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Metabolic Actions
Compounds in this class also may cause retention of nitrogen, sodium, potassium, and phosphorous, and decreased urinary excretion of calcium. Androgens have been reported to increase protein anabolism and decrease protein catabolism. Nitrogen balance is improved only when there is sufficient intake of calories and protein. Androgens have been reported to stimulate production of red blood cells by enhancing production of erythropoietic stimulation factor.
Pharmacokinetics
The compound is mainly eliminated by metabolism, renal excretion of metabolites accounting for 95% of dose. The excretory balance of 14C-compounds in urine and feces totals up to 98.9+/-0.8% of the i.v. dose after 168 h. The 14C-compounds in plasma and urine were separated by HPLC, and three major metabolites were submitted to structural analysis by MS, NMR and UV spectroscopy. One of the metabolites is the direct 4-O-glucuronide of formestane. The other two represent 3-O-sulfates of the exocons 3beta,4beta-dihydroxy-5alpha-androstane-17-one and 3alpha,4beta-dihydroxy-5alpha-androstane-17-one, their ratio being 7:3. These exocons are formed by stereoselective 3-keto reduction, accompanied by reduction of the 4,5-enol function. The exocons do not inhibit human placental aromatase activity in vitro. 5
The half-life orally was approximately 3 h, whereas the apparent half-life of injected drug was between 5 and 10 days after a more rapid clearance during the first 4 days after injection. The formulated material achieved a significantly higher mean peak concentration (88% greater than that obtained using the unformulated powder) and a higher mean AUC (not significant). The median time to peak was 1.5 h for both preparations and the elimination rate constants were similar (0.31 for micronized 4-OHA and 0.36 h-1 for formulated 4-OHA). Significant biological activity was demonstrated with the formulated material in its suppression of plasma oestradiol levels. 6
Efficacy Studies
Subcutaneous treatment of immature male rats with an estrogen precursor, 19-hydroxy-testosterone (19-OHT), at a daily dose of 1 mg/animal for 14 days leads to a significant decrease in the weight of testis, ventral prostate and seminal vesicle. The peripheral levels of LH are lowered. Testicular histology indicates that the effects of 19-OHT are very similar to the known of effect induced by estradiol-17 beta. 19OHT induces a marked impairment of spermato and spermiogenesis. The maturation division is completely inhibited. The effect of 19-OHT on spermatogenesis is partially reversed by concomitant administration of an aromatase inhibitor (4-acetoxy-4-androstene-3.17-dione, (4-AA] at a dose of 1 mg/animal/day s.c. Meiotic activity is restored, and the weights of genital organs and the serum LH values increase. 4-AA alone has no appreciable effect on the parameters examined in this study. The present results suggest that specific inhibitors of estrogen biosynthesis might not only be useful to investigate the patho-physiological role of estrogens on spermatogenesis. 7
Clinical Studies
Another interesting note is the ability of 4-Androsten-4-ol-3, 17-dione acetate to directly stimulate testosterone whether in the presence of LH or not. Researchers examined the effects of placebo, luteinizing hormone (LH), 4-acetoxy-4-androstenedione, and luteinizing hormone (LH) plus 4-acetoxy-4-androstenedione on rat follicles in vitro. In regards to testosterone they found that within the first 8 hours 4-acetoxy-4-androstenedione had the ability to directly stimulate testosterone alone and greatly stimulate testosterone in combination with luteinizing hormone (LH). Interestingly enough within the next 16 hours they discovered 4-acetoxy-4-androstenedione alone was stimulating testosterone 3 times as much as luteinizing hormone (LH) while the combination also continued to stimulate testosterone. 8
INDICATIONS AND USAGE
Primobolan Acetate [4-Androsten-4-ol-3beta,17beta-dione Acetate for oral ingestion] is indicated for the long-term promotion of testosterone and regulation of estrogen in humans.
DOSAGE AND ADMINISTRATION
As a dietary supplement, take 1 to 2 tablets 3 times daily. Do not exceed recommended dose. 9The recommended daily dose in adults is 1-5 mg/kg body weight per day. The usual effective dose is 1-2 mg/kg/day but higher doses may be required, and the dose should be individualized. Response is not often immediate, and a minimum trial of three to six months should be given.
CONTRAINDICATIONS
Not to be used with any other medications especially oral hypoglycemic agents ie. Glyburide. 10
WARNINGS
Primobolan Acetate™ should not be used by children, during pregnancy, or by anyone contemplating pregnancy.
PRECAUTIONS
Do not use with any type of medication and use by individuals with any pre-existing medical condition is not recommended.
ADVERSE REACTIONS
With regard to toxicity, one patient developed a transient skin rash and another patient some facial swelling. A further patient developed a transient leucopaenia and treatment was therefore discontinued. Twenty-seven of the 30 evaluable patients (90%) experienced no side effects. These results indicate that oral administration is acceptable. 11
OVERDOSAGE
The recommended dosage of Primobolan Acetate™ should not be exceeded. Acute overdosage could lead to headache, nausea, vomiting, and/or hypoglycemia.
Manufacturer
PROMATRIX Biotechnologies
Packaged Weight: .4 Lbs.
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