Dosing & Uses
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
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (0)
Serious - Use Alternative (50)
- buprenorphine
bremelanotide will decrease the level or effect of buprenorphine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- carbamazepine
bremelanotide will decrease the level or effect of carbamazepine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- clonidine
bremelanotide will decrease the level or effect of clonidine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- codeine
bremelanotide will decrease the level or effect of codeine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- colchicine
bremelanotide will decrease the level or effect of colchicine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- cyclosporine
bremelanotide will decrease the level or effect of cyclosporine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- digoxin
bremelanotide will decrease the level or effect of digoxin by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- dihydroergotamine
bremelanotide will decrease the level or effect of dihydroergotamine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- disopyramide
bremelanotide will decrease the level or effect of disopyramide by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- divalproex sodium
bremelanotide will decrease the level or effect of divalproex sodium by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- ergotamine
bremelanotide will decrease the level or effect of ergotamine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- ethosuximide
bremelanotide will decrease the level or effect of ethosuximide by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- everolimus
bremelanotide will decrease the level or effect of everolimus by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- fentanyl
bremelanotide will decrease the level or effect of fentanyl by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- fentanyl transmucosal
bremelanotide will decrease the level or effect of fentanyl transmucosal by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- hydrocodone
bremelanotide will decrease the level or effect of hydrocodone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- hydromorphone
bremelanotide will decrease the level or effect of hydromorphone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- levorphanol
bremelanotide will decrease the level or effect of levorphanol by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- levothyroxine
bremelanotide will decrease the level or effect of levothyroxine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- lithium
bremelanotide will decrease the level or effect of lithium by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- loxicodegol
bremelanotide will decrease the level or effect of loxicodegol by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- methadone
bremelanotide will decrease the level or effect of methadone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- methotrexate
bremelanotide will decrease the level or effect of methotrexate by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- midazolam
bremelanotide will decrease the level or effect of midazolam by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- minoxidil
bremelanotide will decrease the level or effect of minoxidil by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- morphine
bremelanotide will decrease the level or effect of morphine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- naltrexone
bremelanotide will decrease the level or effect of naltrexone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid using bremelanotide with an orally administered naltrexone-containing product that is intended to treat alcohol and opioid addiction due to the potential for naltrexone treatment failure.
- oliceridine
bremelanotide will decrease the level or effect of oliceridine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- oxycodone
bremelanotide will decrease the level or effect of oxycodone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- oxymorphone
bremelanotide will decrease the level or effect of oxymorphone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- pentazocine
bremelanotide will decrease the level or effect of pentazocine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- phenobarbital
bremelanotide will decrease the level or effect of phenobarbital by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- phenytoin
bremelanotide will decrease the level or effect of phenytoin by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- pimozide
bremelanotide will decrease the level or effect of pimozide by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- prazosin
bremelanotide will decrease the level or effect of prazosin by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- primidone
bremelanotide will decrease the level or effect of primidone by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- procainamide
bremelanotide will decrease the level or effect of procainamide by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- quinidine
bremelanotide will decrease the level or effect of quinidine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- quinine
bremelanotide will decrease the level or effect of quinine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- sirolimus
bremelanotide will decrease the level or effect of sirolimus by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- sufentanil
bremelanotide will decrease the level or effect of sufentanil by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- sufentanil SL
bremelanotide will decrease the level or effect of sufentanil SL by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- tacrolimus
bremelanotide will decrease the level or effect of tacrolimus by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- temsirolimus
bremelanotide will decrease the level or effect of temsirolimus by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- theophylline
bremelanotide will decrease the level or effect of theophylline by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- thioridazine
bremelanotide will decrease the level or effect of thioridazine by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- topotecan
bremelanotide will decrease the level or effect of topotecan by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- tramadol
bremelanotide will decrease the level or effect of tramadol by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- triazolam
bremelanotide will decrease the level or effect of triazolam by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
- valproic acid
bremelanotide will decrease the level or effect of valproic acid by Other (see comment). Avoid or Use Alternate Drug. Bremelanotide may slow gastric emptying and potentially reduces the rate and extent of absorption of concomitantly administered oral medications. Avoid use when taking any oral drug that is dependent on threshold concentrations for efficacy. Interactions listed are representative examples and do not include all possible clinical examples.
Monitor Closely (0)
Minor (0)
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
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
- To minimize risk of more pronounced blood pressure effects, advise patients to not take more than one dose within 24 hours
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
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.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%)
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
Images
Formulary
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- View the formulary and any restrictions for each plan.
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