Sertraline: Difference between revisions
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| pregnancy = Category C | | pregnancy = Category C | ||
| legal = Rx-only | | legal = Rx-only | ||
| intro = '''Sertraline''' is a selective serotonin reuptake inhibitor (SSRI) commonly prescribed for depression, anxiety disorders, OCD, PTSD, and panic disorder. | | intro = '''Sertraline''' is a selective serotonin reuptake inhibitor (SSRI) commonly prescribed for depression, anxiety disorders, OCD, PTSD, and panic disorder. In the US, it is one of the [https://www.definitivehc.com/resources/healthcare-insights/top-antidepressants-by-prescription-volume most frequently utilized SSRIs at this time]. | ||
| pharmacokinetics = Well-absorbed orally, ~44% bioavailability. Metabolized hepatically via CYP3A4/CYP2C19/CYP2D6 to N-desmethylsertraline (less active). Half-life ~26h; steady state in ~1 week. | | pharmacokinetics = Well-absorbed orally, ~44% bioavailability. Metabolized hepatically via CYP3A4/CYP2C19/CYP2D6 to N-desmethylsertraline (less active). Half-life ~26h; steady state in ~1 week. | ||
| pharmacodynamics = Highly selective inhibitor of the serotonin reuptake transporter (SERT). Mild dopamine reuptake inhibition at higher doses. Minimal affinity for muscarinic, histaminic, or adrenergic receptors — hence cleaner adverse effect profile than TCAs. | | pharmacodynamics = Highly selective inhibitor of the serotonin reuptake transporter (SERT). Mild dopamine reuptake inhibition at higher doses. Minimal affinity for muscarinic, histaminic, or adrenergic receptors — hence cleaner adverse effect profile than TCAs. | ||
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}}<h2 id="Pharmacokinetics">Pharmacokinetics</h2> | }}<h2 id="Pharmacokinetics">Pharmacokinetics</h2> | ||
Well-absorbed orally, ~44% bioavailability. Metabolized hepatically via CYP3A4/CYP2C19/CYP2D6 to N-desmethylsertraline (less active). Half-life ~26h; steady state in ~1 week.<h2 id="Pharmacodynamics">Pharmacodynamics</h2> | |||
Highly selective inhibitor of the serotonin reuptake transporter (SERT). Mild dopamine reuptake inhibition at higher doses. Minimal affinity for muscarinic, histaminic, or adrenergic receptors — hence cleaner adverse effect profile than TCAs.<h2 id="Indications">Indications</h2> | |||
*Major depressive disorder | |||
*Generalized anxiety disorder | |||
*Obsessive-compulsive disorder | |||
*Post-traumatic stress disorder | |||
*Panic disorder | |||
*Premenstrual dysphoric disorder<h2 id="Dosing">Dosing and titration</h2> | |||
Start 25–50 mg PO daily. Titrate by 25–50 mg every 1–2 weeks based on response. Typical effective dose 50–200 mg/day; max 200 mg/day.<h2 id="Effects">Effects</h2><span></span> | |||
''Therapeutic:'' improved mood, reduced anxiety, fewer obsessive thoughts (delayed 2–4 weeks). | |||
<span></span> | |||
''Common adverse:'' nausea, diarrhea, sexual dysfunction, insomnia, somnolence, sweating.<h2 id="Adverse">Adverse effects</h2> | |||
Serotonin syndrome (especially with other serotonergic agents), QT prolongation at high doses, hyponatremia (SIADH, esp. elderly), bleeding risk, suicidality warning in young adults, discontinuation syndrome.<h2 id="Contraindications">Contraindications</h2> | |||
MAOIs (within 14 days), pimozide, severe hepatic impairment. Caution: bipolar disorder (mood switching risk), seizure disorders.<h2 id="Interactions">Interactions</h2> | |||
MAOIs (serotonin syndrome — contraindicated), triptans, tramadol, linezolid, lithium, NSAIDs/anticoagulants (bleeding), CYP2D6 substrates.<h2 id="Pregnancy">Pregnancy and lactation</h2> | |||
Category C. SSRIs in third trimester associated with persistent pulmonary hypertension of the newborn (PPHN) and neonatal adaptation syndrome. Risk-benefit decision; sertraline often preferred in pregnancy among SSRIs.<h2 id="Monitoring">Monitoring</h2> | |||
Mood/suicidality (especially first 4 weeks), sodium (elderly), QT in cardiac risk, response and side effects.<h2 id="Counseling">Patient counseling</h2> | |||
Take with or without food. Effect emerges over 2–4 weeks. Don't stop abruptly — taper to avoid withdrawal. Report serotonin-syndrome symptoms.<h2 id="SeeAlso">See also</h2><span></span> | |||
[[Fluoxetine]], [[Paroxetine]], [[Citalopram]], [[Escitalopram]] | |||
[[Category:Medicines]] | |||
<h2 id="Pharmacokinetics">Pharmacokinetics</h2> | |||
Well-absorbed orally, ~44% bioavailability. Metabolized hepatically via CYP3A4/CYP2C19/CYP2D6 to N-desmethylsertraline (less active). Half-life ~26h; steady state in ~1 week.<h2 id="Pharmacodynamics">Pharmacodynamics</h2> | Well-absorbed orally, ~44% bioavailability. Metabolized hepatically via CYP3A4/CYP2C19/CYP2D6 to N-desmethylsertraline (less active). Half-life ~26h; steady state in ~1 week.<h2 id="Pharmacodynamics">Pharmacodynamics</h2> | ||
Highly selective inhibitor of the serotonin reuptake transporter (SERT). Mild dopamine reuptake inhibition at higher doses. Minimal affinity for muscarinic, histaminic, or adrenergic receptors — hence cleaner adverse effect profile than TCAs.<h2 id="Indications">Indications</h2> | Highly selective inhibitor of the serotonin reuptake transporter (SERT). Mild dopamine reuptake inhibition at higher doses. Minimal affinity for muscarinic, histaminic, or adrenergic receptors — hence cleaner adverse effect profile than TCAs.<h2 id="Indications">Indications</h2> | ||