DESCRIPTION OF ANDROLIC (Anapolon / Oxymetholone)
Androlic (oxymetholone) Tablets for oral administration each contain 50 mg of the steroid oxymetholone, a potent anabolic and androgenic drug.
The chemical name for oxymetholone is 17ß-hydroxy-2- (hydroxymethylene)-17-methyl-5a-androstan-3-one.
CLINICAL PHARMACOLOGY OF ANDROLIC (Anapolon / Oxymetholone)
Anabolic steroids are synthetic derivatives of .
Anabolic steroids may cause suppression of clotting factors II, V, VII and X, and an increase in prothrombin time.
Information for the patient:
The health care provider should instruct patients to report immediately any use of warfarin and any bleeding.
The health care provider should instruction patients to report any of the following side effects of androgens.
Adult or Adolescent Males: Too frequent or persistent erections of the penis, appearance or aggravation of acne.
Women: Hoarseness, acne, changes in menstrual periods or more hair on the face.
All Patients: Any nausea, vomiting, changes in skin color or ankle swelling.
Women with disseminated breast carcinoma should have frequent determination of urine and serum calcium levels during the course of androgenic anabolic steroid therapy (see WARNINGS).
Because of the hepatoxicity associated with the use of 17-alpha-alkylated androgens, liver function tests should be obtained periodically.
Periodic (every 6 months) x-ray examinations of bone age should be made during treatment of prepubertal patients to determine the rate of bone maturation and the effects of androgenic anabolic steroid therapy on the epiphyseal centers.
Anabolic steroids have been reported to lower the level of high-density lipoproteins and raise the level of low-density lipoproteins. These changes usually revert to normal on discontinuation of treatment. Increased low-density lipoproteins and decreased high-density lipoproteins are considered cardiovascular risk factors. Serum lipids and high-density lipoprotein cholesterol should be determined periodically.
Hemoglobin and hematocrit should be checked periodically for polycythemia in patients who are receiving high doses of anabolics.
Because iron deficiency anemia has been observed in some patients treated with oxymetholone, periodic determination of the serum iron and iron binding capacity is recommended. If iron deficiency is detected, it should be appropriately treated with supplementary iron.
Oxymetholone has been shown to decrease 17-ketosteroid excretion.
Warfarin: Clinically significant pharmacokinetic and pharmacodynamic interactions between anabolic steroids and warfarin have been reported in healthy volunteers. When anabolic steroid therapy is initiated in a patient already receiving treatment with warfarin, the INR (international normalized ratio) or prothrombin time (PT) should be monitored closely and the dose of warfarin adjusted as necessary until a stable target INR or PT has been achieved. Furthermore, in patients receiving both Androlic Tablets and warfarin, careful monitoring of the INR or PT and adjustment of the warfarin dosage,
if indicated, are recommended when the Androlic dose is changed or discontinued.
Patients should be closely monitored for signs and symptoms of occult bleeding.
Anticoagulants: Anabolic steroids may increase sensitivity to oral anticoagulants. Dosage of the anticoagulant may have to be decreased in order to maintain the desired prothrombin time. Patients receiving oral anticoagulant therapy require close monitoring, especially when anabolic steroids are started or stopped.
Drug/Laboratory Test Interferences:
Therapy with androgenic anabolic steroids may decrease levels of thyroxine-binding globulin resulting in decreased total T4 serum levels and increased resin uptake of T3 and T4. Free thyroid hormone levels remain unchanged and there is no clinical evidence of thyroid dysfunction. Altered tests usually persist for 2 to 3 weeks after stopping anabolic therapy.
Anabolic steroids may cause an increase in prothrombin time.
Anabolic steroids have been shown to alter fasting blood sugar and glucose tolerance tests.
Carcinogenesis, Mutagenesis, Impairment of Fertility:
A two-year carcinogenicity study in rats given oxymetholone orally was conducted under the auspices of the US National Toxicology Program (NTP). A wide spectrum of neoplastic and non-neoplastic effects was observed. In male rats, no effects were classified as neoplastic in response to doses up to 150 mg/kg/day (5 times therapeutic exposures with 5 mg/kg based on body surface area). Female rats given 30 mg/kg/day (1 fold the maximum recommended clinical dose of 5 mg/kg/day based on the body surface area) had increased incidences of lung alveolar/bronchiolar adenoma and adenoma or carcinoma combined. At 100 mg/kg/day (about 3 fold the maximum recommended clinical dose of 5 mg/kg/day based on BSA), female rats had increased incidences of hepatocellular adenoma and adenoma or carcinoma combined; the combined incidence of squamous cell carcinoma and carcinoma of the sweat glands also was increased.
There are rare reports of hepatocellular carcinoma in patients receiving long-term therapy with androgens in high doses. Withdrawal of the drugs did not lead to regression of the tumors in all cases.
Geriatric patients treated with androgens may be at an increased risk of developing prostatic hypertrophy and prostatic carcinoma although conclusive evidence to support this concept is lacking.
In studies conducted under the auspices of the US National Toxicology Program, no evidence of genotoxicity was found using standard assays for mutagenicity, chromosomal aberrations, or induction of micronuclei in erythrocytes.
Impairment of fertility was not tested directly in animal species. However, as noted below under ADVERSE REACTIONS, oligospermia in males and amenorrhea in females are potential adverse effects of treatment with Androlic Tablets. Therefore, impairment of fertility is a possible outcome of treatment with Androlic Tablets.
Pregnancy category X. (see CONTRAINDICATIONS).
It is not known whether anabolics are excreted in human milk.
Because of the potential for serious adverse reactions in nursed infants from anabolics,
women who take oxymetholone should not nurse.
Anabolic/androgenic steroids should be used very cautiously in children and only by specialists who are aware of their effects on bone maturation.
Anabolic agents may accelerate epiphyseal maturation more rapidly than linear growth in children,
and the effect may continue for 6 months after the drug has been stopped. Therefore,
therapy should be monitored by x-ray studies at 6-month intervals in order to avoid the risk of compromising the adult height.
Clinical studies of Androlic Tablets did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
ADVERSE REACTIONS OF ANDROLIC (Anapolon / Oxymetholone)
Cholestatic jaundice with, rarely, hepatic necrosis and death.
Hepatocellular neoplasms and peliosis hepatis have been reported in association with long-term androgenic anabolic steroid therapy (see WARNINGS).