What is flibanserin, and how does it work (mechanism of action)?
Addyi (flibanserin) is an oral drug used for treating low sexual desire in women. The mechanism of action of flibanserin is not completely understood. Flibanserin affects the way the brain works by interfering with communication among the brain's nerves in areas of the brain that control sexual desire and other pleasurable sensations. Nerves communicate with each other by making and releasing chemicals called neurotransmitters. The neurotransmitters travel to other nearby nerves where they attach to receptors on nerves. The attachment of neurotransmitters either stimulates or inhibits the function of the nearby nerves. Flibanserin blocks several of the receptors on nerves including dopamine type 4, and serotonin type 2A, 2B and 2C receptors. It also stimulates serotonin type 1A. How these effects improve sexual desire in women is unknown. Scientists think that flibanserin may regulate areas of the brain that control sexual desire in premenopausal women with reduced sexual interest and desire. The FDA approved flibanserin on August 18, 2015.
What are the side effects of flibanserin?
WARNING
Flibanserin may cause low blood pressure and fainting. Patients should lie down and seek medical help if they experience fainting.
Flibanserin causes drowsiness and reduces alertness. Patients should avoid operating machinery, driving, or performing other dangerous activities for at least 6 hours after taking each dose of flibanserin.
What is the dosage for flibanserin?
Flibanserin is administered once daily by mouth at bedtime. It should be stopped after 8 weeks if there is no improvement in symptoms.
Which drugs or supplements interact with flibanserin?
Flibanserin can cause low blood pressure and fainting. Therefore, flibanserin should not be combined with alcohol and other drugs that also cause low blood pressure.
Flibanserin is metabolized or broken down by liver enzymes. Drugs that induce the activity of these enzymes will decrease blood levels of flibanserin. Examples of such drugs include
- carbamazepine (Tegretol),
- rifampin (Rifadin),
- St. John's Wort,
- phenobarbital, and
- several other drugs.
Drugs that block the action of enzymes that breakdown flibanserin will increase blood levels and side effects of flibanserin. Therefore, flibanserin should not be combined with
- itraconazole (Sporanox),
- clarithromycin (Biaxin),
- ketoconazole (Nizoral),
- fluconazole (Diflucan),
- ritonavir (Norvir),
- indinavir (Crixivan),
- telithromycin (Ketek),
- diltiazem (Cardizem),
- verapamil (Calan),
- grapefruit juice, and
- other drugs that may increase its blood levels.
Is flibanserin safe to take if I'm pregnant or breastfeeding?
Flibanserin has not been adequately studied in pregnant women.
Flibanserin has not been studied in women who are breastfeeding. It is not known whether flibanserin is present in human milk.
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