flibanserin

Adult Dosing

Hypoactive sexual desire disorder in premenopausal women

Note:

Take flibanserin at bedtime to reduce the risks of hypotension, syncope, accidental injury, and CNS depression (eg. somnolence and sedation)
If a dose is missed at bedtime, take the next dose at bedtime the next day; do not double the next dose
Discontinue therapy after 8 weeks if no improvement in symptoms are reported
Coadministration with moderate or strong CYP3A4 inhibitors is contraindicated
If flibanserin is to be initiated following moderate or strong CYP3A4 inhibitor use, start 2 weeks after the last dose of the CYP3A4 inhibitor
If a moderate or strong CYP3A4 inhibitor is to be initiated following flibanserin use, start the moderate or strong CYP3A4 inhibitor 2 days after the last dose of flibanserin

Pediatric Dosing

[Outline]

Indications ⬆ ⬇

Treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women, characterized by low sexual desire leading to marked distress or interpersonal difficulty and is NOT due to a co-existing medical or psychiatric condition, or problems within the relationship, or the effects of other medications/drugsNote|Not indicated for the treatment of HSDD in postmenopausal women or in men
Not indicated to enhance sexual performance

Contraindications ⬆ ⬇

Black Box Warnings ⬆ ⬇

Contraindicated with alcohol: Use with alcohol increases the risk of severe hypotension and syncope. Before prescribing flibanserin, assess the likelihood of the patient abstaining from alcohol, consider the patient’s current and past drinking behavior, and other pertinent social and medical history. Counsel patients about the importance of abstaining from alcohol use
Flibanserin is available only through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called the ADDYI REMS Programl
Contraindicated with strong or moderate CYP3A4 inhibitors: Concomitant use with moderate or strong CYP3A4 inhibitors increases plasma concentrations of flibanserin which can cause severe hypotension and syncope
Contraindicated in patients with hepatic impairment: Hepatic impairment increases plasma concentrations of flibanserin which can cause severe hypotension and syncope

Dosing Adjustment ⬆ ⬇

Renal Dose Adjustment

Hepatic Dose Adjustment

Warnings/Precautions ⬆ ⬇

Hypotension and syncope due to interaction with alcohol: Alcohol use is contraindicated due to increased risk of severe hypotension and syncope. Before prescribing flibanserin, assess the likelihood of the patient abstaining from alcohol, taking into account the patient’s current and past drinking behavior, and other pertinent social and medical history. Counsel patients about the importance of abstaining from alcohol use. Flibanserin is available only through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called the ADDYI REMS Program
Hypotension and syncope with CYP3A4 inhibitors: Concomitant use with moderate or strong CYP3A4 inhibitors increases plasma concentrations of flibanserin which can cause severe hypotension and syncope; concomitant use of weak CYP3A4 inhibitors including herbal supplements (e.g., ginkgo, resveratrol) or non-prescription drugs (e.g., cimetidine) may increase flibanserin concentrations that can lead to increased risk of hypotension and syncope
Hypotension and syncope can occur with flibanserine alone
Hypotension and syncope in patients with hepatic impairment: Hepatic impairment of any severity can increase flibanserine concentrations leading to hypotension and syncope
CNS depression: Flibanserin can cause CNS depression. Advise patients not to drive or to engage in activities requiring full alertness until at least 6 hours after taking the medication and until they know how it affects them

Interactions ⬆ ⬇

Addyi interacts with :

Pregnancy/Breast Feeding ⬆ ⬇

Pregnancy Category: Not rated

Breastfeeding: Not recommended ||

Adverse Reactions ⬆ ⬇

Clinical Pharmacology ⬆ ⬇

Predominantly a serotonin or 5-HT(1A) receptor agonist (postsynaptic action) and secondarily a 5-HT(2A) receptor antagonist with moderate antagonist activities at the 5-HT(2B), 5-HT(2C), and dopamine D4 receptors; the mechanism of action is unknown, however, it is postulated that the actions of flibanserin on 5-HT receptors at the prefrontal cortex (PFC) pyramidal neurons result in increased dopamine and norepinephrine and decreased 5-HT in the PFC, resulting in enhanced sexual desire in HSDD
Absolute bioavailability: 33%
Metabolism: Metabolized in liver; CYP450; 3A4 (primary substrate), 2C19 (lesser extent)
Excretion: Excreted in feces (51%), and urine (44%)
Half-life: 11 hour

Brands and Availability ⬆ ⬇