Vyleesi (Bremelanotide): Uses, Dosage, Side Effects, & More

What Is Vyleesi?

Vyleesi is a melanocortin receptor agonist and is prescribed to premenopausal women diagnosed with hypoactive sexual desire disorder (HSDD). Females with HSDD feel a persistent and distressing lack of sexual desire that is not caused by any coexisting medical or psychological conditions, relationship issues, or the effects of medication or substances. This condition can lead to emotional distress and place strain on personal relationships.

Vyleesi is an FDA-approved medication for females with HSDD. FDA approval, provided by the U.S. Food and Drug Administration (FDA), means that a particular drug, medical device, biological product, or treatment has completed a thorough evaluation process and has been confirmed as safe and efficacious for its intended purpose.¹ Vyleesi comes in the form of a self-administered injection pen. Most patients take 2-3 doses per month, no more often than once a week.¹

How Does Vyleesi Work?

Vyleesi is a medication that activates specific receptors in the body. It affects and stimulates receptors in the body called MC4R and MC1R. MC4R is a receptor found all over the brain, and MC1R is a receptor found in cells located in the skin, eye, ear, vagina, bones, brain, spinal cord, and heart. Activation of these receptors may influence pathways related to sexual desire and arousal. However, researchers don’t know the exact mechanism of how this medication works to improve this HSDD.¹

How Does Vyleesi Make You Feel?

In research studies, women who have HSDD taking Vyleesi had significant increases in sexual desire and substantial reductions in distress related to low sexual desire. Along with increased desire, patients may experience improved sexual satisfaction and a more enjoyable overall sexual experience. However, individual responses to Vyleesi can vary widely. Some patients may have a very positive response, while others may not notice significant changes in their sexual desire or may experience side effects that influence their overall experience.²

How Long Does Vyleesi Last?

The half-life of Vyleesi in the elimination terminal is about 2.7 hours (range is 1.9 to 4 hours), meaning that Vyleesi can stay in your body for about 10-20 hours after the dose is injected. This can also be influenced by various factors, such as an individual’s metabolism, general health, and unique reaction to Vyleesi.¹

What Is the Difference Between Addyi & Vyleesi?

Addyi and Vyleesi are medications designed to address sexual health concerns in women, specifically targeting HSDD. However, they differ in their mechanisms of action, how they are administered, and their usage. Addyi is taken orally as a daily medication, and it is usually recommended to be taken at bedtime to minimize the risk of side effects during waking hours. Addyi is intended for daily use and may require several weeks to achieve its full effects. Addyi is not meant for occasional use but is rather a chronic treatment.

In contrast, Vyleesi is administered through an injection, typically in the abdomen or thigh, at least 45 minutes before anticipated sexual activity. Vyleesi is taken as needed, meaning you use it specifically before engaging in sexual activity. Unlike Addyi, Vyleesi does not require daily usage.¹

What Is Vyleesi Used to Treat?

Vyleesi is a melanocortin receptor agonist prescribed to premenopausal women who are diagnosed with hypoactive sexual desire disorder (HSDD). HSDD is characterized by an enduring and distressing absence of sexual desire, and this condition is caused by concurrent medical or psychological issues, relationship difficulties, or the effects of medications or substances. HSDD can lead to emotional distress and place strain on personal relationships.

Vyleesi is FDA-approved for HSDD, confirming its safety and effectiveness for its intended purpose, treating female HSDD patients. Vylessi doesn’t have any off-label usages at this time. An off-label use of a medication is a use that is not FDA-approved. Prescribers can decide to use a medication off-label because, in their professional judgment, they believe it may offer a benefit to someone.¹

How Effective is Vyleesi?

Two research trials were separately conducted to look at the safety and effectiveness of Vyleesi (injected under the skin) at a dose of 1.75 mg on an as-needed basis. Both studies confirmed that Vyleesi substantially enhanced sexual desire and alleviated related distress in premenopausal women diagnosed with hypoactive sexual desire disorder. The safety profile of the medication was favorable and the majority of side effects that emerged during treatment were associated with being able to tolerate Vyleesi, and most of these side effects were of mild or moderate intensity.^{1, 2, 3}

Vyleesi Warnings & Precautions

While it may be uncommon, certain individuals may experience severe and potentially life-threatening side effects when using Vyleesi. Seek immediate medical assistance if you or someone you know encounters any of the following signs or symptoms: allergic response, severe fever, wheezing, chest or throat tightness, difficulty breathing, symptoms of high blood pressure, or slow heart rate.¹

Avoid taking Vyleesi if you:¹

• Are diagnosed with “a heart condition or high blood pressure”: Patients who have heart conditions or symptoms of high blood pressure (e.g. severe headache, dizziness, fainting, or changes in vision) should ask their doctor or pharmacist before taking Vyleesi.
• Have an allergic reaction: Symptoms of an allergic response to Vyleesi include skin rash, hives, itching, reddened, swollen, blistered, or peeling skin.
• Have a history of “slow heartbeat”: Patients with a history of slow heartbeat should ask their doctor or pharmacist before taking Vyleesi.
• Are breastfeeding or pregnant: This medication has the potential to harm a developing fetus. If one is of childbearing age, it’s essential to use a form of birth control while using this medication. In the event of pregnancy, contact your doctor or pharmacist immediately. Be sure to inform your healthcare providers if you are currently breastfeeding while on Vyleesi to discuss any potential risks to the infant.
• Taking naltrexone: This medicine should not be taken with naltrexone.
• Are concerned with the side effects of darkened skin: Darkened skin on the face, gums, and breasts is possible with Vyleesi. If you are concerned about this side effect, you should ask your doctor or pharmacist before using it.

Common Side Effects of Vyleesi

Common side effects of Vyleesi may include nausea, flushing, and upset stomach. Generally, the side effects of Vyleesi will disappear gradually as your body gets used to the medication. If patients experience any side effects that are bothersome or concerning, it is important to contact your doctor or pharmacist.^{1, 2, 3}

Common side effects of Vyleesi include:*

• Flushing
• Headache
• Skin hyperpigmentation (darkened skin spots)
• Nausea
• Vomiting
• Cough

*All medications, including Vyleesi, can cause side effects which can be mild or serious. This is not a comprehensive list of all possible side effects. You should talk with your doctor or pharmacist about any questions you have and to understand the potential side effects and benefits of any medication.

Serious Side Effects of Vyleesi

Serious side effects of Vyleesi include but are not limited to limb pain, heart events, and severe allergic reactions. Serious side effects associated with Vyleesi are rare, but if you encounter any severe or alarming side effects, it is important to seek medical assistance immediately. ¹

Serious side effects of Vyleesi include:*

• Increased blood pressure
• Limb pain
• Joint pain
• Severe stomachache
• Heart events
• Severe allergic reactions

*All medications, including Vyleesi, can cause side effects which can be mild or serious. This is not a comprehensive list of all possible side effects. You should talk with your doctor or pharmacist about any questions you have and to understand the potential side effects and benefits of any medication.

Vyleesi Dosages

Vyleesi comes in a pre-filled autoinjector device, each containing a single medication dose. The usual initial dosage for Vyleesi is 1.75 mg, administered subcutaneously (under the skin) at least 45 minutes before the expected sexual activity. It is advised not to exceed a maximum of eight doses per month. Vyleesi is FDA-approved for premenopausal women with hypoactive sexual desire disorder (HSDD). The age spectrum for premenopausal women may differ, but it generally encompasses females in their reproductive years, typically from late adolescence until the start of menopause.¹

How to Take Vyleesi: X Number Steps

Here are 7 number steps to taking Vyleesi:¹

1. Carefully read the instructions: Following the instructions ensures that patients get the maximum benefit from the medication. The instructions will give you information on accurate doses, administration procedures, and the potential side effects or interactions with other medications.
2. Make sure everything is clean: Thoroughly wash hands and effectively clean the injection site with an alcohol wipe before administering Vyleesi. This is vital to reduce the risk of infection and ensure safe and proper administration.
3. Select the Injection Site: Common injection sites include the belly or thigh. After cleaning the area with an alcohol swab, allow it to air dry.
4. Check the Medication: Examine the Vyleesi auto-injector for any visible damage or defects. Make sure the medication is not expired.
5. Administer the Injection: Firmly press the autoinjector against the skin at the selected injection site. It should activate and deliver the medication automatically. Maintain steady pressure during the injection.
6. Dispose of the Autoinjector: Safely dispose of the used auto-injector according to your healthcare provider’s instructions or local regulations. Do not reuse it or share your autoinjector.
7. Wash hands after injection: Wash hands after injection. The leftover medicine on your skin may cause irritation.

What Happens If I Miss a Dose of Vyleesi?

This medication should be used as needed before sexual activity. Therefore, the patient doesn’t need to worry about missing a dose. Refrain from taking it more frequently than once every 24 hours or more than 8 times per month.¹

Can You Overdose on Vyleesi?

Yes, you can overdose on Vyleesi. An increase in blood pressure and an increased risk of heart issues can occur if Vyleesi is used more frequently than directed by your prescriber. To prevent the risk of overdose, one should always follow the prescribed dose and administration instructions for Vyleesi and consult with your doctor or pharmacist if you have any concerns or questions about the medication regimen.¹

What Should You Do If You Take Too Much Vyleesi?

If you suspect that one has exceeded the prescribed Vyleesi dosage or is having severe side effects, it is imperative to seek medical assistance immediately. You may also contact the poison control center (800-222-1222) for guidance. Emergency medical intervention might be required to address any severe complications arising from an overdose.¹

What to Avoid When Taking Vyleesi

Some heart medications and medications for alcohol and opioid addiction interact with Vyleesi. You should always let your doctor or pharmacist know what other medications you are taking to avoid interactions and serious side effects.¹

2 substances you should avoid while taking Vyleesi include:

• Naltrexone: Patients should not combine Vyleesi with naltrexone (a drug designed to address alcohol and opioid addiction), as this can lead to significant naltrexone treatment failure with severe consequences.¹
• Heart disease or high blood pressure medicine: Medications that influence blood pressure, heart rate, or blood flow may have the potential to interact with Vyleesi, which may also impact blood pressure.¹

How to Get a Prescription for Vyleesi

Patients can arrange a consultation with a licensed healthcare provider with the authority to prescribe medications. This may include a primary care physician, gynecologist, or a specialist specializing in sexual health and hormone-related concerns. Your healthcare provider will perform a comprehensive medical assessment, which may involve reviewing the medical history, family history, heart tests, conducting a physical examination, and potentially ordering pertinent tests to exclude any underlying medical issues.

Patients need to notify the healthcare provider about all the medications they are presently using, which includes prescription medications, over-the-counter drugs, supplements, and herbal products. This disclosure aids the provider in evaluating potential interactions and ensuring safety. ¹

How Much Does Vyleesi Cost?

The price of Vyleesi subcutaneous solution (1.75 mg/0.3 mL) can vary, but it’s typically approximately $1000 for a single dose (without insurance). Vyleesi has a copay program where eligible commercially insured patients may get the medication for free. There are some restrictions to these programs, so you can ask your pharmacist if you qualify. If you have prescription insurance, the cost of this medication will vary by plan, and the best way to find out the cost is to call your prescription insurance company directly.¹

Questions to Ask Your Healthcare Provider About Vyleesi

Questions to ask your care team about Vyleesi include:

• How safe is Vyleesi?
• How long will it take for me to adjust to taking Vyleesi?
• Am I at risk for more serious side effects if I am already taking other medications?
• What is the best dosage to ensure fewer side effects?
• When should I take Vyleesi?
• What are the contraindications of Vyleesi?
• What medications should I not take with Vyleesi?
• Should I take Vyleesi with food?

In My Experience

In my experience, many females find it difficult to discuss their sexual health, including sexual problems they may be having. As a pharmacist, I try to promote open conversations about these topics with my patients. If you have any questions or concerns regarding Vyleesi as an option for you, consult your pharmacist, as they will have a good understanding of Vyleesi and its effects.

Vyleesi has been a good option for my patients (who have insurance that will pay for it) because It doesn’t need to be taken daily, and many of Vyleesi’s side effects are relatively mild. Vyleesi is effective, convenient, and works quickly. Some cons to Vyleesi may include the cost and lack of long-term safety data. Vyleesi is a relatively new medication, so long-term safety data is limited.

It is important to note the individual experiences with Vyleesi can vary, and it’s always best to consult with a healthcare professional for personalized advice.¹