Bremelanotide, sold under the brand name Vyleesi, is a medication used to treat low sexual desire in women.
The medication is a peptide and acts by activating the melanocortin receptors.
Specifically it is used for low sexual desire which occurs before menopause and is not due to medical problems, psychiatric problems, or problems within the relationship.
It is given by subcutaneous injection just under the skin of the thigh or abdomen.
Protein binding 21%
Metabolism Hydrolysis of peptide bonds
Elimination half-life 2.7 hours
Excretion Urine: 64.8%, Feces: 22.8%
Common side effects include nausea, pain at the site of injection, and headache, temporary increase in blood pressure and decrease in heart rate after each dose, and darkening of the gums, face, and breasts.
The use of anti-nausea medications prior to administration of bremelanotide may help to reduce the nausea.
Other side effects may include flushing (20.3%), injection site reactions (13.2%), headache (11.3%), vomiting (4.8%), cough (3.3%), fatigue (3.2%), hot flashes (2.7%), paresthesia (2.6%), dizziness (2.2%), and nasal congestion (2.1%).
Bremelanotide is used for the treatment of generalized hypoactive sexual desire disorder that occurs in premenopausal women.
It is only recommended in those who have the condition without an underlying cause, such as medical, psychiatric, or relationship problems.
It used at least 45 minutes before anticipated sexual activity.
Only one dose per 24 hours or no more than eight doses per month is recommended.
It should be stopped after eight weeks if there is no improvement in sexual desire and associated distress.
There is generally a transient increase in systolic blood pressure by 6 mmHg, and diastolic blood pressure by 3 mmHg.
The drug is considered contraindicated in people with uncontrolled high blood pressure or cardiovascular disease.
As long as bremelanotide is not used more than once in one day, it is not expected to cause more severe increases in blood pressure.
Discoloration of the skin (hyperpigmentation), may occur—especially if bremelanotide is used more than eight times in one month.
Hyperpigmentation may not resolve upon stopping use of bremelanotide, and may occur on the face, gums, or breasts.
Obese women reduce their calorie intake and lose weight with this drug.
By slowing gastric motility, it reduces the oral absorption of certain medications, such as naltrexone and indomethacin.
Bremelanotide is a non-selective agonist of the melanocortin receptors, MC1 through MC5, but acting primarily as an MC3 and MC4 receptor agonist.
The bioavailability of bremelanotide with subcutaneous injection is about 100%.
Following a subcutaneous injection of bremelanotide, maximal levels occur after about one hour, with a range of 0.5 to 1.0 hours.
The plasma protein binding of bremelanotide is 21%, and is metabolized via hydrolysis of its peptide bonds.
The elimination half-life of bremelanotide is 2.7 hours, with a range of 1.9 to 4.0 hours.
Bremelanotide is excreted 64.8% in urine and 22.8% in feces.
Bremelanotide is a cyclic heptapeptide lactam analogue of α-melanocyte-stimulating hormone (α-MSH)11] It has the amino acid sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH,[16] and is also known as cyclo-Ac-[Nle4,Asp5,D-Phe7,Lys10]α-MSH-(4-10) (a substitutional name).
Bremelanotide is an active metabolite of melanotan II that lacks the C-terminal amide group.