BREMELANOTIDE

Class

• Nonselective melanocortin receptor agonist

BREMELANOTIDE commonly prescribed for

(Bold for FDA approved)

How BREMELANOTIDE works

• Bremelanotide is a nonselective melanocortin receptor agonist; at therapeutic doses, bremelanotide binding to melanocortin 1 and 4 receptors is most relevant

• Sexual dysfunction is theoretically linked to an imbalance in central excitatory and inhibitory sexual signals

• HSDD hypothetically results from excessive inhibitory signals, inadequate excitatory signals, or a combination of the two

• Melanocortin receptors are located in the medial preoptic area of the hypothalamus, which is implicated in the sexual behavior of both sexes; stimulation of those receptors leads to dopamine release

How long until BREMELANOTIDE works

• Should be used at least 45 minutes before anticipated sexual activity; duration of efficacy after each dose is unknown and optimal window for bremelanotide administration has not been established

Notable Side Effects

• Nausea

• Flushing

• Injection site reactions

• Headache

• Vomiting

• Hyperpigmentation (higher risk with daily dosing)

Life Threatening Side Effects

• Transient increase in blood pressure and decrease in heart rate

weight gain

unusual

sedation

unusual

What to do about BREMELANOTIDE side effects

• Wait

• In most cases nausea improves after the first dose; for persistent or severe nausea, consider discontinuation or initiating antiemetic therapy

• For hyperpigmentation, consider discontinuation

• Switch to another treatment option

usual dosage range

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

Dosage Forms

• Subcutaneous injection 1.75 mg/0.3 mL in a single-dose autoinjector

long term use

• Safe and effective in controlled trials (24 weeks) and open-label extension studies lasting an additional 52 weeks

habit forming

• No

Renal Impairment

• Dose adjustment not necessary for mild to moderate impairment

• Use with caution in patients with severe impairment

Hepatic Impairment

• Dose adjustment not necessary for mild to moderate impairment

• Use with caution in patients with severe impairment

Cardiac Impairment

• Contraindicated

Elderly

• Not approved for use in postmenopausal women, and safety and efficacy have not been established

Children and Adolescents

• Safety and efficacy have not been established

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• In clinical trials of up to 12 months, 7 pregnancies were reported; among these 7 pregnancies, no major congenital anomalies were reported; there was 1 spontaneous abortion (miscarriage), 5 fullterm live births, and 1 outcome unknown as it was lost to follow-up

• When administered to pregnant dogs during organogenesis, embryofetal toxicity occurred at doses approximately 16 times the maximum recommended human dose (MRHD)

• When administered to pregnant mice during pregnancy and lactation, developmental effects occurred at doses approximately 125 times the MRHD

• Advise patients to discontinue bremelanotide if pregnancy is suspected

• Pregnancy registry for bremelanotide: 1-877-411-2510

Breast Feeding

• Unknown if bremelanotide is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Bremelanotide is dosed episodically (average 2–3 times per month) and has a half-life of 2.7 hours