bremelanotide

Action and Spectrum

Actions and spectrum: 

bremelanotide is a medication used for the treat disorder of hypoactive sexual desire in premenopausal women. It is an agonist of melanocortin receptors, specifically targeting the melanocortin 4 receptor (MC4R) in the brain. bremelanotide works by increasing sexual desire and arousal in women.

The mechanism of action is unkown, but it is believed to enhance the release of certain neurotransmitters involved in sexual response. The spectrum of bremelanotide is limited to its approved use for HSDD in premenopausal women. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Cough (3.3%) 

Hot flush (2.7%) 

Dizziness (2.2%) 

Vomiting (4.8%) 

Fatigue (3.2%) 

Paresthesia (2.6%) 

Nasal congestion (2.1%)  

>10% 

Flushing (20%) 

Headache (11.3%) 

Nausea (40%) 

reactions at injection site (13.2%)  

<2% 

Diarrhea 

Arthralgia 

Restless leg syndrome 

Increase in creatine phosphokinase 

Pain in extremities 

Flushing 

Upper abdominal pain 

Myalgia 

Pain 

Rhinorrhea 

increased Blood pressure 

Hyperpigmentation of skin  

<1% 

Flu symptoms 

Black Box Warning

Black Box Warning: 

There is no black box warning associated with bremelanotide. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: bremelanotide is contraindicated in individuals with hypersensitivity or allergic reaction to the drug or any of its components. 
• Uncontrolled Hypertension: bremelanotide is contraindicated in individuals with uncontrolled hypertension (high blood pressure) because it can further increase blood pressure. 
• Cardiovascular Disease: bremelanotide is contraindicated in individuals with cardiovascular disease, including heart attack, stroke, or other serious heart problems. 
• Use with Nitrates or Nitric Oxide Donors: bremelanotide should not be used concurrently with nitrates or nitric oxide donors, as it can potentiate the vasodilatory effects and increase the risk of severe hypotension. 
• Pregnancy: bremelanotide is contraindicated during pregnancy due to potential risks to the developing fetus.

Caution: 

• Blood Pressure Changes: bremelanotide can cause an increase in blood pressure, so caution should be exercised in individuals with pre-existing hypertension or a history of cardiovascular disease.  
• Cardiovascular Conditions: bremelanotide should be used with caution in individuals with cardiovascular conditions such as heart disease, stroke, or arrhythmias, as it may increase the risk of cardiovascular events. 
• Nausea and Vomiting: bremelanotide commonly causes nausea and vomiting, particularly in the first few hours after administration.  
• Interaction with Alcohol: Drinking alcohol while using bremelanotide may enhance the risk of side effects such as lightheadedness, dizziness, and fainting. 
• Use in Specific Populations: bremelanotide should be used under caution in individuals with liver or kidney impairment, as the effects of the drug may be prolonged.

Comorbidities: 

• Cardiovascular Disease: Individuals with cardiovascular disease, such as heart disease, stroke, or blood clotting disorders, may require caution when using bremelanotide.  
• Hypertension: bremelanotide can increase blood pressure, so individuals with uncontrolled or severe hypertension should use caution when using this medication.  
• Liver or Kidney Impairment: bremelanotide is primarily metabolized by liver and excreted through kidneys. 
• Bleeding Disorders: bremelanotide may have anticoagulant properties, and caution is advised in individuals with bleeding disorders or those taking medications that increase the risk of bleeding. 
• Hormonal Disorders: bremelanotide may interact with hormonal medications or therapies, so individuals with hormonal disorders should use caution. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

bremelanotide, also known as PT-141, is a synthetic peptide analog of the naturally occurring hormone alpha-melanocyte stimulating hormone (α-MSH). It acts as an agonist of melanocortin receptors, particularly the MC4 receptor subtype, in the central nervous system. 

The exact mechanism of action of bremelanotide in treating hypoactive sexual desire disorder (HSDD) is not fully understood. However, it is believed to increase sexual desire and arousal by activating melanocortin receptors in the brain, leading to the release of neurotransmitters involved in sexual function and behavior.  

Pharmacodynamics: 

The pharmacodynamics of bremelanotide (PT-141) involve its interaction with melanocortin receptors, particularly the MC4 receptor subtype, in the central nervous system. bremelanotide acts as an agonist of these receptors, leading to the activation of various intracellular signaling pathways. 

By binding to MC4 receptors, bremelanotide stimulates the production and release of cyclic adenosine monophosphate (cAMP) in neurons. This results in the activation of signaling pathways involved in sexual function and behavior. 

bremelanotide is thought to increase sexual desire and arousal by modulating the activity of neurotransmitters involved in these processes, including dopamine, serotonin, and norepinephrine.  

Pharmacokinetics: 

Absorption 

bremelanotide is administered subcutaneously (under the skin) and is rapidly absorbed into the bloodstream. Peak plasma concentrations are typically reached within 30 minutes to 3 hours after administration. 

Distribution 

bremelanotide has a moderate distribution volume, indicating that it distributes evenly throughout the body. It is primarily bound to plasma proteins, such as albumin. 

Metabolism 

bremelanotide undergoes metabolism primarily in the liver. It is metabolized by enzymes, such as cytochrome P450 (CYP) enzymes, into smaller inactive metabolites. 

Elimination and excretion 

The metabolites of bremelanotide are primarily excreted through the kidneys. The elimination half-life of bremelanotide is short, ranging from 2 to 4 hours. 

Adminstartion

Administration: 

bremelanotide is typically administered as a subcutaneous injection using a syringe and needle. The injection is usually given in the abdomen or thigh area.

The exact dosing and administration instructions for bremelanotide may vary depending on the specific indication and the prescribing healthcare professional’s guidance. 

It is essential to receive proper training from a healthcare professional on how to correctly administer bremelanotide if you are self-administering the injections. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: bremelanotide 

Pronounced: (bree-mel-uh-noh-tide)  

Why do we use bremelanotide? 

bremelanotide, also known by its brand name Vyleesi, is used for the treat disorder of hypoactive sexual desire in premenopausal women. HSDD is characterized by a persistent or absence of sexual desire for sexual activity that causes distress or interpersonal difficulties. bremelanotide is specifically indicated for use in women who have not at menopause and who have experienced a persistent lack of sexual desire that is not because of other factors such as a medical or psychiatric condition.