‌

‌
‌
‌
‌

‌

‌

‌
‌
‌

‌

‌
‌
‌

‌

‌

‌
‌
‌

‌

‌
‌
‌

BREMELANOTIDE

ClassBREMELANOTIDE commonly prescribed forHow BREMELANOTIDE worksHow long until BREMELANOTIDE worksNotable Side EffectsLife Threatening Side Effectsweight gainsedationWhat to do about BREMELANOTIDE side effectsusual dosage rangeDosage Formslong term usehabit formingRenal ImpairmentHepatic ImpairmentCardiac ImpairmentElderlyChildren and AdolescentsPregnancyBreast Feeding

THERAPEUTICS

Class

  • Nonselective melanocortin receptor agonist

BREMELANOTIDE commonly prescribed for

(Bold for FDA approved)

• Acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women

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

SIDE EFFECTS

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

unusual

sedation

unusual

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

DOSING AND USE

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

SPECIAL POPULATIONS

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

Based on data Published online by Cambridge University Press

Compiled by Dr. Jash Ajmera