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Published in the Bulletin of Experimental Treatments for AIDS July 1998 issue, by the San Francisco AIDS Foundation. |
DRUG WATCH: OxymetholoneBy Mark Bowers HistoryThe anabolic steroid oxymetholone was developed in 1960 in Mexico as a treatment for anemia that did not respond to standard treatment. However, better treatments (see the article Epoietin Alfa (EPO) for Anemia, this issue) have since all but eliminated the use of anabolic steroids for anemia. Instead, anabolic steroids now play an important role in the aggressive treatment of wasting associated with HIV and other diseases, and may in some cases be used to restore lean body mass after surgery or chemotherapy. Counterfeits of oxymetholone brands command high prices on the black market in Europe, the U.S. and Australia. Unimed Pharmaceuticals of Buffalo Grove, IL, began marketing oxymetholone under the trade name Anadrol-50 in March 1998. Anabolic and Androgenic SteroidsOxymetholone is both an anabolic and an androgenic steroid. Anabolic steroids are named for their ability to promote anabolism, or increased production of protein and lean body mass. Androgenic steroids include the hormone testosterone and many synthetic steroids (e.g., oxandrolone [Oxandrin], nandrolone decanoate [Deca-Durabolin], stanozolol [Winstrol]). Androgens stimulate the development of male sexual characteristics, including growth of facial and pubic hair, enlargement of the genitals, deepening of the voice, increased muscle bulk and increased libido. They also increase the secretion of sebum, which may lead to acne and promote male pattern baldness. The most androgenic steroid is testosterone, and all synthetics are indexed by comparison with testosterone. Oxymetholone is about one-half as androgenic as testosterone, more than most other synthetic steroids. Side effects are rarely associated with the anabolic properties of steroids, but are common with the androgenic properties that are, to a greater or lesser degree, associated with all anabolic hormones and drugs. WastingOxymetholone was FDA-approved as an oral treatment for anemias caused by deficiency in red blood cell production; other uses are considered off-label and may not be reimbursed by third party payers such as health maintenance organizations and private health insurance companies. Furthermore, the drug is a controlled substance listed in Schedule III with other drugs that have a significant potential for abuse. Many physicians prefer to treat wasting with appetite stimulants (e.g., megestrol acetate [Megace], dronabinol [Marinol] or medical marijuana), nutritional supplements and cytokine-modulating drugs (e.g., pentoxifylline or thalidomide) before they suggest anabolic steroids. Testosterone levels may be checked in men with HIV and, when found to be low or low-normal, testosterone injections, scrotal or skin patches or sublingual (under the tongue) tablets may be prescribed (for use of testosterone in HIV positive men with normal testosterone blood levels, see Research Notes, this issue). Oxandrolone and nandrolone decanoate are other anabolic steroids that have been studied for the treatment of HIV-associated wasting. Some studies include the participation of women, and at least one admits only women. DosageThe recommended daily dose of oxymetholone in children and adults is 1-5 mg/kg of 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. Use of anabolic steroids in children is accompanied by the serious risk of interrupting normal growth. When they are used in children, careful X-ray bone studies should be done every 6 months to ensure that normal bone growth continues. EffectsOxymetholone promotes rapid weight gain because of an increase in lean body mass -- particularly when use of the drug is accompanied by a program of strenuous progressive resistance exercise. Physicians and patients may choose to monitor the effects of this weight gain using bioimpedance analysis (BIA) or dual energy X-ray analysis (DEXA) to ensure that lean body mass increases rather than fat mass. Only adequate lean body mass is associated with increased survival among people who are wasting or at risk of wasting. Increased fat stores are irrelevant to this goal. Negative Side EffectsMany side effects have reportedly been associated with chronic use of high doses of all oral anabolic-androgenic hormones including oxymetholone: high blood pressure, water retention, prostate gland enlargement, gynecomastia (abnormal breast tissue growth in males) and liver damage. Oxymetholone is the anabolic steroid most associated with premature hair loss. As with all oral anabolic-androgenic hormones, routine blood tests from people taking oxymetholone show unusual levels of blood lipids (fats), including lowered high density lipoprotein (HDL) and elevated low density lipoprotein (LDL) cholesterol. Rarely are these drugs associated with diarrhea, nausea or vomiting. A 1990 non-scientific poll of 563 U.S. athletes who used anabolic steroids surveyed reasons for drug use, drug sources, perceived effectiveness, side effects and drug preferences. While Anadrol-50 received the greatest number of first-place rankings for effectiveness, it was also associated with the greatest number of troublesome side effects. At least 75% of the steroids used by respondents were counterfeit and obtained illegally, and most were used in doses far higher and for a longer period than most physicians would prescribe. Athletes who use anabolic steroids often use more than 1 at a time, a fact that must be considered when evaluating the potential effects and side effects of oxymetholone. InteractionsConcerns about drug interactions have increased because of the widespread use of combination highly active antiretroviral therapy (HAART). The protease inhibitor drugs that form the backbone of this strategy are broken down and eliminated in the liver by a group of enzymes called the cytochrome P450 system. Anadrol-50 does not interact with cytochrome P450 3A4, the most common enzyme in HIV drug metabolism, so there is no expected interaction with the protease inhibitors indinavir (Crixivan) and ritonavir (Norvir), nor with the antibiotics clarithromycin (Biaxin) and itraconazole (Sporanox). There is some interaction with the antacid cimetidine (Tagamet), the commonly used antidepressant paroxetine (Paxil) and the psychiatric medication haloperidol (Haldol). Patient Assistance Program and Reimbursement Assistance ProgramUnimed will provide assistance to patients who are denied coverage for the cost of Anadrol-50 by their insurance carriers. Call 800-256-8918. Mark Bowers is Managing Editor of treatment publications at the San Francisco AIDS Foundation.
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