Sexual Health Β· NeuralTier 1 β€” Strong clinical evidence (RCTs)

PT-141

Bremelanotide Β· Vyleesi

FDA-approved melanocortin agonist for hypoactive sexual desire disorder (HSDD) in premenopausal women. Also used off-label for erectile dysfunction in men, acting centrally rather than on blood vessels.

πŸ’‰ SC injection / Intranasal🧊 Refrigerate at 2–8Β°C; after removal from fridge use within 30 days

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Mechanism of Action

Activates MC3R and MC4R receptors in the hypothalamus and limbic system, directly enhancing sexual arousal circuits independent of nitric oxide pathways (unlike PDE5 inhibitors).

Clinical Applications

  • βœ“HSDD in premenopausal women (FDA approved)
  • βœ“Erectile dysfunction (off-label, especially psychogenic or centrally-mediated)
  • βœ“Low libido in both sexes
  • βœ“Sexual dysfunction from antidepressant use

Dosing Protocol

Recommended Dosing

SC injection (Vyleesi). 1.75 mg SC, 45 minutes before anticipated sexual activity. Maximum 1 dose per 24 hours and 8 doses per month. Can also use intranasal formulation (compounded).

Safety & Contraindications

Possible Side Effects

  • ⚠Nausea (most common β€” up to 40% in trials)
  • ⚠Flushing
  • ⚠Headache
  • ⚠Transient hypotension
  • ⚠Hyperpigmentation with frequent use
  • ⚠Injection site reactions

Contraindications

  • βœ•Cardiovascular disease (transient BP elevation)
  • βœ•Uncontrolled hypertension
  • βœ•Pregnancy
  • βœ•Use with naltrexone or other opioid antagonists β€” interaction risk

Combinations & Synergies

πŸ”— Kisspeptincentral sexual function synergy
πŸ”— Avoid with Melanotan II (overlapping melanocortin activation β€” increased side effects)