Use of PT-141 (Bremelanotide) for treatment of ED

[Youthful55guy]

I've been meaning to write this post for a while. Finally have the time and inspiration to get it done.

A little history, back before I got my hormones straightened out, I had some pretty bad ED issues. I now have only mild issues that are more than fixed with daily use of 2.5 to 5 mg of generic Cialis. So, for me, ED meds are more of a recreational drug than an absolutely needed medication, but that's not to diminish the importance of its positive effect on quality of life. After reading the following article on PT-141 (Bremelanotide), I decided to try using an inhaled version of the peptide rather than injecting it. It should be noted that in this article, they discuss uses of PT-141 at 7.5mg (7,500 mcg). I don't know if that is a misprint, or if inhalation doses are 10X less potent than injected doses, but my personal experience is that exceeding 0.75 mg in an injected dose can cause nausea and some pretty intense erections. I need to resolve this disconnect in my experiments.

King, S.H., Mayorov, A.V., Balse-Srinivasan, P., Hruby, V.J., Vanderah, T.W., and Wessells, H. (2007). Melanocortin receptors, melanotropic peptides and penile erection. Curr Top Med Chem 7, 1098-1106.

Several years ago, I trialed the use of PT-141 to supplement my use of Cialis. The results were for the most part positive and as long as I kept the daily dose under 750 mcg per day (0.75 mg), the side-effects were tolerable (mostly temporary nausea at higher doses). I found that the peptide worked very well in combination with Cialis. Cialis works at the vascular level for sustaining and intensifying an erection once started and PT-141 makes it easier to spontaneously initiate an erection with just mild stimulation. However, the one side-effect that was limiting for me was that I would experience very intense nocturnal erections. So intense, that they disturbed sleep patterns. The intensity of the erection would wake me up from a sound sleep (mostly during REM) and I'd feel like I had to urinate (which often happens to me after normal erections). The problem was that the erection was extremely rigid (no bend to it at all) and slow to subside. laugh if you will, this makes aiming during urination difficult. Once I got my hormones fixed I abandoned PT-141 and just use small daily doses of Cialis, and my aim got much better at night.

So, here's my plan for moving forward with an experiment of very low daily dosing of PT-141 vial inhalation.

Calculations for PD-141 inhaler (use of Nasacort sprayer)
• Nasacort Sprayer is designed to deliver 16.9 mL/120 sprays = 0.1408333 mL/spray
• PT-141 comes in 10 mg vial
• 10 mg/17 mL = 0.5882 mg/mL [A]
• @ 0.1408333 mL/spray = 0.0828 mg/spray (83 mcg/spray)

Instructions for Dilution & Filling
• Add 3 mL preserved injection saline to a 10 mg vial of PT-141 and gently invert to mix
• Transfer to empty Nasacort sprayer
• Repeat process 3X more times for a total of 12 mL transferred to sprayer
• Add 5 mL preserved injection saline into sprayer [A]
• Close sprayer top and gently invert sprayer several times to mix

Alternative Instructions for Dilution & Filling using Nasacort as the Diluent
• Open the screw cap new Nasacort sprayer and carefully lay the sprayer aside onto a clean cloth or tissue.
• Using a 1 mL insulin syringe, transfer about 3 mL from the sprayer to the PT-141 vial, pulling out and equivalent volume of air with each injection into the vial (to prevent pressure buildup). Alternatively, you can use a 3 mL syringe with a 1.5 inch needle.
• Gently invert the PT-141 vial several times and then transfer the solution back to the sprayer with the same syringe.
• Close sprayer top and gently invert sprayer several times to mix.
• Repeat the fluid transfer, mixing and transfer back to the sprayer 2-3 more times to ensure all of the PT-141 has been transferred to the sprayer.

Instructions for use of sprayer when used in combination with Cialis or other PD5 inhibitor
• Dispense 1 spray into nostril 1-4 times per day
• Recommend starting dose is 1 spray per day (88 mcg)
• Titrate dose to desired effect using intensity of nocturnal erections as a guide
• Titrate dose over a period of at least 1 week until reaching desired effect or a maximum dose of 880 mcg (10 sprays)

[kelkel]

I've fooled around with PT 141 years ago. It's definitly an interesting and effective aphrodisiac. Inhaling it as opposed to injections makes it more appealing as well. I'm impressed that you're seemingly able to feel it's effects for such a long period of time based on it's half-life. I'm sure you've read that it's effects may be related to it's impact on dopamine levels as well.

https://www.ncbi.nlm.nih.gov/pubmed/15833522

I've been a big fan of Selegiline and have been using it for about 7-8 years now. It's an MAO-B inhibitor which ultimately prevents the destruction of domamine in the brain. I'm sure YG55 you'll fine this an interesting topic and somewhat related. I'll attach an article from Life Extension to get you started.

https://www.lifeextension.com/Magazi...g-Drug/Page-01

[Youthful55guy]

Something more to research. It will have to wait until another weekend!

Yes, the effects (for me) last quite a long time. The half life is around 120 minutes, so most of it is gone from your system in 6-8 hours. I suspect you are correct in that stimulation of the melanocortin (specifically MC4) receptors in the brain set of a cascade of neuroendocrine changes in the brain that ultimately turn your 'horny' centers on. I also suspect that when T/DHT is low that there a concomitant decrease in MC4 activity in the brain. There is so much we still don't know about what happens inside our brain when we get hard, or more appropriately, what doesn't happen with ED. The pharmaceutical industry has focused on the vascular end of the equation, and that's a good place to start. However, you have to be able to initiate the chain of events and that's where PT-141 is useful.

[Youthful55guy]

Just a note on the mixing instructions. If you are using the Nasacort fluid as your diluent, note that it foams up quite a bit. Since we don't have to worry about strict sterility with a nasal inhaler, it's easy to work around this problem. Simply turn the vial upside down and let it settle for an hour or so. The foam will eventually liquify at the top of the vial (because it's upside down). You just have to stick the needle in while inverted and suck out the last bit for transfer to the inhaler.

[Youthful55guy]

Quick update. I'm beginning to think that the 10X disconnect from the article I previously cited is not a typo. That is, that inhalation is about 10X less effective than injection. I got pretty much nothing from the inhalation method at around 300-400mcg per day. Whereas that much injected on a daily basis makes me overly rigid during REM sleep.

Back to low dose injection of about 80mcg per day by combining it with my GH releasing peptides. I've found this daily dose gives a good balance of nighttime rigidity that subsides when I need it to and daytime erection on demand when combined with low dose Cialis.