sertraline ZOLOFT

Class: SSRI
FDA Indications: MDD, Panic Disorder, PTSD, OCD, PMDD, Social Anxiety
Off-Label Use: Premature Ejaculation, Binge Eating Disorder, Bulimia Nervosa, GAD
Prescribing
Forms: 25, 50, 100mg tablet; 20 mg/mL po soln
Dose Range: 25-200 mg/day
Starting: 25 mg po qd; may ↑ dose in increments of 25-50 mg weekly to a max of 200 mg/day
Stopping: Gradually taper the dose to minimize the incidence of withdrawal symptoms and allow for the detection of re-emerging symptoms

NAMI drug fact sheet

Precautions
Contraindications: Concomitant use of MAOIs
Serious Side Effects: Serotonin syndrome; ↑ risk of SI in children and young adults; may impair platelet aggregation; SIADH
Side Effects: sedation/somnolence, dizziness, anorgasmia, xerostomia, increased sweating, tremor, diarrhea, nausea, insomnia, weight loss
Pharmacodynamics
1° MOA: Selective serotonin reuptake inhibitor
2° MOA: DA reuptake inhibition, possible σ blockade
Target: SERT, DAT
Pharmacokinetics
t½: 26 (13-45)° TMAX: 4-8°
Substrate of: 2C19, 2D6; 2B6, 2C9, 2D6, 3A4
Inhibits: 2D6 and 3A4 (both weakly); Induces:
Active Metabolites: Norsertraline (~5-10% potent as sertraline)
DDIs
  • - DO NOT CO-PRESCRIBE WITH MAOIs (need a 5 t½ washout period)
  • - serotonin syndrome risk with tramadol
  • - 2D6 can ↑ serum levels & 3A4 inhibitors can ↑ serum levels can ↑ its levels
  • - 3A4 inducers can ↑ serum levels such as carbamazepine can ↓ its levels
  • - as a weak 2D6 inhibitor can ↑ serum levels, can ↑ levels of other 2D6 substrates
Misc
  • - the only dopaminergic SSRI
  • - least likely SSRI to ↑ prolactin
  • - consider 1st choice for atypical depression
  • - best documented CV safety of any antidepressant
  • - σ blockade may confer ↑ anxiolysis
  • - linear & dose-proportional pharmacokinetics
  • - more likely to cause weight loss (1-2 lbs on average) than weight gain
Special Populations

Category C—Appears to result in least placental exposure.

Considered to be 1st-line drug for BF women, with a low RID, ranging from 0.5-3%; very few AEs described in the literature

Avoid use in patients ≥65 with a history of falls or fractures

No dosage adjustment necessary.


↓ dose 50% even in mild impairment. DO NOT USE if moderate-severe impairment.

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Last updated January 20 2018 15:32:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.