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, hyperhidrosis, 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—The limited animal and human data suggest that sertraline is not a major teratogen. Appears to result in least placental exposure. Two large case-control studies did find increased risks for some birth defects, but the absolute risk appears to be small. However, SSRIs have been associated with several developmental toxicities, including spontaneous abortions, low birth weight, preterm delivery, neonatal serotonin syndrome, neonatal behavioral syndrome (withdrawal), possible sustained abnormal neurobehavior beyond the neonatal period, respiratory distress, and persistent pulmonary hypertension of the newborn (PPHN).

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 August 27 2018 18:45:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.