Overview
11 DESCRIPTION The chemical name of flibanserin is 2H-Benzimidazol-2-one, 1,3-dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]. Its empirical formula is C 20 H 21 F 3 N 4 O and its molecular weight is 390.41. The structural formula is: Flibanserin is a white to off-white powder, insoluble in water, sparingly soluble in methanol, ethanol, acetonitrile and toluene, soluble in...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism of action of ADDYI in the treatment of women less than 65 years of age with acquired, generalized HSDD as characterized by low sexual desire that causes marked distress or interpersonal difficulty (not due a co-existing medical or psychiatric condition, problems within the relationship, or the effects of a medication or other drug substance) is not known. 12.2 Pharmacodynamics Receptor Binding: In vitro, flibanserin demonstrated high affinity for the following serotonin (5-hydroxytryptamine or 5-HT) receptors: agonist activity at 5-HT 1A and antagonist activity at 5-HT 2A . Flibanserin also has moderate antagonist activities at the 5-HT 2B , 5-HT 2C , and dopamine D 4 receptors.
Indications
- 1 INDICATIONS AND USAGE ADDYI is indicated for the treatment of women less than 65 years of age with acquired, generalized hypoactive sexual desire disorder (HSDD) as 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. Acquired HSDD refers to HSDD that develops in a patient who previously had no problems with sexual desire.
Common Doses
- 100 mg
Dosage
2 DOSAGE AND ADMINISTRATION • Recommended dosage is 100 mg taken once daily at bedtime (2.1) • ADDYI is dosed at bedtime because administration during waking hours increases risks of hypotension, syncope, accidental injury, and central nervous system (CNS) depression (2.1) �� Discontinue ADDYI treatment after 8 weeks if no improvement (2.3) 2.1 Recommended Dosage The recommended dosage of ADDYI is 100 mg administered orally once per day at bedtime.
Black Box Warning
WARNING: HYPOTENSION and SYNCOPE IN CERTAIN SETTINGS Interaction with Alcohol The use of ADDYI and alcohol together close in time increases the risk of severe hypotension and syncope [see Warnings and Precautions (5.1) ]. Counsel patients to wait at least two hours after consuming one or two standard alcoholic drinks before taking ADDYI at bedtime or to skip their ADDYI dose if they have consumed three or more standard alcoholic drinks that evening.
Contraindications
- 4 CONTRAINDICATIONS ADDYI is contraindicated in patients: • Using concomitant moderate or strong CYP3A4 inhibitors [see Boxed Warning and Warnings and Precautions (5.2) ] . • With hepatic impairment [see Boxed Warning and Warnings and Precautions (5.5) ] . • With known hypersensitivity to ADDYI or any of its components. Reactions, including anaphylaxis, reactions consistent with angioedema (e.g., swelling of the face, lips, and mouth), pruritus, and urticaria have been reported [see Adverse Reactions (6.2) ] . • Moderate or strong cytochrome P450 3A4 (CYP3A4) inhibitors (4, 5.
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are discussed in greater detail in other sections of the labeling: • Hypotension and syncope [see Warnings and Precautions (5.1, 5.2, 5.4, 5.5) ] • CNS depression [see Warnings and Precautions (5.3) ] Most common adverse reactions (incidence ≥2%) are dizziness, somnolence, nausea, fatigue, insomnia, urinary tract infection, anxiety, sinusitis, constipation and dry mouth. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Sprout Pharmaceuticals, Inc. at 1-844-746-5745, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.
Interactions
- 7 DRUG INTERACTIONS Table 3 contains clinically significant drug interactions (DI) with ADDYI. Table 3 Clinically Significant Drug Interactions with ADDYI Alcohol Clinical Implications The coadministration of ADDYI with alcohol increased the risk of hypotension, syncope, and CNS depression compared to the use of ADDYI alone or alcohol alone [see Warnings and Precautions (5.1) and Clinical Pharmacology (12.2) ]. Preventing or Managing DI Counsel patients to wait at least two hours after consuming one or two standard alcoholic drinks before taking ADDYI at bedtime or to skip their ADDYI dose if...