Products
Flibanserin (Addyi) was approved in the United States in 2015 in the form of film-coated tablets. The drug has not yet been registered in many countries. Flibanserin was originally developed at Boehringer Ingelheim as an antidepressant. It was marketed in the United States by Sprout Pharmaceuticals.
Structure and properties
Flibanserin (C20H21F3N4O, Mr = 390.4 g/mol) is a piperazine and a dihydrobenzimidazolone derivative. It exists as a white powder that is insoluble in water.
Effects
Flibanserin (ATC G02CX02) stimulates sexual desire. It is an agonist at postsynaptic serotonin-5-HT1A receptors and an antagonist at serotonin-5-HT2A receptors. It transiently increases concentrations of dopamine and norepinephrine (responsible for sexual arousal) and decreases concentrations of serotonin (responsible for sexual inhibition) in the prefrontal cortex of the brain. The half-life is 11 hours.
Indications
For the treatment of premenopausal women with hypoactive sexual desire disorder (HSDD).
Dosage
According to the SmPC. Tablets are taken once daily in the evening before bedtime.
Contraindications
- Combination with alcohol
- Combination with CYP3A4 inhibitors
- Liver dysfunction
Full precautions can be found in the drug label.
Interactions
Flibanserin is a substrate of CYP3A4 and, to a lesser extent, CYP2C19. Corresponding drug-drug interactions are possible. Other interactions have been described with alcohol, central depressant drugs, and digoxin (P-gp substrates).
Adverse effects
The most common potential adverse effects include dizziness, fatigue, somnolence, nausea, sleep disturbances, and dry mouth.
