Flibanserin: Restoring Desire in Premenopausal Hypoactive Sexual Desire Disorder
Flibanserin
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Synonyms | |||
Flibanserin is a multifunctional serotonin agonist and antagonist (MSAA) approved for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. It represents a significant advancement in the neuropharmacological management of this condition, targeting central neurotransmitter systems to address the complex biopsychosocial nature of female sexual interest/arousal disorders. Unlike hormonal therapies, flibanserin works centrally to rebalance key neurotransmitters implicated in sexual motivation, offering a non-hormonal, daily oral treatment option developed specifically for this indication. Its mechanism of action and clinical profile are distinct from other available agents, positioning it as a specialized therapeutic for a condition that has historically been underserved by pharmacotherapy.
Features
- Active pharmaceutical ingredient: Flibanserin
- Pharmacologic class: Multifunctional serotonin agonist and antagonist (MSAA)
- Available dosage form: 100 mg oral tablets
- Mechanism of action: Acts as a postsynaptic 5-HT1A receptor agonist and 5-HT2A receptor antagonist
- Neurotransmitter effects: Decreases serotonin activity while increasing dopamine and norepinephrine in key brain regions
- Prescription status: Schedule IV controlled substance, available by prescription only
- Manufacturer: Original developer and patent holder
- Regulatory status: FDA-approved for premenopausal women with HSDD
Benefits
- Increases the number of satisfying sexual events (SSEs) per month as measured in clinical trials
- Enhances sexual desire and reduces associated distress, as validated by patient-reported outcome measures
- Provides a non-hormonal treatment approach for women who cannot or prefer not to use hormone therapies
- Addresses the neurochemical imbalance hypothesis of HSDD through targeted neurotransmitter modulation
- Offers a daily oral dosing regimen that integrates into established medication routines
- Demonstrates statistically significant improvement in Female Sexual Function Index (FSFI) desire domain scores
Common use
Flibanserin is specifically indicated for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD). HSDD is characterized by a persistent or recurrent deficiency or absence of sexual fantasies and desire for sexual activity that causes marked distress or interpersonal difficulty, and which is not better accounted for by another medical or psychiatric condition, relationship problems, or the effects of a medication or drug substance. The “acquired” specifier indicates that the disorder developed in a patient who previously had no problems with sexual desire, while “generalized” refers to lack of desire that is not limited to certain types of stimulation, situations, or partners. Clinical use requires careful patient selection, focusing on those who meet diagnostic criteria and have ruled out other potential causes of decreased libido.
Dosage and direction
The recommended dosage is 100 mg taken orally once daily at bedtime. Administration at bedtime is crucial due to the risk of hypotension, syncope, and central nervous system depression. The medication should be taken consistently rather than on an as-needed basis, as its therapeutic effects develop over time through sustained neurotransmitter modulation. Treatment initiation should follow careful patient evaluation and counseling about risks, particularly regarding alcohol consumption. Dose titration is not recommended, and the 100 mg dose should be maintained throughout treatment. Patients should be advised to take the medication approximately the same time each evening. Efficacy typically becomes apparent after 4-8 weeks of continuous dosing, with optimal effects observed after 24 weeks of treatment in clinical trials.
Precautions
Flibanserin carries several important precautions that require careful clinical consideration. It is contraindicated with alcohol consumption due to the risk of severe hypotension and syncope. Hepatic impairment necessitates avoidance or discontinuation, as flibanserin is extensively metabolized by the liver. Concomitant use with moderate or strong CYP3A4 inhibitors is contraindicated due to significantly increased flibanserin exposure. Patients should be cautioned about the potential for dizziness, somnolence, and fatigue, particularly during the initial weeks of treatment. Blood pressure monitoring may be advisable, especially in patients with hypotension or those taking antihypertensive medications. The risk of syncope requires careful patient selection and education about recognizing pre-syncopal symptoms. Driving or operating machinery should be avoided until patients know how flibanserin affects them.
Contraindications
Flibanserin is contraindicated in several clinical scenarios. Concomitant alcohol consumption is absolutely contraindicated due to the risk of severe hypotension, syncope, and CNS depression. Patients with hepatic impairment should not use flibanserin. Concomitant use with moderate or strong CYP3A4 inhibitors, including certain antifungals, antibiotics, and protease inhibitors, is contraindicated. Pregnancy and breastfeeding represent contraindications due to unknown fetal risk and potential secretion in breast milk. Use in postmenopausal women or men has not been studied and is not recommended. Patients with a history of hypersensitivity to flibanserin or any component of the formulation should avoid the medication. Those with cardiovascular disease or predisposition to hypotension require careful risk-benefit assessment.
Possible side effects
The most commonly reported adverse reactions in clinical trials include dizziness (11.4%), somnolence (11.2%), nausea (8.3%), fatigue (7.7%), insomnia (5.4%), and dry mouth (4.6%). These effects are generally mild to moderate in severity and often diminish with continued treatment. More serious but less common side effects include syncope (0.4%), hypotension (0.2%), and accidental injury (2.6%). The risk of syncope and hypotension appears heightened with alcohol consumption or concomitant use of CYP3A4 inhibitors. Some patients may experience anxiety, irritability, or mood changes. Laboratory abnormalities including elevated liver enzymes have been reported, though clinically significant hepatotoxicity appears rare. The side effect profile necessitates careful patient monitoring, particularly during treatment initiation.
Drug interaction
Flibanserin demonstrates significant pharmacokinetic interactions due to its metabolism primarily by CYP3A4 and CYP2C19. Strong and moderate CYP3A4 inhibitors dramatically increase flibanserin exposure and are contraindicated—these include ketoconazole, itraconazole, clarithromycin, and various HIV protease inhibitors. Weak CYP3A4 inhibitors may also increase exposure and require caution. CYP3A4 inducers such as rifampin may decrease flibanserin efficacy. Concomitant use with other CNS depressants, including benzodiazepines, opioids, and sedating antihistamines, may potentiate sedation and impairment. Serotonergic drugs theoretically could increase serotonin syndrome risk, though this has not been prominently reported. Flibanserin may increase exposure to drugs metabolized by CYP2C9, CYP2C19, and CYP3A4, though clinical significance varies. The alcohol interaction is particularly dangerous and absolutely contraindicated.
Missed dose
If a dose is missed at the usual bedtime administration time, patients should skip the missed dose and take the next dose at the regular time the following evening. Patients should not double the dose to make up for a missed administration. The medication’s long half-life and mechanism of action involving gradual neurotransmitter modulation mean that occasional missed doses are unlikely to significantly impact overall efficacy. However, consistent daily dosing is important for maintaining therapeutic effects. Patients should be counseled on establishing a bedtime routine to support adherence. If multiple doses are missed, patients should resume the regular dosing schedule without loading doses or other adjustments.
Overdose
Experience with flibanserin overdose is limited. Based on its pharmacological profile, overdose would be expected to produce exaggerated pharmacological effects including severe dizziness, profound sedation, syncope, and hypotension. There is no specific antidote for flibanserin overdose. Management should focus on supportive care, including continuous hemodynamic monitoring and appropriate symptomatic treatment. Activated charcoal may be considered if ingestion was recent. Given the medication’s extensive protein binding, dialysis is unlikely to be effective. Patients should be monitored for at least 24 hours due to the drug’s half-life of approximately 11 hours. Supportive measures for hypotension may include intravenous fluids and, if necessary, vasopressors under careful monitoring. CNS depression may necessitate respiratory support in severe cases.
Storage
Flibanserin tablets should be stored at room temperature between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). The medication should be kept in its original container with the lid tightly closed to protect from moisture and light. Storage should be in a secure location out of reach of children and pets, particularly given the serious risks associated with accidental ingestion. Patients should be advised to properly dispose of any expired or unused medication through drug take-back programs or according to FDA-recommended disposal methods. The medication should not be stored in bathrooms or other areas with high humidity, which could degrade the formulation.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Flibanserin is a prescription medication that should be used only under the supervision of a qualified healthcare provider. Individual patient responses may vary, and the benefits and risks must be carefully evaluated for each patient. This summary does not include all possible information about this medication, and healthcare providers should consult the full prescribing information before initiating treatment. Patients should not make changes to their medication regimen without consulting their healthcare provider. The information presented reflects knowledge available at the time of writing and may become outdated as new research emerges.
Reviews
Clinical trial data demonstrate that flibanserin provides statistically significant improvements in measures of sexual desire and distress compared to placebo. In phase III trials, women taking flibanserin experienced approximately 0.5-1.0 additional satisfying sexual events per month and showed improvement on the Female Sexual Function Index desire domain score. Patient-reported outcomes indicated reduced distress related to sexual desire. However, the magnitude of effect has been subject to discussion within the medical community, with some experts noting modest absolute benefits. Real-world evidence continues to accumulate regarding its effectiveness in clinical practice. Patient satisfaction appears variable, with some women reporting meaningful improvement while others discontinue due to side effects or lack of efficacy. The risk-benefit profile necessitates careful patient selection and ongoing monitoring.