Bremelanotide Injection - Uses, Contraindications, and Side Effects.

Introduction

Hypoactive sexual desire disorder (HSDD) is the absence or deficiency of sexual desires or fantasies which results in significant distress and interpersonal difficulty. Females with this condition not only show a lack of motivation for sexual acts but also avoid the situations that can lead to such activities. Bremelanotide injection is used in the treatment of HSDD in females who have not experienced menopause (end of menstrual periods) and who have previously not had any problems with sexual desire. It must not be used by men and by women who have already attained menopause and also not for people who want to improve their sexual performance.

What Is Bremelanotide Injection?

Bremelanotide injection is a solution available for subcutaneous injection (under the skin), administered at least 45 minutes before sexual activity in women with HSDD. It belongs to a class of medications called melanocortin receptor agonists. It is recommended for females with generalized and acquired hypoactive sexual desire disorder. It must not be used by women with co-existing psychiatric or medical conditions, relationship problems, or low sexual desire due to side effects of certain medications. Bremelanotide injection was approved by the United States Food and Drug Administration (USFDA) in 2019.

How Does Bremelanotide Injection Work?

Neurotransmitters such as melanocortin and dopamine are responsible for stimulating sexual desire and attention, while oxytocin and norepinephrine stimulate sexual arousal. Hypoactive sexual desire disorder in women is associated with an imbalance of neurotransmitters, causing abnormal sexual responses. Bremelanotide mainly works by non-selectively activating melanocortin receptors in the brain, stimulating dopamine release, and modifying certain pathways involved in sexual responses. Stimulating these receptors may sometimes cause an increase in blood pressure and a decrease in heart rate.

How Effective Is Bremelanotide Injection?

Bremelanotide injection is moderately safe and usually well-tolerated by most women. The most common adverse effect reported during the clinical studies was nausea (around 40 percent). The data from clinical trials showed a significant change in different validated questionnaires, and the overall clinical benefit appeared modest. Clinical trials involved premenopausal females (aged between 19 and 56 years) with generalized and acquired HSDD of at least six months. Participants were instructed to administer a Bremelanotide injection approximately 45 minutes before sexual activity and were also required to use an effective form of contraception. Most patients used the drug two or three times a month but not more than once a week. The result was that the patients reported an improvement in sexual desire and also in the level of distress associated with low sexual desire.

How Is Bremelanotide Injection Administered?

• The recommended dose of Bremelanotide injection is 1.75 mg/0.3 mL, which is administered subcutaneously in front of the thigh or into the skin of the abdomen (stomach area) approximately 45 minutes before sexual activity. It must be avoided within the two-inch area around the belly button.

• It can be self-administered using a prefilled, single-dose auto-injector pen (syringe). Before injecting, the solution must be checked for any clogging or discoloration. It must be discarded if the solution appears discolored or cloudy or if visible particles are observed.

• More than one dose must not be administered within 24 hours as it can increase the risk of blood pressure variations. Administration of more than eight doses a month is not recommended.

• If the patient does not experience any improvement in the symptoms after eight weeks, the treatment can be discontinued.

What Are the Contraindications of Bremelanotide Injection?

• Bremelanotide injection is contraindicated in patients with uncontrolled hypertension or with a history of cardiovascular diseases.

• Pregnant women must not use it as the drug may have the potential to cause harm to the fetus. Hence, females must use effective contraception during the treatment with Bremelanotide injection or discontinue the treatment if pregnancy is suspected.

• No information is available regarding the presence of Bremelanotide in human milk or milk production or its effects on the breastfed infant or the mother. Therefore, the benefits of breastmilk to the infant and any potential adverse effects associated with Bremelanotide injection must be considered before using the drug.

What Are the Side Effects of Bremelanotide Injection?

The possible serious side effects of Bremelanotide injection include;

• Nausea commonly occurs following the first dose of Bremelanotide injection but can also occur in the subsequent doses. It usually resolves in about two hours. However, if the patient experiences severe nausea, a doctor can be consulted for a prescription of anti-nausea medicines.

• A temporary increase in blood pressure and a decrease in heart rate can occur, which usually resolves within 12 hours after administration. There can be an increased risk of cardiovascular problems if Bremelanotide injection is used more often.

• Darkening of skin can be noticed in certain parts of the body, such as the face, breasts, and gums. It is mostly increased in people with dark skin and in people who frequently use Bremelanotide injections.

Some of the common side effects include:

• Nasal congestion.

• Cough.

• Vomiting.

• Injection site reactions.

• Flushing or hot flushes.

• Tingling sensation.

What Are the Precautions to Be Followed Before Using Bremelanotide Injection?

• Before starting the treatment, the patient must inform the doctor if they are allergic to Bremelanotide, its components, or any other medications.

• Patients must tell the doctor if they have or previously experienced high blood pressure, heart problems, or any other diseases or medical conditions before starting the treatment with Bremelanotide.

• Female patients must inform the healthcare provider if they are pregnant, planning to become pregnant, or breastfeeding before taking Bremelanotide.

• Bremelanotide injection can cause darkening of the skin in some regions of the body, which may not go away. Hence, the doctor must consult about skin concerns before using the medication.

• The patient must inform the doctor if taking medications such as Indomethacin, Naltrexone, antibiotics, vitamins, nutritional supplements, over-the-counter (OTC) drugs, or any other medicines before taking Bremelanotide injection.

Conclusion

Bremelanotide injection is a prescription medicine used in the treatment of hypoactive sexual desire disorder in premenopausal women. It is associated with nausea and a temporary increase in blood pressure. However, it is a moderately safe and well-tolerated drug, but must not be used by men, post-menopausal women, or to improve sexual performance. The drug can be self-administered. However, a healthcare professional must be consulted to know the proper technique and precautions before using Bremelanotide injection.