Flibanserin

Flibanserin is the first drug to be approved for hypoactive sexual desire disorder (HSDD) in premenopausal women. It was originally developed as an antidepressant medication by Boehringer Ingelheim, but showed lack of efficacy in trials and was further developed as a hypoactive sexual disorder drug by Sprout Pharmaceuticals. Flibanserin's mechanism of action is attributed to its high affinity for 5-HTA1 and 5-HTA2 receptors, displaying agonist activity on 5-HTA1 and antagonist on 5-HTA2, resulting in lowering of serotonin in the brain as well as an effect on increasing norepinephrine and dopamine neurotransmitters.

Flibanserin is a 5-HT receptor modulator used for the treatment of selected premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD).

For the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women.

• Hypoactive Sexual Desire Disorder (HSDD)

Flibansetrin has high affinity for serotonin receptors in the brain: it acts as an agonist on 5-HT1A and an antagonist on 5-HT2A. In vivo, flibanserin binds equally to 5-HT1A and 5-HT2A receptors. However, under higher levels of brain 5-HT (i.e., under stress), flibanserin may occupy 5-HT2A receptors in higher proportion than 5-HT(1A) receptors. It may also moderately antagonize D4 (dopamine) receptors and 5-HT2B and 5-HTB2C. Its action on neurotransmitter receptors may contribute to reduction in serotonin levels and increase in dopamine and norepinephrine levels, all of which may play part in reward processing.

Flibanserin has an absolute oral availability of 33%.

~98%, highly bound to proteins (mostly albumin) in serum.

Elimination via feces (51%) and urine (44%) following a single oral 50 mg dose of flibanserin solution.

≈11 hours

• Avoid alcohol. Avoid alcohol. Ingesting alcohol may increase the CNS depressant and hypotensive effects of flibanserin. If you have consumed two drinks, wait two hours before taking flibanserin. Do not take flibanserin if you have consumed more than three drinks.
• Avoid grapefruit products.
• Avoid St. John's Wort.
• Take with or without food. Taking flibanserin with food (especially a high-fat meal) may increase its AUC, Cmax, and Tmax.