The first and only FDA-approved pill proven to increase a woman’s sex drive.

Although strong CYP3A4 inducers are not expected to compromise medication safety, they may diminish efficacy by enhancing the metabolism of flibanserin. Weak CYP3A4 inhibitors: Weak CYP3A4 inhibitors, such as oral contraceptives, ranitidine, and ginkgo, are examples of substances that may have a modest impact.

Related/similar drugs

Distribution: Flibanserin binds primarily to albumin, exhibiting a plasma protein binding of approximately 98%. Metabolism: Flibanserin undergoes primary metabolism through the cytochrome P450 enzymes CYP3A4 and CYP2C19,[12] with minimal contributions to its metabolism made from CYP1A2, CYP2B6, CYP2C8, CYP2C9, and CYP2D6 based on in vitro and in vivo data. Flibanserin undergoes extensive metabolism, resulting in at least 35 metabolites, most of which are present in low concentrations in plasma. Among these, only 2 metabolites—6,21-dihydroxy-flibanserin-6,21-disulfate and 6-hydroxy-flibanserin-6-sulfate—exhibit plasma concentrations comparable to flibanserin. Notably, both of these metabolites are inactive.

Generic Name

The average terminal half-life of flibanserin is approximately 11 hours. Flibanserin is available in a 100 mg oral tablet form and is administered once daily at bedtime. Flibanserin is recommended to be taken at bedtime to minimize the risk of hypotension, syncope, accidental injury, or central nervous system (CNS) depression during waking hours. In case of a missed dose, patients are recommended to take it the following night without doubling the dosage. If the patient does not report any improvement in their symptoms after 8 weeks of compliance with the medication, flibanserin should be discontinued.

Already Own This Product?

Healthcare professionals should carefully consider concomitant medications outlined in the drug interactions. Healthcare providers should exercise caution when prescribing flibanserin in conjunction with potent CYP2C19 inhibitors. The combination of these medications has been associated with heightened adverse reactions, likely stemming from presumed elevated levels of flibanserin. Upon its approval in August 2015, flibanserin required a Risk Evaluation and Mitigation Strategy (REMS) program that included Elements to Assure Safe Use (ETASU), which mandated certification for both prescribers and pharmacists. [14] However, in 2019, the FDA replaced the original REMS with a medication-guide-only REMS, eliminating the certification requirement for prescribers or pharmacists. Concurrent use of multiple weak CYP3A4 inhibitors with flibanserin may elevate the risk of adverse reactions.

• Flibanserin should be discontinued if no benefit is observed after several weeks.
• The medication's influence on mental health conditions is still being studied.
• Flibanserin was recognized as a breakthrough therapy for female sexual desire issues.
• Its use is guided by strict medical protocols due to safety concerns.
• Women are encouraged to report any adverse effects during treatment.
• Continued research aims to improve treatment options for female sexual health.
• Flibanserin is one of a few FDA-approved drugs for Female Sexual Desire Disorder.
• Clinical improvements may include increased frequency of satisfying sexual events.
• The drug's use should be combined with counseling when appropriate.

Healthcare professionals should discuss with their patients the potential risks and benefits of combining flibanserin with weak CYP3A4 inhibitors.

Antidepressants: A randomized controlled trial (RCT) reported no severe adverse effects or suicidal ideation when combining a daily dosage of flibanserin 100 mg with a stable selective serotonin reuptake inhibitor (SSRI) or serotonin-norepinephrine reuptake inhibitor (SNRI) regimen.

Strong CYP2C19 inhibitors: Strong CYP2C19 inhibitors, such as proton pump inhibitors and certain antifungals, require careful consideration by healthcare providers when prescribing flibanserin to ensure patient safety and efficacy. These medications, when used in combination with flibanserin, have been associated with increased adverse reactions, likely due to presumed increased levels of flibanserin. To mitigate this risk, healthcare professionals should discuss using strong CYP2C19 inhibitors with the patient when prescribing flibanserin and consider alternative medications or strategies if necessary.

P-glycoprotein substrates: P-glycoprotein substrates, such as digoxin or sirolimus, may require increased monitoring of drug concentrations when administered concurrently with flibanserin, as flibanserin can inhibit p-glycoprotein. Flibanserin use is contraindicated with strong or moderate CYP3A4 inhibitors and hepatic impairment due to the heightened risk of syncope and hypotension.

IMPORTANT WARNING:

Pharmacogenetics: Clinicians should be mindful of pharmacogenetic variations to mitigate the risk of adverse effects related to flibanserin, particularly in patients identified as poor CYP2C19 metabolizers. Individuals classified as poor CYP2C19 metabolizers may experience elevated levels of flibanserin, heightening the risk of adverse events such as hypotension, syncope, and CNS depression. This subgroup constitutes 2% to 5% of Caucasians and Africans and 2% to 15% of Asians. Hepatic impairment: Mild hepatic impairment (Child-Pugh score of 5 to 6 points) showed that single 50 mg oral doses of flibanserin led to increased systemic exposure and a longer half-life than those with normal hepatic function. Due to the limited sample size in moderate hepatic impairment (Child-Pugh score of 8 to 9 points), conclusive statements regarding the impact of flibanserin exposure cannot be asserted.

Does Addyi interact with other medicines (drug interactions)?

Notably, flibanserin is contraindicated for hepatic impairment. Renal impairment: The pharmacokinetic data in the labeling indicates a slight increase in the area under the curve (AUC) by 1.1-fold in mild-to-moderate renal impairment and a 1.2-fold increase in AUC for severe renal impairment compared to healthy individuals. In addition, the data suggest that patients with renal impairment may not require dosage adjustments, as the observed alteration in AUC is minimal. The FDA-approved labeling does not specify any dosage adjustments for renal impairment. Pregnancy considerations: An ongoing flibanserin pregnancy registry study assesses pregnancy outcomes in women exposed to flibanserin at any stage of pregnancy ( To date, no studies on pregnant women have conclusively identified any drug-associated risks.

Pharmacogenetic associations and support therapeutic management recommendations

However, studies based on animals have indicated certain adverse effects on reproduction and development, including diminished fetal weight, structural anomalies, and increased fetal loss, observed at exposures significantly exceeding the maximum recommended human dosage. Notably, although flibanserin is not recommended during pregnancy, it is also not contraindicated in this population. Breastfeeding considerations: Although flibanserin has been detected in rat milk, its presence in human milk and its impact on the breastfed infant and milk production remains unknown. Due to the potential for adverse reactions, including sedation in a breastfed infant, breastfeeding is not recommended during flibanserin treatment. Pediatric patients: Flibanserin is not approved by the FDA for use in the pediatric population. [13][8] Known hypersensitivity to flibanserin or its excipients is also contraindicated, with reported reactions including anaphylaxis, angioedema, pruritus, and urticaria. Simultaneous alcohol use is not a contraindication but is highlighted with a box warning in the latest FDA-approved labeling. Alcohol should be avoided within 2 hours of using flibanserin, especially if 1 or 2 drinks have been consumed.

Continuing Education Activity

Older patients: Flibanserin lacks FDA approval for use in older individuals, as its safety and efficacy in this age group have not been confirmed. The most frequently reported adverse effects of flibanserin, with an incidence of over 2%, include dizziness, somnolence, nausea, fatigue, insomnia, and dry mouth, listed in descending order of frequency. [15][14] Hypotension and syncope may manifest if flibanserin is combined with moderate or potent CYP3A4 inhibitors in individuals with hepatic impairment, alcohol, or other medications known for inducing hypotension and syncope. Less frequently reported adverse effects in clinical trials include anxiety, constipation, abdominal pain, sedation, accidental injury, appendicitis, and vertigo. CNS depressants: CNS depressants, such as diphenhydramine, opioids, hypnotics, and benzodiazepines, pose an elevated risk of CNS depression when used concurrently with flibanserin compared to the use of flibanserin alone.

Last Reviewed Date

Healthcare professionals should engage in a comprehensive discussion with the patient regarding the concomitant use of other CNS depressants when prescribing flibanserin, considering the potential risks and benefits. The tadacip 20 mg tablet online coadministration of flibanserin with alcohol is addressed explicitly in box warnings. Strong or moderate CYP3A4 inhibitors: Strong or moderate CYP3A4 inhibitors, including azole antifungals and protease inhibitors, warrant careful consideration in assessing a patient's current medication regimen. Healthcare professionals should know and inquire about these potential interactions to ensure safe prescribing practices. [15] Moderate or strong CYP3A4 inhibitors increase the plasma levels of flibanserin, thereby increasing the risk of syncope and hypotension. If 3 or more drinks have been consumed, alcohol should be skipped to mitigate the risk of CNS depression.

StatPearls [Internet].

Consequently, the combination of these medications with flibanserin is contraindicated. When a patient is taking a moderate or strong CYP3A4 inhibitor and plans to start taking flibanserin, it is essential to wait for at least 2 weeks after the last dose of the inhibitor to help minimize the risk of potential drug interactions and having elevated levels of flibanserin in the body. Clinicians or prescribers should commence the moderate or strong CYP3A4 inhibitor 2 days after the last dose of flibanserin. This allows sufficient time for the drug's clearance from the system, ensuring safe and effective treatment while minimizing the risk of potential drug interactions and adverse effects. CYP3A4 inducers: CYP3A4 inducers, including carbamazepine, phenobarbital, phenytoin, rifampin, rifabutin, rifapentine, and St John's Wort, significantly reduce flibanserin exposure when used concurrently. [21] Additional warnings include hepatic impairment and the concurrent use of moderate to strong CYP3A4 inhibitors. As a centrally acting drug, flibanserin frequently causes somnolence. Therefore, it is advised to take the medicine at bedtime.

• Reporting of adverse events is encouraged through the FDA MedWatch program.
• Healthcare providers should report syncope, severe hypotension, or liver injury.
• Post-marketing surveillance is critical for understanding rare, long-term risks.
• Drug utilization reviews track prescribing patterns and potential misuse.
• In case of suspected pregnancy, patients should contact their doctor immediately.
• Animal studies showed developmental toxicity at doses much higher than human dose.
• Lactation studies in animals showed excretion in milk; human data are lacking.
• Decision to breastfeed while on flibanserin requires weighing potential risks.
• The benefit for an individual patient must justify the potential risk to a fetus/infant.

Furthermore, using flibanserin in conjunction with centrally acting depressants, such as benzodiazepines, opioids, and sedating antihistamines, should be monitored cautiously due to the increased risk of CNS depression.