Medically reviewed by Drugs.com. Last updated on Apr 29, 2020.
(BRE me LAN oh tide)
- Bremelanotide Acetate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Auto-injector, Subcutaneous, as acetate [preservative free]:
Vyleesi: 1.75 mg/0.3 mL (0.3 mL)
Brand Names: U.S.
- Melanocortin Receptor Agonist
Nonselective melanocortin receptor agonist that activates several receptor subtypes, most notably MC4R (present throughout the CNS) and MC1R (expressed on melanocytes). Mechanism for improvement of hypoactive sexual desire disorder is unknown.
Vd: 25 ± 5.8 L
Primarily amide hydrolysis of the cyclic peptide
Urine (64.8%); feces (22.8%)
Time to Peak
Terminal: ~2.7 hours (range: 1.9 to 4 hours)
Special Populations: Renal Function Impairment
In patients with mild (eGFR 60 to 89 mL/minute/1.73 m2), moderate (eGFR 30 to 59 mL/minute/1.73 m2), and severe (eGFR <30 mL/minute/1.73 m2) renal impairment, AUC increased by 1.2-, 1.5-, and 2-fold, respectively.
Special Populations: Hepatic Function Impairment
In patients with mild (Child-Pugh class A) and moderate (Child-Pugh class B) hepatic impairment, AUC increased by 1.2- and 1.7-fold, respectively.
Use: Labeled Indications
Hypoactive sexual desire disorder: 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 coexisting medical or psychiatric condition, problems with the relationship, or the effects of a medication or drug substance.
Limitations of use: Not indicated for the treatment of HSDD in postmenopausal women or in men or to enhance sexual performance.
Uncontrolled hypertension or known cardiovascular disease
Note: Discontinue use of bremelanotide if no improvement in symptoms after 8 weeks.
Hypoactive sexual desire disorder: SubQ: 1.75 mg as needed, ≥45 minutes before sexual activity (maximum: 1.75 mg/24 hours). No more than 8 doses per month are recommended.
Refer to adult dosing.
SubQ: Administer SubQ in the abdomen or thigh.
Store at ≤25°C (77°F). Do not freeze. Protect from light.
Indomethacin: Bremelanotide may decrease the serum concentration of Indomethacin. Monitor therapy
Naltrexone: Bremelanotide may decrease the serum concentration of Naltrexone. Avoid combination
Cardiovascular: Flushing (20%)
Central nervous system: Headache (11%)
Dermatologic: Skin hyperpigmentation (1% to 38%)
Gastrointestinal: Nausea (40%)
Local: Injection site reaction (13%)
1% to 10%:
Cardiovascular: Increased blood pressure (<2%)
Central nervous system: Fatigue (3%), paresthesia (3%), dizziness (2%), pain (<2%), restless leg syndrome (<2%)
Endocrine & metabolic: Hot flash (3%)
Gastrointestinal: Vomiting (5%), diarrhea (<2%), upper abdominal pain (<2%)
Neuromuscular & skeletal: Arthralgia (<2%), increased creatine phosphokinase in blood specimen (<2%), limb pain (<2%), myalgia (<2%)
Respiratory: Cough (3%), nasal congestion (2%), rhinorrhea (<2%)
Frequency not defined:
Cardiovascular: Decreased heart rate
Central nervous system: Hypoesthesia
Dermatologic: Injection site pruritus
Respiratory: Flu-like symptoms
Concerns related to adverse effects:
• Cardiovascular: A transient increase in blood pressure and reduction in heart rate may occur after each dose; peak effects occur 2 to 4 hours post-dose and typically return to baseline within 12 hours. Use is not recommended in patients at high risk for cardiovascular disease and is contraindicated in patients with uncontrolled hypertension or established cardiovascular disease.
• Focal hyperpigmentation: Focal hyperpigmentation, including involvement of the face, gingiva, and breasts, has been reported. May occur more frequently in patients with dark skin and with more frequent administration. Consider discontinuation if focal hyperpigmentation develops; may resolve in some patients.
• Gastrointestinal: Nausea, especially after the initial dose, has been reported. Onset usually occurs within 1 hour post-dose and may last approximately 2 hours. Incidence commonly decreases with subsequent doses. Use of an antiemetic may be effective; discontinuation of therapy may be considered for persistent or severe nausea.
Concurrent drug therapy issues:
• Delayed gastric emptying: May delay gastric emptying and reduce the rate and extent of absorption of concurrently administered oral drugs. Monitor for efficacy of concurrently administered oral drugs and consider discontinuation of bremelanotide if efficacy is affected. Additionally, concurrent use with oral drugs dependent on threshold concentrations for efficacy (eg, antibiotics) may need to be avoided.
Blood pressure and heart rate (if clinically indicated)
Females of reproductive potential should use effective contraception during bremelanotide therapy.
Outcome information following maternal use of bremelanotide during pregnancy is limited. Discontinue if pregnancy is suspected.
Data collection to monitor pregnancy and infant outcomes following exposure to bremelanotide is ongoing. Health care providers are encouraged to enroll females exposed to bremelanotide during pregnancy in the Vyleesi Pregnancy Registry (1-877-411-2510).
What is this drug used for?
• It is used in some women to raise interest in sex.
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
• Injection site irritation
• Stuffy nose
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:
• Severe headache
• Severe dizziness
• Passing out
• Vision changes
• Slow heartbeat
• 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, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
More about bremelanotide
- Side Effects
- During Pregnancy or Breastfeeding
- Dosage Information
- Drug Interactions
- En Español
- 3 Reviews
- Drug class: melanocortin receptor agonists
Other brands: Vyleesi