Addyi

Name: Addyi

Descriptions

Flibanserin is used to treat hypoactive sexual desire disorder (HSDD) in women who have not gone through menopause. This medicine should only be used by women who have low sexual desire that is troubling to them and is not caused by a medical or mental problem, problems in the relationship, or medicine or other drug use.

Women who have gone through menopause and men should not use flibanserin. Do not use this medicine to improve sexual performance.

This medicine is available only with your doctor's prescription.

This product is available in the following dosage forms:

  • Tablet

Why is this medication prescribed?

Flibanserin is used to treat women with hypoactive sexual desire disorder (HSDD; a low sexual desire that causes distress or interpersonal difficulty) who have not experienced menopause (change of life; the end of monthly menstrual periods). Flibanserin should not be used for the treatment of HSDD in women who have gone through menopause or in men or to improve sexual performance. Flibanserin is in a class of medications called a serotonin receptor 1A agonist/serotonin receptor 2A antagonist. It works by changing the activity of serotonin and other natural substances in the brain.

What other information should I know?

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

What is flibanserin, and how does it work (mechanism of action)?

Addyi (flibanserin) is an oral drug used for treating low sexual desire in women. The mechanism of action of flibanserin is not completely understood. Flibanserin affects the way the brain works by interfering with communication among the brain's nerves in areas of the brain that control sexual desire and other pleasurable sensations. Nerves communicate with each other by making and releasing chemicals called neurotransmitters. The neurotransmitters travel to other nearby nerves where they attach to receptors on nerves. The attachment of neurotransmitters either stimulates or inhibits the function of the nearby nerves. Flibanserin blocks several of the receptors on nerves including dopamine type 4, and serotonin type 2A, 2B and 2C receptors. It also stimulates serotonin type 1A. How these effects improve sexual desire in women is unknown. Scientists think that flibanserin may regulate areas of the brain that control sexual desire in premenopausal women with reduced sexual interest and desire. The FDA approved flibanserin on August 18, 2015.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Flibanserin 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.

Introduction

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

Addyi Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common
  • Blurred vision
  • confusion
  • dizziness, fainting, or lightheadedness, especially when getting up suddenly from a lying or sitting position
  • sweating
  • unusual tiredness or weakness
  • sleepiness or unusual drowsiness
Less common
  • Feeling of constant movement of self or surroundings
  • sensation of spinning
Rare
  • Bloating
  • fever
  • nausea
  • severe cramping
  • stomach or lower abdominal pain
  • vomiting

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common
  • Constipation
  • dry mouth
  • nervousness
  • normal menstrual bleeding occurring earlier, possibly lasting longer than expected
  • rash
  • trouble sleeping

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

What do I need to tell my doctor BEFORE I take Addyi?

  • If you have an allergy to this medicine or any part of Addyi.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you are breast-feeding. Do not breast-feed while you take this medicine.
  • If you are taking any of these drugs: Carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, or St. John's wort.

This is not a list of all drugs or health problems that interact with Addyi.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

Addyi Dosage and Administration

Recommended Dosage

The recommended dosage of Addyi is 100 mg administered orally once per day at bedtime. Addyi is dosed at bedtime because administration during waking hours increases the risks of hypotension, syncope, accidental injury, and central nervous system (CNS) depression (such as somnolence and sedation).

Missed Dose

If a dose of Addyi 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.

Discontinuation of Addyi

Discontinue Addyi after 8 weeks if the patient does not report an improvement in her symptoms.

Initiation of Addyi Following Moderate or Strong CYP3A4 Inhibitor Use

If initiating Addyi following moderate or strong CYP3A4 inhibitor use, start Addyi 2 weeks after the last dose of the CYP3A4 inhibitor.

If initiating a moderate or strong CYP3A4 inhibitor following Addyi use, start the moderate or strong CYP3A4 inhibitor 2 days after the last dose of Addyi [see Warnings and Precautions (5.3)].

Pharmacology

Mechanism of Action

Postsynaptic serotonin-1A (5HT-1A) receptor agonist and 5HT-2A receptor antagonist; also elicits moderate antagonist activities at the 5-HT2B, 5-HT2C, and dopamine D4 receptors

The mechanism of action HSDD is not known; may work by restoring prefrontal cortex control over the brain's motivation/rewards structures, enabling sexual desire to manifest; this may occur by increasing dopamine and norepinephrine while transiently decreasing serotonin in the brain's prefrontal cortex, which may be accomplished by reduced glutamate transmission

Absorption

Bioavailability: 33%

Peak plasma time: 0.75 hr

Peak plasma concentration: 419 ng/mL

AUC: 1543 ng·hr/mL

Food increased the extent of absorption and slowed the rate of absorption

Distribution

Protein bound: 98%, primarily to albumin

Metabolism

Primarily metabolized by CYP3A4 and, to a lesser extent, by CYP2C19

Elimination

Half-life: 11 hr

Excretion: 51% feces; 44% urine

Pharmacogenomics

CYP2C19 poor metabolizers had increased flibanserin exposures compared with CYP2C19 extensive metabolizers

Additionally, syncope occurred in a subject who was a CYP2C19 poor metabolizer

The frequencies of poor CYP2C19 metabolizers are ~2–5% among whites and blacks and ~2–15% among Asians

Drug Interactions

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Amifampridine
  • Amprenavir
  • Aprepitant
  • Atazanavir
  • Boceprevir
  • Ciprofloxacin
  • Clarithromycin
  • Colchicine
  • Conivaptan
  • Diltiazem
  • Dronedarone
  • Erythromycin
  • Fluconazole
  • Fosamprenavir
  • Fosaprepitant
  • Imatinib
  • Indinavir
  • Itraconazole
  • Ketoconazole
  • Lopinavir
  • Nefazodone
  • Nelfinavir
  • Posaconazole
  • Ritonavir
  • Saquinavir
  • Telaprevir
  • Telithromycin
  • Verapamil
  • Voriconazole

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Acepromazine
  • Alfentanil
  • Alprazolam
  • Amisulpride
  • Amobarbital
  • Anileridine
  • Aripiprazole
  • Asenapine
  • Baclofen
  • Benperidol
  • Bromazepam
  • Buprenorphine
  • Buspirone
  • Butabarbital
  • Butorphanol
  • Carbinoxamine
  • Carisoprodol
  • Carphenazine
  • Chloral Hydrate
  • Chlordiazepoxide
  • Chlorpromazine
  • Chlorzoxazone
  • Clobazam
  • Clonazepam
  • Clorazepate
  • Clozapine
  • Codeine
  • Cyclobenzaprine
  • Dabigatran Etexilate
  • Dexmedetomidine
  • Diacetylmorphine
  • Diazepam
  • Dichloralphenazone
  • Difenoxin
  • Dihydrocodeine
  • Diphenhydramine
  • Diphenoxylate
  • Doxylamine
  • Droperidol
  • Eluxadoline
  • Enflurane
  • Estazolam
  • Eszopiclone
  • Ethchlorvynol
  • Ethopropazine
  • Ethylmorphine
  • Fentanyl
  • Fluphenazine
  • Flurazepam
  • Fluspirilene
  • Fospropofol
  • Halazepam
  • Haloperidol
  • Halothane
  • Hexobarbital
  • Hydrocodone
  • Hydromorphone
  • Hydroxyzine
  • Isoflurane
  • Ketamine
  • Ketazolam
  • Ketobemidone
  • Levorphanol
  • Lorazepam
  • Loxapine
  • Meclizine
  • Melperone
  • Meperidine
  • Mephobarbital
  • Meprobamate
  • Meptazinol
  • Mesoridazine
  • Metaxalone
  • Methadone
  • Methdilazine
  • Methocarbamol
  • Methohexital
  • Methotrimeprazine
  • Methylene Blue
  • Midazolam
  • Molindone
  • Moricizine
  • Morphine
  • Morphine Sulfate Liposome
  • Nalbuphine
  • Nicomorphine
  • Nitrazepam
  • Nitrous Oxide
  • Olanzapine
  • Opium
  • Opium Alkaloids
  • Orphenadrine
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Papaveretum
  • Paregoric
  • Pentazocine
  • Pentobarbital
  • Perampanel
  • Perazine
  • Periciazine
  • Perphenazine
  • Pimozide
  • Piperacetazine
  • Pipotiazine
  • Piritramide
  • Pitolisant
  • Prazepam
  • Primidone
  • Prochlorperazine
  • Promazine
  • Promethazine
  • Propofol
  • Quazepam
  • Quetiapine
  • Ramelteon
  • Remifentanil
  • Remoxipride
  • Secobarbital
  • Sertindole
  • Sodium Oxybate
  • Sufentanil
  • Sulpiride
  • Suvorexant
  • Tapentadol
  • Temazepam
  • Thiethylperazine
  • Thiopental
  • Thiopropazate
  • Thioridazine
  • Tilidine
  • Tizanidine
  • Tolonium Chloride
  • Topiramate
  • Tramadol
  • Triazolam
  • Trifluoperazine
  • Trifluperidol
  • Triflupromazine
  • Trimeprazine
  • Zaleplon
  • Zolpidem
  • Zopiclone
  • Zotepine

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Digoxin

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For treatment of hypoactive sexual desire disorder:
      • Adults—100 milligrams (mg) once a day at bedtime.
      • Children—Use is not recommended.

How should I take Addyi?

Take Addyi exactly as prescribed by your doctor. Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Take Addyi only at bedtime.

Addyi can lower your blood pressure, which can make you dizzy. If you feel light-headed after taking this medicine, lie down if you are not already in bed.

It may take up to 8 weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

Store at room temperature away from moisture and heat.

Addyi dosing information

Usual Adult Dose for Hypoactive Sexual Desire Disorder:

100 mg orally once per day at bedtime

Duration of therapy: This drug should be discontinued after 8 weeks if the patient does not report an improvement in symptoms.

Comments: This drug is not indicated to enhance sexual performance, and is not indicated for treatment in postmenopausal women or in men.

Use: Treatment of 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 due to a co-existing medical or psychiatric condition, problems within the relationship, or the effects of a medication or other drug substance.

For the Consumer

Applies to flibanserin: oral tablet

Along with its needed effects, flibanserin (the active ingredient contained in Addyi) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking flibanserin:

More common
  • Blurred vision
  • confusion
  • dizziness, fainting, or lightheadedness, especially when getting up suddenly from a lying or sitting position
  • sweating
  • unusual tiredness or weakness
  • sleepiness or unusual drowsiness
Less common
  • Feeling of constant movement of self or surroundings
  • sensation of spinning
Rare
  • Bloating
  • fever
  • nausea
  • severe cramping
  • stomach or lower abdominal pain
  • vomiting

Some side effects of flibanserin may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common
  • Constipation
  • dry mouth
  • nervousness
  • normal menstrual bleeding occurring earlier, possibly lasting longer than expected
  • rash
  • trouble sleeping

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