Description

dihydro-testosterone, which is -methyl compound of 5 Mesterolone is the 1 considered to be the proper active androgen in many androgen-dependent target organs. Proviron is an oral androgen preparation which has only a slight central inhibitory effect and, consequently, no restrictive effect on testicular function. Proviron balances a deficiency of androgen formation which begins to fall gradually with increasing age. Therefore, Proviron is suitable for the treatment of all conditions caused by deficient endogenous androgen formation. In the recommended therapeutic dosage, Proviron will not impair spermatogenesis. Proviron is especially well tolerated by the liver. PHARMACOKINETICS AND METABOLISM Following oral ingestion mesterolome is rapidly and almost completely absorbed in a wide dose range of 10 – 100 mg. The intake of Proviron generates maximum serum drug levels of 3.1 1.1 mg/ml after 1.6 0.2 hours. Thereafter drug levels in serum decrease with a terminal half-life of 12 13 hours. Mestorelone is bound to serum proteins by 98%. Binding to albumin accounts for 40% and binding to SHBG to 58%. Mestorelone is rapidly inactivated by metabolism. The metabolic clearance rate from serum accounts for 4.4 1.6 ml. min 1.kg1 . There is no renal excretion of unchanged drug. The main metabolite has been identified as 1- methyl-androsterone, which – in conjugated form – accounts for 55 – 70% of renally excreted metabolites. The ratio of main metabolite glucoronide to sulphate was about 12:1. As a further metabolite 1- methyl- 5androstane-3, 17- diol has been recognized, which accounted for about 3% of renally eliminated metabolites. No metabolic conversion into estrogens or corticoids has been observed. In form of metabolites mesterolone is excreted by about 85% of dose with the urine and by about 14% of dose with the faeces. Within 7 days 93% of dose have been recovered in excreta, the half of which had been excreted within 24 hours.

Usual dose:

Proviron 50 mg every 12 hours.