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Bremelanotide – Uses, Effects & Side Effects
Bremelanotide is a medication approved for treating hypoactive sexual desire disorder (HSDD) in premenopausal women. It acts on melanocortin receptors in the brain and is administered by injection.
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Bremelanotide is a medication approved for treating hypoactive sexual desire disorder (HSDD) in premenopausal women. It acts on melanocortin receptors in the brain and is administered by injection.
What is Bremelanotide?
Bremelanotide is a synthetic peptide drug approved for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women. It is marketed in the United States under the brand name Vyleesi and received FDA approval in 2019. It belongs to the pharmacological class of melanocortin receptor agonists.
Mechanism of Action
Bremelanotide acts as an agonist at melanocortin receptors, particularly the MC3R and MC4R subtypes located in the central nervous system. By activating these receptors in the brain, it modulates pathways involved in sexual arousal and desire. The precise neurobiological mechanism is not yet fully understood, but it is believed that dopaminergic signaling pathways play a key role in mediating the increase in sexual desire.
Indication
Bremelanotide is specifically approved for premenopausal women with acquired, generalized HSDD. HSDD is characterized by:
- Persistently low or absent sexual desire
- Significant personal distress caused by the lack of desire
- Exclusion of other medical or psychological causes, or relationship problems as the primary cause
It is not approved for use in men, postmenopausal women, or for sexual dysfunction caused by other factors such as medication side effects.
Administration and Dosage
Bremelanotide is administered as a subcutaneous injection (under the skin), typically into the abdomen or thigh. It is used on an as-needed basis, approximately 45 minutes before anticipated sexual activity. The recommended dose is 1.75 mg per administration. It should not be used more than once per day or more than eight times per month.
Side Effects
Like all medications, bremelanotide can cause side effects. The most common include:
- Nausea (occurring in more than 40% of patients and being the most frequent side effect)
- Flushing (redness and warmth in the face, neck, and chest)
- Headache
- Injection site reactions (pain, redness, bruising)
- Hyperpigmentation (darkening of the skin), particularly with prolonged use
- Transient increase in blood pressure following injection
Due to the potential for a transient increase in blood pressure, bremelanotide is contraindicated in patients with known cardiovascular disease.
Contraindications and Warnings
- Known cardiovascular disease (e.g., coronary artery disease, heart failure)
- Uncontrolled high blood pressure
- Pregnancy: bremelanotide may harm the fetus; effective contraception is required during use
- Caution in patients with darker skin tones due to the risk of permanent hyperpigmentation
References
- U.S. Food and Drug Administration (FDA): Vyleesi (bremelanotide) Prescribing Information (2019). Available at: www.fda.gov
- Clayton AH et al. - Bremelanotide for Female Sexual Dysfunctions in Premenopausal Women: A Randomized, Placebo-Controlled Dose-Finding Trial. Women's Health, 2016.
- Simon JA et al. - Efficacy and Safety of Bremelanotide for Hypoactive Sexual Desire Disorder. Obstetrics & Gynecology, 2019.
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