sexual dysfunction agents
melanocortin receptor agonists
Treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD) that is characterized by low sexual desire that causes marked distress or interpersonal difficulty and is NOT due to a concomitant medical or psychiatric condition, relationship problems, or the effects of a medication or drug substance.
Stimulates various melanocortin receptors, with the most notable being MC4R (present in the CNS) and MC41 (present on melanocytes). The precise mechanism by which this receptor activation improves HSDD is unknown.
Improved sexual desire.
Absorption: Completely absorbed following SUBQ administration.
Distribution: Not distributed to the tissues.
Metabolism and Excretion: Primarily undergoes hydrolysis; 65% excreted in urine, 23% in feces.
Half-life: 2.7 hr
TIME/ACTION PROFILE (plasma concentrations)
- Uncontrolled hypertension;
- Cardiovascular disease;
- OB: Pregnancy.
Use Cautiously in:
- Patients at high risk for cardiovascular disease;
- Patients with dark skin (↑ risk for focal hyperpigmentation);
- Severe hepatic impairment;
- Severe renal impairment (CCr <30 mL/min);
- Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
- Rep: Women of reproductive potential;
- Pedi: Safety and effectiveness not established in children.
Adverse Reactions/Side Effects
CV: ↓ heart rate, ↑ blood pressure
Derm: flushing, focal hyperpigmentation
EENT: nasal congestion, rhinorrhea
GI: nausea, abdominal pain, diarrhea, vomiting
Local: injection site reactions
MS: ↑ creatine kinase, arthralgia, myalgia, pain
Neuro: headache, dizziness, fatigue, paresthesia, restless leg syndrome
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- May ↓ absorption of concomitantly administered medications; avoid using bremelanotide when using antibiotics or analgesics.
- May ↓ naltrexone levels; avoid using bremelanotide in patients using naltrexone for substance use disorders.
PO (Adults): 1.75 mg given on an as needed basis ≥45 min before anticipated sexual activity (not to exceed one dose/24 hr or 8 doses/mo). Discontinue after 8 wk if no improvement in symptoms.
Solution for injection (auto-injectors): 1.75 mg/0.3 mL
- Assess sexual desire prior to and periodically during therapy.
- Assess cardiovascular risk and control of BP periodically during therapy. Systolic BP ↑ 6 mmHg, diastolic BP ↑ 3 mmHg and HR ↓ up to 5 bpm transiently after dose; usually return to normal within 12 hr of dose.
- Assess for focal hyperpigmentation of face, gingiva, and breasts periodically during therapy. More common in patients with dark skin or with >8 doses/month. Consider discontinuation of therapy if hyperpigmentation occurs; may not resolve with discontinuation.
- Assess for nausea during therapy; may require antiemetics. Usually improves with 2nd dose; may require discontinuation.
- SUBQ Using auto-injector, inject into abdomen or thigh 45 min before anticipated sexual activity. Do not administer more than 1 dose/24 hr or more than 8 doses/month.
- Instruct patient to take medication as directed with no more than 1 dose/24 hr or no more than 8 doses/month. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
- Inform patient that increases in BP and decreases in HR may occur after each dose; usually resolve within 12 hr.
- Inform patient that darkening of the skin of the face, gums, and breasts may occur, especially in patients with darker skin. Risks increase with daily use. Advise patient that changes may not resolve after stopping the medication. Contact health care professional for concerns about skin changes.
- Inform patient that nausea may occur, especially after first dose, lasting 2 or more hr. May require antiemetics. Advise patient to notify health care professional if nausea is problematic.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Rep: Advise women of reproductive potential to use effective contraception during therapy and to notify health care professional if pregnancy is planned or expected or if breastfeeding. Discontinue bremelanotide if pregnancy is suspected. Encourage pregnant women exposed to bremelanotide to call the VYLEESI Pregnancy Exposure Registry at (877) 411-2510.
Improved sexual desire in premenopausal women. If no improvement in 8 wk, discontinue medication.