Bremelanotide

Bremelanotide Uses, Dosage, Side Effects, Food Interaction and all others data.

Bremelanotide is a 7 amino acid peptide used to treat hypoactive sexual desire disorder in premenopausal women. Bremelanotide does not interact with alcohol. The mechanism by which bremelanotide's action on receptors translates to a clinical effect is still unknown.

Bremelanotide was first described in the literature in 2003 when it was known by the investigational code PT-141. Since then it was investigated for its place in treating sexual dysfunction in men and women but is now only indicated for women. Other drugs used to treat female sexual dysfunction include flibanserin, estrogen, ospemifene, and prasterone.

Bremelanotide was granted FDA approval on 21 June 2019.

Bremelanotide
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Bremelanotide
Availability	Prescription only
Generic	Bremelanotide
Bremelanotide Other Names	Bremelanotida, Bremelanotide, Brémelanotide, Bremelanotidum
Related Drugs	Addyi, flibanserin, Vyleesi
Weight	1.75mg/0.3ml,
Type	Subcutaneous Solution, Subcutaneous
Formula	C₅₀H₆₈N₁₄O₁₀
Weight	Average: 1025.182 Monoisotopic: 1024.524284446
Protein binding	Bremelanotide is 21% protein bound in serum.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Bremelanotide is indicated to treat premenopausal women with hypoactive sexual desire disorder that is not due to a medical or psychiatric condition, problems with the relationship, or the effects of a medication or drug.

Bremelanotide is also used to associated treatment for these conditions: Hypoactive Sexual Desire Disorder (HSDD)

How Bremelanotide works

Bremelanotide is an agonist of many melanocortin receptors which in order of potency are MC1R, MC4R, MC3R, MC5R, and MC2R. The mechanism by which agonism of these receptors translates to an improvement in hypoactive sexual desire disorder is currently unknown, however MC4R receptors are present in many areas of the central nervous system. MC3R and MC4R are found in the hypothalamus and are involved in food intake and energy homeostasis.

One theory is that bremelanotide stimulates dopamine in the medial preoptic area, which is involved in the sexual behaviour of a number of organisms.

Toxicity

Currently there are no reports of overdoses of bremelanotide. Patients taking higher doses are more likely to experience nausea, focal hyperpigmentation, and increases in blood pressure. In the event of an overdose, supportive measures should be used to address the associated symptoms.

Food Interaction

No interactions found.

[Moderate] GENERALLY AVOID: Bremelanotide may slow gastric emptying and reduce the rate and extent of absorption of concomitantly administered oral medications.

In clinical pharmacology studies, bremelanotide 1.75 mg given subcutaneously did not affect the absorption of most of the tested oral medications to any clinically relevant degree, including amlodipine, bupropion, celecoxib, ethinyl estradiol, furosemide, hydrochlorothiazide, lisinopril, losartan, metformin, metoprolol, norethindrone, phentermine, pseudoephedrine, sertraline, and venlafaxine.

However, naltrexone peak plasma concentration (Cmax) and systemic exposure (AUC) decreased by approximately 60% and 40%, respectively, relative to administration alone.

Indomethacin Cmax and AUC decreased by approximately 35% and 20%, respectively, relative to administration alone.

MANAGEMENT: Patients should avoid the use of bremelanotide when taking concomitant oral medications that are dependent on threshold concentrations for efficacy (e.g., antibiotics).

Patients should also consider avoiding bremelanotide when a quick onset of therapeutic effect is desired for concomitant oral medications (e.g., drugs for pain relief such as indomethacin).

Bremelanotide Hypertension interaction

[Major] Bremelanotide is contraindicated in patients who have uncontrolled hypertension or known cardiovascular disease, as it transiently increases blood pressure and reduces heart rate after each dose.

Before initiating bremelanotide, and periodically during treatment, consider the patient's cardiovascular risk and ensure blood pressure is well-controlled.