Flibanserin

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Information about Flibanserin

Flibanserin is a serotonergic antidepressant used to treat hypoactive sexual desire disorder.

Liver safety of Flibanserin

Flibanserin has been associated with a low rate of minor serum aminotransferase elevations during treatment, but has not been linked to instances of clinically apparent acute liver injury.

Mechanism of action of Flibanserin

Flibanserin (flib an' ser in) is a serotonergic mixed agonist and antagonist that was initially developed as an antidepressant when it was found to have possible effects on sexual desire and drive. In vitro, flibanserin acts predominantly as a serotonin (5-HT) 1A receptor agonist, but it also has antagonist activity against other serotonin receptors, such as 5-HT 2C and 2B, as well as less defined activity at dopamine D4 receptors. Flibanserin also has variable regional activities, increasing or decreasing serotonin, dopamine and norepinephrine in different brain areas. While its exact mechanism of action is unclear, flibanserin was found to improve subjective measures of sexual desire and satisfaction in multiple large clinical trials done mostly in premenopausal women who fulfilled the clinical criteria for hypoactive sexual desire disorder.

FDA approval information for Flibanserin

Flibanserin was approved for use in the United States in 2015 for use in treatment of hypoactive sexual desire disorder in premenopausal women. There is limited clinical experience with its use. Concurrent alcohol use is considered contraindicated when taking flibanserin, and caution is recommended against its use with antidepressants or sedatives and in patients wtih hepatic impairment.

Dosage and administration for Flibanserin

Flibanserin is available in tablets of 100 mg under the commercial name Addyi. The recommended dose is 100 mg once daily at bedtime.

Side effects of Flibanserin

Common side effects include dizziness, fatigue, somnolence, insomnia, nausea and drug mouth. Less common, but potentially serious side effects include hypotension, syncope and next day somnolence or sedation. Because of the severity of these adverse events, flibanserin is available only as a part of a rigorous Risk Evaluation and Mitigration Strategy (REMS) that requires registration, certification of the prescribers and pharmacies, and regular reporting.

The following are antidepressant subclasses and drugs

MAO Inhibitors Isocarboxazid, Phenelzine, Tranylcypromine

SNRIs Duloxetine, Levomilnacipran, Venlafaxine

SSRIs Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Vilazodone, Vortioxetine

Tricyclics Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin, Imipramine, Nortriptyline, Protriptyline, Trimipramine

Miscellaneous Bupropion, Flibanserin, Mirtazapine, Nefazodone, Trazodone


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