Bremelanotidum
Bremelanotidum Uses, Dosage, Side Effects, Food Interaction and all others data.
Bremelanotidum is a 7 amino acid peptide used to treat hypoactive sexual desire disorder in premenopausal women. Bremelanotidum does not interact with alcohol. The mechanism by which bremelanotide's action on receptors translates to a clinical effect is still unknown.
Bremelanotidum 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.
Bremelanotidum was granted FDA approval on 21 June 2019.
| Trade Name | Bremelanotidum |
| Availability | Prescription only |
| Generic | Bremelanotide |
| Bremelanotide Other Names | Bremelanotida, Bremelanotide, Brémelanotide, Bremelanotidum |
| Related Drugs | Addyi, flibanserin, Vyleesi |
| Type | |
| 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 | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Bremelanotidum 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.
Bremelanotidum is also used to associated treatment for these conditions: Hypoactive Sexual Desire Disorder (HSDD)
How Bremelanotidum works
Bremelanotidum 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: Bremelanotidum 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).
Bremelanotidum Hypertension interaction
[Major] Bremelanotidum 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.
Bremelanotidum Disease Interaction
Major: hypertension/CV diseaseModerate: severe hepatic impairment, severe renal impairment
Volume of Distribution
The mean volume of distribution of bremelanotide is 25.0±5.8L.
Elimination Route
Bremelanotidum has a Tmax or 1.0 hour (0.5-1.0 hours) and is 100% bioavailable. The Cmax is 72.8ng/mL and the AUC is 276hr*ng/mL.
Half Life
The half life of bremelanotide is 2.7 hours (1.9-4.0 hours).
Clearance
The mean clearance of bremelanotide is 6.5±1.0L/hr.
Elimination Route
64.8% of a radiolabelled dose is excreted in the urine and 22.8% of the dose is recovered in the feces.
Innovators Monograph
You find simplified version here Bremelanotidum
