhibiting presynaptic reuptake of serotonin from the synaptic cleft 3.
  • It is a selective serotonin reuptake inhibitor (SSRI) that has been used and studied extensively throughout the world and found to be safe and well tolerated in numerous patient populations 4.

Therapeutic Uses

  • Sertraline was initially marketed for the treatment of major depressive disorder and is now approved for the management of panic disorder, obsessive-compulsive disorder, and post-traumatic stress disorder 3.
  • It is an effective treatment for depressive and anxiety disorders, including social anxiety disorder, posttraumatic stress disorder, panic disorder, and generalized anxiety disorder 4.
  • Sertraline has been used as a treatment for anxiety disorders since the mid 1990s and has proven itself an effective, well-tolerated, and economically viable treatment for panic disorder 5.

Pharmacokinetics and Tolerability

  • Sertraline is slowly absorbed following oral administration and undergoes extensive first-pass oxidation to form N-desmethyl-sertraline, a weakly active metabolite 3.
  • It has a good tolerability profile and has low fatal toxicity, with the most common adverse events being nausea, sexual dysfunction, somnolence, asthenia, headache, constipation, dizziness, sweating, tremor, and decreased appetite 4, 6.
  • Sertraline has minimal inhibitory effects on the major cytochrome P450 enzymes, and few drug-drug interactions of clinical significance have been documented 3.

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Clinical pharmacokinetics of sertraline.

Clinical pharmacokinetics, 2002

Research

Sertraline in the treatment of panic disorder.

Drugs of today (Barcelona, Spain : 1998), 2009

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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