Anavar (Oxandrolone)

02 Details

Anavar

(Oxandrolone)

Anavar (Oxandrolone) 15mg/tab 100 tabs

NSC-67068; Oxandrolona; Oxandrolonum; SC-11585. 17β-Hydroxy-17α-methyl-2-oxa-5α-androstan-3-one. Оксандролон

C19H30O3 = 306.4.

CAS — 53-39-4.

ATC — A14AA08.

ATC Vet — QA14AA08.

Pharmacopoeias. In US. USP 31(Oxandrolone). A white odourless crystalline powder. Soluble 1 in 5200 of water, 1 in 57 of alcohol, 1 in 69 of acetone, 1 in less than 5 of chloroform, and 1 in 860 of ether. Protect from light.

Pharmacologic Category

Androgen

Dosing: Adult

Weight gain (adjunct): Oral: 2.5-20 mg in divided doses 2-4 times daily based on individual response; a course of therapy of 2-4 weeks is usually adequate. This may be repeated intermittently as needed.

Dosing: Geriatric

Weight gain (adjunct): Oral: 5 mg twice daily

Dosing: Pediatric

Weight gain (adjunct): Oral: Children: Total daily dose: ≤0.1 mg/kg; may be repeated intermittently as needed

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution due to propensity to cause edema.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution.

Use: Labeled Indications

Adjunctive therapy to promote weight gain after weight loss following extensive surgery, chronic infections, or severe trauma, and in some patients who, without definite pathophysiologic reasons, fail to gain or to maintain normal weight; to offset protein catabolism with prolonged corticosteroid administration; relief of bone pain associated with osteoporosis

Storage/Stability

Store at 20°C to 25°C (68°F to 77°F).

Extemporaneously Prepared

A 1 mg/mL oral suspension may be made with tablets and either a 1:1 mixture of Ora-Sweet® and Ora-Plus®, or a 1:1 mixture of Ora-Sweet® SF and Ora-Plus®. Crush twenty-four 2.5 mg tablets in a mortar to a fine powder. Add small portions of chosen vehicle and mix to a uniform paste; mix while adding the vehicle in incremental proportions to almost 60 mL; transfer to a calibrated bottle, rinse mortar with vehicle, and add quantity of vehicle sufficient to make 60 mL. Thoroughly mix the suspension by shaking. Label “shake well” and “protect from light”. Stable for 90 days at room temperature (Johnson, 2011).

Johnson CE, Cober MP, Hawkins KA, et al, “Stability of Extemporaneously Prepared Oxandrolone Oral Suspensions,” Am J Health-Syst Pharm, 2011, 68(6):519-21.

Medication Patient Education with HCAHPS Considerations

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

Contraindications

Nephrosis; carcinoma of breast (women with hypercalcemia or men) or prostate; hypercalcemia; pregnancy

Warnings/Precautions

Concerns related to adverse effects:

• Blood lipid changes: [U.S. Boxed Warning]: May cause blood lipid changes with increased risk of arteriosclerosis.
• Hepatic effects: [U.S. Boxed Warning]: Anabolic steroids may cause peliosis hepatis or liver cell tumors which may not be apparent until liver failure or intra-abdominal hemorrhage develops. Discontinue in case of cholestatic hepatitis with jaundice or abnormal liver function tests. Use with caution in patients with hepatic impairment.

Disease-related concerns:

• Breast cancer: Use with caution in patients with breast cancer; may cause hypercalcemia by stimulating osteolysis. Discontinue use if hypercalcemia occurs.
• Carbohydrate intolerance: May have adverse effects on glucose tolerance; use caution in patients with diabetes.
• COPD: Use with caution in patients with COPD.
• Edematous conditions: Use with caution in patients with conditions influenced by edema (eg, cardiovascular disease, migraine, seizure disorder, renal impairment); may cause fluid retention.

Concurrent drug therapy issues:

• Warfarin: Use caution with concomitant warfarin therapy; warfarin dose may need to be significantly decreased.

Special populations:

• Elderly: Use with caution in elderly patients, they may be at greater risk for prostatic hyperplasia, prostate cancer, fluid retention, and transaminase elevations.
• Pediatric: May accelerate bone maturation without producing compensatory gain in linear growth in children; effect may continue for 6 months after the drug is stopped; in prepubertal children perform radiographic examination of the left hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers.
• Females: May cause mild virilization in females; monitor for signs of virilization (deepening of the voice, hirsutism, acne, clitoromegaly). Discontinue with evidence of mild virilization in female patients; early discontinuation may prevent irreversible virilization.

Other warnings/precautions:

• Appropriate use: Anabolic steroids have not been shown to improve athletic ability.

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

Use is contraindicated in women who are or may become pregnant; masculinization of the fetus has been reported.

Lactation

Excretion in breast milk unknown/not recommended

Breast-Feeding Considerations

It is not known if oxandrolone is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, breast-feeding is not recommended.

Adverse Reactions

Frequency not defined.

Cardiovascular: Edema

Central nervous system: Depression, excitation, insomnia

Dermatologic: Acne (females and prepubertal males)

Also reported in females: Hirsutism, male-pattern baldness

Endocrine & metabolic: Electrolyte imbalances, glucose intolerance, gonadotropin secretion inhibited, gynecomastia, HDL decreased, LDL increased, libido changes

Also reported in females: Clitoral enlargement, menstrual irregularities

Genitourinary:

Prepubertal males: Increased or persistent erections, penile enlargement

Postpubertal males: Bladder irritation, epididymitis, impotence, oligospermia, priapism (chronic), testicular atrophy, testicular function inhibited

Hematologic: Prothrombin time increased, suppression of clotting factors

Hepatic: Alkaline phosphatase increased, ALT increased, AST increased, bilirubin increased, cholestatic jaundice, hepatic necrosis (rare), hepatocellular neoplasms, peliosis hepatis (with long-term therapy)

Neuromuscular & skeletal: CPK increased, premature closure of epiphyses (in children)

Renal: Creatinine excretion increased

Miscellaneous: Bromsulfophthalein retention, habituation, voice alteration (deepening, in females)

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 Cyclosporine (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

 

May suppress factors II, V, VII, and X; may increase PT; may decrease thyroxine-binding globulin and radioactive iodine uptake

Monitoring Parameters

Liver function tests, cholesterol profile, hemoglobin/hematocrit; INR/PT in patients on anticoagulant therapy

Children: Radiographs of left wrist and hand every 6 months (to assess bone maturation)

Adult females: Signs of virilization (deepening voice, hirsutism, acne, clitoromegaly); urine and serum calcium in women with breast cancer

Dosage Forms

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

Tablet, Oral: 2.5 mg, 10 mg

Anatomic Therapeutic Chemical (ATC) Classification

• A14AA08

Mechanism of Action

Synthetic testosterone derivative with similar androgenic and anabolic actions.

Pharmacodynamics/Kinetics

 

Half-life elimination: 10-13 hours

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