flibanserin ADDYI
Class: Norepinephrine-Dopamine DisinhibitorFDA Indications: Hypoactive Sexual Desire Disorder
Off-Label Use:
Prescribing
Forms: 100mg tabletDose Range: 100 mg/day
Starting: 100 mg taken once daily at bedtime. Discontinue treatment after 8 weeks if no improvement.
Precautions
Contraindications: Concomitant alcohol use; hepatic impairmentSerious Side Effects: Severe hypotension and syncope with concomitant alcohol use
Side Effects: dizziness, nausea, fatigue, xerostomia, sedation/somnolence, insomnia, transaminitis
Pharmacodynamics
1° MOA: Postsynaptic 5-HT1A agonist/5-HT2A antagonistTarget: Agonist at Postsynaptic 5HT1A, antagonist at 5HT2A, moderate partial agonist at D4, 5HT2B, & 5HT2C
Pharmacokinetics
t½: 11° TMAX: 2-4°Substrate of: 3A4; 2C19
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels
Misc
- - preferentially activates 5-HT1A in the prefrontal cortex increasing downstream DA and NE levels; its 5HT2C antagonism also enhances mesocorticolimbic DA function
- - was developed as an antidepressant, but failed to show efficacy
- - dosed QHS because administration during waking hours ↑ risk of hypotension, syncope, accidental injury, and central nervous system depression
Special Populations
Category Not assigned.—Safety has not been established during pregnancy; data from animal studies cannot rule out the potential for fetal harm
Not recommended
Not indicated for use in geriatric patients
AUC ↑'d 1.1-fold in patients with mild to moderate renal impairment and 1.2-fold in patients with severe renal impairment
Contraindicated for use in patients with any degree of hepatic impairment
Thank you for using psychopharmacopeia.com!