Addyi

Name: Addyi

Addyi Side Effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • severe drowsiness; or
  • a light-headed feeling, like you might pass out.

Common side effects may include:

  • dizziness, drowsiness;
  • tiredness;
  • nausea;
  • dry mouth; or
  • sleep problems (insomnia).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What brand names are available for flibanserin?

Addyi

Is flibanserin safe to take if I'm pregnant or breastfeeding?

Flibanserin has not been adequately studied in pregnant women.

Flibanserin has not been studied in women who are breastfeeding. It is not known whether flibanserin is present in human milk.

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Reviewed on 11/3/2015 References REFERENCE: FDA Prescribing Information

What is the most important information I should know about flibanserin?

Follow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use.

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

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.)

Precautions While Using Addyi

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly and to check for unwanted effects.

Do not use this medicine if you are also using amprenavir, atazanavir (Reyataz®), boceprevir (Victrelis®), ciprofloxacin (Cipro®), clarithromycin (Biaxin®), conivaptan (Vaprisol®), diltiazem (Cardizem®), erythromycin (Ery-Tab®), fluconazole (Diflucan®), fosamprenavir (Lexiva®), indinavir (Crixivan®), itraconazole (Sporanox®), ketoconazole (Nizoral®), nefazodone, nelfinavir (Viracept®), posaconazole (Noxafil®), ritonavir (Norvir®), saquinavir (Invirase®), telaprevir, telithromycin (Ketek®), or verapamil (Calan®).

Do not drink alcohol while you are using flibanserin. This medicine will add to the effects of alcohol and other CNS depressants (medicines that may make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicines for hay fever, allergies, or colds, sedatives, tranquilizers, or sleeping medicine, prescription pain medicine or narcotics, medicine for seizures or barbiturates, muscle relaxants, or anesthetics, including some dental anesthetics. Check with your doctor before taking any of these medicines while you are using flibanserin.

Do not eat grapefruit or drink grapefruit juice while you are using this medicine. Grapefruit and grapefruit juice may change the amount of this medicine that is absorbed in the body.

If your condition does not improve within 8 weeks, or if it become worse, check with your doctor.

This medicine may cause you to feel dizzy, drowsy, or lightheaded. Avoid driving, using machines, or doing anything else that could be dangerous if you are not alert for at least 6 hours after you take this medicine and until you know how this medicine affects you. If you feel lightheaded, getting up slowing after sitting or lying down may help.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

What are some side effects that I need to call my doctor about right away?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Dizziness or passing out.
  • Feeling very sleepy.

Dosage Forms and Strengths

Tablets: 100 mg, oval, pink, debossed on one side with "f100" and blank on the other side.

Dosing & Uses

Dosage Forms & Strengths

tablet

  • 100mg

Hypoactive Sexual Desire Disorder

Indicated for premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD) as characterized by low sexual desire that causes marked distress or interpersonal difficulty and is not caused by a coexisting medical or psychiatric condition, problems within the relationship, or the effects of a medication or other drug substance

100 mg PO once daily at bedtime

Dosed at bedtime because administration during waking hours increases risks of hypotension, syncope, accidental injury, and CNS depression

Discontinued after 8 weeks if no improvement

Missed dose

  • If a dose is missed at bedtime, instruct the patient to take the next dose at bedtime on the next day
  • Instruct the patient to not double the next dose

CYP3A4 inhibitors

  • Coadministration with moderate or strong CYP3A4 inhibitors is contraindicated
  • If initiating flibanserin following moderate or strong CYP3A4 inhibitor use, start flibanserin 2 weeks after the last dose of the CYP3A4 inhibitor
  • If initiating a moderate or strong CYP3A4 inhibitor following flibanserin use, start the moderate or strong CYP3A4 inhibitor 2 days after the last dose of flibanserin

Dosing Considerations

Acquired HSDD refers to HSDD that develops in a patient who previously had no problems with sexual desire

Generalized HSDD refers to HSDD that occurs regardless of the type of stimulation, situation, or partner

Limitations of use

  • Not indicated for HSDD in postmenopausal women or in men
  • Not indicated to enhance sexual performance

Not indicated

Patient Handout

Print without Office InfoPrint with Office Info

What is Addyi?

Addyi (flibanserin) is available only from a certified pharmacy under a special program.

Addyi is used to treat decreased sexual desire in women who have not gone through menopause and who have never had low sexual desire in the past. Addyi is for use only when low sexual desire is NOT caused by a medical condition, a mental disorder, relationship problems, or by using drugs or other medicines.

Addyi is not for women who have already gone through menopause. This medicine is also not for use by men.

Flibanserin Breastfeeding Warnings

Breastfeeding is not recommended during treatment with this drug. Excreted into human milk: Unknown Excreted into animal milk: Yes Comments: The effects on the breastfed infant and on milk production are unknown.

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