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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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Things worth knowing about "Bremelanotide"

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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