We need you! See something you could improve? Make an edit and help improve WikSM for everyone.

Oxandrolone

From WikiSM
Jump to: navigation, search

Other Names

  • Oxandrin
  • Anavar

General

  • Classified as an androgenic-anabolic steroid used to build muscle mass and treat catabolic/wasting conditions
  • Administered orally
  • Derived from DHT.
    • Testosterone converts to DHT via 5-alpha reductase (the popular hair-loss medication finasteride, works by blocking 5-akpha reductase to reduce DHT levels)
  • Used as a performance-enhancing drug in many sports
    • Especially popular in bodybuilding and powerlifting

Performance Enhancing Effects

  • Muscle growth
    • Via stimulation of protein synthesis; protein breakdown unchanged [1]
  • Increased utilization of intracellular amino acids
  • 6x the anabolic activity of testosterone in assays with no estrogenic or pregestational activity and significantly less androgenicity [2]

Medical Indications

  • FDA approval:
    • Bone pain associated with osteoporosis [3]
    • Counteracting the catabolic effects of long-term corticosteroid use [3]
    • Promoting weight gain following surgery, physical trauma, or chronic infection
    • Unexplained weight loss
  • Administration improves long-term recovery of severely burned children
    • Improvements in height, bone mineral content, cardiac work, and muscle strength [4]
    • Benefits occurred for up to 5 years post burn

Contraindications

  • Known or suspected cancers[3]
    • Carcinoma of the prostate or male breast
    • Carcinoma of the breast in females with hypercalcemia
  • Anabolic steroids may stimulate osteolytic bone resorption
  • Pregnancy due to masculinization of the fetus (category X)
  • Hypercalcemia
  • Nephrotic syndrome

Adverse Reactions

  • May increase sensitivity to oral anticoagulants like warfarin (requires close monitoring)[3]
  • Hepatic tumors
    • Liver cell tumors have been reported in patients receiving long-term androgenic anabolic steroids in higher doses and withdrawal of steroids did not always lead to regression of tumor
  • Patients with moderate to severe COPD should be monitored closely for COPD exacerbations and fluid retention.
  • Adverse reactions seen with the use of androgenic anabolic steroids:

Males:

  • Phallic enlargement
  • Increased frequency/persistence of erection
  • Inhibition of testicular function
  • Testicular atrophy

Females:

  • Clitoral enlargement
  • Menstrual irregularities
  • Deepening of the voice
  • Male pattern baldness

By system/organ

  • CNS: habituation, excitation, insomnia, depression, changes in libido
  • Hematologic: bleeding when used with anticoagulants (see above)
  • Breast: gynecomastia
  • Hair: hirsutism
  • Skin: acne
  • Skeletal: premature closure of epiphyses
  • FLuid/electrolytes: edema, retention of sodium, chloride, potassium, phosphate, and calcium
  • Metabolic/endocrine: decreased glucose tolerance, increased creatinine excretion, increased creatine phosphokinase levels

Pharmacology

  • Agonist of androgen receptor
  • Mechanism of action is like that of testosterone:
    • Oxandrolone binds to androgen receptors in the cytoplasm of muscle cells
    • This complex translocates to the nucleus
    • Binds to androgen-receptor binding sites that induce the transcription of genes that are responsible for muscle growth and repair
  • Oral bioavailability is 97% [5]
  • Primarily metabolized by the kidneys and the liver to a lesser extent (therefore less hepatotoxic compared to other anabolics)[5]
    • Elimination half-life 9.4-10.4 hours and up to 13.3 hours in the elderly [5]

WADA Considerations

  • Prohibited at all times by WADA (in and out of competition)
  • Classified as a controlled substance under the Anabolic Steroids Control Act of 1990 and assigned to schedule 3 (non-narcotic) [3]

Testing

  • Blood or urine testing may be used
  • Long-term use of steroids suppresses endogenous steroids levels in urine samples
    • May be the earliest indication of steroid use [6]
  • Newer technologies have lengthened the drug detection window by testing for steroid metabolites [6]
    • Many athletes are caught years later due to advancements in technology

See Also


References

  1. Sheffield-Moore, M. 1999. “Short-Term Oxandrolone Administration Stimulates Net Muscle Protein Synthesis in Young Men.” Journal of Clinical Endocrinology & Metabolism 84(8):2705 11.
  2. Llewellyn, William. 2017. William Llewellyn's Anabolics. Jupiter, FL: Molecular Nutrition, LLC.
  3. 3.0 3.1 3.2 3.3 3.4 Anon. n.d. “Oxandrolone Tablets, USP.” FDA Gov. Retrieved (https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/076761lbl.pdf)
  4. Porro, Laura J. et al. 2012. “Five-Year Outcomes after Oxandrolone Administration in Severely Burned Children: A Randomized Clinical Trial of Safety and Efficacy.” Journal of the American College of Surgeons 214(4):489–502.
  5. 5.0 5.1 5.2 Mozayani, Ashraf and Lionel Raymon. 2016. Handbook of Drug Interactions a Clinical and Forensic Guide. Totowa: Humana Press.
  6. 6.0 6.1 NIH. 2018. “Steroids and Other Appearance and Performance Enhancing Drugs (APEDs) Research Report.” Retrieved (https://nida.nih.gov/publications/research-reports/steroids-other-appearance-performance-enhancing-drugs-apeds/introduction).
Created by:
Khashayar ( Khash ) Farzam on 12 July 2019 02:43:43
Last edited:
15 June 2022 00:26:20