Vyleesi
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Omid Afkhami Ardakani
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Overview
Vyleesi is a Melanocortin receptor agonist that is FDA approved for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women. Common adverse reactions include nausea (40%), flushing (20%), injection site reactions (13%), headache (11%), and vomiting (4.8%).
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Vyleesi is indicated for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women.
The recommended dose is 1.75 mg, injected subcutaneously at least 45 minutes before anticipated sexual activity. No more than 1 dose in 24 hours should be administered, and no more than 8 doses per month
Off-Label Use and Dosage (Adult)
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Vyleesi FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Contraindications
Uncontrolled hypertension Cardiovascular disease
Warnings
Transient Increase in Blood Pressure and Reduction in Heart Rate Focal Hyperpigmentation
Adverse Reactions
Clinical Trials Experience
nausea (8%), headache (2%), vomiting (1%), flushing (1%), injection site reactions (1%), flu-like symptoms (<1%) and increased blood pressure (<1%).
Postmarketing Experience
There is limited information regarding Vyleesi Postmarketing Experience in the drug label.
Drug Interactions
Vyleesi may slow gastric emptying, which could affect the absorption of oral medications. Interaction with medications such as antibiotics, pain medicines, and naltrexone
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
Not recommended
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Vyleesi in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Vyleesi during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Vyleesi in women who are nursing.
Pediatric Use
There is no FDA guidance on the use of Vyleesi in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Vyleesi in geriatric settings.
Gender
Vyleesi is indicated only for premenopausal women with hypoactive sexual desire disorder (HSDD). It is not indicated for men.
Race
The majority of clinical trials for Vyleesi were conducted on White women. There is limited data on the efficacy and side effects in other races. However, some reports suggest that hyperpigmentation occurred more frequently in Black or African American women.
Renal Impairment
Mild to moderate renal impairment does not require dosage adjustment. However, Vyleesi should be used with caution in patients with severe renal impairment, as they may experience an increased incidence of adverse reactions such as nausea and vomiting
Hepatic Impairment
Vyleesi has not been evaluated in patients with severe hepatic impairment. It should be used with caution in such patients due to the potential for increased adverse reactions
Females of Reproductive Potential and Males
Vyleesi is indicated only for use in premenopausal women. Women of reproductive potential should use effective contraception while taking Vyleesi, and discontinue use if pregnancy is suspected.
Immunocompromised Patients
There is no FDA guidance one the use of Vyleesi in patients who are immunocompromised.
Administration and Monitoring
Administration
Vyleesi is administered subcutaneously via an auto-injector. The recommended dose is 1.75 mg, injected 45 minutes before anticipated sexual activity. Patients should not administer more than one dose in 24 hours, and use should not exceed eight doses per month
Monitoring
Monitoring is necessary for patients at risk of hypertension or those with cardiovascular concerns due to the risk of transient increases in blood pressure and decreases in heart rate. Blood pressure monitoring may be advisable, especially during the first doses. Additionally, monitoring for adverse effects, such as nausea, is recommended.
IV Compatibility
There is limited information regarding the compatibility of Vyleesi and IV administrations.
Overdosage
There are no reported cases of Vyleesi overdose from clinical trials. However, taking higher doses than recommended may increase the likelihood of experiencing nausea, focal hyperpigmentation, and more pronounced increases in blood pressure. In the event of an overdose, supportive treatment should be provided.
Pharmacology
There is limited information regarding Vyleesi Pharmacology in the drug label.
Mechanism of Action
Vyleesi (bremelanotide) is a melanocortin receptor agonist. It works by activating melanocortin receptors, particularly MC1R and MC4R, which are involved in modulating sexual desire and the central nervous system. The exact mechanism by which it treats hypoactive sexual desire disorder (HSDD) in premenopausal women is unknown.
Structure
Vyleesi is a synthetic cyclic heptapeptide. It is administered as bremelanotide acetate. The structure includes an acetylated amino group and a free acid at the carboxyl terminus
Pharmacodynamics
Vyleesi activates melanocortin receptors, particularly MC1R and MC4R. Activation of these receptors in the central nervous system is believed to modulate sexual desire, though the exact mechanism in treating hypoactive sexual desire disorder (HSDD) is unknown. MC1R activation also explains the hyperpigmentation side effect seen in some patients
Pharmacokinetics
After subcutaneous administration, Vyleesi reaches its peak plasma concentration in about 1 hour. It is primarily metabolized via proteolysis, and its elimination half-life is approximately 2.7 hours
Nonclinical Toxicology
In animal studies, increased pigmentation in the skin and organs was observed. There was no evidence of mutagenicity or carcinogenicity associated with bremelanotide. However, reproductive toxicity was noted in animal studies
Clinical Studies
The efficacy of Vyleesi was evaluated in two randomized, double-blind, placebo-controlled trials involving 1,247 premenopausal women with HSDD. The trials measured the change in sexual desire and distress related to low sexual desire. Vyleesi significantly improved sexual desire scores in women, although nausea and increased blood pressure were commonly reported side effects
How Supplied
Vyleesi is supplied as 1.75 mg bremelanotide in a 0.3 mL solution in a single-dose, disposable prefilled autoinjector. It is available in cartons of 4 autoinjectors or 2 autoinjectors.
Storage
Vyleesi should be stored at or below 25°C (77°F). It should be protected from light and should not be frozen.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
Patients should be advised about potential side effects, including nausea, increased blood pressure, and focal hyperpigmentation. They should also be counseled to: Not use more than 1 dose within 24 hours and no more than 8 doses per month. Be cautious of using Vyleesi with underlying cardiovascular conditions due to blood pressure increases. Contact their healthcare provider if they experience severe or persistent nausea, which might require antiemetic treatment
Precautions with Alcohol
Patients should be cautious when consuming alcohol while using Vyleesi. Clinical studies indicated that Vyleesi might not be well tolerated with alcohol use, especially due to its effects on blood pressure and nausea
Brand Names
Vyleesi is the primary brand name under which bremelanotide is marketed.
Look-Alike Drug Names
There is limited information regarding Vyleesi Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.