- Reaction score
- 3,025
Sexual side effects seem to be common on hairloss meds. I have experienced varying degrees of chemical castration on finasteride 5 mg/day (but not 1.25 mg/day), spironolactone 200 mg/day, and cyproterone 100 mg/day. Daro, which doesn't cross the blood brain barrier, has not caused any negative erectile effects at all even in the highest doses I have used.
This tells me that sexual side effects are mediated by compounds exerting their anti-androgenic effect primarily in the brain.
Trying to counteract that with PDE5 inhibitors (cialis, v****) is therefore likely not a perfect strategy, but I think it is probably useful anyway if the side effects are just mild. PDE5 inhibitors for me are just nice to keep around the house in case I one day have a hot date and want to be sure I perform.
The biggest problem I've had when I've played with PDE5 inhibitors (both cialis & v****) is they seem to cause me awful heartburn. I mean killer heartburn. For 2 days at a time. And even strong prescription antacids like pantoprazole don't stop or slow it down when it happens. So up until now I've considered them off limits.
This happens because these medications relax smooth muscle, and this in turn means relaxation of the lower esophageal sphincter. In principle, I have thought that applying it topically to the skin instead of orally into the stomach could reduce this side effect.
I've been bored today so I've just run an experiment that I think shows using cialis transdermally does in fact work well and very considerably reduces heartburn side effects.
Solubility/Penetration of Tadalafil
Tadalafil solubility is best given by this table:
The highest solubility in common solvents are Transcutol aka Carbitol (sources here) & PEG400 (commonly available).
Some different data for other agents including ethyl oleate (EO) and isopropyl myristate (IPM) are described here. Solubility for both of these other two agents is poor:
However, EO, IPM, and ethanol all give the greatest skin penetration by far:
So it is evident ethyl oleate, IPM, and OE have the highest penetration but provide poor solubility. PEG 400 provides high solubility but poor penetration. Propylene glycol provides moderate solubility but poor penetration. Transcutol provides good solubility and unknown penetration.
Likely a good solvent will then be a mix of agents that are good for solvency and also good for penetration. Probably this will have to be trial and error to work out. I am guessing Transcutol + ethanol + IPM/OE will be the best solution though.
Dosing/Preparation
The full dose of Cialis is 20 mg. I had some old brand name tablets lying around from when I previously tried this med years ago. One branded 20 mg Cialis tablet weighs 370 mg, so this med is 95% fillers.
I crushed one Cialis tablet up in a bowl with a spoon. After crushing I had 346 mg powder (some got lost as I was sloppy about my crushing technique the pill initially almost exploded), so proportionately this was probably ~18.7 mg cialis.
I added 1 mL PEG400 that I had already to it, 0.5 mL ethanol, and 0.5 mL polyethylene glycol. I simply swished this around for a while and let it sit for a bit. A lot of powder still remained in the mixture as would be expected given it is 95% filler and most of these fillers won't dissolve.
Administration
I then simply rubbed the liquid from this on my dick and left it there for 20 minutes. The "gritty" last remainder of liquid I applied on my skin other places of my body so it wouldn't be wasted. I figure it doesn't really matter where you rub it on your skin, as long as the skin is thin enough to absorb it.
Effect
I can generally feel these meds when they kick in as they tend to give me a bit of a "headrush" or almost headachy feeling from the vascular relaxation. After about 15-20 minutes this started to kick in. I also started feeling a very mild sense of "gassiness" that goes along with what it usually does to me if I take it orally. But no heartburn and everything has been very tolerable.
Erection effect was consistent with when I've taken it orally. It is hard for me to judge the percentage strength of the effect compared to taking it orally. I'm coming off finasteride 5 mg side effects as I've been taking that daily for 3 weeks (due to not being able to use my topicals as much the past few weeks) so that makes it harder still to judge. But I'd guess I probably got at least 1/4 to 1/2 of the oral effect which is more than enough for me.
Conclusions
Almost certainly (from my subjective experience) tadalafil is therefore a medication that can be effectively used transdermally. I'm trying to order some transcutol so I can mix that in as a solvent as well, just because I think PEG400 does not go through the skin very well. I've ordered some ethyl oleate (commonly used in steroid injections so easy to find).
I will likely try this experiment a few more times with the crushed pills, then if it gives consistent results, buy some pure powder on Alibaba (very cheap/common) and mix up a pure solution to keep on hand for as needed use.
Penis anatomy is such that I don't think topical application to the penis will necessarily increase the effect at the penis. I don't think it will get through directly to the corpus cavernosa just from topical application.
I would guess that applying to the skin anywhere is going to work by going into the circulation same as if you take it orally. The only benefit of this approach is then to avoid the stomach as the first site it hits if you're prone to the heartburn effect as I am.
This will likely then not be relevant for many other guys, but I note some forum posts like this one where other guys online have been struggling with the same problem, so I figure it's worth posting my results in case anyone else Googles the subject in the future.
It's been a few hours since I applied. I'll update if anything new happens but so far this is very tolerable and certainly much better than oral administration for me.
This tells me that sexual side effects are mediated by compounds exerting their anti-androgenic effect primarily in the brain.
Trying to counteract that with PDE5 inhibitors (cialis, v****) is therefore likely not a perfect strategy, but I think it is probably useful anyway if the side effects are just mild. PDE5 inhibitors for me are just nice to keep around the house in case I one day have a hot date and want to be sure I perform.
The biggest problem I've had when I've played with PDE5 inhibitors (both cialis & v****) is they seem to cause me awful heartburn. I mean killer heartburn. For 2 days at a time. And even strong prescription antacids like pantoprazole don't stop or slow it down when it happens. So up until now I've considered them off limits.
This happens because these medications relax smooth muscle, and this in turn means relaxation of the lower esophageal sphincter. In principle, I have thought that applying it topically to the skin instead of orally into the stomach could reduce this side effect.
I've been bored today so I've just run an experiment that I think shows using cialis transdermally does in fact work well and very considerably reduces heartburn side effects.
Solubility/Penetration of Tadalafil
Tadalafil solubility is best given by this table:
The highest solubility in common solvents are Transcutol aka Carbitol (sources here) & PEG400 (commonly available).
Some different data for other agents including ethyl oleate (EO) and isopropyl myristate (IPM) are described here. Solubility for both of these other two agents is poor:
However, EO, IPM, and ethanol all give the greatest skin penetration by far:
So it is evident ethyl oleate, IPM, and OE have the highest penetration but provide poor solubility. PEG 400 provides high solubility but poor penetration. Propylene glycol provides moderate solubility but poor penetration. Transcutol provides good solubility and unknown penetration.
Likely a good solvent will then be a mix of agents that are good for solvency and also good for penetration. Probably this will have to be trial and error to work out. I am guessing Transcutol + ethanol + IPM/OE will be the best solution though.
Dosing/Preparation
The full dose of Cialis is 20 mg. I had some old brand name tablets lying around from when I previously tried this med years ago. One branded 20 mg Cialis tablet weighs 370 mg, so this med is 95% fillers.
I crushed one Cialis tablet up in a bowl with a spoon. After crushing I had 346 mg powder (some got lost as I was sloppy about my crushing technique the pill initially almost exploded), so proportionately this was probably ~18.7 mg cialis.
I added 1 mL PEG400 that I had already to it, 0.5 mL ethanol, and 0.5 mL polyethylene glycol. I simply swished this around for a while and let it sit for a bit. A lot of powder still remained in the mixture as would be expected given it is 95% filler and most of these fillers won't dissolve.
Administration
I then simply rubbed the liquid from this on my dick and left it there for 20 minutes. The "gritty" last remainder of liquid I applied on my skin other places of my body so it wouldn't be wasted. I figure it doesn't really matter where you rub it on your skin, as long as the skin is thin enough to absorb it.
Effect
I can generally feel these meds when they kick in as they tend to give me a bit of a "headrush" or almost headachy feeling from the vascular relaxation. After about 15-20 minutes this started to kick in. I also started feeling a very mild sense of "gassiness" that goes along with what it usually does to me if I take it orally. But no heartburn and everything has been very tolerable.
Erection effect was consistent with when I've taken it orally. It is hard for me to judge the percentage strength of the effect compared to taking it orally. I'm coming off finasteride 5 mg side effects as I've been taking that daily for 3 weeks (due to not being able to use my topicals as much the past few weeks) so that makes it harder still to judge. But I'd guess I probably got at least 1/4 to 1/2 of the oral effect which is more than enough for me.
Conclusions
Almost certainly (from my subjective experience) tadalafil is therefore a medication that can be effectively used transdermally. I'm trying to order some transcutol so I can mix that in as a solvent as well, just because I think PEG400 does not go through the skin very well. I've ordered some ethyl oleate (commonly used in steroid injections so easy to find).
I will likely try this experiment a few more times with the crushed pills, then if it gives consistent results, buy some pure powder on Alibaba (very cheap/common) and mix up a pure solution to keep on hand for as needed use.
Penis anatomy is such that I don't think topical application to the penis will necessarily increase the effect at the penis. I don't think it will get through directly to the corpus cavernosa just from topical application.
I would guess that applying to the skin anywhere is going to work by going into the circulation same as if you take it orally. The only benefit of this approach is then to avoid the stomach as the first site it hits if you're prone to the heartburn effect as I am.
This will likely then not be relevant for many other guys, but I note some forum posts like this one where other guys online have been struggling with the same problem, so I figure it's worth posting my results in case anyone else Googles the subject in the future.
It's been a few hours since I applied. I'll update if anything new happens but so far this is very tolerable and certainly much better than oral administration for me.
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