get the benifits of propecia without the side effects.

[CCS]

people with finasteride side effects can buy generic over seas finasteride, take it orally to see if it is real, stop taking it until the sides go away, and then apply it topically untill they they get sides and know they are getting some through their skin, and then back down the dose till they go away, and then they have the ideal topical. their body gets a percent the concentration their scalp gets, so they can always find a dose that works for both hair and body. I WISH I had side effects from finasteride so i would not have so much guess work.

please tell us what topical dose gives you side effects.
i suggest using 1 proscar pill per week topically, and changing the dose from there. grind it very good, mix it up in a table spoon of grain alcohol or rubbing alcohol, let it sit a minute, and then pour the liquid into a 1/4 full minoxidil bottle and use it for a week, and discard the powder.

 

[CCS]

no one on this forum knows how much you need to put on your scalp each day, or what liquid will give you the best absorption without irritating your scalp.

here are some numbers, though.

0.2mg finasteride grows 80% as much hair as 1mg, which grows 80% as much as 5mg.

the dht produced in the hair follicle for the hair follicle is by far the biggest cause of hair loss. the contribution from dht in the blood is so small that when researchers transplanted a balding hair out of the scalp onto an arm, it went bald just as fast as the hairs it used to be next to. also when they used a drug that stopped dht production in just the sebum glands, it had no measureable effect on hair loss. side effects come from systemic absorption, and hair loss treatment comes from stopping the dht production in just the follicle. some topical finasteride experiments did treat facial hair on women, showing that it can be absorbed. but the right liquid to use is in question. i think minoxidil is your best bet. skin absorption occurs primarily though the pours, and sweating during applicaiton can push it back out some.

We don't know how long finasteride would linger in your scalp before getting washed away in the blood, but we know from graphs that once it is in the blood, it enters cells fast and shuts down 2/3 of the dht that will be shut down in just 1-2 hours. I've seen on graphs that cells absorb 2/3 of the finasteride theywill absorb that day in the first 1-2 hours. so if it is absorbing through your scalp over 2 hours, you are probably safe for the whole day, since dht levels take 3-4 days to rise 50%.

1.5-5% of minoxidil is absorbed through the scalp. so if 1mL of 5% minoxidil has 50mg of minoxidil, only 2.5 mg is absorbed, and the rest dries to a yellow powder that looks like dandruff.

the finasteride molecule is very similar looking to testosterone, which is how it competes for the 5ar2 enzyme.

30% of the testosterone in testosterone patches is absorbed through the skin in 23 hours. They are 12g patches, and about 4 goes in.

60% of finasteride is absorbed in your gut, so if you take a 5mg pill, only 3mg enters your blood.

If you weigh 80kg, and your scalp is 1cm deep, then the 200cm2 male pattern baldness area is 1/400th the volume of your body, which means a little goes a long way.

If you want your scalp to get the same benifit that 1mg/day orally would give, and if 5% were absorbed though your scalp, you would need 1mg / 400 * 0.6 / 0.05 in that order, which equals 0.03 mg per day, and your body would get 0.03mg * 0.05= 0.0015 mg per day of used finasteride. however, you might only absorb 1%, and maybe 2/3 will rinse away in the blood before getting to your follicles. this would mean you would need 0.03*5*3= 0.45 mg per day, which is 1 pill every 10 days. In case you don't grind the pill well enough, and some of it's unexposed volume has finasteride that is not dissolved, you might want to error on using 1 pill per week. If the 1% estimate is wrong, and actually 5% is aborbed, then your body will get 0.45/5= 0.09 mg per day. this is still less than 1/5 what you are taking now.

So try 1 pill per week, and if you get sides, you know you are getting enough and can reduce the dose, and if you don't get sides, you can raise the dose and see when you do and then cut back. And please tell us all what that dose is, since those of us without side effects can't do this experiment like you can.

 

[CCS]

i think topical spironolactone combined with oral propecia would have somewhat similar effects to a strong topical finasteride.

and since i was not able to predict that spironolactone would react with minoxidil, I can't be too sure finasteride won't react with minoxidil either. Just watch out for color changes or smell changes or bubbles. I'll dig out my organic chemistry book and try to figure out what is going on. did any pharmacy ever mix minoxidil and spironolactone together in a smelly way? if so, that is pathetic since they should know that stuff.

 

[Felk]

...doesn't topical finasteride just work through systematic absoprtion anyway, however?

If not, cool, but i think that's how it goes...

 

[CCS]

only the DHT made in the follicle causes hair loss. the only way systemic absorption treats hair loss is by bringing finasteride to the follicle, not by reducing serum DHT. Even Bryan will back me up on that point.

Since some women responded to topical finasteride, we know that a therapudic concentration was absorbed, showing that it is possible to have some absorption.

I've seen study results that show that 0.05mg/day orally is the lowest tested dose that reduces DHT, and that 0.01mg/day orally reduces it maybe 5%.

Therefore, if 0.05mg/day were absorbed, sytemic effects could account for the hair reduction. However, I must point out that the volume of the body is 400 times the volume of the face, and the daily dose is not what inhibits DHT. Rather, the concentration in the blood around the follicles is what determines how much enters the follicles. Since the finasteride enters mainly through the pours (as all topicals do) the follicles would be surrounded by a high concentration of finasteride for the hour or so that absorption takes place.

I've seen grafts of serum finasteride levels vs time after dose, and could see that once finasteride enters the blood its concentration rapidily drops in the first hour (on a log plot) and then drops linearly on this plot after that. Obviously the first drop the blood levels is the finasteride entering the cells, and the slower linear drop afterwards is the metabolism by the liver. Bryan would varify that once finasteride enters the cells, it knocks out DHT production in an hour or less and DHT levels drop in to their low in an hour as DHT is metabolised by the liver. This means that the topical finasteride needs to be passing by the follicle for only 1 hour in order to do its job. 0.01mg/day in one hour through the skin would give the skin a concentration 400x that, the amount that 4mg/day would have distributed throughthe body. This is more than the 3mg that is absorbed from a 5mg proscar pill. Since 0.1mg/day does drops systemic DHT levels by only 5%, almost no one would get side effects. They'd just grow 20% more hair than they would with 1mg/day.

So 0.01mg/day is the target for those with side effects. Assume that only 1% of finasteride is absorbed through the skin. That means you would need 1mg of finasteride in your daily solution applied to your skin. So this does not cost you any more than propecia. It just gives you better results than Proscar with no side effects. If someone gets side effects, that means that more than 1% was absorbed, and they can use 0.5mg/ day in their topical instead.


Best of all, if you are sensitive to Rogaine, just use 70% isopropyl alcohol instead, and add a 2mL of oil (preferably flax or borage, but vegetable if you want) to 60mL of alcohol if even the alcohol irritates you.

 

[CCS]

Some find the blood flow rate to the scalp (volume per time)

I believe the problem with topical finasteride has two branches:

A: problems for people with finasteride side effects: 1. It leaves the scalp into the blood stream to fast. 2. Once it stops entering through the skin, and the blood has rinsed the excess into the main body and fresh blood is passing by, diffusion (always in the direction of higher concentration to lower concentration) causes finasteride to diffuse back out of the follicle and into the blood before it has bonded with most 5ar2 in the follicle.
B: problems for people who want a huge concentration in their scalp, but
don't want a huge concentration in their body: 1. Not a high enough percent of finasteride is absorbed through the skin, wasting most of it. 2. the same problems as in group B.

Goals:
To avoid side effects, most sensitive people need less than 0.04 mg entering their body, and probably as little as 0.01mg, based on graphs of DHT inhibition vs dose, and assuming DHT inhibition causes the side effects. However, they want the same concentration in their scalp that betweem 0.05 and 1mg orally would give.
Scalp megadosers would like to have the concentration in their scalp that 30mg orally would give, to REALLY inhibit DHT, but they'd prefer to pay for and subject their body to 1mg per day.

Both need it enter the scalp slowly and evenly over at about 3 hours. If it is all delivered at once, it just goes into circulation and then the follicle has none around unless the body is full enough for some to come back. It takes about 1-3 hours for most 5ar2 to bond to finasteride (Bryan, is that right?), so our vehicle must deliver the dose slowly over time, to keep the finasteride concentration in the micro arteries around the follicles high enough to balance the finasteride diffusing out of the follicles into the micro veins.

We can safely assume that all finasteride that enters the skin will go systemic eventually. Our goal should be to take advantage of the small volume of the scalp compared to the body and the flow rate of the drug into the scalp so that the concentration of drug in the small scalp is greater than the concentration in the body, even though there is more drug in the body than in the scalp.

Most of the drug enters through the pours. That is common pharmaceutical knowledge for most topicals. While a good diagram might tell us how much finasteride is likely to diffuse into the follicle directly instead of first into the blood, we know that if it has to leave the scalp eventually, it will leave through a micro vein. When the drug first enters, it will diffuse to the follicle and other structures, and it will diffuse down to the micro arteries and veins in equal amounts (50-50 chance of each). The half that enters micro veins is wasted, and the half that enters micro arteries will enter follicles and other structures so that the whole scalp is hit. Remember that veins go from the cells to the heart and arteries go from the heart to the cells.

I think the whole body has a volume of 75 L (for a 75kg person) and the blood has a volume of 11 L (please correct me on that).

For people with side effects, if everyone can handle 0.01mg per day, then that is the most we can have them absorb per day. We need a vehicle that will give them 0.01mg in 3 hours. So if our vehicle has a 0.5% penetration rate, then each dose of solution should have 2mg, which is affordable. We need a vehicle that is steady over 3 hours and has at least a 0.2% penetration rate, which is one proscar pill per day. This is very feasible.

Next, we have to know if this dose will be therapudic. In order for it to be therapudic, the finasteride in the blood in the micro arteries must be kept at at least the same concentration that 0.05mg/day orally would give. I'll say 0.2 mg/day orally, just to be safe, and will throw out the 60% absorption of the gut for further safety. We know that half our dose will be wasted since it will go straight into the micro veins. We need to know the blood flow rate of blood in the male pattern baldness part of the scalp. Someone needs to find the blood flow rate to the whole scalp, in mL per minute, which is probably in a reference somewhere.

We need to multiply the blood flow rate times 3 hours to know how much blood will flow through the follicles in 3 hours. Next, we divide 0.2mg by 75 liters, or make that 50 liters to be safe and account for bones, to get the finasteride concentration that is therapeudic. Next, we multiply this concentration by the 3 hour blood volume to get the mg finasteride that is needed to be therapudic. For the topical to work for people who are sensitive to finasteride, the number must me less than 0.01 mg.

Now 0.01 mg may be an underestimate. Some people may handle 0.05 or even 0.1 mg/day. Also, the assumption of 0.2 mg/day for therapudic needs is an overestimate, since 0.05 mg/day lowers DHT as much as 1mg/day, and any DHT inhibition is better than nothing, especially if it can be applied at the same time as minoxidil just by modifying minoxidil's vehicle.

Find me the blood flow rate through through the scalp (and I'll divide by 2 or 3 to just have the male pattern baldness area) and find a vehicle that has at least 0.2% penetration steadily over 3 hours, and I will tell you how much finasteride to put in it to give people with oral side effects the same benifits as everyone else, but without the side effects.

 

[Rage]

apply it topically untill they they get sides and know they are getting some through their skin, and then back down the dose till they go away, and then they have the ideal topical.

I've done that. I have dissolved 10mg of proscar into 60ml of minoxidil 5%. As soon as I applied it, I got nut pain soon after - seemed like my DHT levels crashed. But I continued through the month (30 days of 2x mixture) and side effects are confirmed - breast tenderness and mr.limpy.

After finishing that bottle, I'm on my second 60ml - this time with 7.5mg of finasteride. I've been on this for a week, and so far the side effects are still there - less or not I can't be sure yet.

My hair has shed badly since I stopped oral finasteride (6months) and diffused, the switch to spironolactone did not help. Sorry I can't quantify whether topical "finasteride" works because I also just recently started folligen.

 

[CCS]

topical vehicle and dosing

Rage,

Thank you for the information that 10mg monthly in minoxdil gives you side effects.

There is a faster, less expensive way to do this, if you can judge if you have side effects in less than 1 month, preferably a week.

Use your 7.5 mg/month bottle to make other dilutions with. After a week of use, if you are sure it is giving you side effects, use your dropper to put 7 mL into an empty minoxidil bottle, if you are using it twice a day, or 3.5 mL if you apply once a day. Pick your volume but just be consistent and tell us what you do. Then use that dropper (or a fresh one) to add 7 mL of fresh minoxidil from a third bottle to the second one. Mix, and you have a 1 week supply of 3.5 mg/month solution. If you want a dose with half that much finasteride, use 3.5 mL of your 7.5 mg/month solution and use 10.5 mL of fresh minoxidil. Check to see that there are 33 drops in a mL, and use this for fine tuning. It is best to go halfway between previously tried amounts, unless you think you can guess the most likely amount. Please write down the mixtures you made, how long you were on them, and how strong you think the side effects are, and find the range where the side effects start dropping off and then go to zero.

Next, cut pills in small pieces, and take them every other day if need be, and try to figure out what oral dose range the side effects taper off at. Start low. Your goal here is to figure out how finasteride made it into your system by using your side effects to measure it, and you want to do this efficiently. We can already guess the starting amount will be less than 0.1 mg per day. I hope you already experimented with this before and know a good starting point.

But before you do the topical application, we first have to make it evaporate slower. I think it might be possible to make the finasteride in you follicles 6 to maybe 12 times as concentrated for 3 hours as the finasteride in you blood after all this leaves your scalp. Hopefully the amount that does not give you side effects is high enough that 6-12 times this concentration will knock out the 5ar2 in those 3 hours, which will suppress DHT the rest of the day if not the next two days. You need a solution that will evaporate slowly, giving a steady supply of finasteride to your scalp over 3 hours.

I think you should slow the evaporation of the minoxidil by mixing glycerol and maybe some flaxseed oil into it, and you will need the glycerol to dissolve the flaxseed oil fully. But we won't do any guessing here. Buy masking tape and put five 5 inch strips next to each other on a plate to make a square. Do this only if you can't spread 1mL of minoxdil on a plate. I think the masking tape will help do this. Do this with 7 plates at once. Your 1mL dropper probably has 33 drops. Lable each plate, and squirt the following on the center of the 7 quares:

1. 33 drops of minoxidil
2. 28 drops of min with 5 drops of glycerol
3. 23 drops of min with 10 drops of gly
4. 18 drops of min with 15 drops of gly
5. 23 drops of min with 5 drops of gly and 5 drops of flaxseed oil
6. 18 drops of min with 10 drops of gly and 5 drops of flaxseed oil
7. 18 drops of min with 5 drops of gly and 10 drops of flax oil.

Smear the puddles around each plate over an area of at least 3 inches by 3 inches. Note how liquidy they feel. Come back every hour and write down how dry each one looks or feels. Continue for up to 4 hours. You can do variations on this, and pick the one that feels the least greasy and evaporates in about 4 hours so that it is still liquidy at 3 hours.

If you have a few mixtures that look good (or even if you don't) apply them to your head without finasteride for a few days to see how your scalp likes this. You can do this while you are testing the oral finasteride. Please tell us which one you thought was best.

Dilute your 7.5 mg/month solution the way I discribed in the first paragraph, but instead of 14 mL total, multiply this by 25/33 to get 10 mL and .6x33 = 20 drops. If your miture had 10 drops of glycerol, the calculation is the same but with 10 instead of 25 in the math. Write down how much of each you used, then use it for the week and record how bad your side effects were. When you get down to tollerable side effects, look back at your chart of the oral side effects and tell use what topical dose and what oval doses gave you tolerable side effects or no side effects. If this oral dose is at least 0.01 mg/day, there is a good chance you will get therapudic effects from the topical.










Flax oil is about $6 per 300mL at health food stores.

This glycerine looks a little under priced ($7.10 for 16 oz)
http://www.cqconcepts.com/chem_glycerine.php

 

[CCS]

and 10 mg per month topically is probably about 10mg*0.0076/0.6/30= 0.004 mg per day orally, as far as your system is concerned, assuming the penetration is 0.76% is occuring now. A study said that an alcohol water vehicle gives finasteride 0.76% penetration, but I don't know if your minoxidil is giving you more than that. I hope it is, because that would mean you are less sensitive. However, your scalp will get 6 to 12 times the concentration that would produce, hopefully, and that might be therapudic. I'm still trying to estimate the pathway of finasteride through the skin into the blood.

 

[Felk]

As always, this sounds very interesting, but i cant follow it, as I am no chemist.

For me, topical finasteride would only ever be a supplementary treatment, as I agree with Old Baldy in that a kitchen sink approach is always going to be the best way. Im going to use it alongside spironolactone 5% cream on the thinning areas at the front, and fluridil at night. This might seem like a lot, but i don't place muc faith in any of them really, but im hoping if i use 3, i might get lucky with 1 of them...

 

[CCS]

0.2mg/day oral finasteride regrows 80% as much hair as 1mg. 0.05mg might be the lowest therapudic oral dose, though I don't know, but 0.01mg/day will not help anyone orally. I'm looking over my math. and even if drug dose enter some arteries, and the scalp has 1/3 the blood flow rate per unit volume of flesh as the rest of the body, topical users can still only get the benifit that 0.2mg/day orally would give, and still stay below 0.02 mg/day in their body to guarantee no side effects.

Some people with side effects say they have only mild side effects on 0.25 mg/day. Others say they tried very low doses and still got them.

It looks to me like the sensitive people will not be able to get the benifits that a full propecia dose has. They can at best get the benifits that a small dose would have. As for me, my point of using topical dutasteride was to get a high dose to my scalp and not too much to my body, and save money. But if i'm only getting a 6x factor, and want the effect of 2.5mg/day, then I have to use about 0.5mg/day, which is expensive. ($60/month). But that is the price of RU.

Which do you think keeps the most androgen activity away from your androgen receptors, RU by itself, or 2.5mg dutasteride per day by itself?

If I did the RU, i'd do 0.2 mg finasteride with it just because that would take away and extra 60% of the remainder and cost almost nothing.

 

[Felk]

Im not sure if that was addressed to me (probably wasnt) but ill answer anyway.

Put it this way, if the RU one gets from Faith Eagle is good, and we mix it and apply it properly and everything, then you pretty much dont need to worry about DHT on your scalp anymore

However, Dutasteride inhibits about 90% of type 2 5AR, so this would also be very effective. Also, you know dutasteride works, and what youre getting is good quality and theres no problems with "applying" it.

The main difference I see is that RU has no side effects, apparently, whereas Dutasteride is a oral pill, and isnt approved for hair loss. Especially at 2.5mg a day, side effects could be a major factor. Also, youre on finasteride, and its working right? Why change things?

If you were dead set on comparing the two, and if side effects werent a worry, then id go for dutasteride. RU should be much better, but i cant speak for faith eagle. stax once posted that some of their substances were tested and found to be 99% pure, though im not sure where he got this figure from. People at hairsite disagree, im sure. Anyway i wont go over the long RU discussion again... Dont get me wrong, Im still very interested in the stuff...

 

[CCS]

yeah, the 90% reduction of scalp DHT (98% in the follicle) sounds good to me. tempting to do avodart once a day, but pricy. i'm thinking of doing it once every 4 days so I get a litle more than the effect of a full proscar pill, but at the price of 1.25 mg.

Bryan, does 0.5mg dutasteride / day inhibit 98% of DHT from 5ar2? and Finasteride 5mg about 80%? I think I read that but that sounds like a lot.

 

[Rage]

Re: topical vehicle and dosing

*snip snip*

Your 1mL dropper probably has 33 drops. Lable each plate, and squirt the following on the center of the 7 quares:

1. 33 drops of minoxidil
2. 28 drops of min with 5 drops of glycerol
3. 23 drops of min with 10 drops of gly
4. 18 drops of min with 15 drops of gly
5. 23 drops of min with 5 drops of gly and 5 drops of flaxseed oil
6. 18 drops of min with 10 drops of gly and 5 drops of flaxseed oil
7. 18 drops of min with 5 drops of gly and 10 drops of flax oil.

Smear the puddles around each plate over an area of at least 3 inches by 3 inches. Note how liquidy they feel. Come back every hour and write down how dry each one looks or feels. Continue for up to 4 hours. You can do variations on this, and pick the one that feels the least greasy and evaporates in about 4 hours so that it is still liquidy at 3 hours.

*snip snip*

Wholey crap! You can certainly see the chemical engineer in you..



I assume you are suggesting that by slowing the release of finasteride into the scalp, it would replace the finasteride that diffuses out of the follicles and into the blood stream? There is one thing you are missing - finasteride is an irreversible inhibitor! After binding the enzyme, the complex is stable and the finasteride will not dissociate.

Lots of biochemical information here:
http://finasteride.health-effects.net/

So, if the finasteride does reach the follicle (from side effects, I know it reaches systematically), it will permanently bind DHT. Where your suggestion does have merit is that the finaseride/DHT complex may take some time to form - hence the need for a solution that evaporates slower. However, the link doesn't say how slow is "slow". People with some time on their hands, and a sizeable brain, take a look at this article on the kinetics of complex formation:

http://pubs.acs.org/cgi-bin/abstract.cg ... 3069t.html

It may be entirely possible that the 10 minute time frame offered by the finasteride/minoxidil solution is sufficient for total inhibition. Maybe..


I think I'm going to stick with the 1month trials of each finasteride concentration, as I am also not sure 1 week is sufficient time to gauge side-effects. Perhaps other people want to give this a try? A 1 person trial isn't exactly statistically significant ;p

 

[Rage]

Re: topical vehicle and dosing

(double post)

 

[CCS]

from the graphs I looked at, it appeared to me that it took at least an hour and maybe 3 hours for 60-80% of the finasteride that would complex that day, to complex that day. However, the graphs were estimated, not measured, by the scientists. They were graphs of 5ar2 concentrations vs time in days after daily doses of finasteride 5mg, and were presented along side graphs of dutasteride at different doses. I'm sure bryan will know what graphs i'm talking about and if there are any that show hour by hour estimated levels. he can also comment on how accurated those estimated graphs likely are. i have to go now, and can't post the link just yet.

at least with monthly trials, there will be no questions as to whether the side effects are genuine. thank you for you efforts.

 

[CCS]

i'll read that link later. if it complexes fast enough, we may just need a carier that will get it into the follicle.

 

[Bryan]

Bryan, does 0.5mg dutasteride / day inhibit 98% of DHT from 5ar2? and Finasteride 5mg about 80%? I think I read that but that sounds like a lot.

Do you still have that link I provided a week or two ago to the graphs in the Gisleskog et al studies? They do show that 0.5 mg/day of dutasteride inhibits the type 2 enzyme by around 98% to 99%. Finasteride at 5 mg/day inhibits it at what looks like a daily average of around 90%.

Bryan

 

[CCS]

hope for topical finasteride

we know that topical spironolactone and topical fluridil get into follicle where the androgen receptor is, right? that means that at least some chemicals can get in there, though I don't know the pathway. if either went into the blood first, it would be very ineffective, unless it was just breifly in a micro artery.

as for the vehicle, fluridil uses almost 100% isopropyl alcohol, and minoxdil is most efficient with 90% alcohol. if minoxidil is to protect blood vessels, it has to get to the micro arteries that supply the follicle, not just the veins it dumps into. So it seems entry into the arteries does occure. now finasteride and dutasteride might behave differently.

if anyone wants to know the minimum about of systemic finasteride they can handle each day, they should dissolve their finasteride in ethanol and use the dropper to deliver individual drops orally. this is much more accurate than guessing at chip sizes, or even using a balance since the balance can't be repeated the next time.

It you get 90% of the finasteride because of non-perfect grounding and small lactose affinity, that is 4.5 mg of finasteride in 60 mL. next count the number of drops per mL. Brian got 33 on his, i got 36 on mine. 4.5mg/34/60 = 0.002 mg/day. 0.01 mg per day is supposed to lower DHT levels by 5% and 0.05mg/day is supposed to do 70%. That is 5 drops and 25 drops. Would someone please test that the first does not give side effects and the second one does? If you are using propecia, that is 5 tablets instead of 1, if it has 1mg.

but some people here get less side effects on 1/4 tablet, so who knows what is going on, or if that 0.05mg figure in the graph I saw was right.

 

[Rage]

Just a bit of an update:

I don't have finasteride related side effects anymore!!!

This is using finasteride dissolved in 5% minoxidil, giving an average of 0.25mg / day.