Oxymetholone 50 mg

Oxymetholone 50 mg (Oxymetholone) · ATC A14AA05

Anabolic steroid · oral 17α-methylated

Each tablet contains Oxymetholone 50 mg.

For the full list of excipients, see section 6.1.

Tablet for oral administration.

Therapeutic indications

Adjunct in the treatment of selected anaemias and catabolic states, as determined by a physician.

Posology and method of administration

Take orally as directed by a physician. Swallow whole with water. Do not exceed the prescribed dose.

Contraindications

Known hypersensitivity to the active substance or excipients. Known or suspected carcinoma of the prostate or male breast. Not for use in women, in pregnancy or while breastfeeding. Use with caution in cardiac, renal or hepatic impairment.

Special warnings and precautions for use

Keep out of the reach and sight of children. Contains a substance prohibited in sport (WADA).

Interaction with other medicinal products

Coumarin anticoagulants

Substantial potentiation of anticoagulant effect with prolonged prothrombin time and serious bleeding risk; anticoagulant dosage must be reduced and INR monitored closely, particularly relevant in thrombocytopenic patients with marrow failure.

Insulin and oral antidiabetic agents

Glucose tolerance may be altered and hypoglycaemia can occur; antidiabetic therapy should be reviewed and blood glucose monitored.

Ciclosporin

Reduced hepatic clearance of ciclosporin with raised blood concentrations and increased nephrotoxicity, a combination of practical importance in aplastic anaemia.

Corticosteroids and corticotrophin

Additive sodium and water retention with a substantial risk of oedema; oxymetholone is itself markedly sodium-retaining.

Other hepatotoxic medicinal products and alcohol

Additive hepatic injury; concurrent use should be avoided and liver function monitored, given the high baseline hepatotoxic potential of oxymetholone.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Oxymetholone is a potent virilising agent that may masculinise a female foetus and must not be used during pregnancy or breastfeeding; effective contraception is required in women of childbearing potential.

Paediatric population

Where used in childhood marrow failure syndromes under specialist haematological supervision, radiological monitoring of bone age is mandatory every six months; androgen-induced advance of skeletal maturation may continue after withdrawal and compromise final height.

Elderly

Older men are at increased risk of prostatic hypertrophy, occult prostatic carcinoma, hyperviscosity and cardiac decompensation from fluid retention; prostatic assessment, haematocrit and cardiovascular status should be monitored.

Hepatic impairment

Contraindicated in hepatic impairment and hepatic tumours. Peliosis hepatis and hepatic neoplasia may occur without warning and may present only at rupture or with haemorrhage; liver function tests and periodic hepatic imaging are warranted during prolonged therapy.

Renal impairment and cardiac failure

Marked sodium and water retention may precipitate oedema, hypertension or congestive cardiac failure; weight, blood pressure and serum electrolytes require regular monitoring and concomitant diuretic therapy may be needed.

Athletes

Oxymetholone is prohibited in and out of competition as an exogenous anabolic androgenic steroid under class S1.1a of the WADA Prohibited List; administration will produce an adverse analytical finding in doping control.

Undesirable effects

Hepatobiliary disorders

Cholestatic jaundice, marked elevation of transaminases and alkaline phosphatase, peliosis hepatis with potentially fatal intra-abdominal haemorrhage, hepatic adenoma and hepatocellular carcinoma with prolonged high-dose use

Reproductive system and breast disorders

Gynaecomastia and breast tenderness in men, priapism, oligospermia and testicular atrophy, prostatic hypertrophy; in women, menstrual disturbance and clitoral enlargement

Blood and lymphatic system disorders

Polycythaemia with raised haematocrit and hyperviscosity, leukaemia reported in patients with aplastic anaemia treated with androgens, iron-deficiency anaemia on withdrawal

Metabolism and nutrition disorders

Pronounced sodium and water retention with oedema and weight gain, hypercalcaemia, impaired glucose tolerance

Investigations

Severe reduction in HDL-cholesterol with rise in LDL-cholesterol, suppressed gonadotrophins and endogenous testosterone, altered thyroid function tests

Endocrine disorders

Virilisation in women, including hirsutism, deepening of the voice and androgenic alopecia, which may be irreversible

Skin and subcutaneous tissue disorders

Severe acne, seborrhoea, hirsutism, striae

Psychiatric and nervous system disorders

Excitation, aggression, insomnia, headache, depressed mood on withdrawal

Overdose

Overdosage may present with nausea, vomiting, gross oedema, hypertension and gynaecomastia, and with continued excessive exposure cholestatic jaundice, polycythaemia and hepatic injury. There is no specific antidote; management consists of withdrawal of the product with symptomatic and supportive treatment, including close monitoring of liver function, full blood count, haematocrit and fluid balance.

Pharmacodynamic properties

Oxymetholone (ATC A14AA05) is a potent 17alpha-alkylated anabolic steroid derived from dihydrotestosterone, bearing a 2-hydroxymethylene substituent on the A-ring. It is an androgen receptor agonist that markedly stimulates protein anabolism and erythropoiesis, in part through increased production of erythropoietin and enhanced responsiveness of erythroid progenitor cells, and is used in anaemias caused by deficient red cell production, including acquired and congenital aplastic anaemia, myelofibrosis and hypoplastic anaemia due to myelotoxic drugs. Although the saturated A-ring precludes aromatisation, oxymetholone displays pronounced oestrogenic-type adverse effects such as gynaecomastia and fluid retention, attributed to intrinsic activity at the oestrogen receptor rather than to conversion by aromatase. It is among the most hepatotoxic agents of its class and produces severe suppression of HDL-cholesterol.

Pharmacokinetic properties

Oxymetholone is absorbed from the gastrointestinal tract and, being 17alpha-alkylated, escapes complete hepatic first-pass inactivation. It is extensively bound to plasma proteins, with low affinity for sex hormone binding globulin. Hepatic metabolism includes loss or reduction of the 2-hydroxymethylene group to yield mestanolone (17alpha-methyl-5alpha-dihydrotestosterone), reduction of the 3-keto function to 2-hydroxymethyl-17alpha-methyl-5alpha-androstane-3,17-diols, and conjugation to glucuronides and sulphates. Excretion is chiefly urinary as conjugated metabolites; the reported elimination half-life is approximately 8 to 9 hours, with hepatic exposure to the intact 17alpha-alkylated molecule sustained by biliary recirculation.

List of excipients

Microcrystalline cellulose (PH-102), maize starch, povidone K30, sodium starch glycolate (type A), colloidal anhydrous silica, magnesium stearate. Uncoated tablet; the formulation is lactose-free, the high drug load at 50 mg being carried on a cellulose-based diluent system. All excipients comply with the current Ph. Eur. or USP-NF monograph.

Excipient warnings

This medicine contains less than 1 mmol sodium (23 mg) per tablet, that is to say essentially sodium-free.

Incompatibilities

Not applicable.

Shelf life

36 months from the date of manufacture in the unopened container. Do not use after the expiry date printed on the carton and bottle label.

After first opening

After first opening of the bottle, use within 60 days. Keep the bottle tightly closed between withdrawals and leave the desiccant canister in place; it is part of the container-closure system and is not for consumption.

Storage

Store below 25 °C in a dry place. Keep tablets in the outer carton until use.

Container

White opaque high-density polyethylene (HDPE) bottle with a desiccant canister, closed with a child-resistant, tamper-evident polypropylene cap over an induction-sealed liner. Pack size: 50 uncoated tablets in one bottle per serialised carton, with the patient information leaflet, GS1 DataMatrix, human-readable serial and verification code.

Disposal

No special requirements for destruction. Any unused medicinal product or waste material should be disposed of in accordance with local requirements. Tablets must not be disposed of via wastewater or with household waste; unused tablets, part-used bottles and empty packaging should be returned to the point of supply for controlled disposal.

Pack

50 Tablets

GTIN

05012345678922

Serial

5418 3296 1074 22

LOT

OY2708H

MFG

10 / 2027

EXP

10 / 2030

Every carton carries a GS1 DataMatrix and a verification code; a pack can be checked at ergopharm.net/verify.

Ergopharm Advanced Research Centre, Tandalja, Vadodara, Gujarat 390012, India. For Export Only.

Report a suspected adverse reaction or quality defect to pv@ergopharm.net.