Oral activation of steroids has usually been accomplished by the introduction of a 17 a-alkyl substitute into the molecule. The presence of the alkyl group affects the metabolic course of the steroid by preventing its excretion as a 17 -ketosteroid. The presence of the alkyl group, however, is responsible for undesirable side-effects including hepatotoxicity. 17 a-alkyl substitutes have been reported to cause reversible, intrahepatic, obstructive jaundice due to cholestasis (Peters, 1958; Kaupp, 1962; Gilbert, 1963; Hogarth, 1963). Methenolone (dianabol), an orally active agent lacking the 17a-alkyl group, also caused changes in sulfobromophthalein retention and an increase in blood coagulation factors V and X (Kruskemper, 1966).
Oral steroids are generally not as active due to inactivation; therefore larger doses must be taken. Injectable steroids are as a rule low in hepatotoxicity and other side-effects associated with oral steroids. Dosage can also be maintained at lower levels. During "stacking," a method used to achieve a proper or desired ratio and effect, orals can effectively be utilized. Esterification of steroids
The formation of esters is an effective means of protection against metabolic inactivation and also produces a prolonged effect. oral steroids for sale The 17-B-hydroxy esters are an important group of steroids in this regard (acetates, propionates, n decanoates, plienylpropionates).
The esters of testosterone exhibit slightly higher values because of their resistance to metabolic inactivation and prolonged biological effect.
The esters, propionate, cypionate and enanthate are the most commonly used by athletes. The propionate form in aqueous solution is more androgenic than in the oil form, and is used by power lifters to attain a peak level in a short period of time. The cypionate and enanthate forms have duration of two to three weeks, the enanthate having a slightly longer duration than the cypionate.
The esters of testosterone produce excellent results, with low hepatotoxicity in subcutaneous form. Testosterone can be aromatized to estrogens and we have noted side-effects caused by this conversion, i.e., gynecomastia. Other common side-effects noted are:
1. acne 2. testicular degeneration 3. increased and/ or decreased libido These have all been seen to be temporary and reversible.
Dromostanolone is metabolized quickly and must be administered frequently. Dromostanolone is rather weak in biological activity.
Water retention and hypercalcemia are frequent problems with Dromostanolone. Conversion to estrogen in vivo is also a factor in the use of Dromostanolone. Oxymetholone is a potent, orally active anabolic agent with low androgenic activity. However, in doses required to achieve good anabolic effect considerable side-effects are noted (hypophysis inhibition; antiICSH effect).
Glucose tolerance is altered with prolonged use, producing hypoglycemic effect. Edgren (1963) has also reported that the androgenic response with anadrol is markedly higher than indicated by seminal vesicle studies. Oxymetholones popularity with powerlifters also indicates greater androgenic effect than research indicates. It also comes in high dosage per tablet (50 m.g./ tablet).