Skip to Content

Addyi

Generic Name: Flibanserin
Class: Central Nervous System Agents, Miscellaneous
Chemical Name: 1,3-Dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-2H-benzimidazol-2-one
Molecular Formula: C20H21F3N4O
CAS Number: 167933-07-5

Warning(s)

  • Hypotension and Syncope with Alcohol
  • Alcohol use is contraindicated in patients receiving flibanserin because of the increased risk of severe hypotension and syncope.1

  • 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 relevant social and medical history.1

  • Advise patients about the importance of abstaining from alcohol.1 (See REMS and also see Hypotension and Syncope with Alcohol under Cautions.)

  • Hypotension and Syncope with CYP3A4 Inhibitors
  • Concomitant use of flibanserin and moderate or potent CYP3A4 inhibitors is contraindicated because of substantially increased flibanserin exposure and risk of hypotension and syncope.1 (See Hypotension and Syncope with CYP3A4 Inhibitors under Cautions and also see Interactions.)

  • Hypotension and Syncope in Patients with Hepatic Impairment
  • Flibanserin is contraindicated in patients with hepatic impairment because of substantially increased flibanserin exposure and risk of hypotension and syncope.1 (See Absorption: Special Populations, under Pharmacokinetics.)

REMS:

FDA approved a REMS for flibanserin to ensure that the benefits outweigh the risk. The REMS may apply to one or more preparations of flibanserin and consists of the following: elements to assure safe use and implementation system. See the FDA REMS page () or the ASHP REMS Resource Center ().

Introduction

5-HT1A receptor agonist and 5-HT2A receptor antagonist.1 6 7 8

Uses for Addyi

Hypoactive Sexual Desire Disorder (HSDD)

Used in premenopausal women for treatment of acquired, generalized HSDD, which is characterized by low sexual desire that causes marked distress or interpersonal difficulty and is not due to a coexisting medical or psychiatric condition, problems within the relationship, or the effects of medication or other drug substances.1 2 3 4 12

HSDD may be categorized as acquired if the sexual dysfunction develops only after a period of normal functioning and as generalized if it is not limited to certain types of stimulation, situations, or partners.1 12

In 3 randomized, controlled trials and an extension trial conducted in premenopausal women with HSDD, flibanserin was associated with an increased number of satisfying sexual events (SSEs), improved sexual desire, and decreased sexual distress.1 2 3 4 15

Psychotherapy and cognitive behavioral therapy also may be helpful.18

Manufacturer states not indicated for treatment of HSDD in postmenopausal women or in men.1

Manufacturer also states not indicated to enhance sexual performance.1

Addyi Dosage and Administration

General

  • Allow at least 2 weeks to elapse between discontinuance of a moderate or potent CYP3A4 inhibitor and initiation of flibanserin and allow at least 2 days to elapse between discontinuance of flibanserin and initiation of a moderate or potent CYP3A4 inhibitor.1 (See Hypotension and Syncope with CYP3A4 Inhibitors under Cautions and also see Interactions.)

Restricted Distribution Program

  • Distribution of flibanserin is restricted because of the increased risk of severe hypotension and syncope if used with alcohol.1 11 (See Hypotension and Syncope with Alcohol under Cautions.)

  • Flibanserin is only available through a REMS program.1 11 Healthcare providers and pharmacies must be certified with the program before they can prescribe or dispense flibanserin.1 11

  • For further information, contact the Addyi REMS Program at 844-746-5745 or at .1 11

Administration

Oral Administration

Once daily at bedtime without regard to meals.1 Because taking flibanserin during waking hours increases the risk of hypotension, syncope, accidental injury, and CNS depression, do not administer at any other time of the day.1 (See CNS Depressant Effects under Cautions.)

Dosage

Adults

HSDD
Oral

100 mg once daily at bedtime.1

Discontinue if HSDD symptoms are not improved after 8 weeks of therapy.1

Special Populations

Hepatic Impairment

Contraindicated in patients with hepatic impairment.1 (See Hypotension and Syncope in Patients with Hepatic Impairment under Cautions.)

Renal Impairment

Manufacturer provides no specific dosage recommendations at this time.1 Dosage adjustments unlikely to be necessary because of only slight increases in exposure in patients with mild to severe renal impairment.1 (See Absorption: Special Populations, under Pharmacokinetics.)

Cautions for Addyi

Contraindications

  • Alcohol use.1 (See Boxed Warning and also see Hypotension and Syncope with Alcohol under Cautions.)

  • Concurrent use of moderate or potent CYP3A4 inhibitors.1 (See Hypotension and Syncope with CYP3A4 Inhibitors under Cautions and also see Interactions.)

  • Hepatic impairment.1 (See Hypotension and Syncope in Patients with Hepatic Impairment under Cautions.)

Warnings/Precautions

Warnings

Hypotension and Syncope with Alcohol

Concomitant use of flibanserin and alcohol increases the risk of severe hypotension and syncope.1 Syncope requiring therapeutic intervention (e.g., ammonia salts and/or placement in supine or Trendelenburg position), hypotension, and somnolence occurred at a higher incidence when flibanserin was administered with alcohol in the morning during an alcohol interaction study.1

Alcohol use is contraindicated in patients taking flibanserin.1 Before prescribing flibanserin, the clinician must assess the likelihood of the patient abstaining from alcohol, taking into account the patient's social and medical history, including current and past drinking behavior.1 (See Boxed Warning and also see Specific Drugs and Foods under Interactions.)

Hypotension and Syncope with CYP3A4 Inhibitors

Moderate or potent CYP3A4 inhibitors substantially increase flibanserin exposure and the risk of hypotension and syncope; therefore, concomitant use of flibanserin and moderate or potent CYP3A4 inhibitors is contraindicated.1

If treatment with a moderate or potent CYP3A4 inhibitor is required, discontinue flibanserin at least 2 days prior to initiation of therapy.1 If the benefit of initiating therapy with a moderate or potent CYP3A4 inhibitor within 2 days of flibanserin discontinuance clearly outweighs the risk of hypotension and syncope, monitor patient for signs of hypotension and syncope.1 Allow at least 2 weeks to elapse between discontinuance of the CYP3A4 inhibitor and reinitiation of flibanserin therapy.1

Concomitant use of flibanserin with multiple weak CYP3A4 inhibitors, including dietary or herbal supplements (e.g., ginkgo, resveratrol) and OTC drugs (e.g., cimetidine), also may increase flibanserin exposure and lead to hypotension and syncope.1 (See Interactions.)

Hypotension and Syncope in Patients with Hepatic Impairment.

Use in patients with any degree of hepatic impairment substantially increases flibanserin concentrations, which can cause hypotension and syncope.1 Flibanserin is therefore contraindicated in patients with hepatic impairment.1 (See Absorption: Special Populations, under Pharmacokinetics.)

Other Warnings and Precautions

CNS Depressant Effects

Risk of somnolence and sedation when given alone;1 CNS depressant effects are most prominent approximately 1–4 hours after oral administration.9

Risk of CNS depression is increased if flibanserin is taken during waking hours, with alcohol or other CNS depressants, or with drugs that increase flibanserin concentrations (e.g., CYP3A4 inhibitors).1 (See Dosage and Administration, Interactions, and Advice to Patients.)

Hypotension and Syncope with Flibanserin Alone

Use of flibanserin alone can cause hypotension and syncope.1 In controlled studies of premenopausal women with HSDD, hypotension and syncope were reported in 0.2 and 0.4% of flibanserin-treated patients, respectively.1 The risk of hypotension and syncope is increased if taken during waking hours or in higher than recommended dosages.1

Consider the clinical benefits of flibanserin therapy and the risks of hypotension and syncope in patients with preexisting conditions that predispose to hypotension.1 (See Warnings under Cautions.)

If presyncope occurs, patient should immediately lie supine and promptly seek medical attention if symptoms do not resolve.1 If syncope occurs, patient should promptly obtain medical attention.1

Mammary Tumors in Female Mice

Dose-related increase in incidence of malignant mammary tumors observed in female mice at exposures 3 and 10 times those attained with recommended human dosage; effect not observed in male mice or in male or female rats.1 Clinical relevance not known.1

Specific Populations

Pregnancy

No studies to date in pregnant women.1 In animal studies, fetal toxicity occurred only in conjunction with substantial maternal toxicity (e.g., reduced weight gain, sedation).1 Decreased fetal weight, structural abnormalities, and increases in fetal loss occurred at exposures >15 times those achieved with recommended human dosage.1 Manufacturer states that animal studies cannot exclude potential for fetal harm.1

Lactation

Distributed into milk in rats; not known whether distributed into human milk.1 Because of the potential for serious adverse reactions, including sedation, in nursing infants, breast-feeding during flibanserin therapy not recommended.1

Pediatric Use

Not indicated for pediatric patients.1

Geriatric Use

Not FDA labeled for use in geriatric patients; safety and efficacy not established.1 Manufacturer states not indicated for treatment of HSDD in postmenopausal women.1 (See Absorption: Special Populations, under Pharmacokinetics.)

Hepatic Impairment

Contraindicated in patients with hepatic impairment.1 (See Hypotension and Syncope in Patients with Hepatic Impairment under Cautions and also see Absorption: Special Populations, under Pharmacokinetics.)

Renal Impairment

Exposure only increases slightly in patients with mild to severe renal impairment.1 Dosage adjustment unlikely to be necessary.1 (See Absorption: Special Populations, under Pharmacokinetics.)

Poor CYP2C19 Metabolizers

Peak plasma concentrations and AUC are increased and elimination half-life is prolonged in poor CYP2C19 metabolizers compared with extensive CYP2C19 metabolizers.1 (See Pharmacokinetics.) Increased monitoring for adverse effects (e.g., hypotension) recommended.1 Approximately 2–5% of Caucasians and Africans and approximately 2–15% of Asians are poor CYP2C19 metabolizers.1

Common Adverse Effects

Dizziness,1 somnolence,1 nausea,1 fatigue,1 insomnia,1 dry mouth.1 Most of these adverse effects began during first 14 days of therapy.1

Interactions for Addyi

Metabolized principally by CYP3A4 and, to a lesser extent, by CYP2C19.1 CYP 1A2, 2B6, 2C8, 2C9, and 2D6 contribute minimally (<10%) to metabolism.1 10

Inhibits P-glycoprotein (P-gp).1 5 10

Drugs Affecting Hepatic Microsomal Enzymes

Moderate or potent CYP3A4 inhibitors: Substantially increased flibanserin exposure possible; may lead to hypotension and syncope.1 Concomitant use contraindicated.1 18 (See General under Dosage and Administration and also see Hypotension and Syncope with CYP3A4 Inhibitors under Cautions.)

Weak CYP3A4 inhibitors: Possible increased flibanserin exposure with concurrent use of multiple weak CYP3A4 inhibitors; advise patients of increased risk of adverse effects (e.g., hypotension, syncope, CNS depression).1 (See Hypotension and Syncope with CYP3A4 Inhibitors under Cautions.)

CYP3A4 inducers: Substantially decreased flibanserin exposure possible.1 Concomitant use not recommended.1

Potent CYP2C19 inhibitors: Potential increased flibanserin exposure; advise patients of increased risk of adverse effects (e.g., hypotension, syncope, CNS depression).1 18

Substrates of P-glycoprotein Transport

Potential increased exposure to P-gp substrates resulting in possible toxicity; more frequent monitoring of concentrations of P-gp substrates with a narrow therapeutic index recommended.1

Specific Drugs and Foods

Drug or Food

Interaction

Comments

Alcohol

Increased risk of severe hypotension, syncope, and CNS depression1 10 (see Hypotension and Syncope with Alcohol under Cautions)

Pharmacokinetics of flibanserin not substantially altered1 10

Concomitant use contraindicated1

Before prescribing flibanserin, clinician must assess likelihood of patient abstaining from alcohol, taking into account the patient's social and medical history, including current and past drinking behavior1

Anticonvulsants (carbamazepine, phenobarbital, phenytoin)

Possible decreased flibanserin exposure1

Concomitant use not recommended1

Antidepressants, SSRIs

Possible increased flibanserin exposure with SSRIs that are potent CYP2C19 inhibitors (e.g., fluvoxamine); may lead to hypotension, syncope, and CNS depression1 18 20

Fluoxetine (weak CYP3A4 inhibitor): Possible increased flibanserin exposure with multiple weak CYP3A4 inhibitors1

Paroxetine: No clinically important effects on flibanserin pharmacokinetics1

Fluoxetine and fluvoxamine: Advise patients of the increased risk for adverse effects1

Antifungals, azole (fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole)

Possible increased flibanserin exposure with moderate or potent CYP3A4 inhibitors (fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole) and/or potent CYP2C19 inhibitors (fluconazole); may lead to hypotension, syncope, and CNS depression1 18 20

Fluconazole: Increased peak concentrations and AUC of flibanserin 2.2- and 7-fold, respectively; hypotension and syncope reported1 10

Itraconazole: Increased peak concentrations and AUC of flibanserin 1.7- and 2.6-fold, respectively1

Ketoconazole: Increased peak concentrations and AUC of flibanserin 1.8- and 4.5-fold, respectively1

Concomitant use contraindicated1

If treatment with an azole antifungal is necessary, discontinue flibanserin ≥2 days prior to initiation of the azole antifungal1

If benefit of initiating azole antifungal therapy within 2 days of flibanserin discontinuance clearly outweighs risk of hypotension and syncope, monitor for hypotension and syncope1

Allow ≥2 weeks to elapse between discontinuance of the azole antifungal and reinitiation of flibanserin1

Antimycobacterials (rifabutin, rifampin, rifapentine)

Possible decreased flibanserin exposure1

Rifampin: Decreased flibanserin exposure by about 95%1 10

Concomitant use not recommended1

Bupropion

No clinically important effects on bupropion pharmacokinetics1

Ciprofloxacin

Possible increased flibanserin exposure; may lead to hypotension and syncope1

Concomitant use contraindicated1

If treatment with ciprofloxacin is necessary, discontinue flibanserin ≥2 days prior to initiation of ciprofloxacin1

If benefit of initiating ciprofloxacin therapy within 2 days of flibanserin discontinuance clearly outweighs risk of hypotension and syncope, monitor for hypotension and syncope1

Allow ≥2 weeks to elapse between discontinuance of ciprofloxacin and reinitiation of flibanserin1

CNS depressants (e.g., benzodiazepines, diphenhydramine, sedatives and hypnotics, opiates)

Possible additive CNS depression1

Advise patients of increased risk for adverse CNS effects1

Conivaptan

Possible increased flibanserin exposure; may lead to hypotension and syncope1

Concomitant use contraindicated1

If treatment with conivaptan is necessary, discontinue flibanserin ≥2 days prior to initiation of conivaptan1

If benefit of initiating conivaptan therapy within 2 days of flibanserin discontinuance clearly outweighs risk of hypotension and syncope, monitor for hypotension and syncope1

Allow ≥2 weeks to elapse between discontinuance of conivaptan and reinitiation of flibanserin1

Contraceptives, hormonal

Possible increased flibanserin exposure and increased risk of adverse effects (e.g., nausea, dizziness, somnolence, fatigue)1 5 10

Pharmacokinetics of oral contraceptive components (ethinyl estradiol and levonorgestrel; weak CYP3A4 inhibitor) not substantially affected1

Advise patients of the increased risk of adverse effects, particularly when used with other weak CYP3A4 inhibitors1

Digoxin

Increased AUC and peak concentrations of digoxin (a P-gp substrate) by 2- and 1.5-fold, respectively; digoxin toxicity possible1

More frequent monitoring of digoxin concentrations recommended1

Diltiazem

Possible increased flibanserin exposure; may lead to hypotension and syncope1

Concomitant use contraindicated1

If treatment with diltiazem is necessary, discontinue flibanserin ≥2 days prior to initiation of diltiazem1

If benefit of initiating diltiazem therapy within 2 days of flibanserin discontinuance clearly outweighs risk of hypotension and syncope, monitor for hypotension and syncope1

Allow ≥2 weeks to elapse between discontinuance of diltiazem and reinitiation of flibanserin1

Etravirine

Etravirine (moderate CYP3A4 inducer) decreased flibanserin exposure by about 21%1 10

Concomitant use not recommended1

Gingko

Possible increased flibanserin exposure with multiple weak CYP3A4 inhibitors1

Advise patients of the increased risk for adverse effects1

Grapefruit

Grapefruit juice (moderate CYP3A4 inhibitor) increased flibanserin AUC and peak concentrations by 1.4- and 1.1-fold, respectively; concomitant use may lead to hypotension and syncope1

Concomitant use contraindicated; advise patients to avoid grapefruit during flibanserin therapy1

Histamine H2-receptor antagonists (cimetidine, ranitidine)

Possible increased flibanserin exposure with multiple weak CYP3A4 inhibitors1

Advise patients of the increased risk for adverse effects1

HIV protease inhibitors (PIs) (atazanavir, fosamprenavir, indinavir, nelfinavir, ritonavir, saquinavir)

Possible increased flibanserin exposure; may lead to hypotension and syncope1

Concomitant use contraindicated1

If treatment with the HIV PI is necessary, discontinue flibanserin ≥2 days prior to initiation of the HIV PI1

If benefit of initiating HIV PI therapy within 2 days of flibanserin discontinuance clearly outweighs risk of hypotension and syncope, monitor for hypotension and syncope1

Allow ≥2 weeks to elapse between discontinuance of the HIV PI and reinitiation of flibanserin1

Macrolides (clarithromycin, erythromycin, telithromycin)

Possible increased flibanserin exposure; may lead to hypotension and syncope1

Concomitant use contraindicated1

If treatment with the macrolide is necessary, discontinue flibanserin ≥2 days prior to initiation of the macrolide antibiotic1

If benefit of initiating macrolide therapy within 2 days of flibanserin discontinuance clearly outweighs risk of hypotension and syncope, monitor for hypotension and syncope1

Allow ≥2 weeks to elapse between discontinuance of the macrolide and reinitiation of flibanserin1

Nefazodone

Possible increased flibanserin exposure; may lead to hypotension and syncope1

Concomitant use contraindicated1

If treatment with nefazodone is necessary, discontinue flibanserin ≥2 days prior to initiation of nefazodone1

If benefit of initiating nefazodone therapy within 2 days of flibanserin discontinuance clearly outweighs risk of hypotension and syncope, monitor for hypotension and syncope1

Allow ≥2 weeks to elapse between discontinuance of nefazodone and reinitiation of flibanserin1

Proton-pump inhibitors (PPIs)

Possible increased flibanserin exposure with PPIs that are potent CYP2C19 inhibitors1

Advise patients of the increased risk for adverse effects1

Resveratrol

Possible increased flibanserin exposure with multiple weak CYP3A4 inhibitors1

Advise patients of the increased risk for adverse effects1

Simvastatin

AUC and peak concentrations of simvastatin (CYP3A4 substrate) increased by 1.3- and 1.2-fold, respectively, and AUC and peak concentrations of simvastatin acid increased by 1.5- and 1.4-fold, respectively1 10

Sirolimus

Possible increased sirolimus (P-gp substrate) exposure and risk of toxicity1

St. John's wort (Hypericum perforatum)

Possible decreased flibanserin exposure1

Concomitant use not recommended1

Verapamil

Possible increased flibanserin exposure; may lead to hypotension and syncope1

Concomitant use contraindicated1

If treatment with verapamil is necessary, discontinue flibanserin ≥2 days prior to initiation of verapamil1

If benefit of initiating verapamil therapy within 2 days of flibanserin discontinuance clearly outweighs risk of hypotension and syncope, monitor for hypotension and syncope1

Allow ≥2 weeks to elapse between discontinuance of verapamil and reinitiation of flibanserin1

Addyi Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed following oral administration; peak concentrations attained within approximately 45 minutes (range: 0.75–4 hours).1 9

Undergoes extensive first-pass metabolism; absolute oral bioavailability is 33%.1 9

Steady-state concentrations achieved after 3 days.1 Exhibits dose-proportional pharmacokinetics.1 Exposure with once-daily dosing is 1.4-fold higher compared with single-dose administration.1

Food

Administration with food delays time to achieve peak concentrations and increases peak concentrations and AUC.1

Special Populations

Mild hepatic impairment: AUC increased 4.5-fold.1

Renal impairment: AUC slightly increased in patients with mild or moderate and severe renal impairment (by 1.1- and 1.2-fold, respectively).1

Effect of age on exposure not systematically evaluated.1

Poor CYP2C19 metabolizers: Peak concentrations and AUC are 1.5- and 1.3-fold higher, respectively, than in extensive CYP2C19 metabolizers.1

Race: Approximately 1.4-fold higher exposure observed among Japanese women compared with Caucasian women; however, weight-adjusted AUCs were similar, suggesting that difference is likely related to weight rather than race.1

Distribution

Extent

Distributed into milk in rats; not known whether distributed into human milk.1

Plasma Protein Binding

Approximately 98%, mainly to albumin.1

Elimination

Metabolism

Extensively metabolized, principally by CYP3A4 and, to a lesser extent, by CYP2C19; CYP isoenzymes 1A2, 2B6, 2C8, 2C9, and 2D6 contribute minimally (<10%).1

Metabolized to at least 35 metabolites, mostly in low concentrations; 2 of these appear in substantial concentrations in plasma but are pharmacologically inactive.1

Elimination Route

44 and 51% recovered in urine and feces, respectively.1

Half-life

Approximately 11 hours.1

Special Populations

Mild hepatic impairment: Half-life is prolonged (26 hours).1

Poor CYP2C19 metabolizers: Half-life is prolonged to 13.5 hours compared with 11.1 hours in extensive metabolizers.1

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).1

Actions

  • 5-HT1A receptor agonist and 5-HT2A receptor antagonist.1 6 7 8 Also a moderate antagonist at 5-HT2B, 5-HT2C, and dopamine D4 receptors.1 6 7 8

  • Precise mechanism of action in treating HSDD in premenopausal women not fully understood,1 6 7 but thought to be related to enhancement of dopaminergic and noradrenergic activity and reduction of serotonergic activity in the prefrontal cortex.6 7

  • Generally, dopamine and norepinephrine are thought to be excitatory and serotonin inhibitory to sexual desire and arousal.6 7 16 17 Flibanserin-induced activation of inhibitory 5-HT1A receptors and inhibition of excitatory 5-HT2A receptors may result in decreased serotonin release and increased dopamine and norepinephrine concentrations in areas of the prefrontal cortex thought to be involved in sexual interest and desire.6 7 16 17

Advice to Patients

  • Importance of advising patients to read the manufacturer's medication guide prior to initiating flibanserin therapy and each time the prescription is refilled.1

  • Importance of advising patients that flibanserin is only available through the Addyi REMS Program and can only be obtained from certified pharmacies participating in the program.1 Provide patients with the telephone number and website for the program for information on obtaining flibanserin.1

  • Importance of advising patients to take the prescribed dose exactly as directed (once daily at bedtime) and not to take the drug at any other time of the day,1 since taking flibanserin during waking hours increases the risk of hypotension, syncope, accidental injury, and CNS depression.1

  • If a dose of flibanserin is missed at bedtime, the missed dose should be skipped and the next dose taken at bedtime on the following day.1 Importance of advising patients not to take the missed dose the next morning or 2 doses of the drug at the same time.1

  • Risk of severe hypotension and syncope, particularly when used concurrently with alcohol or moderate or potent CYP3A4 inhibitors or used in patients with hepatic impairment.1 Importance of informing patients that alcohol use and moderate or potent CYP3A4 inhibitors are contraindicated during flibanserin therapy and that the drug also is contraindicated in patients with hepatic impairment.1 Counsel patients to abstain from alcohol and to ask about drug interactions before beginning any new prescription or OTC medication (e.g., cimetidine) or using other products that contain CYP3A4 inhibitors (e.g., grapefruit juice, gingko, resveratrol, St. John's wort).1 (See Interactions.) Importance of advising patients who experience presyncope or lightheadedness to lie down and to seek medical attention if symptoms persist.1

  • Risk of somnolence or sedation.1 Importance of advising patients that concomitant use of other CNS depressants (e.g., alcohol, benzodiazepines, sedative and hypnotic drugs, opiates, diphenhydramine) and taking flibanserin during waking hours can increase the risk of CNS depression.1 10 Importance of advising patients not to drive, operate complex machinery, or engage in other activities requiring full alertness until at least 6 hours after taking a dose of flibanserin and until the effects of drug are known.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed; advise women to avoid breast-feeding during flibanserin therapy.1

  • Importance of informing clinician of existing or contemplated concomitant therapy, including prescription, OTC, and recreational drugs and dietary or herbal supplements, as well as any concomitant illnesses (e.g., psychiatric disorders, liver disease, conditions that may predispose to hypotension).1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Distribution of flibanserin is restricted.1 11 (See Restricted Distribution Program under Dosage and Administration: General.)

Flibanserin

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, film-coated

100 mg

Addyi

Sprout

AHFS DI Essentials. © Copyright 2016, Selected Revisions August 2, 2016. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Sprout Pharmaceuticals, Inc. Addyi (flibanserin) film-coated tablets prescribing information. Raleigh, NC; 2015 Aug.

2. DeRogatis LR, Komer L, Katz M et al. Treatment of hypoactive sexual desire disorder in premenopausal women: efficacy of flibanserin in the VIOLET Study. J Sex Med. 2012; 9:1074-85. [PubMed 22248038]

3. Thorp J, Simon J, Dattani D et al. Treatment of hypoactive sexual desire disorder in premenopausal women: efficacy of flibanserin in the DAISY study. J Sex Med. 2012; 9:793-804. [PubMed 22239862]

4. Katz M, DeRogatis LR, Ackerman R et al. Efficacy of flibanserin in women with hypoactive sexual desire disorder: results from the BEGONIA trial. J Sex Med. 2013; 10:1807-15. [PubMed 23672269]

5. US Food and Drug Administration. Center for Drug Evaluation and Research: Application number 022526Orig1s000: Summary review. 2015 Feb 18. From FDA website.

6. Stahl SM, Sommer B, Allers KA. Multifunctional pharmacology of flibanserin: possible mechanism of therapeutic action in hypoactive sexual desire disorder. J Sex Med. 2011; 8:15-27. [PubMed 20840530]

7. Stahl SM. Mechanism of action of flibanserin, a multifunctional serotonin agonist and antagonist (MSAA), in hypoactive sexual desire disorder. CNS Spectr. 2015; 20:1-6. [PubMed 25659981]

8. Borsini F, Evans K, Jason K et al. Pharmacology of flibanserin. CNS Drug Rev. 2002; 8:117-42. [PubMed 12177684]

9. Trocóniz IF, Boland K, Staab A. Population pharmacokinetic/pharmacodynamic model for the sedative effects of flibanserin in healthy volunteers. Pharm Res. 2012; 29:1518-29. [PubMed 22219166]

10. Sprout Pharmaceuticals, Inc. Addyi (flibanserin) - drug interaction overview. Raleigh, NC; 2015 Sep 3.

11. NDA 22526 Addyi (flibanserin) risk evaluation and mitigation strategy (REMS). From FDA website. Accessed 2015 Sep 9.

12. American Psychiatric Association. DSM-IV-TR: Diagnostic and statistical manual of mental disorders. 4th ed. Text revision. Washington, DC: American Psychiatric Association; 2000.

13. American Psychiatric Association. DSM-5: Diagnostic and statistical manual of mental disorders. 5th ed. Arlington, VA: American Psychiatric Association; 2013:433–7.

14. Simon JA, Kingsberg SA, Shumel B et al. Efficacy and safety of flibanserin in postmenopausal women with hypoactive sexual desire disorder: results of the SNOWDROP trial. Menopause. 2014; 21:633-40. [PubMed 24281236]

15. Jayne C, Simon JA, Taylor LV et al. Open-label extension study of flibanserin in women with hypoactive sexual desire disorder. J Sex Med. 2012; 9:3180-8. [PubMed 23057791]

16. Pfaus JG. Pathways of sexual desire. J Sex Med. 2009; 6:1506-33. [PubMed 19453889]

17. Stahl SM. Circuits of sexual desire in hypoactive sexual desire disorder. J Clin Psychiatry. 2010; 71:518-9. [PubMed 20492849]

18. Anon. Flibanserin (Addyi) for hypoactive sexual desire disorder. Med Lett Drugs Ther. 2015; 57:133-5.

19. Joffe HV, Chang C, Sewell C et al. FDA approval of flibanserin--treating hypoactive sexual desire disorder. N Engl J Med. 2016; 374:101-4.

20. US Food and Drug Administration. Drug development and drug interactions: table of substrates, inhibitors and inducers. From FDA website. Accessed 2016 Mar 1.

21. Robinson K, Cutler JB, Carris NW. First pharmacological therapy for hypoactive sexual desire disorder in premenopausal women: flibanserin. Ann Pharmacotherapy. 2016; 50:125-32.

22. Leiblum SR, Koochaki PE, Rodenberg CA et al. Hypoactive sexual desire disorder in postmenopausal women: US results from the Women's International Study of Health and Sexuality (WISHeS). Menopause. 2006; 13:46-56.

Hide