Table 1419

Anabolic Activity of 17 Methyl Derivatives

Androgenic: Agent Anabolic Activity

Indications

Hepatotoxicity

Testosterone Nandrolone Oxymetholone Oxandrolonea

Hypogonadism

Anemia

Anemia

Loss of body weight from injury or Mild, rare infection

Moderate to severe Severe aThe anabolic steroid oxandrolone is the only approved drug for restoration of lost body weight and lost lean mass.

The quality of a testosterone analog is determined by the ratio of androgenic to anabolic activity — the lower the better. A low value indicates very little masculinizing effects compared to a very potent anabolic effect (Table 14.19).

The anabolic steroid oxandrolone also happens to have the greatest anabolic and least androgenic side effects in the class of anabolic steroids.112 Oxandrolone is the only steroid that has a carbon atom within the phenanthrene nucleus that has been replaced by another element, namely, oxygen. In addition, oxandrolone is cleared by the kidney and not the liver, so hepatotoxicity is rare.

Clinical Use of Anabolic Steroids (Effect on Lean Body Mass)

Most of the recent studies on anabolic steroids and lean body mass have used the anabolic steroid oxandrolone (Table 14.20).112-121

Oxandrolone is a 17-P-hydroxy-17-a-methyl ester of testosterone that is cleared primarily by the kidney. Hepatotoxicity is minimal, even at doses higher than the 20 mg/d recommended by the U.S. Food and Drug Administration (FDA). Oxandrolone has potent anabolic activity, being up to 13 times that of methyltestosterone. In addition, its androgenic effect is considerably less than testosterone, minimizing this complication common to other testosterone derivatives. The increased anabolic activity and decreased androgenic (masculinizing) activity markedly increase its

Oral 17-a analog Metabolized mainly by kidney Not hepatotoxic

Readily absorbed by intestine with 99% bioavailability

Biologic life of 9 to 12 h

Highly anabolic

Minimal androgenic effects

TABLE 14.20 Oxandrolone

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