Fliban100 mg

Fliban is FDA-approved for the following indication:

Established / FDA-Approved Use

• Treatment of acquired, generalized Hypoactive Sexual Desire Disorder (HSDD) in premenopausal women, characterized by low sexual desire that causes marked distress or interpersonal difficulty, and is not due to a co-existing medical or psychiatric condition, problems within the relationship, or the effects of a medication or other drug substance.

Important Scope Limitations

• Fliban is not approved for use in men.
• Fliban is not approved for use in postmenopausal women.
• Fliban is not approved to enhance sexual performance in individuals who do not have HSDD.

There is no well-established guideline-supported or off-label indication for Fliban outside of acquired, generalized HSDD in premenopausal women; it should not be prescribed for other forms of sexual dysfunction.

Each film-coated tablet contains Flibanserin 100 mg as the active pharmaceutical ingredient, along with standard pharmaceutical excipients.

Fliban is a non-hormonal, centrally acting agent used for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. Unlike earlier hormonal approaches to female sexual dysfunction, Fliban works through modulation of serotonin and, indirectly, dopamine and norepinephrine pathways in the brain that are believed to be involved in sexual desire.

Fliban is taken orally, once daily at bedtime, on a continuous (not on-demand) basis. It carries a boxed warning for severe hypotension and syncope, particularly when combined with alcohol, moderate/strong CYP3A4 inhibitors, or in patients with hepatic impairment.

Mechanism

Flibanserin is a mixed serotonin receptor agonist and antagonist, acting as an agonist at 5-HT1A receptors and an antagonist at 5-HT2A receptors, with lower affinity for other serotonin, dopamine (D4), and norepinephrine receptor subtypes.

The precise mechanism by which Flibanserin improves sexual desire is not fully established, but it is thought to produce a transient decrease in serotonin activity together with an increase in dopamine and norepinephrine activity in the prefrontal cortex, which is postulated to help restore the balance between excitatory and inhibitory pathways governing sexual desire.

Pharmacokinetics

• Absorption: Rapidly absorbed after oral dosing; absolute bioavailability is low (about 33%) due to first-pass metabolism. High-fat meals delay absorption and increase exposure.
• Metabolism: Extensively metabolized, mainly via CYP3A4 and, to a lesser extent, CYP2C19, which is why interactions with CYP3A4 inhibitors/inducers are clinically significant for Flibanserin.
• Elimination: Half-life is approximately 11 hours; eliminated via both renal and fecal routes as metabolites.

• Take Fliban orally, once daily, at bedtime, with or without food (note: taking with a high-fat meal or with alcohol increases blood levels and the risk of hypotension/syncope - see Contraindications).
• Swallow the tablet whole; do not split, crush, or chew.
• Do not consume alcohol at bedtime or overnight while on therapy; stop Fliban at least 2 days before an anticipated occasion of alcohol use, on medical advice.
• If a dose is missed at bedtime, skip it and resume the normal schedule the next night; do not take it in the morning or double the next dose.

The most clinically significant interactions with Fliban involve drugs and substances that raise its blood levels or add to its sedative/hypotensive effects. The combinations that are absolutely contraindicated (alcohol, and moderate/strong CYP3A4 inhibitors) are detailed fully under Contraindications and are only summarized here.

Contraindicated Combinations (see Contraindications for full detail)

• Alcohol - markedly increases risk of severe hypotension and syncope.
• Moderate or strong CYP3A4 inhibitors (e.g., fluconazole, ketoconazole, itraconazole, clarithromycin, erythromycin, ritonavir and other protease inhibitors, diltiazem, verapamil, grapefruit juice) - substantially increase Fliban blood levels and hypotension/syncope risk.

Other Clinically Significant Interactions

• CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort) - can substantially reduce Fliban concentrations and effectiveness; concomitant use should generally be avoided.
• CNS depressants (benzodiazepines, opioids, sedating antihistamines, other sedative-hypnotics) - additive sedation and CNS depression with Fliban; use cautiously.
• Digoxin - Fliban may increase digoxin concentrations; monitor digoxin levels if co-administered.
• Weak CYP3A4 inhibitors - may still increase Fliban exposure to a lesser extent; monitor for hypotension-related symptoms.

Common Side Effects

• Dizziness
• Somnolence (sleepiness/drowsiness)
• Nausea
• Fatigue
• Insomnia
• Dry mouth

Serious Side Effects

• Severe hypotension and syncope - the subject of the boxed warning for Fliban; risk is markedly increased with alcohol, moderate/strong CYP3A4 inhibitors, or hepatic impairment (see Contraindications).
• CNS depression (sedation, somnolence) that may impair the ability to perform activities requiring alertness, such as driving, particularly if Fliban is taken other than at bedtime or combined with alcohol or other CNS depressants.

Patients should seek prompt medical attention for fainting, severe dizziness, or loss of consciousness while taking Fliban.

Pregnancy

Fliban is not indicated for use during pregnancy, as hypoactive sexual desire disorder is not a condition treated in pregnant women. Available data on use of Fliban in pregnancy are limited and are insufficient to establish a drug-associated risk of major birth defects or miscarriage. Fliban should be used during pregnancy only if clearly needed and if the potential benefit justifies the potential risk to the fetus; a physician should be consulted before use in anyone who is or may become pregnant.

Lactation

It is not known whether Fliban or its metabolites are present in human milk, and effects on the breastfed infant or on milk production are unknown. Because sedation and hypotension have been reported with Fliban, and because it is not indicated in this population, a physician should be consulted to weigh the need for therapy against any potential risk before use while breastfeeding.

Boxed Warning: Hypotension and Syncope

Fliban carries a boxed warning for severe hypotension and syncope. This risk is markedly increased by concomitant alcohol use, use with moderate or strong CYP3A4 inhibitors, and in patients with hepatic impairment - all of which are absolute contraindications (see Contraindications) rather than mere precautions.

CNS Depression

Fliban commonly causes sedation, dizziness, and somnolence. Patients should be counseled about the risk of accidental injury (e.g., falls) and should not drive or operate heavy machinery until they know how Fliban affects them, especially if a dose is taken other than at bedtime or is combined with alcohol.

Use Restricted to Approved Population

Fliban is approved only for acquired, generalized HSDD in premenopausal women. It should not be used in men, in postmenopausal women, or simply to enhance sexual performance, as safety and efficacy have not been established in these settings.

Renal Impairment

Use with caution in moderate-to-severe renal impairment because of potentially increased exposure to Fliban (see Dosage and Administration).

Overdose with Fliban may cause pronounced hypotension, syncope, drowsiness/sedation, dizziness, and nausea. There is no specific antidote for Fliban overdose.

Anyone suspected of having taken an overdose of Fliban should seek immediate medical attention or contact emergency services / a poison control center. Management is supportive and should be provided under medical supervision (e.g., monitoring of blood pressure and level of consciousness); specific home-treatment measures are not recommended.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Hepatic Impairment

Fliban is contraindicated in patients with any degree of hepatic impairment (see Contraindications).

Renal Impairment

No adjustment is needed for mild renal impairment; use with caution in moderate-to-severe renal impairment due to potentially increased Fliban exposure.

Elderly

Clinical trials of Fliban did not include substantial numbers of women older than the reproductive/premenopausal age range for which it is indicated; it is not indicated in postmenopausal women, so specific elderly dosing data are not applicable.

Men

Fliban is not approved and should not be used in men; safety and efficacy in men have not been established.

Pediatric Patients

Safety and efficacy of Fliban in patients under 18 years of age have not been established; it is not indicated for use in children or adolescents.

Fliban is intended for continuous, once-daily use rather than as-needed dosing. Response should be assessed after approximately 8 weeks of continuous therapy; if there has been no meaningful improvement in sexual desire and related distress by that time, Fliban should generally be discontinued, since continuing beyond this point without benefit is unlikely to help and exposes the patient to ongoing risks unnecessarily.

Flibanserin acts as an agonist at serotonin 5-HT1A receptors and as an antagonist at 5-HT2A receptors, with additional lower-affinity activity at other serotonin, dopamine D4, and norepinephrine receptors. This receptor profile is believed to produce a modest, transient decrease in serotonergic tone together with increased dopamine and norepinephrine activity in brain regions (such as the prefrontal cortex) involved in sexual desire, which is thought to underlie the therapeutic effect of Flibanserin in HSDD. The exact mechanism has not been fully elucidated.

Fliban is not indicated for use in pediatric patients. Safety and efficacy in individuals under 18 years of age have not been established, and there is no approved pediatric dosing regimen. Fliban should not be prescribed to children or adolescents.