Proviraplex Axiolabs

Description

Pharmacodynamics

Proviron is an active androgen intended for oral administration. The presence of a methyl group at position C-1 determines the special properties of this steroid, which, unlike testosterone and all its derivatives used for androgen therapy, is not metabolised to estrogen.

This difference explains the fact that at usual therapeutic doses in healthy men, Proviron slightly inhibits the synthesis of gonadotropin by the pituitary gland, and, accordingly, there is no decrease in spermatogenesis. Unlike other androgens that replace endogenous androgens and inhibit their synthesis, Proviron complements the effect of endogenous androgens.

Also, unlike other androgens active when administered orally, Proviron is very well tolerated by the liver (which is probably due to the absence of a 17-alkyl steroid substituent).

Pharmacokinetics

After oral administration, mestenerolone is rapidly and almost completely absorbed in the dose range of 25-100 mg. The maximum serum concentration of 3.1 ± 1.1 ng/ml is reached in 1.6 ± 0.6 hours after taking Proviron.

In view of this, the level of active substance in the blood serum decreases with a final half-life of 12-13 hours. 98% of mestenerolone is bound to serum proteins: 40% of mesterolone is bound to albumin and 58% to sex hormone binding globulin (SHBG).

Mesterolone is rapidly metabolised. The rate of metabolic clearance from the blood serum is 4.4±1.6 ml-min-1-kg-1. The substance is not excreted unchanged by the kidneys. The main metabolites are 1α-methyl androsterone, which in conjugated form makes up 55-70% of the metabolites excreted by the kidneys. The ratio of glucoronides of the main metabolite to sulfates is about 12:1. The other metabolite is 1α-methyl-5α-androstane-3α,17β-diol, which accounts for about 3% of metabolites excreted by the kidneys. No metabolic transformations into estrogens or corticoids have been observed. 77% of the dose of mestenerolone is excreted in the form of metabolites in the urine, and approximately 13% of the dose is excreted in the faeces. Within 7 days, 90% of the administered dose was detected in urine and faeces, of which 50% was excreted in the urine within the first 24 hours.

The absolute bioavailability of mestenerolone is approximately 3% of the dose administered orally.