Vyleesi (bremelanotide) is a medication used to treat hypoactive sexual desire disorder (HSDD) in premenopausal women. HSDD is defined as low sexual desire that causes marked distress or interpersonal difficulties. Acquired HSDD refers to HSDD that develops in a patient who previously had no problems with sexual desire. It is not intended for those whose low sex drive is caused by medical or mental health problems, relationship issues, or medications.
How Vyleesi Works: The Mechanism of Action
Vyleesi may work by activating specific receptors in your brain, including those that affect mood and sexual desire. Bremelanotide Acetate works by activating melanocortin receptors in the central nervous system, primarily the melanocortin 4 receptor (MC4R). The melanocortin system is known to play a critical role in a variety of physiological processes, including energy homeostasis, inflammation, and sexual function. By binding to and activating MC4R, Bremelanotide Acetate modulates neuronal pathways that influence sexual desire and arousal.
The exact mechanism by which Bremelanotide Acetate enhances sexual desire is not entirely understood. However, it is believed that activation of MC4R leads to increased production and release of neurotransmitters and neuropeptides that are involved in the regulation of mood, arousal, and reward. This, in turn, may enhance sexual motivation and interest, addressing the core symptoms of HSDD. Unlike other treatments for sexual dysfunction that may focus on hormonal pathways or direct vascular effects, Bremelanotide Acetate's action on central nervous system receptors represents a unique therapeutic approach.
Regulation of central melanocortin signaling may enhance sexual desire. Bremelanotide is a cyclic heptapeptide lactam analogue of α-melanocyte-stimulating hormone (α-MSH). It has the amino acid sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH, and is also known as cyclo-Ac-[Nle4,Asp5,D-Phe7,Lys10]α-MSH-(4-10) (a substitutional name). Studies in the early 1960s showed that administration of α-MSH caused sexual arousal in rats, sparking interest in α-MSH. In the 1980s, scientists at University of Arizona began developing α-MSH and analogs as potential sunless tanning agents. Very early in the process one of the scientists, Mac Hadley, was conducting self-experiments with melanotan II. The drug was then reformulated to be delivered by injection and trials continued in FSD.
Dosage and Administration
Vyleesi is supplied as a 1.75 mg/0.3 mL solution for injection in an autoinjector. Bremelanotide Acetate is administered via subcutaneous injection, typically using an auto-injector device for ease of use. The drug is designed to be self-administered on an as-needed basis, approximately 45 minutes before anticipated sexual activity. The recommended dosage is 1.75 mg per injection, and it is advised not to exceed one dose within 24 hours or more than eight doses per month.
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The onset of action for Bremelanotide Acetate is relatively rapid, with effects typically beginning within 30 to 45 minutes of administration. This allows for a degree of spontaneity in sexual activity, unlike some other treatments that require more advanced planning. Patients are instructed to inject the drug into the abdomen or thigh, rotating injection sites to avoid irritation. Proper training on the use of the auto-injector device is provided by healthcare professionals to ensure correct administration.
Side Effects
While Bremelanotide Acetate offers a promising option for treating HSDD, it is associated with several potential side effects. The most common side effects of Vyleesi are listed below. Tell your health care provider if you have any of these side effects that bother you:
- Nausea (see below)
- Flushing or hot flashes
- Pain, itching, swelling, or bruising near the injection site
- Headache
- Vomiting
- Cough
- Tiredness
- Tingling
- Dizziness
- Stuffy nose
There may be other side effects of Vyleesi that are not listed here. Contact your health care provider if you think you are having a side effect of a medicine.
Nausea was very common and occurred after a median time of 30 minutes for a median duration of 2.4 hours. Nausea was reported in 40% of patients, often within an hour of dosing, and 13% of those patients reported having nausea bad enough to necessitate anti-nausea medications. Nausea improves for most patients with the second dose. VYLEESI may slow gastric emptying and impact absorption of concomitantly administered oral medications.
Serious Side Effects:
While less common, the most serious side effects of Vyleesi are described below, along with what to do if they happen.
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- Severe Allergic Reactions: Vyleesi may cause allergic reactions, which can be serious. Stop using Vyleesi and get help right away if you have any of the following symptoms of a serious allergic reaction.
- Breathing problems or wheezing
- Racing heart
- Fever or general ill feeling
- Swollen lymph nodes
- Swelling of the face, lips, mouth, tongue, or throat
- Trouble swallowing or throat tightness
- Itching, skin rash, or pale red bumps on the skin called hives
- Nausea or vomiting
- Dizziness, feeling lightheaded, or fainting
- Stomach cramps
- Joint pain
- Blood Pressure and Heart Rate Effects: VYLEESI transiently increases blood pressure and reduces heart rate after each dose. Advise patients that these changes usually resolve within 12 hours. VYLEESI is not recommended in patients at high risk for cardiovascular disease. Consider the patient’s cardiovascular risk before initiating VYLEESI and periodically during treatment and ensure blood pressure is well-controlled. To minimize the risk of more pronounced blood pressure effects, patients should not take more than one VYLEESI dose within 24 hours.After each dose of Vyleesi, your blood pressure may go up and your heart rate may slow down. These changes are usually small and go away within 12 hours, but they may cause serious problems in people with heart disease. Using Vyleesi more often than prescribed may increase the risk of these problems. If you measure your blood pressure and the top number (systolic) is 180 or higher or the bottom number (diastolic) is 120 or higher, get medical attention right away. Tell your health care provider right away if you have any of the following symptoms:
- Chest pain
- Feeling lightheaded or fainting
- Confusion
- Feeling weak or unusually tired
- Slow heartbeat or feeling of skipped heartbeats
- Shortness of breath
- Focal Hyperpigmentation: Vyleesi may cause darkening (hyperpigmentation) of your face, breasts, and gums. The risk may be higher if you use Vyleesi every day and if you have darker skin. Skin darkening may not go away after stopping Vyleesi. Tell your health care provider if you have skin or gum darkening that bothers you.Reported by 1% of patients who received up to 8 doses per month, including involvement of the face, gingiva and breasts. Patients are at higher risk of developing focal hyperpigmentation if they have darker skin and with daily dosing. Resolution of the focal hyperpigmentation was not confirmed in all patients after discontinuation of VYLEESI.
Contraindications and Precautions
Who should not use Vyleesi? Allergies to Ingredients. People who are allergic to any of the following should not use Vyleesi:
- Bremelanotide
- Vyleesi
- Any of the ingredients in the specific product dispensed
Your pharmacist can tell you all of the ingredients in Vyleesi.
- Uncontrolled High Blood Pressure: Vyleesi should not be used by people who have high blood pressure that is not controlled. Using Vyleesi could worsen this condition.
- Heart or Blood Vessel Disease: Vyleesi should not be used by people with conditions affecting the heart and blood vessels (cardiovascular disease). This includes people with coronary artery disease, peripheral artery disease, or vascular disease. Using Vyleesi could worsen these problems.
What should I know about Vyleesi before using it?
- Do not use Vyleesi unless it has been prescribed to you by a health care provider. Use it as prescribed. Do not use more than one dose within 24 hours or more than 8 doses within one month.
- Do not share Vyleesi with other people, even if they have the same condition as you. It may harm them.
- Keep Vyleesi out of the reach of children.
- Vyleesi is injected under the skin (subcutaneously). Read and follow the instructions that come with the medicine and make sure that you or a caregiver understands how to properly prepare, use, and throw away Vyleesi. If you have any questions, talk to your health care provider.
- Keep all appointments with your health care provider, including for blood pressure checks, before starting Vyleesi and during treatment. This will help your health care provider see if it is safe for you to use Vyleesi.
- Tell your health care provider if your symptoms do not improve after eight weeks of using Vyleesi.
- Advise patients to discontinue VYLEESI if pregnancy is suspected. Advise patients to use effective contraception while taking VYLEESI. A pregnancy exposure registry monitors pregnancy outcomes in women exposed to VYLEESI during pregnancy.
What should I tell my health care provider before using Vyleesi?
Tell your health care provider about all of your health conditions and any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. This will help them determine if Vyleesi is right for you.
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In particular, make sure that you discuss any of the following:
- Risk Factors for Heart Disease: Vyleesi is not recommended for people at high risk for heart disease. Examples of risk factors include smoking, high blood pressure, diabetes, and obesity. Tell your health care provider about all of your health conditions and any family history of heart or blood vessel disease. Your health care provider can help decide if Vyleesi is safe for you.
- Other Current and Past Health Conditions: Tell your health care provider if you have any of the following:
- Heart problems
- Kidney problems
- Liver problems
- Other Medicines and Supplements: Vyleesi may interact with other medicines and supplements. Before using Vyleesi, tell your health care provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using.
- Pregnancy: It is not known if or how Vyleesi could affect pregnancy or harm a fetus. If you can become pregnant, you should use effective birth control while using Vyleesi. If you become pregnant or think you might be pregnant, stop using Vyleesi and contact your health care provider right away. This registry collects safety information about the use of Vyleesi during pregnancy.
- Breastfeeding: It is not known if Vyleesi passes into breast milk. Tell your health care provider if you are breastfeeding or plan to breastfeed.
Drug Interactions
Does Vyleesi interact with foods or drinks?
There are no known interactions between Vyleesi and foods or drinks.
It is unknown if drinking alcohol will affect Vyleesi. The risk of certain side effects, such as dizziness, may increase if you drink alcohol while using Vyleesi. Bremelanotide does not meaningfully interact with alcohol, unlike flibanserin (for which the interaction with alcohol is a major barrier to its use).
Does Vyleesi interact with other medicines (drug interactions)?
Always tell your health care provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using.
In particular, make sure that you discuss if you are using any of the following before using Vyleesi:
- An antibiotic that is taken by mouth, which is a medicine used for bacterial infections
- Naltrexone taken by mouth, which is a medicine that may be used to treat alcohol use disorder or opioid use disorder. VYLEESI may significantly decrease the systemic exposure of orally-administered naltrexone; avoid use with orally administered naltrexone-containing products intended to treat alcohol or opioid addiction.
- Indomethacin, which is a medicine used for pain or swelling
Vyleesi may affect the absorption of other medicines that are taken by mouth. Tell your health care provider about all medicines that you take or have recently taken.
This may not be a complete list of medicines that can interact with Vyleesi. Always check with your health care provider. Does interact with other drugs you are taking? You should not use more than one dose in 24 hours. Use it as recommended by your health care provider. Do not use double or extra doses.
Bremelanotide Acetate can interact with several other medications, potentially altering their effectiveness or increasing the risk of adverse effects. One notable interaction is with medications that affect blood pressure, such as antihypertensives or vasodilators. Given that Bremelanotide Acetate can cause an increase in blood pressure, concurrent use with these drugs requires careful monitoring and possible dose adjustments.
Additionally, Bremelanotide Acetate may interact with medications metabolized by the cytochrome P450 enzyme system, particularly CYP3A4. This includes a wide range of drugs such as certain antifungals, antibiotics, and antivirals. These interactions could either increase the levels of Bremelanotide Acetate, raising the risk of side effects, or decrease its efficacy.
Other drugs that may influence the effectiveness of Bremelanotide Acetate include central nervous system depressants and stimulants, as they may affect the neural pathways involved in sexual desire. Patients should inform their healthcare provider of all medications and supplements they are taking to avoid potential interactions and ensure the safe use of Bremelanotide Acetate.
Vyleesi vs. Addyi
Vyleesi (bremelanotide) and Addyi (flibanserin) are drugs used to treat hypoactive sexual desire disorder (HSDD) in premenopausal women. Vyleesi is self-administered via subcutaneous injection under the skin of the abdomen or thigh using a single use autoinjector pen. Addyi is an oral tablet taken once daily, every day, only at bedtime. Discontinue treatment after 8 weeks if there is no improvement in symptoms.
Based on the manufacturer's data, there does not appear to be an interaction between Vyleesi and alcohol. Vyleesi however may significantly decrease the blood levels of naltrexone in patients who take a naltrexone-containing medication by mouth to treat alcohol or opioid dependence. When Addyi was first approved, patients were warned to completely abstain from drinking alcohol due to the increased risk of severe low blood pressure and fainting. In 2019, the warnings were revised to clarify that while there was still concern about consuming alcohol close in time to taking Addyi, it does not have to be avoided completely.
In clinical trials, about 10 percent more Addyi-treated patients than placebo-treated patients reported meaningful improvements in satisfying sexual events, sexual desire or distress. The most common side effects (incidence > 4%) reported during clinical trials were nausea, flushing, injection site reactions, headache, and vomiting. Nausea was reported in 40% of patients, often within an hour of dosing, and 13% of those patients reported having nausea bad enough to necessitate anti-nausea medications. fatigue, insomnia, and dry mouth.