From the Guidelines
Bremelanotide should be used to treat acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women as a subcutaneous injection of 1.75 mg using a prefilled autoinjector pen, with dosing limited to at least 45 minutes before anticipated sexual activity, not more than one dose within 24 hours, and not more than eight doses per month. This recommendation is based on the most recent and highest quality study available, which evaluated the safety and efficacy of bremelanotide in premenopausal individuals with HSDD in two phase III, randomized, double-blind, placebo-controlled, multicenter clinical trials 1.
Administration and Dosage
- The injection should be given in the abdomen or thigh.
- Before injecting, clean the site with alcohol and allow it to dry.
- Remove the cap, place the pen firmly against your skin at a 90-degree angle, and press and hold the button until you hear a click.
- Hold for 5 seconds before removing.
Important Considerations
- Common side effects include nausea, flushing, headache, and injection site reactions.
- Bremelanotide works by activating melanocortin receptors in the brain, which play a role in sexual function.
- The medication should not be used in women with uncontrolled high blood pressure or cardiovascular disease.
- If you experience severe nausea or blood pressure changes, contact your healthcare provider immediately.
Clinical Context
The use of bremelanotide is considered an appropriate option for some survivors with HSDD, although it has not been studied in cancer survivors 1. Other options for survivors with low or lack of desire, libido, or intimacy include off-label use of bupropion and buspirone, as well as discussion of available drugs, topical vaginal therapies, vaginal dilators, and pelvic physical therapy 1.
From the FDA Drug Label
The FDA drug label does not answer the question.
From the Research
Administration of Bremelanotide
- Bremelanotide is administered as a subcutaneous injection, approximately 45 minutes prior to sexual activity 2.
- The recommended dosing is no more than 1 dose in 24 hours and no more than 8 doses per month 2.
- Individuals should discontinue use after 8 weeks without benefit 2.
Mechanism of Action
- Bremelanotide is a melanocortin receptor agonist that nonselectively activates several receptor subtypes, including subtype 4 (MC4R) 3.
- MC4R is predominantly expressed in the medial preoptic area (mPOA) of the hypothalamus in the brain and is important for female sexual function 3.
- Bremelanotide may affect female sexual desire by activating presynaptic MC4Rs on neurons in the mPOA of the hypothalamus, leading to increased release of dopamine, an excitatory neurotransmitter that increases sexual desire 3.
Safety and Efficacy
- Bremelanotide has been shown to be safe and effective in treating hypoactive sexual desire disorder (HSDD) in premenopausal women 2, 4.
- Common adverse effects include nausea, facial flushing, and headache 2.
- Bremelanotide has limited drug-drug interactions, including no clinically significant interactions with ethanol 2.