Review of oxymetholone: a 17alpha-alkylated anabolic-androgenic steroid.

Article Details

Citation

Pavlatos AM, Fultz O, Monberg MJ, Vootkur A, Pharmd

Review of oxymetholone: a 17alpha-alkylated anabolic-androgenic steroid.

Clin Ther. 2001 Jun;23(6):789-801; discussion 771.

PubMed ID
11440282 [ View in PubMed
]
Abstract

BACKGROUND: Oxymetholone (17beta-hydroxy-2-[hydroxymethylene]-17-methyl-5alpha-androstan-3-one) is a 17alpha-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.

DrugBank Data that Cites this Article

Drugs
Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
Oxymetholone3-oxo-5-alpha-steroid 4-dehydrogenase 1ProteinHumans
No
Substrate
Activator
Details
OxymetholoneCytochrome P450 2D6ProteinHumans
Unknown
Inhibitor
Details