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Sertraline

From Pharmacopedia
SSRI, Antidepressant, Anxiolytic
Sertraline
Zoloft, Lustral
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 most frequently utilized SSRIs at this time.

Experience

πŸ‘₯ No personal reports yet
βš• No clinical reports yet

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Problems

  • Major depressive disorder
  • Generalized anxiety disorder
  • Obsessive-compulsive disorder
  • Post-traumatic stress disorder
  • Panic disorder
  • Premenstrual dysphoric disorder
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Titration strategies

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.

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Effects

Therapeutic

  • Improved moodπŸ‘€ no reports yetβš•οΈ no reports yet
    Onset typically 2–4 weeks.
  • AnxiolysisπŸ‘€ no reports yetβš•οΈ no reports yet
    Onset typically 2–4 weeks.
  • Reduced obsessive thoughtsπŸ‘€ no reports yetβš•οΈ no reports yet
    Delayed onset; full benefit often takes 4+ weeks.

Common

  • NauseaπŸ‘€ 100% -67.0 (n=1)βš•οΈ no reports yet
    Often improves over the first 1–2 weeks.
  • DiarrheaπŸ‘€ no reports yetβš•οΈ no reports yet
  • Sexual dysfunctionπŸ‘€ no reports yetβš•οΈ no reports yet
    Decreased libido, delayed orgasm, anorgasmia. Can persist long-term in some patients (PSSD).
  • InsomniaπŸ‘€ no reports yetβš•οΈ no reports yet
  • Somnolence / sedationπŸ‘€ no reports yetβš•οΈ no reports yet
  • Sweating / diaphoresisπŸ‘€ no reports yetβš•οΈ no reports yet

Serious

  • Serotonin syndromeπŸ‘€ no reports yetβš•οΈ no reports yet
    Especially with other serotonergic agents (triptans, tramadol, MAOIs, linezolid).
  • QT prolongationπŸ‘€ no reports yetβš•οΈ no reports yet
    Dose-dependent; check ECG in cardiac risk.
  • Hyponatremia / SIADHπŸ‘€ no reports yetβš•οΈ no reports yet
    Especially in elderly patients.
  • Bleeding riskπŸ‘€ no reports yetβš•οΈ no reports yet
    Particularly with concurrent NSAIDs or anticoagulants.
  • SuicidalityπŸ‘€ no reports yetβš•οΈ no reports yet
    Black box warning in patients under 25; close monitoring in first 4 weeks.
  • Discontinuation syndromeπŸ‘€ no reports yetβš•οΈ no reports yet
    "Brain zaps," dizziness, irritability, flu-like symptoms with abrupt cessation. Taper to avoid.
    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.

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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 β€” hence cleaner adverse effect profile than TCAs.

Interactions

MAOIs (serotonin syndrome β€” contraindicated), triptans, tramadol, linezolid, lithium, NSAIDs/anticoagulants (bleeding), CYP2D6 substrates.

Pregnancy and lactation

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.

Monitoring

Mood/suicidality (especially first 4 weeks), sodium (elderly), QT in cardiac risk, response and side effects.

Patient counseling

Take with or without food. Effect emerges over 2–4 weeks. Don't stop abruptly β€” taper to avoid withdrawal. Report serotonin-syndrome symptoms.

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Relevant Literature

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See also

Fluoxetine, Paroxetine, Citalopram, Escitalopram
Structure of Sertraline
Summary
Classes
SSRI, Antidepressant, Anxiolytic
Common uses
  • Depressive disordersβ€”
  • Anxiety disorders broadlyβ€”
  • Panic disorderβ€”
  • Social anxiety disorderβ€”
  • Generalized Anxiety Disorderβ€”
+ 4 more uses β†’
Pharmacy
Pharmacology
Routes
Oral
Onset
2–4 weeks for full effect
Half-life
26 hours (parent); norsertraline 62–104 hours
Bioavailability
~44%
Pregnancy
Category C
Legal status
Rx-only
Purported mechanism
SSRI; weak DRI

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 β€” hence cleaner adverse effect profile than TCAs.

Indications

  • Major depressive disorder
  • Generalized anxiety disorder
  • Obsessive-compulsive disorder
  • Post-traumatic stress disorder
  • Panic disorder
  • Premenstrual dysphoric disorder

    Dosing and titration

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.

Effects

Therapeutic: improved mood, reduced anxiety, fewer obsessive thoughts (delayed 2–4 weeks).

Common adverse: nausea, diarrhea, sexual dysfunction, insomnia, somnolence, sweating.

Adverse effects

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.

Contraindications

MAOIs (within 14 days), pimozide, severe hepatic impairment. Caution: bipolar disorder (mood switching risk), seizure disorders.

Interactions

MAOIs (serotonin syndrome β€” contraindicated), triptans, tramadol, linezolid, lithium, NSAIDs/anticoagulants (bleeding), CYP2D6 substrates.

Pregnancy and lactation

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.

Monitoring

Mood/suicidality (especially first 4 weeks), sodium (elderly), QT in cardiac risk, response and side effects.

Patient counseling

Take with or without food. Effect emerges over 2–4 weeks. Don't stop abruptly β€” taper to avoid withdrawal. Report serotonin-syndrome symptoms.

See also

Fluoxetine, Paroxetine, Citalopram, Escitalopram

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 β€” hence cleaner adverse effect profile than TCAs.

Indications

  • Major depressive disorder
  • Generalized anxiety disorder
  • Obsessive-compulsive disorder
  • Post-traumatic stress disorder
  • Panic disorder
  • Premenstrual dysphoric disorder

    Dosing and titration

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.

Effects

Therapeutic: improved mood, reduced anxiety, fewer obsessive thoughts (delayed 2–4 weeks).

Common adverse: nausea, diarrhea, sexual dysfunction, insomnia, somnolence, sweating.

Adverse effects

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.

Contraindications

MAOIs (within 14 days), pimozide, severe hepatic impairment. Caution: bipolar disorder (mood switching risk), seizure disorders.

Interactions

MAOIs (serotonin syndrome β€” contraindicated), triptans, tramadol, linezolid, lithium, NSAIDs/anticoagulants (bleeding), CYP2D6 substrates.

Pregnancy and lactation

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.

Monitoring

Mood/suicidality (especially first 4 weeks), sodium (elderly), QT in cardiac risk, response and side effects.

Patient counseling

Take with or without food. Effect emerges over 2–4 weeks. Don't stop abruptly β€” taper to avoid withdrawal. Report serotonin-syndrome symptoms.

See also

Fluoxetine, Paroxetine, Citalopram, Escitalopram