Psychopharmacopeia: Online Searchable Psychopharmacology Drug Database for Clinicians

flibanserin ADDYI

Class: Norepinephrine-Dopamine Disinhibitor
FDA Indications: Hypoactive Sexual Desire Disorder
Off-Label Use:

Prescribing

Forms: 100mg tablet
Dose Range: 100 mg/day
Starting: 100 mg taken once daily at bedtime. Discontinue treatment after 8 weeks if no improvement.

NAMI drug fact sheet

Precautions

Contraindications: Concomitant alcohol use; hepatic impairment
Serious 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-HT_1A agonist/5-HT_2A antagonist
Target: Agonist at Postsynaptic 5HT_1A, antagonist at 5HT_2A, moderate partial agonist at D₄, 5HT_2B, & 5HT_2C

Pharmacokinetics

t½: 11° T_MAX: 2-4°
Substrate of: 3A4; 2C19
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅

DDIs

- 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels

Misc

- preferentially activates 5-HT_1A in the prefrontal cortex increasing downstream DA and NE levels; its 5HT_2C 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

References

Foye's Principles Of Medicinal Chemistry
Pharmacology Of Flibanserin
Flibanserin For Hypoactive Sexual Desire Disorder In Premenopausal Women
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Last updated August 14 2025 21:35:12. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.

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