Review of oxymetholone: a 17α-alkylated anabolic-androgenic steroid

doi:10.1016/S0149-2918(01)80070-9

Clinical Therapeutics

Volume 23, Issue 6, June 2001, Pages 789-801

https://doi.org/10.1016/S0149-2918(01)80070-9 Get rights and content

Abstract

Background: Oxymetholone (17β-hydroxy-2-[hydroxymethylene]-17-methyl-5α-androstan-3-one) is a 17α-alkylated anabolic-androgenic steroid and a synthetic derivative of testosterone. It has been approved by the US Food and Drug Administration for the treatment of anemias caused by deficient red cell production.

Objectives: This review summarizes the pharmacokinetics, current and future clinical applications, and adverse effects of oxymetholone. Relevant studies were identified using a search of MEDLINE^® through March 2001, supplemented by conference abstracts and presentations.

Results: Because of its anabolic properties, oxymetholone has been studied for the treatment of HIV-associated wasting, antithrombin III deficiency, pediatric growth impairment, and damaged myocardium, with varying degrees of success. Hepatotoxicity is a major adverse effect associated with the use of oxymetholone, with cholestatic jaundice the most important hepatic side effect. Less common hepatic side effects associated with the use of anabolic-androgenic steroids include peliosis hepatis and formation of hepatic tumors. All anabolic-androgenic steroids can cause androgenic side effects, including acne, hirsutism, hair loss, clitoral/phallic enlargement, vocal changes, erectile tissue stimulation, gynecomastia, amenorrhea, and changes in libido and sexual potency.

Conclusions: As is the case with many anabolic-androgenic steroids, few pharmacokinetic and tolerability studies were performed before oxymetholone's approval in the 1960s. It has proved, however, to be an appropriate treatment choice for selected patients with anemia, if carefully monitored.

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Review of oxymetholone: a 17α-alkylated anabolic-androgenic steroid

Abstract

Am J Med

Am J Cardiol

Steroids

J Steroid Biochem Mol Biol

Blood

Blood

Am J Med

Blood

Blood

Über kristallines männliches hormon aus hoden (testosteron), wirksamer als aus harn oder cholesterin bereitetes androsteron

Hoppe Seylers Z Physiol Chem

Metabolism of anabolic androgenic steroids

Clin Chem

Androgens

Steroids. CV. 2-Methyl and 2-hydroxymethylene-androstane derivatives

J Am Chem Soc

Effects of various 17 alpha-alkyl substitutions and structural modifications of steroids on sulfobromophthalein (BSP) retention in rabbits

Steroids

Relative potency of steroids in an anabolic-androgenic assay using the castrated rat

Endocrinology

Oxymetholone promotes weight gain in patients with advanced human immunodeficiency virus (HIV-1) infection

Br J Nutr

Oxymetholone therapy in patients with familial antithrombin III deficiency

Thromb Haemost

Study of an anabolic steroid. Certain effects of oxymetholone on small children

Am J Dis Child

Bone growth in nonambulatory children on oxymetholone and fluoride therapies

Growth

Absorption, metabolism, and excretion of oral testosterone in humans by mass fragmentography

J Clin Endocrinol Metab

Metabolism of an anabolic androgenic steroid, oxymetholone, by human cytochrome P450s

Clin Pharmacol Ther