Flibanserin: Restoring Desire in Premenopausal Women
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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 novel, non-hormonal, centrally-acting pharmacologic approach to a complex neuropsychiatric condition. Unlike therapies that focus solely on physiological aspects of sexual function, flibanserin targets the neurochemical imbalance in brain regions associated with sexual motivation and inhibitory control. This daily oral medication requires careful patient selection and adherence to a specific risk management strategy due to its potential for significant hypotension and syncope, particularly in conjunction with alcohol consumption or moderate-to-strong CYP3A4 inhibitors.
Features
- Active Pharmaceutical Ingredient: Flibanserin
- Pharmacologic Class: Multifunctional Serotonin Agonist and Antagonist (MSAA)
- Approved Indication: Treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women
- Dosage Form: Oral tablet (100 mg)
- Mechanism of Action: Acts as a postsynaptic 5-HT1A receptor agonist and a presynaptic 5-HT2A receptor antagonist, modulating neurotransmitter activity in brain circuits governing sexual desire
- Prescription Status: Available only through a restricted program called the FDA-required Risk Evaluation and Mitigation Strategy (REMS)
Benefits
- Increases the number of satisfying sexual events (SSEs) per month from baseline
- Elevates sexual desire scores as measured by validated patient-reported outcome instruments
- Reduces distress associated with low sexual desire, improving overall quality of life and emotional well-being
- Provides a non-hormonal treatment option for a condition with limited therapeutic alternatives
- Offers a daily oral dosing regimen for consistent central nervous system effect
- Targets the core neurobiological mechanisms believed to underlie HSDD, rather than peripheral physiological factors
Common use
Flibanserin is 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, causing marked distress or interpersonal difficulty, which is not better accounted for by a co-existing medical or psychiatric condition, problems within the relationship, or the effects of a medication or other drug substance. The “acquired” subtype denotes that the low desire developed in a patient who previously experienced no such concerns, while “generalized” refers to the lack of desire that is not limited to certain types of stimulation, situations, or partners. It is not intended for use in postmenopausal women or in men, and its efficacy in treating sexual dysfunction due to comorbid medical or psychiatric disorders, or the effects of concomitant medications, has not been established.
Dosage and direction
The recommended dosage is 100 mg taken orally once daily at bedtime. Administration at bedtime is intended to mitigate the risk of hypotension, syncope, and central nervous system depression (e.g., somnolence, sedation), as these adverse reactions are most common during the hours after flibanserin is taken. The tablet should be swallowed whole and can be taken with or without food; however, patients should be consistent in their choice to avoid variable absorption. Dose escalation or a dosage other than 100 mg once daily at bedtime is not recommended. Patients must be enrolled in the Flibanserin REMS program and must acknowledge that they understand the risks of severe hypotension and syncope associated with flibanserin, especially with concomitant alcohol use.
Precautions
Flibanserin carries a Boxed Warning regarding the risks of severe hypotension and syncope. These risks are increased with concomitant alcohol use, and patients must be advised to avoid alcohol consumption. Concomitant use with moderate or strong CYP3A4 inhibitors is contraindicated. Due to its central nervous system depressant effects, patients should exercise caution when engaging in potentially hazardous activities until they know how flibanserin affects them, especially the next day after taking a dose. Flibanserin can cause somnolence, sedation, and fatigue. It is not recommended in patients with hepatic impairment. A healthcare provider should assess the potential for drug interactions, particularly with other CNS depressants, prior to initiation. Blood pressure should be monitored in patients taking antihypertensive medications.
Contraindications
Flibanserin is contraindicated in the following patient populations and scenarios:
- Concomitant use with alcohol
- Concomitant use with moderate or strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, nefazodone, ritonavir, clarithromycin, grapefruit juice)
- Patients with hepatic impairment
- Postmenopausal women and men
- Use in combination with other CNS depressants is not recommended due to additive sedative effects, though not an absolute contraindication
Possible side effect
The most common adverse reactions (≥2% incidence and greater than placebo) associated with flibanserin use include:
- Dizziness
- Somnolence (sleepiness)
- Nausea
- Fatigue
- Insomnia
- Dry mouth
- Other reported side effects can include anxiety, flushing, abdominal pain, and constipation. The most serious risks are syncope (fainting) and severe hypotension, particularly if taken with alcohol or CYP3A4 inhibitors.
Drug interaction
Flibanserin is primarily metabolized by CYP3A4 and, to a lesser extent, by CYP2C19. It is a weak CYP3A4 inhibitor and a CYP2C9/CYP2C19 inducer. Significant interactions include:
- Alcohol: Contraindicated. Concomitant use profoundly increases the risk of hypotension and syncope.
- Strong/Moderate CYP3A4 Inhibitors: Contraindicated (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin, grapefruit juice). These agents significantly increase flibanserin exposure.
- Weak CYP3A4 Inhibitors: Use with caution; may increase flibanserin exposure (e.g., oral contraceptives, cimetidine).
- CYP2C19 Inhibitors: May increase flibanserin exposure (e.g., fluconazole, omeprazole).
- CNS Depressants: Additive sedative effects are likely with benzodiazepines, opioids, antipsychotics, and antidepressants.
- Antihypertensives: Potential for additive hypotensive effects.
- CYP2C9/CYP2C19 Substrates: Flibanserin may decrease exposure to drugs metabolized by these enzymes (e.g., warfarin, phenytoin, diazepam).
Missed dose
If a dose is missed, the patient should skip that dose and take the next dose at the usual time the following night at bedtime. Patients should not take two doses of flibanserin within the same day to “make up” for a missed dose, as this increases the risk of hypotension, syncope, and CNS depression.
Overdose
There is limited clinical experience with flibanserin overdose. Given its pharmacological profile, overdose would be expected to manifest as an exaggeration of its known adverse effects, including severe hypotension, syncope, and profound CNS depression (somnolence, sedation). There is no specific antidote for flibanserin overdose. Management should consist of supportive care, including continuous ECG and blood pressure monitoring. Assisted respiration should be instituted if necessary. Due to high protein binding, flibanserin is not expected to be dialyzable. In case of suspected overdose, contact a Poison Control Center immediately.
Storage
Store flibanserin tablets at room temperature between 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C to 30°C (59°F to 86°F). Keep the medication in its original container to protect from light and moisture. Keep out of reach of children and pets.
Disclaimer
This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The efficacy and safety of flibanserin are specific to its approved indication and patient population. The full prescribing information, including Boxed Warning and REMS requirements, should be reviewed prior to initiation of therapy.
Reviews
Clinical trials and post-marketing surveillance provide the following insights:
- Efficacy Data: In phase III clinical trials, premenopausal women with HSDD treated with flibanserin 100 mg daily experienced a statistically significant increase in the number of satisfying sexual events (SSEs) and sexual desire score, alongside a decrease in distress score, compared to placebo, over a 24-week treatment period.
- Tolerability Profile: Discontinuation rates due to adverse events in trials were higher in the flibanserin group (~13%) than in the placebo group (~6%), with dizziness, somnolence, and nausea being the most common reasons for discontinuation.
- Real-World Evidence: Post-marketing data continues to underscore the critical importance of strict adherence to the REMS program, particularly absolute alcohol avoidance. Reports of syncope and severe hypotension are strongly associated with protocol violations.
- Patient-Reported Outcomes: Many patients who respond to therapy report a meaningful improvement in desire and a reduction in HSDD-related distress, which they describe as life-changing. However, a significant portion of patients do not experience a clinically meaningful benefit or cannot tolerate the side effects.