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Oxandrin

Generic Name: Oxandrolone
Class: Androgens
ATC Class: A14AA
VA Class: HS100
Chemical Name: 17β-Hydroxy-17-αmethyl-2-oxa-5α-androstan-3-one
Molecular Formula: C19H30O3
CAS Number: 53-39-4

Warning(s)

  • Peliosis Hepatis
  • Peliosis hepatis, a condition in which the liver contains blood-filled cysts, reported with androgen therapy.1 4 30 31 34 May present with minimal hepatic dysfunction,1 4 34 or effects may not be apparent until complicated by life-threatening liver failure or rupture of the cysts resulting in intra-abdominal hemorrhage.1 4 5 7 31 34 (See Hepatic Effects under Cautions.)

  • Discontinuance of androgen therapy usually results in resolution of liver lesions.1 4 32 34

  • Hepatic Adenoma and Carcinoma
  • Liver cell tumors reported with androgen therapy.1 4 5 7 30 31 34 Tumors are usually benign and androgen dependent; hepatocellular carcinoma, sometimes fatal, also reported.1 4 5 7 34

  • Liver cell tumors associated with androgens are more vascular than other hepatic tumors; hepatic effects may not be apparent until complicated by life-threatening intra-abdominal hemorrhage.1 4 5 34

  • Discontinuance of androgen therapy often but not always results in regression or cessation of progression of the tumor.1 4 5 34

  • Lipid Abnormalities
  • May markedly alter serum lipoprotein concentrations; decreased HDL- and increased LDL-cholesterol reported with androgen therapy.1 4 30 31 34 Consider increased risk of cardiovascular disease (e.g., atherosclerosis and CAD).1 4 31 34 (See Lipid Abnormalities under Cautions.)

Introduction

Synthetic androgenic anabolic steroid hormone.1 4

Uses for Oxandrin

Catabolic and Wasting Disorders

Adjunct to conventional therapy to promote weight gain in individuals who experience weight loss following extensive surgery, chronic infections (e.g., HIV-associated wasting syndrome; designated an orphan drug by FDA for this use),3 or severe trauma (e.g., burns, spinal cord injury).1 5 17 19 22 32

Adjunct to conventional therapy for management of unexplained weight loss.1

Slideshow: Can Prescription Drugs Lead to Weight Gain?

Corticosteroid-induced Protein Catabolism

Adjunct to conventional therapy to offset protein catabolism (e.g., muscle wasting, muscle pain or weakness, delayed wound healing, atrophy of protein matrix of bone) associated with long-term corticosteroid therapy.1 4 20 21 33

Osteoporosis

Labeled for the symptomatic treatment of bone pain accompanying osteoporosis.1 4 23

Misuse and Abuse

Androgens have been misused and abused by athletes, bodybuilders, weight lifters, and others to enhance athletic performance or physique.6 7 8 9 10 32

Medical and sports experts (e.g., International Olympic Committee) consider such use to be inappropriate and unacceptable because of known adverse effects and potential long-term sequelae.9 Such misuse by athletes is contrary to rules and ethical principles of athletic competition.7 8 9 10

Manufacturer states that androgens have not been shown to enhance athletic performance.1

Oxandrin Dosage and Administration

General

  • Individualize dosage and duration of therapy carefully according to individual requirements, response, and tolerance.1 4 Use the minimum effective dosage; intended for intermittent use.1 4 22

Administration

Oral Administration

Administer orally 2–4 times daily in adults.1 4

Dosage

Pediatric Patients

Catabolic and Wasting Disorders
Oral

≤0.1 mg/kg daily for 2–4 weeks.1 4 Repeat course of therapy intermittently as needed to maintain weight.1 4 32

Manufacturer states that a 2- to 4-week course of therapy usually is adequate to observe a response (i.e., slowing or cessation of weight loss).1 4 32 A longer period of treatment is necessary to regain lost weight, especially if ongoing catabolic stressors are present.32

Higher than recommended dosage of 0.1 mg/kg twice daily for 5 days to 12 months has been evaluated in pediatric patients with burns.1 4 5 16 17 18 32

Corticosteroid-induced Protein Catabolism
Oral

≤0.1 mg/kg daily.1 4 Manufacturer states that a 2- to 4-week course of therapy usually is adequate to observe a response.1 4 32 Repeat course of therapy intermittently as needed.1 4 32

Adults

Catabolic and Wasting Disorders
Oral

2.5–20 mg daily in 2–4 divided doses for 2–4 weeks.1 4 Repeat course of therapy intermittently as needed to maintain weight.1 4 32

Manufacturer states that a 2- to 4-week course of therapy usually is adequate to observe a response (i.e., slowing or cessation of weight loss).1 4 32 A longer period of treatment is necessary to regain lost weight, especially if ongoing catabolic stressors are present.32 Continuous administration for 3–4 months has been evaluated in patients with HIV-associated wasting syndrome.5 19

Corticosteroid-induced Protein Catabolism
Oral

2.5–20 mg daily in 2–4 divided doses.1 4 Manufacturer states that a 2- to 4-week course of therapy usually is adequate to observe a response.1 4 32 Repeat course of therapy intermittently as needed.1 4 32

Osteoporosis
Bone Pain
Oral

2.5–20 mg daily in 2–4 divided doses.1 4 Manufacturer states that a 2- to 4-week course of therapy usually is adequate to observe a response.1 4 Repeat course of therapy intermittently as needed.1 4

Special Populations

Geriatric Patients

5 mg twice daily for 2–4 weeks recommended.1 Repeat course of therapy intermittently as needed.1 (See Geriatric Use under Cautions.)

Cautions for Oxandrin

Contraindications

  • Males with breast cancer or known or suspected prostate cancer.1 4

  • Women with hypercalcemia associated with metastatic breast cancer.1 4 (See Hypercalcemia under Cautions.)

  • Known or suspected pregnancy.1 4 (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

  • Nephrosis.1 4

  • Hypercalcemia.1 4 (See Hypercalcemia under Cautions.)

Warnings/Precautions

Warnings

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; potential for virilization of fetus.1 4

Fetotoxicity, embryotoxicity, infertility, and virilization of female offspring demonstrated in animals.1 4

Hepatic Effects

Potentially serious and/or life-threatening adverse hepatic effects (e.g., peliosis hepatis, hepatic adenomas, hepatocellular carcinoma) associated with prolonged use of high dosages of androgens.5 6 7 9 10 22 (See Boxed Warning.)

If cholestatic hepatitis with jaundice occurs, or if liver function test results become abnormal during therapy, discontinue oxandrolone and investigate etiology of these disorders.1 4 Drug-induced jaundice usually is reversible after discontinuance of drug.1 4

Monitor liver function periodically.1 4 17 22

Hypercalcemia

Possible hypercalcemia resulting from osteolysis in women with metastatic carcinoma of the breast.1 4 Monitor urine and serum calcium concentrations frequently during the course of androgen therapy in women with metastatic breast cancer.1 4 30

If hypercalcemia occurs, discontinue the drug.1 4 (See Contraindications under Cautions.)

Fluid Retention

Edema, with or without CHF, possible as a result of sodium and water retention and may be a serious complication in patients with preexisting cardiac, renal, or hepatic disease.1 4 30 (See Geriatric Use under Cautions.)

Misuse and Abuse

Potential for serious adverse effects (e.g., increased aggression,6 7 8 10 13 22 antisocial behavior,6 7 manic episode,6 22 depression,9 changes in libido,6 7 8 9 10 22 increased risk of cardiovascular disease,6 7 8 9 hepatotoxicity6 7 8 9 10 ) associated with misuse and abuse of androgens (see Misuse and Abuse under Uses); oxandrolone preparations currently subject to control under the Federal Controlled Substances Act of 1970, as amended by the Anabolic Steroids Control Act of 1990 and 2004, as schedule III (C-III) drugs.11 32

General Precautions

Virilization

Virilization, including baldness, clitoral enlargement, deepening of voice, hirsutism, and menstrual irregularities, may occur in females.1 4 5 6 9 13

Monitor women receiving oxandrolone therapy for signs of virilization.1 4 If virilization occurs, promptly discontinue therapy.1 4 Some changes may not be reversible (e.g., clitoral enlargement, voice changes) after discontinuance of the drug; concomitant use of estrogen with androgens does not prevent these effects.1 4 6 7 32

Hematologic Effects

Possible polycythemia, especially with high dosages of androgens.1 4 30 Perform periodic hemoglobin and hematocrit determinations in patients receiving high dosages of androgens.1 4 30

Anabolic steroids may suppress clotting factors II, V, VII, and X and prolong PT.1 4 (See Specific Drugs and Laboratory Tests under Interactions.)

Lipid Abnormalities

Androgens may increase LDL-cholesterol and decrease HDL-cholesterol concentrations; consider the increased risk for cardiovascular disease.1 4 5 6 7 10 12 13 19 22 32 Lipid concentrations return to baseline values approximately 1 month after discontinuance of androgen therapy.22

Use with caution in patients with cardiovascular disease or risk factors for cardiovascular disease.1 4 Determine serum lipid concentrations periodically; adjust therapy accordingly.1 4

Specific Populations

Pregnancy

Category X.1 4 (See Fetal/Neonatal Morbidity and Mortality and also Contraindications under Cautions.)

Lactation

Not known whether oxandrolone is distributed into milk.1 4 Discontinue nursing or the drug.1 4

Pediatric Use

May accelerate bone maturation without producing compensatory gain in linear growth, possibly resulting in compromised adult stature.1 4 10 The younger the child, the greater the risk of the drug compromising final mature stature.1 4

Use with extreme caution in children and only under the supervision of a specialist who is aware of the adverse effects of oxandrolone on bone maturation.1 4 Perform radiographic examination of the left hand and wrist every 6 months to determine rate of bone maturation and to assess the effect of treatment on epiphyseal centers.1 4

Geriatric Use

Possible increased risk of developing prostatic hypertrophy and prostate cancer during androgen therapy.1 4 30

Response in patients ≥65 years of age does not appear to differ from that in younger adults.1 Increased sensitivity to fluid retention and increases in hepatic transaminase values reported, particularly in geriatric women.1 Use lower dosage to minimize adverse effects.1 (See Geriatric Patients under Dosage and Administration.)

Common Adverse Effects

Elevated aminotransferases (ALT, AST),1 4 5 13 17 19 lipid abnormalities (e.g., decreased HDL cholesterol concentrations).1 4 5 13 19

Interactions for Oxandrin

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

Anticoagulants, oral

May potentiate action of oral anticoagulants and decrease anticoagulant requirements1 4 22 24 26 32

Increases AUC and half-life of warfarin; minor bleeding reported;1 4 80-85% decrease in warfarin dosage (from a mean of 6.13 mg daily to a mean of 1.13 mg daily) were needed to maintain target INR of 1.5 in one study1 4 32

Monitor PT or INR when oxandrolone therapy is initiated or discontinued in patients receiving oral anticoagulants and adjust anticoagulant dosage as needed1 4 32

Initial anticoagulant dosage may be substantially lower in patients receiving oxandrolone32

Monitor for signs and symptoms of occult bleeding1 4

Antidiabetic agents, oral (sulfonylureas)

Possible inhibition of sulfonylurea metabolism1 4 32

Use concomitantly with care6

Corticotropin (ACTH) and corticosteroids

May exacerbate edema1 4

Consider possibility of interaction before use13

Tests for thyroid function

Possible decreased thyroxine-binding globulin concentrations, resulting in decreased total serum thyroxine (T4) concentrations and increased resin uptake of triiodothyronine (T3) and T41 4 16

Free thyroid hormone concentrations remain unchanged1 4

May decrease protein-bound iodine (PBI) concentrations and radioactive iodine uptake1 4

Oxandrin Pharmacokinetics

Absorption

Bioavailability

Well absorbed after oral administration, with peak serum concentrations attained in approximately 1 hour.5 13

Distribution

Plasma Protein Binding

95%.5 13

Elimination

Metabolism

Partially metabolized via sulfation to 17-epioxandrolone; other metabolites also identified.5 13 14 25 27 28

Elimination Route

Excreted principally in urine as unchanged and unconjugated oxandrolone (28%).5 25 27

Half-life

Biphasic; distribution half-life is 30 minutes and elimination half-life is approximately 10.4 hours in adults.1 5 25

Special Populations

In geriatric individuals, elimination half-life is 13.3 hours.1

Stability

Storage

Oral

Tablets

20–25°C.4

Actions

  • Produces marked anabolic activity and relatively few androgenic effects.5 6 7 13 14 22

  • Produces retention of nitrogen,5 7 13 17 22 increases protein anabolism and amino acid utilization, and decreases urinary calcium concentrations.2 5 13 16 18 23

  • Increases lean body mass, body cell mass, and muscle strength.7 9 16 17 18 19 20 22

  • Increases bone mineral density and content.5 13 16 22

  • Inhibits protein catabolism induced by corticosteroids.5 6 8 17 22

  • Androgens stimulate production of erythrocytes, apparently by enhancing production of erythropoietin.22 (See Hematologic Effects under Cautions.)

  • Inhibits release of endogenous testosterone via feedback inhibition of pituitary luteinizing hormone (LH).1 4 7 8 10 19 22 32

  • Large doses of androgens may suppress spermatogenesis.1 4 6 7 8 9 22

Advice to Patients

  • Risk of virilization in females.1 2 4 6 Advise female patients to contact their clinician if they notice hoarseness, acne, menstrual changes, baldness, genital changes, or growth of facial hair.1 2 4

  • Risk of priapism; importance of males informing clinicians if too frequent or persistent penile erections occur.1 4

  • Advise male patients to contact their clinician if they notice new or worsening acne.1 4

  • Importance of periodic assessments to determine rate of bone maturation in pediatric patients.1 4

  • Importance of informing clinician if nausea, vomiting, changes in skin color, or ankle swelling occurs.1 4

  • Risk of potential liver toxicity and/or lipid abnormalities (e.g., increased LDL-cholesterol concentrations and decreased HDL-cholesterol concentrations.1 4 Importance of regular laboratory monitoring of liver function and cholesterol concentrations.1 4

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1 4

  • Importance of informing clinician of existing or contemplated concomitant therapy, including prescription (e.g., warfarin, antidiabetic medications) and OTC drugs and herbal supplements, as well as any concomitant illnesses.1 4

  • Importance of informing patients of other important precautionary information.1 4 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Oxandrolone is subject to control under the Federal Controlled Substances Act of 1970, as amended by the Anabolic Steroids Control Act of 1990 and 2004, as a schedule III (C-III) drug.11

Oxandrolone

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

2.5 mg

Oxandrin (C-III; scored)

Savient

Oxandrolone Tablets (C-III; scored)

10 mg

Oxandrin (C-III)

Savient

Oxandrolone Tablets (C-III)

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2013. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Oxandrin 10MG Tablets (SAVIENT PHARMACEUTICALS INC.): 30/$822.73 or 60/$1,621.34

Oxandrin 2.5MG Tablets (SAVIENT PHARMACEUTICALS INC.): 30/$249.24 or 90/$725.97

Oxandrolone 10MG Tablets (WATSON LABS): 30/$545.98 or 90/$1,580.05

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2013, Selected Revisions April 1, 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Savient Pharmaceuticals. Oxandrin (oxandrolone) tablets prescribing information. East Brunswick, NJ; 2006 Jan.

2. AHFS consumer medication information. Oxandrolone. Bethesda, MD: American Society of Health-System Pharmacists; 2004 Oct 1. Available from website. Accessed 2008 Mar 7.

3. Food and Drug Administration. List of orphan designations and approvals. Rockville, MD; 2007 Oct 4. From FDA website. Accessed 2008 Mar 7.

4. Par Pharmaceutical Companies. Oxandrolone tablets prescribing information. Spring Valley, NY; 2007 Mar 3.

5. Orr R, Singh MF. The anabolic androgenic steroid oxandrolone in the treatment of wasting and catabolic disorders: review of efficacy and safety. Drugs. 2004; 64:725-50. [PubMed 15025546]

6. Kam PCA, Yarrow M. Anabolic steroid abuse: physiological and anaesthetic considerations. Anaesthesia. 2005; 60:685-92. [PubMed 15960720]

7. American College of Sports Medicine. Position stand on the use of anabolic-androgenic steroids in sports. Med Sci Sports Exerc. 1987; 19:534-9. [PubMed 3316907]

8. Committee on Sports Medicine and Fitness, American Academy of Pediatrics. Adolescents and anabolic steroids: a subject review. Pediatrics. 1997; 99:904-8. [PubMed 9190555]

9. Council on Scientific Affairs, American Medical Association. Medical and nonmedical uses of anabolic-androgenic steroids. JAMA. 1990; 264:2923-7. [IDIS 274793] [PubMed 2232088]

10. Council on Scientific Affairs, American Medical Association. Drug abuse in athletes: anabolic steroids and human growth hormone. JAMA. 1988; 259:1703-5. [IDIS 239600] [PubMed 3278150]

11. Drug Enforcement Administration (DEA), Department of Justice. Implementation of the Anabolic Steroid Control Act of 2004. Final rule. [21 CFR Part 1300 and 1308] Fed Regist. 2005; 70:74653-8.

12. American Association of Clinical Endocrinologists. American Association of Clinical Endocrinologists medical practice guidelines for clinical practice for the evaluation and treatment of hypogonadism in adult male patients—2002 update. Endocr Pract. 2002; 8:440-56. [PubMed 15260010]

13. Akyurek M, Dunn RM. Oxandrolone. Plast Reconstr Surg. 2006; 118:791-4. [PubMed 16932191]

14. Schänzer W. Metabolism of anabolic androgenic steroids. Clin Chem. 1996; 42:1001-20.

16. Przkora R, Jeschke MG, Barrow RE et al. Metabolic and hormonal changes in severely burned children receiving long-term oxandrolone treatment. Ann Surg. 2005; 242:384-91. [PubMed 16135924]

17. Jeschke MG, Finnerty CC, Suman OE et al. The effect of oxandrolone on the endocrinologic, inflammatory, and hypermetabolic reponses during the acute phase postburn. Ann Surg. 2007; 246:351-62. [PubMed 17717439]

18. Wolf SE, Thomas SJ, Dasu MR et al. Improved net protein balance, lean mass, and gene expression changes with oxandrolone treatment in the severely burned. Ann Surg. 2003; 237:801-11. [PubMed 12796576]

19. Grunfeld C, Kotler DP, Dobs A et al. Oxandrolone in the treatment of HIV-associated weight loss in men: a randomized, double-blind, placebo-controlled study. J Acquir Immune Defic Syndr. 2006; 41:304-14. [PubMed 16540931]

20. Kravetz JD, Lee C, Dieterich DT. Oxandrolone use in Crohn’s disease. Am J Gastroenterol. 1997; 92:2330-1. Letter [PubMed 9399787]

21. Dickerman RD, Joseph AM, Bennett MT. Corticosteroid-induced myopathy in spinal cord injury patients: a role for anticatabolic agents? Spinal Cord. 2006; 44:263-4. Letter

22. Shahidi NT. A review of the chemistry, biological action, and clinical applications of anabolic-androgenic steroids. Clin Ther. 2001; 23:1355-90. [PubMed 11589254]

23. Riggs BL, Jowsey J, Kelly PJ et al. Studies on pathogenesis and treatment in postmenopausal and senile osteoporosis. Clin Endocrinol Metab. 1973; 2:317-32. [PubMed 4373194]

24. Bristol-Myers Squibb. Coumadin (warfarin sodium) tablets crystalline and Coumadin (warfarin sodium) for injection prescribing information. Princeton, NJ; 2007 Aug.

25. Massé R, Bi H, Ayotte C et al. Studies on anabolic steroids II—Gas chromatographic/mass spectrometric characterization of oxandrolone urinary metabolites in man. Biomed Environ Mass Spectrom. 1989; 18:429-38.

26. Koller EA, Wei X, Johnson TE. Oxandrolone steroid use and impaired coagulation. Arch Intern Med. 2006; 166:125. Letter. [PubMed 16401821]

27. Bi H, Massé R. Studies on anabolic steroids—12. Epimerization and degradation of anabolic 17β-sulfate-17α-methyl steroids in human: qualitative and quantitative GC/MS analysis. J Steroid Biochem Molec Biol. 1992; 42:533-46. [PubMed 1616883]

28. Gonzalez FJ, Tukey RH. Drug metabolism. In: Brunton L, Lazo JS, Parker KL, eds. Goodman and Gilman’s the pharmacological basis of therapeutics. 11th ed. New York: McGraw-Hill; 2006:82.

29. August D, Teitelbaum D, Albina J et al. Guidelines for the use of parenteral and enteral nutrition in adult and pediatric patients. Section XI: Specific guidelines for disease—adults. JEPN. 2002; 26:61S-96SA.

30. ICN Pharmaceuticals. Android (methyltestosterone) capsules prescribing information. Costa Mesa, CA; 2001 Sep.

31. Upsher-Smith Laboratories. Androxy (fluoxymesterone) tablets prescribing information. Minneapolis, MN; 2006 May.

32. Savient Pharmaceuticals, East Brunswick, NJ: Personal communication

33. AHFS drug information 2008. McEvoy GK, ed. Corticosteroids general statement. Bethesda, MD: American Society of Health-System Pharmacists; 2008:3088.

34. Alaven Pharmaceutical. Anadrol (oxymetholone) prescribing information. Marietta, GA; 2006 Dec.

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