Cyclosporine A increases 5AR & Adiol-G activity.

Therapeutic Efforts Pharmaceutical
#1

Unfortunately, this is an immune surpressant drug typically given to prevent organ transplant failure and can cause many serious side effects.

Still, interesting to note the effects in this study.

Increase in plasma 5 alpha-androstane-3 alpha,17 beta-diol glucuronide as a marker of peripheral androgen action in hirsutism: a side-effect induced by cyclosporine A.

ncbi.nlm.nih.gov/pubmed/2137888

Dose-dependent hypertrichosis is a common dermatological side-effect affecting the majority of patients treated with cyclosporine A (CSA). Previous studies have not demonstrated the influence of CSA on specific sex hormone levels. The aim of this study is to investigate whether CSA increases the activity of 5 alpha-reductase, an enzyme which transforms androgens into dihydrotestosterone in peripheral tissues.

The metabolite which best reflects this activity is 5 alpha-androstane-3 alpha,17 beta-diol glucuronide (Adiol G). The study was carried out on 49 insulin-dependent diabetes patients participating in the double-blind “Cyclosporine-Diabète-France” clinical trial, of which 28 were treated with CSA (16 males and 12 females), and 21 received only placebo (10 males and 11 females).

All patients underwent extensive clinical and laboratory evaluations prior to and during the present study. In addition to Adiol G, testosterone (T), dehydroepiandrosterone sulfate (DHEA S) and sex hormone-binding globulin (SHBG) were assayed. Levels of Adiol G increased significantly in CSA-treated groups: males, 11.86 +/- 2.58 vs 7.83 +/- 2.30 nmol/l; females, 4.48 +/- 2.70 vs 2.10 +/- 1.22 nmol/l; P less than 0.02 (comparison of means).

There were no significant differences in this parameter before and during treatment in either the male or female placebo groups (paired t-test). During the treatment period, T, DHEA S, SHBG and the T/SHBG ratio did not significantly change with respect to their baseline values in any of the groups studied (comparison of means). Comparison (using paired t-test) showed a significant increase of DHEA S in CSA-treated groups: males, delta = 3.08 +/- 3.33 nmol/l, P less than 0.01; females, delta = 0.98 +/- 1.13 nmol/l, P less than 0.05.

In conclusion, it is possible that CSA induces hypertrichosis or hirsutism by increasing 5 alpha-reductase activity in peripheral tissues. Nevertheless the role of increased DHEA S as a possible Adiol G precursor cannot be excluded.

PMID: 2137888 [PubMed - indexed for MEDLINE]

#2

Another article on this

rheumatology.oxfordjournals.org/ … /4/433.pdf

It seems this drug does a good job in raising Adiol-G levels…the safety of it…im more concerned about…

#3

Will the 3AdiolG levels remain elevated after the the end of the treatment… I’d be willing to try.

#4

Has anyone tried this? I’m not seeing any other methods for increasing 3-adiol G.

#5

Greater conversion of testosterone to 5 alpha-dihydrotestosterone, reflecting increased peripheral 5 alpha-reductase activity in nude mice treated with high doses of cyclosporine A.

Following cyclosporine A (CsA) immunosuppressive therapy in kidney grafts, increased body hair growth (hypertrichosis and/or hirsutism) without significant variation in normal circulating plasma androgen levels (as observed in idiopathic hirsutism) has been reported by several authors. Other authors have described increased hair growth in nude mice treated with CsA. In order to evaluate the action of this drug in target tissues, using dorsal skin homogenates from nude mice treated with various doses of CsA, we measured the metabolic conversion of testosterone (T) to its 5 alpha-reduced products, reflecting 5 alpha-reductase activity (5 alpha-RA). Three groups of 5 female nude mice were treated with an oral suspension containing CsA 5 mg/kg (group 1), 25 mg/kg (group 2) and 100 mg/kg (group 3), respectively, and the results, including 5 alpha-DHT and Adiol formation, were compared with those obtained in a control group (n = 5) receiving only the olive oil vehicle. Cutaneous metabolic conversion of T was determined using tritiated T as substrate. After 1 h of incubation, 5 alpha-DHT and other 5 alpha-reduced products formed were separated and quantified using a reverse-phase chromatography column fitted to a flow-through radioactivity detector. Mean +/- SD 5 alpha-DHT formation (expressed as pmol per 100 mg of protein per h) was found to be increased in the treated groups (group 1: 3.17 +/- 0.37, group 2: 3.10 +/- 0.13, group 3: 4.26 +/- 0.20), respectively 7.5% (NS), 5.10% (NS) and 44.4% (P = 0.01) higher than in the control group (2.95 +/- 0.13). In addition to 5 alpha-DHT, enhanced formation of delta 4-androstenedione (delta 4), 5 alpha-androstan-3 beta,17 beta-diol (3 beta-diol) and 5 alpha-androstan-3 alpha,17 beta-diol (3 alpha-diol) were also observed in the treated groups. These results show a significantly increased formation of 5 alpha-DHT (and Adiol) in nude mice treated with high dose-levels of CsA.

ncbi.nlm.nih.gov/pubmed/2214776

#6

what are the serious side effects?

#7

I’ve seen blood test where someone used DHEA to drive up the 3-Alpha-Diol-G. Still not safe, but safer than this. He didn’t feel any better and his 3adG’s were out of this world high. This shows that fat men have high 3-alpha-diol-G numbers. ncbi.nlm.nih.gov/pubmed/3654916. I found another one on how 3-alpha-diol-G is made mainly in the liver and inst a good reporting tool for intracellular androgen activity, but I’ll have to find it later. I’m off to trick-or-treat.

#8

Been on cyclosporine for 2 months and has really helped my digestive problems and now I can say that I am about 75% back to normal regarding to ED, and libido, still hasn’t helped my “worst symptom” horrible brain fog(complete cognitive shift), but it has helped how food effects my brain fog etc.

Definitely helps, just have to get my creatinine levels check every month for kidney function

Out of all the meds I tried (30+ Rx, Countless supplements) Cyclosporine(for Sexual, digestive), Ritalin(for motivation, energy), tianpetine(helps a bit for brain fog) are the only ones that have helped

#9

What’s the update on the meds??? Are you recovered? What was the dose? I may want to try this even at the risk of messing up my immune system.

#10

What’s the update on this? What was your dose? I’m interested! Did you recover your dht and 5a?