From the Research
Bremelanotide (PT-141) is not effectively absorbed sublingually, as its molecular structure and chemical properties limit its absorption through the sublingual route 1. The medication is primarily administered via subcutaneous injection because of its poor oral bioavailability.
Key Points
- The molecular structure of bremelanotide makes it unsuitable for sublingual administration as it cannot efficiently cross the oral mucosa to enter the bloodstream in therapeutic amounts.
- The peptide is relatively large (molecular weight around 1025 daltons) and has chemical properties that limit its absorption through the sublingual route.
- For proper therapeutic effect, patients should use the medication as prescribed - typically as a subcutaneous injection administered 45 minutes before anticipated sexual activity.
- Attempting sublingual administration would likely result in minimal absorption and ineffective treatment outcomes.
- The medication works by activating melanocortin receptors in the brain that influence sexual behavior and desire, but this mechanism requires adequate blood levels that sublingual administration cannot reliably achieve 2.
Administration and Efficacy
The recommended dosage of bremelanotide is 1.75 mg injected subcutaneously in the abdomen or thigh at least 45 min before sexual activity, as supported by studies showing improvements in desire, arousal, and orgasm scores when administered before sexual activity compared to a placebo 1, 3.
Safety and Interactions
Bremelanotide is safe and has limited drug-drug interactions, including no clinically significant interactions with ethanol, but prescribing guidelines recommend no more than 1 dose in 24 hours and no more than 8 doses per month 2. Individuals should discontinue use after 8 weeks without benefit.