Description

Bremelanotide (or PT-141) is a compound which is developed for the treatment of female sexual dysfunction, hemorrhagic shock and reperfusion injury. It acts by activating the MC1R and MC4R melanocortin receptors, modulating inflammation and limiting ischemia.  Initially, the drug was studied for intranasal use for female sexual dysfunction treatment, but in 2008 development of the drug for such use was temporarily discontinued after reports of adverse side effects associated with increased blood pressure. As of March 2012, Palatin technologies was conducting a phase 2B study in human beings using subcutaneous injection of the drug, which the manufacturer claims will have a very small effect on blood pressure.

Bremelanotide was developed from the peptide hormone Melanotan 2, which has been investigated as a tanning agent without sun exposure. Melanotan 2 was shown in initial testing to induce sexual arousal and spontaneous erections in addition to tanning.  Bremelanotide has been shown in studies to be effective in the treatment of sexual dysfunction in both men (erectile dysfunction) and women (sexual arousal disorder. Unlike Viagra and other related drugs, Bremelanotide does not effect the vascular system, but increases desire directly through its effect on the nervous system.

Mechanism of action

Bremelanotide is an alpha-melanocyte-stimulating hormone (alpha-MSH) analogue that activates the melanocortin MC3-R and MC4-R receptors in the central nervous system. Due to its centrally mediated activity, Bremelanotide has potential for the treatment of erectile dysfunction, as well as for possible use in unmet medical needs associated with decreased sexual motivation and loss of libido.

PT-14 is powerful erection initiator with minimal side effects, a fast onset of action and a fairly long duration of action. Notably, recent phase II studies confirm that erectile responses are enhanced with sexual stimulation.  Due to its central mechanism of action, PT-141 can act independently or synergistically with PDE-5 inhibitors (Viagra, Cialis) and provide a useful alternative therapy for erectile dysfunction of both organic and psychogenic origin. A randomized, prospective, placebo-controlled trial compared ED treatment with Sildenafil . mg intranasal PT-with 141. The combined use of two drugs led to a significant increase in the time to increase the stiffness of the base (>60%) compared with taking only Sildenafil  during a 2,5 hour monitoring session. The drug combination was well tolerated with no significant increase in side effects compared to Sildenafil pot PT- alone.

Effects

• The erectogenic potential of PT-, its tolerability profile, and its ability to induce significant erections in patients who do not have an adequate response to a PDE inhibitor (Syslais, Viagra) suggest that PT- may provide an alternative treatment.
• Increase of sexual desire and erection

Side effects 

• Nausea
• Hot flush
• Headache

How to use 

• The first erection occurs in about 30 minutes. The peak concentration of the substance in the blood falls in 60 minutes after the injection and gradually decreases in 4 hours.
• Combination with other drugs
• For a better effect, it can be used with drugs such as Sildenafil and Tadafil.

How to prepare a solution

In order to prepare a solution for injection, you take a syringe already containing a diluent and inject it into a vial containing a lyophilized powder. Tilt the vial so that the needle touches the vial wall. Avoiding injecting the diluent directly into the lyophilized powder. The solvent should slowly flow down the wall of the bottle (do not fill everything at once and take your time). Once all the diluent has been added to the peptide vial, mix gently (but do not agitate or shake the vial) until the lyophilized powder has dissolved and you are left with a clear liquid. Now the drug is ready for use.

Never mix one peptide with another in the same syringe. This creates risks that fragile peptide molecules will be destroyed.

Usage 

• The injection can be subcutaneous, intramuscular depending on personal preference.

Storage 

• The resulting solution can be stored for approximately 21 days in a refrigerator at a temperature of 2-8 degree Celsius. The storage time increases if the solution was prepared using bacteriostatic water.