Anadrol (Oxymetholone)

02 Details

Anadrol

(Oxymetholone)

Anadrol (Oxymetholone ) 100mg/tab 100 tabs

 

CI-406; HMD; Oksimetolon; Oksimetoloni; Oximetolon; Oximetolona; Oxymétholone; Oxymetholonum. 17β-Hydroxy-2-hydroxymethylene-17α-methyl-5α-androstan-3-one. Оксиметолон

C21H32O3 = 332.5.

CAS — 434-07-1.

ATC — A14AA05.

ATC Vet — QA14AA05.

Pharmacopoeias. In Br., Jpn,and US.  BP 2008(Oxymetholone). A white to creamy-white, odourless or almost odourless, crystalline powder. It exhibits polymorphism. Practically insoluble in water; soluble in alcohol; freely soluble in chloroform; slightly soluble in ether. Protect from light. Avoid contact with ferrous metals.

USP 31(Oxymetholone). A white to creamy-white, odourless crystalline powder. Practically insoluble in water; soluble 1 in 40 of alcohol, 1 in 5 of chloroform, 1 in 82 of ether, and 1 in 14 of dioxan.

Pharmacologic Category

Anabolic Steroid

Dosing: Adult

Note: The National Kidney Foundation does not recommend the use of androgens as an adjuvant to ESA treatment in anemic patients with chronic kidney disease (KDOQI, 2006).

Erythropoietic effects: Oral: 1-5 mg/kg/day once daily; usual effective dose: 1-2 mg/kg/day; give for a minimum trial of 3-6 months because response may be delayed

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Refer to adult dosing.

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling. Use with caution due to risk of edema in patients with renal impairment.

Dosing: Hepatic Impairment

Mild to moderate impairment: There are no dosage adjustments provided in the manufacturer’s labeling.

Severe impairment: Use is contraindicated.

Use: Labeled Indications

Treatment of anemias caused by deficient red cell production

Clinical Practice Guidelines

 

Storage/Stability

Store at room temperature 20° to 25°C (68° to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light.

Medication Patient Education with HCAHPS Considerations

  • Patient may experience diarrhea, insomnia, or sexual dysfunction. Have patient report immediately to prescriber priapism, acne vulgaris, dyspnea, excessive weight gain, edema of extremities, urinary retention, oliguria, asthenia, ecchymosis, hemorrhaging, considerable anxiety, signs of hepatic impairment, or signs of virilization (HCAHPS).

Contraindications

Hypersensitivity to oxymetholone or any component of the formulation; breast cancer in men; breast cancer in women with hypercalcemia; prostate cancer; severe hepatic dysfunction; nephrosis or nephrotic phase of nephritis; pregnancy or use in women who may become pregnant

Warnings/Precautions

Concerns related to adverse effects:

  • Blood lipid changes: [U.S. Boxed Warning]: Anabolic steroids may cause changes in blood lipids (decreased high density lipoproteins and sometimes increased low density lipoproteins), increasing the risk of arteriosclerosis and coronary artery disease.
  • Clotting factor alterations: Anabolic steroids may suppress factors II, V, VII, and X; prothrombin time may be increased.
  • Hepatic effects: [U.S. Boxed Warning]: Androgenic anabolic steroid treatment may cause peliosis hepatis, which occurs when splenic or hepatic tissue is replaced by cysts (blood-filled); may only cause minimal hepatic dysfunction although has been associated with hepatic failure. Androgenic liver cell tumors, which may be benign, although malignant tumors have also been reported; generally regress when anabolic steroid treatment is withdrawn. Both conditions (peliosis and tumors) may not be apparent until liver failure or intra-abdominal hemorrhage develops. Androgen use (low doses) has also been associated with cholestatic hepatitis and jaundice; may be associated with hepatomegaly and right upper-quadrant pain; jaundice is typically reversible upon discontinuation (continuing treatment has been associated with coma and death). Monitor liver function periodically.
  • Prostate conditions: Androgenic anabolic steroid use may cause prostatic hypertrophy or prostate cancer in elderly men.

Disease-related concerns:

  • Breast cancer: May cause hypercalcemia in women with breast cancer by stimulating osteolysis.
  • Diabetes: Use with caution in patients with diabetes mellitus; insulin or oral hypoglycemic needs may be altered; monitor carefully.
  • Edematous conditions: Use with caution in patients with conditions influenced by edema (eg, cardiovascular disease, migraine, seizure disorder, renal impairment); may cause fluid retention.

Special populations:

  • Pediatric: May accelerate bone maturation without producing compensatory gain in linear growth in children; effect may continue for 6 months after treatment discontinuation; in prepubertal children perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers.
  • Women: Discontinue with evidence of mild virilization in women.

Other warnings/precautions:

  • Appropriate use: Oxymetholone should not replace other anemia treatment supportive measures such as transfusion, correction of iron, folic acid, vitamin B12 or pyridoxine deficiency, antibacterial therapy, and the appropriate use of corticosteroids.

Geriatric Considerations

Theoretically, androgens may increase the risk of prostatic hyperplasia.

Pregnancy Risk Factor

X

Category X: Studies in animals or human beings have demonstrated fetal abnormalities, or there is evidence of fetal risk based on human experience, or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

 

Pregnancy Considerations

Oligospermia or amenorrhea may occur resulting in an impairment of fertility. Use is contraindicated in women who are or may become pregnant.

Lactation

Excretion in breast milk unknown/not recommended

Breast-Feeding Considerations

It is not known if oxymetholone is excreted in breast milk. Breast-feeding is not recommended by the manufacturer.

Adverse Reactions

Frequency not defined.

Cardiovascular: Coronary artery disease, peripheral edema

Central nervous system: Chills, excitation, insomnia

Dermatologic: Acne, hirsutism (women), hyperpigmentation, male-pattern baldness (postpubertal males, women)

Endocrine & metabolic: Amenorrhea, clitoromegaly, glucose tolerance decreased, gynecomastia, HDL-cholesterol decreased, hypercalcemia, hyperchloremia, hyperkalemia, hypernatremia, hyperphosphatemia, LDL-cholesterol increased, libido increased/decreased, menstrual irregularities, virilism (women)

Gastrointestinal: Diarrhea, nausea, vomiting

Genitourinary: Bladder irritability, epididymitis, impotence, oligospermia, penile enlargement, penile erections increased (prepubertal males), priapism, prostate cancer, prostatic hyperplasia (elderly males), seminal volume decreased, testicular atrophy, testicular dysfunction

Hematologic: Bleeding, INR increased, iron-deficiency anemia, leukemia, prothrombin time increased, clotting factors (II, V, VII, X) suppressed

Hepatic: Alkaline phosphatase increased, bilirubin increased, cholestatic hepatitis, cholestatic jaundice, hepatic failure, hepatic necrosis, hepatocellular carcinoma, liver cell tumors, peliosis hepatis, transaminases increased

Neuromuscular & skeletal: Creatine phosphokinase increased, premature closure of epiphysis (children)

Renal: Creatinine increased

Respiratory: Hoarseness (women)

Miscellaneous: Voice deepening (women)

Postmarketing and/or case reports:

Hepatotoxicity (idiosyncratic) (Chalasani, 2014)

Metabolism/Transport Effects

None known.

Drug Interactions

Blood Glucose Lowering Agents: Androgens may enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Risk C: Monitor therapy

C1 inhibitors: Androgens may enhance the thrombogenic effect of C1 inhibitors. Risk C: Monitor therapy

Corticosteroids (Systemic): May enhance the fluid-retaining effect of Androgens. Risk C: Monitor therapy

Cyclosporine (Systemic): Androgens may enhance the hepatotoxic effect of Cyclosporine (Systemic). Androgens may increase the serum concentration of Cyclosproine (Systemic). Risk D: Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Androgens may enhance the anticoagulant effect of Vitamin K Antagonists. Risk D: Consider therapy modification

Test Interactions

Decreased thyroxine-binding globulin, T4; increased resin uptake of T3 and T4

Monitoring Parameters

Periodic liver function tests, lipid profile, hemoglobin and hematocrit; iron studies; serum glucose (may be decreased by testosterone, monitor patients with diabetes); radiologic examination of bones every 6 months (when using in prepubertal children); monitor urine and serum calcium and signs of virilization in women treated for breast cancer

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral: 50 mg [scored]

Anatomic Therapeutic Chemical (ATC) Classification

  • A14AA05

Mechanism of Action

Enhances production of erythropoietin in patients with anemias which are due to bone marrow failure; stimulates erythropoiesis in anemias due to deficient red cell production

Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions

Effects on Dental Treatment

No significant effects or complications reported

Effects on Bleeding

No information available to require special precautions