sertraline ZOLOFT
Class: SSRIFDA 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 solnDose 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
Precautions
Contraindications: Concomitant use of MAOIsSerious Side Effects: Serotonin syndrome; ↑ risk of SI in children and young adults; may impair platelet aggregation; SIADH
Side Effects: anorgasmia, xerostomia, hyperhidrosis, sedation/somnolence, dizziness, tremor, diarrhea, nausea, insomnia, weight loss
Pharmacodynamics
1° MOA: Selective serotonin reuptake inhibitor2° 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: Desmethylsertraline aka norsertraline (~5-10% potent as sertraline, behaves as a serotonin-norepinephrine-dopamine reuptake inhibitor [SNDRI])
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.