Oxandrolone: Difference between revisions

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{{DrugProjectFormSinglePage
|authorTag=


{{VP}}


{{drugbox
<!--Overview-->
| IUPAC_name = (1S,3aS,3bR,5aS,9aS,9bS,11aS)-1-hydroxy-1,9a,11a-trimethyl-2,3,3a,3b,4,5,5a,6,9,9b,10,11-dodecahydroindeno[7,6-h]isochromen-7-one
 
| image = Oxandrolone.svg
|genericName=
| width = 225px
 
| CAS_number = 53-39-4
 
| ATC_prefix = A14
 
| ATC_suffix = AA08
|aOrAn=
| ATC_supplemental =  
 
| PubChem = 5878
an
| DrugBank = APRD01151
 
| C = 19 | H = 30 | O = 3
|drugClass=
| molecular_weight = 306.44 g/mol
 
| bioavailability = 97%
anabolic steroid
| protein_bound =  
 
| metabolism = Hepatic
|indication=
| elimination_half-life = 9 hour
 
| pregnancy_category = X
weight gain
| legal_status = Prescription only (US)
 
| routes_of_administration = Oral
|hasBlackBoxWarning=
| excretion = Urinary:90%; Fecal:6%
 
}}
Yes
{{SI}}
 
'''Oxandrolone''' ('''Oxandrin''') is an [[anabolic steroid]] created by [[Searle Laboratories]] under the trademark '''Anavar''', and introduced into the US in 1964. It is taken orally, and unlike other steroids delivered in this manner, most of which are Class II steroids, the majority of its effects are due to reaction with the [[androgen receptor]]. In sufficient dosage, Oxandrolone is highly likely to bind well with the receptor, and is therefore a Class I steroid, while having few other side-effects.  
|adverseReactions=
 
edema, increased risk of atherosclerosis, cholestatic hepatitis, jaundice, atrophy of testis, erectile dysfunction, and priapism
 
<!--Black Box Warning-->
 
|blackBoxWarningTitle=
WARNING
 
|blackBoxWarningBody=
<i><span style="color:#FF0000;"> </span></i>
 
*Peliosis hepatis, a condition in which liver and sometimes splenic tissue is replaced with blood-filled cysts, has been reported in patients receiving androgenic anabolic steroid therapy. these cysts are sometimes present with minimal hepatic dysfunction, but at other times they have been associated with liver failure. They are often not recognized until life-threatening liver failure or intra-abdominal hemorrhage develops. withdrawal of drug usually results in complete disappearance of lesions. Liver cell tumors are also reported. Most often these tumors are benign and androgen-dependent, but fatal malignant tumors have been reported. Withdrawal of drug often results in regression or cessation of progression of the tumor. However, hepatic tumors associated with androgens or anabolic steroids are much more vascular than other hepatic tumors and may be silent until life-threatening intra-abdominal hemorrhage develops. Blood lipid changes that are known to be associated with increased risk of atherosclerosis are seen in patients treated with androgens or anabolic steroids. These changes include decreased high-density lipoproteins and sometimes increased low-density lipoproteins. The changes may be very marked and could have a serious impact on the risk of atherosclerosis and coronary artery disease.
 
<!--Adult Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Adult)-->
 
|fdaLIADAdult=
 
Oxandrolone is indicated as 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 the protein catabolism associated with prolonged administration of corticosteroids, and for the relief of the bone pain frequently accompanying osteoporosis (See DOSAGE AND ADMINISTRATION).
 
Therapy with anabolic steroids is adjunctive to and not a replacement for conventional therapy. The duration of therapy with oxandrolone will depend on the response of the patient and the possible appearance of adverse reactions. Therapy should be intermittent.
 
Adults: The response of individuals to anabolic steroids varies. The daily adult dosage is 2.5 mg to 20 mg given in 2 to 4 divided doses. The desired response may be achieved with as little as 2.5 mg or as much as 20 mg daily. A course of therapy of 2 to 4 weeks is usually adequate. This may be repeated intermittently as indicated.
 
Children: For children the total daily dosage of oxandrolone is ≤0.1 mg per kilogram body weight or ≤0.045 mg per pound of body weight. This may be repeated intermittently as indicated.
 
Geriatric Use: Recommended dose for geriatric patients is 5 mg bid.
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
* Dosing Information
 
:* Dosage
 
=====Condition3=====
 
* Dosing Information
 
:* Dosage
 
=====Condition4=====
 
* Dosing Information
 
:* Dosage
 
<!--Off-Label Use and Dosage (Adult)-->
 
<!--Guideline-Supported Use (Adult)-->
 
|offLabelAdultGuideSupport=
 
=====Condition1=====
 
* Developed by:
 
* Class of Recommendation:
 
* Strength of Evidence:
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
 
<!--Non–Guideline-Supported Use (Adult)-->
 
|offLabelAdultNoGuideSupport=
 
 
Alcoholic hepatitis
 
Burn, Severe; Adjunct
 
Cachexia associated with AIDS
 
Turner syndrome
 
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
 
<!--Pediatric Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Pediatric)-->
 
|fdaLIADPed=
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Off-Label Use and Dosage (Pediatric)-->
 
<!--Guideline-Supported Use (Pediatric)-->
 
|offLabelPedGuideSupport=
 
=====Condition1=====
 
* Developed by:
 
* Class of Recommendation:
 
* Strength of Evidence:
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Non–Guideline-Supported Use (Pediatric)-->
 
|offLabelPedNoGuideSupport=
 
=====Condition1=====
 
* Dosing Information
 
:* Dosage
 
=====Condition2=====
 
There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Contraindications-->
 
|contraindications=
 
*Known or suspected carcinoma of the prostate or the male breast.
 
*Carcinoma of the breast in females with hypercalcemia (androgenic anabolic steroids may stimulate osteolytic bone resorption).
 
*Pregnancy, because of possible masculinization of the fetus. Oxandrolone has been shown to cause embryotoxicity, fetotoxicity, infertility, and masculinization of female animal offspring when given in doses 9 times the human dose.
 
*Nephrosis, the nephrotic phase of nephritis.
 
*Hypercalcemia.
 
<!--Warnings-->
 
|warnings=
 
*Cholestatic hepatitis and jaundice may occur with 17-alpha-alkylated androgens at a relatively low dose. If cholestatic hepatitis with jaundice appears or if liver function tests become abnormal, oxandrolone should be discontinued and the etiology should be determined. Drug-induced jaundice is reversible when the medication is discontinued.
 
*In patients with breast cancer, anabolic steroid therapy may cause hypercalcemia by stimulating osteolysis. Oxandrolone therapy should be discontinued if hypercalcemia occurs.
 
*Edema with or without congestive heart failure may be a serious complication in patients with pre-existing cardiac, renal, or hepatic disease. Concomitant administration of adrenal cortical steroid or ACTH may increase the edema.
 
*In children, androgen therapy may accelerate bone maturation without producing compensatory gain in linear growth. This adverse effect results in compromised adult height.  The younger the child, the greater the risk of compromising final mature height. The effect on bone maturation should be monitored by assessing bone age of the left wrist and hand every 6 months (See PRECAUTIONS: Laboratory Tests).
 
*Geriatric patients treated with androgenic anabolic steroids may be at an increased risk for the development of prostatic hypertrophy and prostatic carcinoma.
 
*Anabolic steroids have not been shown to enhance athletic ability.
 
====Precautions====
 
* Concurrent dosing of oxandrolone with warfarin may result in unexpectedly large increases in the INR or prothrombin time (PT). When oxandrolone is prescribed to patients being treated with warfarin, doses of warfarin may need to be decreased significantly to maintain the desirable INR level and diminish the risk of potentially serious bleeding (See PRECAUTIONS: Drug Interactions).
 
*General
:*Women should be observed for signs of virilization (deepening of the voice, hirsutism, acne, clitoromegaly). Discontinuation of drug therapy at the time of evidence of mild virilism is necessary to prevent irreversible virilization. Some virilizing changes in women are irreversible even after prompt discontinuance of therapy and are not prevented by concomitant use of estrogens. Menstrual irregularities may also occur.
:*Anabolic steroids may cause suppression of clotting factors II, V, VII, and X, and an increase in prothrombin time.
 
<!--Adverse Reactions-->
 
<!--Clinical Trials Experience-->
 
|clinicalTrials=
 
*Patients with moderate to severe COPD or COPD patients who are unresponsive to bronchodilators should be monitored closely for COPD exacerbation and fluid retention.
 
*The following adverse reactions have been associated with use of anabolic steroids: Hepatic: Cholestatic jaundice with, rarely, hepatic necrosis and death. Hepatocellular neoplasms and peliosis hepatis with long-term therapy (See WARNINGS). Reversible changes in liver function tests also occur including increased bromsulfophthalein (BSP) retention, changes in alkaline phosphatase and increases in serum bilirubin, aspartate aminotransferase (AST, SGOT) and alanine aminotransferase (ALT, SGPT)
 
*In males:
:*Prepubertal: Phallic enlargement and increased frequency or persistence of erections.
:*Postpubertal: Inhibition of testicular function, testicular atrophy and oligospermia, impotence, chronic priapism, epididymitis, and bladder irritability.
 
*In females:
:*Clitoral enlargement, menstrual irregularities.
 
=====CNS=====
 
Habituation, excitation, insomnia, depression, and changes in libido.
 
=====Hematologic=====
 
Bleeding in patients on concomitant oral anticoagulant therapy.
 
=====Breast=====
 
Gynecomastia.
 
=====Larynx=====
 
Deepening of the voice in females.
 
=====Hair=====
 
Hirsutism and male pattern baldness in females.
 
=====Skin=====
 
Acne (especially in females and prepubertal males).
 
=====Skeletal=====
 
Premature closure of epiphyses in children.
 
=====Fluid and electrolytes=====
 
Edema, retention of serum electrolytes (sodium chloride, potassium, phosphate, calcium).
 
=====Metabolic/Endocrine=====
 
Decreased glucose tolerance, increased creatinine excretion, increased serum levels of  creatinine phosphokinase (CPK). Masculinization of the fetus. Inhibition of gonadotropin secretion.
 
<!--Postmarketing Experience-->
 
|postmarketing=
 
There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
 
<!--Drug Interactions-->
 
|drugInteractions=
 
* Anticoagulants
:*Anabolic steroids may increase sensitivity to oral anticoagulants. Dosage of the anticoagulant may have to be decreased in order to maintain desired prothrombin time. Patients receiving oral anticoagulant therapy require close monitoring, especially when anabolic steroids are started or stopped.
 
*Warfarin
:*A multidose study of oxandrolone, given as 5 or 10 mg bid in 15 healthy subjects concurrently treated with warfarin, resulted in a mean increase in S-warfarin half-life from 26 to 48 hours and AUC from 4.55 to 12.08 ng*hr/mL; similar increases in R-warfarin half-life and AUC were also detected. Microscopic hematuria (9/15) and gingival bleeding (1/15) were also observed. A 5.5-fold decrease in the mean warfarin dose from 6.13 mg/day to 1.13 mg/day (approximately 80-85% reduction of warfarin dose), was necessary to maintain a target INR of 1.5. When oxandrolone therapy is initiated in a patient already receiving treatment with warfarin, the INR 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 drugs, careful monitoring of the INR or PT, and adjustment of the warfarin dosage if indicated are recommended when the oxandrolone dose is changed or discontinued. Patients should be closely monitored for signs and symptoms of occult bleeding.
 
*Oral hypoglycemic agents
:*Oxandrolone may inhibit the metabolism of oral hypoglycemic agents.
 
*Adrenal steroids or ACTH
:*In patients with edema, concomitant administration with adrenal cortical steroids or ACTH may increase the edema.
 
<!--Use in Specific Populations-->
 
|useInPregnancyFDA=
* '''Pregnancy Category X'''
 
|useInPregnancyAUS=
* '''Australian Drug Evaluation Committee (ADEC) Pregnancy Category'''
 
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of {{PAGENAME}} in women who are pregnant.
 
|useInLaborDelivery=
There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
 
|useInNursing=
 
*It is not known whether anabolic steroids are excreted in human milk. Because of the potential of serious adverse reactions in nursing infants from oxandrolone, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
 
|useInPed=
 
*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 adult height. Androgenic anabolic steroid therapy should be used very cautiously in children and only by specialists who are aware of the effects on bone maturation (See WARNINGS).
 
|useInGeri=
There is no FDA guidance on the use of {{PAGENAME}} with respect to geriatric patients.
 
|useInGender=
There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
 
|useInRace=
There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
 
|useInRenalImpair=
There is no FDA guidance on the use of {{PAGENAME}} in patients with renal impairment.
 
|useInHepaticImpair=
There is no FDA guidance on the use of {{PAGENAME}} in patients with hepatic impairment.
 
|useInReproPotential=
There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
 
|useInImmunocomp=
There is no FDA guidance one the use of {{PAGENAME}} in patients who are immunocompromised.
 
<!--Administration and Monitoring-->
 
|administration=
 
* Oral
 
|monitoring=
 
There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.
 
<!--IV Compatibility-->
 
|IVCompat=
 
There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.
 
<!--Overdosage-->
 
|overdose=
 
===Acute Overdose===
 
*No symptoms or signs associated with overdosage have been reported. It is possible that sodium and water retention may occur.
 
*The oral LD50 of oxandrolone in mice and dogs is greater than 5,000 mg/kg. No specific antidote is known, but gastric lavage may be used.
 
===Chronic Overdose===
 
There is limited information regarding <i>Chronic Overdose</i> of {{PAGENAME}} in the drug label.
 
<!--Pharmacology-->
 
<!--Drug box 2-->
 
|drugBox=
 
 
 
<!--Mechanism of Action-->
 
|mechAction=
 
*Anabolic steroids are synthetic derivatives of testosterone. Certain clinical effects and adverse reactions demonstrate the androgenic properties of this class of drugs. Complete dissociation of anabolic and androgenic effects has not been achieved. The actions of anabolic steroids are therefore similar to those of male sex hormones with the possibility of causing serious disturbances of growth and sexual development if given to young children. Anabolic steroids suppress the gonadotropic functions of the pituitary and may exert a direct effect upon the testes.
 
*During exogenous administration of anabolic androgens, endogenous testosterone release is inhibited through inhibition of pituitary luteinizing hormone (LH). At large doses, spermatogenesis may be suppressed through feedback inhibition of pituitary follicle-stimulating hormone (FSH)
 
<!--Structure-->
 
|structure=
 
* Oxandrolone oral tablets contain 2.5 mg or 10 mg of the anabolic steroid oxandrolone. Oxandrolone is 17β-hydroxy-17α-methyl-2-oxa-5α-androstan-3-one with the following structural formula:
 
: [[File:{{PAGENAME}}01.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
 
*Inactive ingredients include cornstarch, lactose, magnesium stearate, and hydroxypropyl methylcellulose.
 
<!--Pharmacodynamics-->
 
|PD=
 
There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.
 
<!--Pharmacokinetics-->
 
|PK=
 
*In a single dose pharmacokinetic study of oxandrolone in elderly subjects, the mean elimination half-life was 13.3 hours. In a previous single dose pharmacokinetic study in younger volunteers, the mean elimination half-life was 10.4 hours. No significant differences between younger and elderly volunteers were found for time to peak, peak plasma concentration or AUC after a single dose of oxandrolone. The correlation between plasma level and therapeutic effect has not been defined.
 
<!--Nonclinical Toxicology-->
 
|nonClinToxic=
 
*Oxandrolone has not been tested in laboratory animals for carcinogenic or mutagenic effects. In 2-year chronic oral rat studies, a dose-related reduction of spermatogenesis and decreased organ weights (testes, prostate, seminal vesicles, ovaries, uterus, adrenals, and pituitary) were shown.
 
<!--Clinical Studies-->
 
|clinicalStudies=
 
There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.
 
<!--How Supplied-->
 
|howSupplied=
 
* Oxandrolone 2.5 mg tablets are oval, white, and scored with OX on one side and “11” on each side of the scoreline on the other side; bottles of 100 (NDC 0591-3544-01).
 
*Oxandrolone 10 mg tablets are capsule shaped, white, with OX on one side and “10” on the other side; bottles of 60 (NDC 0591-3545-60).
 
<!--Patient Counseling Information-->
 
|fdaPatientInfo=
 
*The physician should instruct patients to report immediately any use of warfarin and any bleeding.
 
*The physician should instruct patients to report any of the following side effects of androgens:
 
*Males: Too frequent or persistent erections of the penis, appearance or aggravation of acne.
 
*Females: Hoarseness, acne, changes in menstrual periods, or more facial hair.
 
*All patients: Nausea, vomiting, changes in skin color, or ankle swelling.
 
<!--Precautions with Alcohol-->
 
|alcohol=
 
* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
 
<!--Brand Names-->
 
|brandNames=
 
* OXANDROLONE®<ref>{{Cite web | title = OXANDROLONE  oxandrolone tablet | url = http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=52bc111a-c4a4-44fc-ac45-82e00d64f65e }}</ref>


As opposed to most other anabolic steroids Oxandrolone has two major advantages: First of all it does not aromatize (convert to estrogen which causes gynecomastia - breast tissue) and it does not significantly influence on low dosages (10mg) body's normal testosterone production (HPTA axis). When dosages are high (this goes for any anabolic steroid) then your body feels that it has enough testosterone and it reduces the production of LH (luteinizing hormone) which no longer stimulates Leydig cells in testicles to produce testosterone therefore causing testicular atrophy (shrinking).
<!--Look-Alike Drug Names-->
Post Cycle Therapy (PCT) is of course needed for high dosages (40-50mg) of this synthetic derivative of testosterone because as the dosage increases the influence on HPTA is bigger. Lack of PCT will of course lead to protein catabolism until body's normal testosterone secretion is back to normal.


The drug was prescribed for a number of medical disorders causing involuntary weight loss, in order to promote muscle regrowth. It had also been shown to be partially successful in treating cases of [[osteoporosis]]. However, in part due to bad publicity from its abuses by bodybuilders, Oxandrolone was discontinued by Searle Laboratories in 1989. It was picked up by Bio-Technology General Corporation, now Savient Pharmaceuticals, Inc. who, following successful clinical trials in 1995, released it under the tradename Oxandrin.
|lookAlike=


It was approved for orphan drug status by the [[Food and Drug Administration]] (FDA) in treating alcoholic hepatitis, Turner's syndrome, and weight loss caused by HIV. In addition, the drug has shown positive results in treating anaemia and hereditary angioedema.
* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
In a randomized, double-blind study,  patients with 40% total body surface area burns were selected to receive standard burn care plus Oxandrolone, or without Oxandrolone. Those treated with Oxandrolone showed improve body composition, preserved muscle mass and reduced hospital stay time. <ref name="S">[http://www.shrinershq.org/Hospitals/Galveston Shriners Burns Hospital for Children]. The Effect of Oxandrolone On the Endocrinologic, Inflammatory and Hypermetabolic Responses During the Acute Phase Postburn. 2006.  [http://www.americansurgical.info/abstracts/2007/1.cgi]</ref> Other studies however have shown links between prolonged use of the drug and problems of [[Cirrhosis|liver toxicity]] similar to those found with other 17α-alkylated steroids. Even in small dosages, many users reported [[Gastro-intestinal tract|gastro-intestinal]] problems such as [[bloating]], [[nausea]], skin rash and itching (hives), black, tarry stools or light-colored stools, depression, unusual bleeding, unusual swelling, yellowing of the eyes or skin,  and [[diarrhoea]].


In rare cases, serious and even fatal cases of liver problems have developed during treatment with oxandrolone. Oxandrolone may increase the amount of low density lipoprotein (LDL; 'bad cholesterol') and decrease the amount of high density lipoprotein (HDL; 'good cholesterol') in the blood. This may increase the risk of developing heart disease. Oxandrolone may damage the liver or increase LDL without causing symptoms. It is important to have regular laboratory tests to be sure that the liver is working properly and that LDL has not increased. Oxandrolone may also decrease fertility in men.
<!--Drug Shortage Status-->


Before the [[Controlled Substances Act]] was passed to restrict the production, sale, and usage of anabolic steroids, Oxandrolone's characteristics lent itself well towards use by female athletes. Its specificity targeting the androgen receptor meant that, unlike many other steroids, it had not been reported to cause stunted growth in younger users (because it doesn't convert to estrogen, thats the reason women typically don't grow as tall as men -- they have more estrogen) and at typical dosage rarely caused noticeable  masculinising effects outside of stimulating muscle growth. It is not easily metabolised into [[Dihydrotestosterone|DHT]] or [[estrogen]]. As such, a typical dose of 20-30 [[milligram|mg]] provided elevated [[androgen]] levels for up to eight hours. To increase effectiveness, bodybuilders typically "stacked" the drug with others such as [[Testosterone]], further enhancing body mass gain.
|drugShortage=
}}


Besides the obvious health risks (liver and coronary), the biggest problem with Oxandrolone  (and with any anabolic steroid) is of course abuse and addiction without the supervision of a physician. Addiction rate for steroids is so high that the U.S. Controlled Substances Act considers anabolic steroids a Schedule III drug therefore even possession is a felony. Abuse being one major problem most bodybuilders  consider a normal dose for a novice being 20-30mg's per day when in fact 10 mg is more then enough for someone who never had used. Higher dosages not only lead to AR (Androgen Receptor) damage and HPTA suppression but also damages the liver being a 17α-alkylated. It is specially made 17α-alkylated because if it would not be then the liver would consider it a toxin and would destroy it.
<!--Pill Image-->


Since Searle stopped production, biggest sellers are La Pharma Italy and British Dragon Thailand. It is considered by the medical community the safest of all steroids in terms of side effects.
{{PillImage
|fileName=No image.jpg|This image is provided by the National Library of Medicine.
|drugName=
|NDC=
|drugAuthor=
|ingredients=
|pillImprint=
|dosageValue=
|dosageUnit=
|pillColor=
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}}


==Further reading==
<!--Label Display Image-->
*Journal of Parenteral and Enteral Nutrition. 2002. [http://jpen.aspenjournals.org/cgi/content/abstract/26/6/357 Body cell mass repletion and improved quality of life in HIV-infected individuals receiving oxandrolone]
*Annals of Surgery. 2001. [http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=1421286 Anabolic Effects of Oxandrolone After Severe Burn]


==References==
{{LabelImage
* {{cite journal|author = |title =The Effects of Oxandrolone and Exercise on Muscle Mass and Function in Children With Severe Burns
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
|journal = Pediatrics|volume = 119|year = 2006|url = http://pediatrics.aappublications.org/cgi/content/abstract/119/1/e109}}
}}
* {{cite journal|author = |title = Oxandrolone induced lean mass gain during recovery from severe burns is maintained after discontinuation of the anabolic steroid
|journal = Burns|volume = 8|year = 2003|url = http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&list_uids=14636753}}
<div class="references-small">
{{reflist|2}}
</div>


==External links==
{{LabelImage
* [http://www.fda.gov/ohrms/dockets/dockets/05p0383/05p-0383-prc0001-03-Labeling-vol1.pdf Oxandrin® Label]
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
* [http://www.savientpharma.com/products/index.asp Oxandrin® Homepage]
}}
* [http://www.actupny.org/Vancouver/oxbackground.html Oxandrolone Background - News Article]
* [http://www.drugs.com/MTM/oxandrolone.html]


{{Anabolic steroids}}
<!--Category-->
[[Category:Anabolic steroids]]
[[Category:Endocrinology]]


[[de:Oxandrolon]]
[[Category:Drug]]
[[es:Oxandrolona]]
[[pt:Oxandrolona]]
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Revision as of 19:59, 6 January 2015

Oxandrolone
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Vignesh Ponnusamy, M.B.B.S. [2]

Disclaimer

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Black Box Warning

WARNING
See full prescribing information for complete Boxed Warning.
  • Peliosis hepatis, a condition in which liver and sometimes splenic tissue is replaced with blood-filled cysts, has been reported in patients receiving androgenic anabolic steroid therapy. these cysts are sometimes present with minimal hepatic dysfunction, but at other times they have been associated with liver failure. They are often not recognized until life-threatening liver failure or intra-abdominal hemorrhage develops. withdrawal of drug usually results in complete disappearance of lesions. Liver cell tumors are also reported. Most often these tumors are benign and androgen-dependent, but fatal malignant tumors have been reported. Withdrawal of drug often results in regression or cessation of progression of the tumor. However, hepatic tumors associated with androgens or anabolic steroids are much more vascular than other hepatic tumors and may be silent until life-threatening intra-abdominal hemorrhage develops. Blood lipid changes that are known to be associated with increased risk of atherosclerosis are seen in patients treated with androgens or anabolic steroids. These changes include decreased high-density lipoproteins and sometimes increased low-density lipoproteins. The changes may be very marked and could have a serious impact on the risk of atherosclerosis and coronary artery disease.

Overview

Oxandrolone is an anabolic steroid that is FDA approved for the {{{indicationType}}} of weight gain. There is a Black Box Warning for this drug as shown here. Common adverse reactions include edema, increased risk of atherosclerosis, cholestatic hepatitis, jaundice, atrophy of testis, erectile dysfunction, and priapism.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Oxandrolone is indicated as 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 the protein catabolism associated with prolonged administration of corticosteroids, and for the relief of the bone pain frequently accompanying osteoporosis (See DOSAGE AND ADMINISTRATION).

Therapy with anabolic steroids is adjunctive to and not a replacement for conventional therapy. The duration of therapy with oxandrolone will depend on the response of the patient and the possible appearance of adverse reactions. Therapy should be intermittent.

Adults: The response of individuals to anabolic steroids varies. The daily adult dosage is 2.5 mg to 20 mg given in 2 to 4 divided doses. The desired response may be achieved with as little as 2.5 mg or as much as 20 mg daily. A course of therapy of 2 to 4 weeks is usually adequate. This may be repeated intermittently as indicated.

Children: For children the total daily dosage of oxandrolone is ≤0.1 mg per kilogram body weight or ≤0.045 mg per pound of body weight. This may be repeated intermittently as indicated.

Geriatric Use: Recommended dose for geriatric patients is 5 mg bid.

Condition1
  • Dosing Information
  • Dosage
Condition2
  • Dosing Information
  • Dosage
Condition3
  • Dosing Information
  • Dosage
Condition4
  • Dosing Information
  • Dosage

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Oxandrolone in adult patients.

Non–Guideline-Supported Use

Alcoholic hepatitis

Burn, Severe; Adjunct

Cachexia associated with AIDS

Turner syndrome


Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Oxandrolone in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Oxandrolone in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Oxandrolone in pediatric patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Oxandrolone in pediatric patients.

Contraindications

  • Known or suspected carcinoma of the prostate or the male breast.
  • Carcinoma of the breast in females with hypercalcemia (androgenic anabolic steroids may stimulate osteolytic bone resorption).
  • Pregnancy, because of possible masculinization of the fetus. Oxandrolone has been shown to cause embryotoxicity, fetotoxicity, infertility, and masculinization of female animal offspring when given in doses 9 times the human dose.
  • Nephrosis, the nephrotic phase of nephritis.
  • Hypercalcemia.

Warnings

WARNING
See full prescribing information for complete Boxed Warning.
  • Peliosis hepatis, a condition in which liver and sometimes splenic tissue is replaced with blood-filled cysts, has been reported in patients receiving androgenic anabolic steroid therapy. these cysts are sometimes present with minimal hepatic dysfunction, but at other times they have been associated with liver failure. They are often not recognized until life-threatening liver failure or intra-abdominal hemorrhage develops. withdrawal of drug usually results in complete disappearance of lesions. Liver cell tumors are also reported. Most often these tumors are benign and androgen-dependent, but fatal malignant tumors have been reported. Withdrawal of drug often results in regression or cessation of progression of the tumor. However, hepatic tumors associated with androgens or anabolic steroids are much more vascular than other hepatic tumors and may be silent until life-threatening intra-abdominal hemorrhage develops. Blood lipid changes that are known to be associated with increased risk of atherosclerosis are seen in patients treated with androgens or anabolic steroids. These changes include decreased high-density lipoproteins and sometimes increased low-density lipoproteins. The changes may be very marked and could have a serious impact on the risk of atherosclerosis and coronary artery disease.
  • Cholestatic hepatitis and jaundice may occur with 17-alpha-alkylated androgens at a relatively low dose. If cholestatic hepatitis with jaundice appears or if liver function tests become abnormal, oxandrolone should be discontinued and the etiology should be determined. Drug-induced jaundice is reversible when the medication is discontinued.
  • In patients with breast cancer, anabolic steroid therapy may cause hypercalcemia by stimulating osteolysis. Oxandrolone therapy should be discontinued if hypercalcemia occurs.
  • Edema with or without congestive heart failure may be a serious complication in patients with pre-existing cardiac, renal, or hepatic disease. Concomitant administration of adrenal cortical steroid or ACTH may increase the edema.
  • In children, androgen therapy may accelerate bone maturation without producing compensatory gain in linear growth. This adverse effect results in compromised adult height. The younger the child, the greater the risk of compromising final mature height. The effect on bone maturation should be monitored by assessing bone age of the left wrist and hand every 6 months (See PRECAUTIONS: Laboratory Tests).
  • Geriatric patients treated with androgenic anabolic steroids may be at an increased risk for the development of prostatic hypertrophy and prostatic carcinoma.
  • Anabolic steroids have not been shown to enhance athletic ability.

Precautions

  • Concurrent dosing of oxandrolone with warfarin may result in unexpectedly large increases in the INR or prothrombin time (PT). When oxandrolone is prescribed to patients being treated with warfarin, doses of warfarin may need to be decreased significantly to maintain the desirable INR level and diminish the risk of potentially serious bleeding (See PRECAUTIONS: Drug Interactions).
  • General
  • Women should be observed for signs of virilization (deepening of the voice, hirsutism, acne, clitoromegaly). Discontinuation of drug therapy at the time of evidence of mild virilism is necessary to prevent irreversible virilization. Some virilizing changes in women are irreversible even after prompt discontinuance of therapy and are not prevented by concomitant use of estrogens. Menstrual irregularities may also occur.
  • Anabolic steroids may cause suppression of clotting factors II, V, VII, and X, and an increase in prothrombin time.

Adverse Reactions

Clinical Trials Experience

  • Patients with moderate to severe COPD or COPD patients who are unresponsive to bronchodilators should be monitored closely for COPD exacerbation and fluid retention.
  • The following adverse reactions have been associated with use of anabolic steroids: Hepatic: Cholestatic jaundice with, rarely, hepatic necrosis and death. Hepatocellular neoplasms and peliosis hepatis with long-term therapy (See WARNINGS). Reversible changes in liver function tests also occur including increased bromsulfophthalein (BSP) retention, changes in alkaline phosphatase and increases in serum bilirubin, aspartate aminotransferase (AST, SGOT) and alanine aminotransferase (ALT, SGPT)
  • In males:
  • Prepubertal: Phallic enlargement and increased frequency or persistence of erections.
  • Postpubertal: Inhibition of testicular function, testicular atrophy and oligospermia, impotence, chronic priapism, epididymitis, and bladder irritability.
  • In females:
  • Clitoral enlargement, menstrual irregularities.
CNS

Habituation, excitation, insomnia, depression, and changes in libido.

Hematologic

Bleeding in patients on concomitant oral anticoagulant therapy.

Breast

Gynecomastia.

Larynx

Deepening of the voice in females.

Hair

Hirsutism and male pattern baldness in females.

Skin

Acne (especially in females and prepubertal males).

Skeletal

Premature closure of epiphyses in children.

Fluid and electrolytes

Edema, retention of serum electrolytes (sodium chloride, potassium, phosphate, calcium).

Metabolic/Endocrine

Decreased glucose tolerance, increased creatinine excretion, increased serum levels of creatinine phosphokinase (CPK). Masculinization of the fetus. Inhibition of gonadotropin secretion.

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Oxandrolone in the drug label.

Drug Interactions

  • Anticoagulants
  • Anabolic steroids may increase sensitivity to oral anticoagulants. Dosage of the anticoagulant may have to be decreased in order to maintain desired prothrombin time. Patients receiving oral anticoagulant therapy require close monitoring, especially when anabolic steroids are started or stopped.
  • Warfarin
  • A multidose study of oxandrolone, given as 5 or 10 mg bid in 15 healthy subjects concurrently treated with warfarin, resulted in a mean increase in S-warfarin half-life from 26 to 48 hours and AUC from 4.55 to 12.08 ng*hr/mL; similar increases in R-warfarin half-life and AUC were also detected. Microscopic hematuria (9/15) and gingival bleeding (1/15) were also observed. A 5.5-fold decrease in the mean warfarin dose from 6.13 mg/day to 1.13 mg/day (approximately 80-85% reduction of warfarin dose), was necessary to maintain a target INR of 1.5. When oxandrolone therapy is initiated in a patient already receiving treatment with warfarin, the INR 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 drugs, careful monitoring of the INR or PT, and adjustment of the warfarin dosage if indicated are recommended when the oxandrolone dose is changed or discontinued. Patients should be closely monitored for signs and symptoms of occult bleeding.
  • Oral hypoglycemic agents
  • Oxandrolone may inhibit the metabolism of oral hypoglycemic agents.
  • Adrenal steroids or ACTH
  • In patients with edema, concomitant administration with adrenal cortical steroids or ACTH may increase the edema.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category X


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Oxandrolone in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Oxandrolone during labor and delivery.

Nursing Mothers

  • It is not known whether anabolic steroids are excreted in human milk. Because of the potential of serious adverse reactions in nursing infants from oxandrolone, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

  • 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 adult height. Androgenic anabolic steroid therapy should be used very cautiously in children and only by specialists who are aware of the effects on bone maturation (See WARNINGS).

Geriatic Use

There is no FDA guidance on the use of Oxandrolone with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Oxandrolone with respect to specific gender populations.

Race

There is no FDA guidance on the use of Oxandrolone with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Oxandrolone in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Oxandrolone in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Oxandrolone in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Oxandrolone in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral

Monitoring

There is limited information regarding Monitoring of Oxandrolone in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Oxandrolone in the drug label.

Overdosage

Acute Overdose

  • No symptoms or signs associated with overdosage have been reported. It is possible that sodium and water retention may occur.
  • The oral LD50 of oxandrolone in mice and dogs is greater than 5,000 mg/kg. No specific antidote is known, but gastric lavage may be used.

Chronic Overdose

There is limited information regarding Chronic Overdose of Oxandrolone in the drug label.

Pharmacology

There is limited information regarding Oxandrolone Pharmacology in the drug label.

Mechanism of Action

  • Anabolic steroids are synthetic derivatives of testosterone. Certain clinical effects and adverse reactions demonstrate the androgenic properties of this class of drugs. Complete dissociation of anabolic and androgenic effects has not been achieved. The actions of anabolic steroids are therefore similar to those of male sex hormones with the possibility of causing serious disturbances of growth and sexual development if given to young children. Anabolic steroids suppress the gonadotropic functions of the pituitary and may exert a direct effect upon the testes.
  • During exogenous administration of anabolic androgens, endogenous testosterone release is inhibited through inhibition of pituitary luteinizing hormone (LH). At large doses, spermatogenesis may be suppressed through feedback inhibition of pituitary follicle-stimulating hormone (FSH)

Structure

  • Oxandrolone oral tablets contain 2.5 mg or 10 mg of the anabolic steroid oxandrolone. Oxandrolone is 17β-hydroxy-17α-methyl-2-oxa-5α-androstan-3-one with the following structural formula:
This image is provided by the National Library of Medicine.
  • Inactive ingredients include cornstarch, lactose, magnesium stearate, and hydroxypropyl methylcellulose.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Oxandrolone in the drug label.

Pharmacokinetics

  • In a single dose pharmacokinetic study of oxandrolone in elderly subjects, the mean elimination half-life was 13.3 hours. In a previous single dose pharmacokinetic study in younger volunteers, the mean elimination half-life was 10.4 hours. No significant differences between younger and elderly volunteers were found for time to peak, peak plasma concentration or AUC after a single dose of oxandrolone. The correlation between plasma level and therapeutic effect has not been defined.

Nonclinical Toxicology

  • Oxandrolone has not been tested in laboratory animals for carcinogenic or mutagenic effects. In 2-year chronic oral rat studies, a dose-related reduction of spermatogenesis and decreased organ weights (testes, prostate, seminal vesicles, ovaries, uterus, adrenals, and pituitary) were shown.

Clinical Studies

There is limited information regarding Clinical Studies of Oxandrolone in the drug label.

How Supplied

  • Oxandrolone 2.5 mg tablets are oval, white, and scored with OX on one side and “11” on each side of the scoreline on the other side; bottles of 100 (NDC 0591-3544-01).
  • Oxandrolone 10 mg tablets are capsule shaped, white, with OX on one side and “10” on the other side; bottles of 60 (NDC 0591-3545-60).

Storage

There is limited information regarding Oxandrolone Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

  • The physician should instruct patients to report immediately any use of warfarin and any bleeding.
  • The physician should instruct patients to report any of the following side effects of androgens:
  • Males: Too frequent or persistent erections of the penis, appearance or aggravation of acne.
  • Females: Hoarseness, acne, changes in menstrual periods, or more facial hair.
  • All patients: Nausea, vomiting, changes in skin color, or ankle swelling.

Precautions with Alcohol

  • Alcohol-Oxandrolone interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

  • OXANDROLONE®[1]

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. ↑ "OXANDROLONE oxandrolone tablet".
  2. ↑ "http://www.ismp.org". External link in |title= (help)


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