VYLEESI (AUTOINJECTOR)
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VYLEESI (AUTOINJECTOR) (VYLEESI (AUTOINJECTOR)).
VYLEESI (bremelanotide) is a melanocortin receptor agonist, specifically activating the melanocortin-4 receptor (MC4R), which is involved in the central regulation of sexual desire and arousal. It is thought to modulate endogenous pathways in the brain that control sexual response.
| Metabolism | Primarily hydrolyzed by peptidases in plasma and tissues; minimal hepatic metabolism via CYP450 enzymes. |
| Excretion | Primarily renal (approximately 80% as unchanged drug) with minor fecal elimination (5-10%). |
| Half-life | Terminal elimination half-life is approximately 4 hours; clinically, steady-state is achieved within 1-2 days. |
| Protein binding | Approximately 60% bound primarily to albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.4 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Subcutaneous injection: approximately 95%. |
| Onset of Action | Subcutaneous injection: onset within approximately 30 minutes. |
| Duration of Action | Duration of action is approximately 4-6 hours for the intended effect; effects peak at 1-2 hours post-dose. |
| Molecular Weight | 1025.2 |
1.5 mg subcutaneously as needed, at least 45 minutes prior to sexual activity, not to exceed one dose per 24 hours.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (eGFR <30 mL/min/1.73 m²). |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C). No dose adjustment recommended for mild to moderate impairment (Child-Pugh class A or B). |
| Pediatric use | Not approved for use in pediatric patients. Safety and efficacy not established. |
| Geriatric use | No specific dose adjustment recommended, but consider lower starting dose due to potential increased sensitivity and comorbidities; clinical experience limited in patients >75 years. |
| 1st trimester | No adequate human data; animal studies show no teratogenicity but potential for maternal toxicity at high doses. Use only if benefit outweighs risk. |
| 2nd trimester | Limited human data; no evidence of fetal harm from brief systemic exposure. Consider risk-benefit. |
| 3rd trimester | Use near term may cause uterine hyperstimulation or fetal distress; avoid in active labor. |
Clinical note
Comprehensive clinical and safety monograph for VYLEESI (AUTOINJECTOR) (VYLEESI (AUTOINJECTOR)).
| Placental transfer | Unknown; molecular weight suggests possible minimal transfer, but no human studies. |
| Breastfeeding | Bremelanotide is not absorbed orally, so infant exposure via breast milk is minimal; however, no human data on milk transfer. Caution if breastfeeding. |
■ FDA Black Box Warning
None
| Serious Effects |
Uncontrolled hypertensionCardiovascular disease (including arrhythmias, coronary artery disease)Concomitant use with naltrexone or other opioid antagonists
| Precautions | Hypertension: May increase blood pressure; contraindicated in patients with uncontrolled hypertension or cardiovascular disease., Nausea: Commonly reported, especially at higher doses; may require dose reduction or discontinuation., Injection site reactions., Fetal risk: Not recommended during pregnancy; advise effective contraception., Coadministration with alcohol may increase risk of hypotension and syncope. |
| Food/Dietary | No specific food interactions reported. However, avoid alcohol consumption due to increased risk of hypotension and syncope. |
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| Lactation Rating |
| L3 (Moderately Safe) |
| Teratogenic Risk | Vyleesi (bremelanotide) is contraindicated in pregnancy due to embryo-fetal toxicity. In animal studies, administration during organogenesis resulted in increased postimplantation loss and reduced fetal body weight. No data exist in pregnant women; therefore, avoid use in women who are or may become pregnant. If pregnancy occurs, discontinue immediately and report to the FDA. |
| Fetal Monitoring | No specific clinical monitoring for maternal or fetal effects is recommended. Pregnancy testing is recommended before initiating therapy and monthly during treatment due to contraindication in pregnancy. Monitor for hypertensive crisis if used with other drugs affecting blood pressure. |
| Fertility Effects | Bremelanotide may impair fertility. In animal studies, no effects on fertility were observed in female rats; however, reduced corpora lutea and implantation sites were noted. Effects on human fertility are unknown. Given its pharmacology as a melanocortin receptor agonist, it may affect the hypothalamic-pituitary-gonadal axis. |
| Clinical Pearls | Bremelanotide (VYLEESI) is a melanocortin receptor agonist for hypoactive sexual desire disorder (HSDD) in premenopausal women. Administer subcutaneously in the abdomen or thigh at least 45 minutes before anticipated sexual activity. Do not exceed one dose per 24 hours. Avoid use with alcohol due to increased risk of hypotension and syncope. Monitor blood pressure, as it can cause transient increases. Contraindicated with uncontrolled hypertension or cardiovascular disease. Onset is rapid; duration up to 8 hours. Nausea is common; consider antiemetic pretreatment if needed. |
| Patient Advice | Inject VYLEESI in the abdomen or thigh at least 45 minutes before sexual activity. · Do not use more than one dose in 24 hours. · Avoid alcohol while using VYLEESI; it can cause dizziness or fainting. · Common side effects include nausea, flushing, and headache. Nausea may occur shortly after injection. · Seek medical attention if you experience severe dizziness, chest pain, or loss of consciousness. · This medicine does not protect against sexually transmitted infections. · Do not use if you have uncontrolled high blood pressure or heart problems. |