bremelanotide (Rx)

Brand and Other Names:Vyleesi
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

prefilled autoinjector

  • 1.75mg/0.3mL (single-dose)

Hypoactive Sexual Desire Disorder

1.75 mg SC as needed, at least 45 minutes before anticipated sexual activity

Do not administer >1 dose/24 hr

>8 doses/month not recommended

Duration of efficacy after each dose is unknown; optimal window for administration has not been fully characterized

Efficacy of consecutive doses within 24 hr has not been established, and administering doses close together may increase the risk of additive effects on blood pressure

Indication

  • Indicated for treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD)
  • Characterized by low sexual desire that causes marked distress or interpersonal difficulty
  • Not due to a coexisting medical or psychiatric condition, problems with the relationship, or effects of a medication or drug substance
  • Acquired HSDD refers to HSDD that develops in a patient who previously had no problems with sexual desire
  • Generalized HSDD refers to HSDD that occurs regardless of the type of stimulation, situation, or partner

Dosage Modifications

Renal impairment

  • Mild-to-moderate (eGFR 30-89 mL/min/1.73 m²): No dosage adjustment necessary
  • Severe (eGFR 30-89 mL/min/1.73 m²): Use with caution; patients may have an increase in the incidence and severity of adverse reactions (eg, nausea, vomiting)

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A and B; score 5-9): No dosage adjustment necessary
  • Severe (Child-Pugh C; score 10-15): Not evaluated; use with caution; patients may have an increase in the incidence and severity of adverse reactions (eg, nausea, vomiting)

Dosing Considerations

Discontinuing treatment

  • Discontinue after 8 weeks if symptoms not improved

Limitations of use

  • Not indicated for HSDD in postmenopausal women or in men
  • Not indicated to enhance sexual performance

Safety and efficacy not established

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Interactions

Interaction Checker

and bremelanotide

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Nausea (40%)

            Flushing (20%)

            Injection site reactions (13.2%)

            Headache (11.3%)

            1-10%

            Vomiting (4.8%)

            Cough (3.3%)

            Fatigue (3.2%)

            Hot flush (2.7%)

            Paresthesia (2.6%)

            Dizziness (2.2%)

            Nasal congestion (2.1%)

            <2%

            • Upper abdominal pain
            • Diarrhea
            • Myalgia
            • Arthralgia
            • Pain
            • Restless leg syndrome
            • Rhinorrhea
            • Increased creatine phosphokinase
            • Blood pressure increased
            • Pain in extremity
            • Focal skin hyperpigmentation
            • Flushing

            <1%

            Flulike symptoms

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            Warnings

            Contraindications

            Uncontrolled hypertension

            Known cardiovascular disease

            Cautions

            Most commonly reported adverse reaction was nausea, which improves for most patients with the second dose; consider discontinuing treatment for persistent or severe nausea or initiating antiemetic therapy in patients who are bothered by nausea but are continuing treatment

            Focal hyperpigmentation

            • Focal hyperpigmentation, including involvement of the face, gingiva, and breasts, was reported
            • Patients with dark skin were more likely to develop focal hyperpigmentation
            • Resolution of focal hyperpigmentation was not confirmed in all patients after discontinuation
            • Consider discontinuing treatment if hyperpigmentation develops

            Increased blood pressure and heart rate reduction

            • Transient increase in blood pressure and reduction in heart rate may occur after each dose
            • Blood pressure and heart rate returned to baseline usually within 12 hr postdose
            • No additive effects were seen for blood pressure or heart rate following repeat daily dosing 24-hours apart for up to 16 day
            • Before initiating treatment, and periodically during treatment, consider patient’s cardiovascular risk and ensure blood pressure is well-controlled

            Drug interactions overview

            • Effect of bremelanotide on other drugs
              • Administration may slow gastric emptying and thus potentially reducing the rate and extent of absorption of concomitantly administered oral medications
              • Avoid use when taking concomitant oral drugs that are dependent on threshold concentrations for efficacy (eg, antibiotics)
              • Consider discontinuing treatment if there is a delayed drug effect of concomitant oral medications when a quick onset of drug effect is desired (eg, drugs for pain relief such as indomethacin)
            • Naltrexone
              • Avoid use with an orally administered naltrexone-containing product that is intended to treat alcohol and opioid addiction, owing to the severe consequence of naltrexone treatment failure
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            Pregnancy

            Pregnancy

            Few pregnancies in women exposed to bremelanotide in clinical trials are insufficient for determining whether there is a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes

            Pregnancy exposure registry

            • Pregnancy exposure registry monitors pregnancy outcomes in women exposed to bremelanotide during pregnancy
            • Encourage women exposed to drug to register in the Vyleesi pregnancy exposure registry at (877) 411-2510

            Animal data

            • Based on findings in animal studies, use in pregnant women may be associated with potential for fetal harm
            • In animal reproduction and development studies, daily SC administration of bremelanotide to pregnant dogs during organogenesis at exposures ≥16 times the maximum recommended dose (based on AUC) produced fetal harm
            • SC bremelanotide doses in mice during pregnancy and lactation produced developmental effects in offspring at ≥125-times the maximum recommended dose (based on AUC)
            • Lowest bremelanotide dose associated with fetal harm has not been identified for either species

            Contraception

            • Not recommended during pregnancy
            • Females of reproductive potential: Use effective contraception during treatment; discontinue treatment if pregnancy is suspected

            Lactation

            There is no information on presence of bremelanotide or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production

            Consider developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Melanocortin receptor (MCR) agonist nonselectively activates several receptor subtypes with the following order of potency: MC1R, MC4R, MC3R, MC5R, MC2R

            At therapeutic dose levels, binding 9 of 17 to MC1R and MC4R is most relevant

            Neurons expressing MC4R are present in many areas of the central nervous system

            Mechanism to improve HSDD in women is unknown

            MC1R is expressed on melanocytes; binding at this receptor leads to melanin expression and increased pigmentation

            Absorption

            Peak plasma concentration: 72.8 ng/mL

            Peak plasma time: ~1 hr

            AUC: 276 hr·ng/mL

            Absolute bioavailability: ~100% (following SC dose)

            Distribution

            Protein bound: 21%

            Vd: 25 L

            Metabolism

            Primary metabolic pathway involves multiple hydrolyses of the amide bond of cyclic peptide

            Elimination

            Half-life: ~2.7 hr

            Clearance: 6.5 L/hr

            Excretion: Urine (64.8%); feces (22.8%)

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            Administration

            SC Administration

            SC administration use only

            Administer in the abdomen or thigh, as needed, at least 45 minutes before anticipated sexual activity

            Optimal time for administration will be determined by the patient based on duration of effect and any adverse reactions such as nausea

            Do not administer more than 1 dose within 24 hr

            Administering more than 8 doses/month is not recommended; more frequent dosing increases the risk for focal hyperpigmentation and length of time per month when blood pressure is increased

            Visually inspect for particulate matter and discoloration before administration

            Discard if solution is cloudy, discolored, or visible particles are observed

            Storage

            Store at or below 25°C (77°F)

            Do not freeze

            Protect from light

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.