Oxandrolone 10 mg

Oxandrolone 10 mg (Oxandrolone) · ATC A14AA08

Anabolic steroid · oral, DHT-derived

Each tablet contains Oxandrolone 10 mg.

For the full list of excipients, see section 6.1.

Tablet for oral administration.

Therapeutic indications

Adjunct to promote weight gain and offset protein catabolism in selected conditions, 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 (warfarin)

Oxandrolone markedly potentiates warfarin, with reported reductions in warfarin dose requirement of the order of 80 to 85 per cent; anticoagulant dose must be reduced and INR monitored frequently at initiation, dose change and withdrawal.

Insulin and oral antidiabetic agents

Blood glucose and insulin requirements may fall; glycaemic monitoring and dose adjustment of antidiabetic therapy are required.

Corticosteroids

Oxandrolone is used to offset corticosteroid-induced protein catabolism, but the combination increases the risk of oedema; sodium and fluid balance should be monitored, particularly in patients with cardiac or hepatic disease.

Other hepatotoxic medicinal products and alcohol

Additive hepatocellular and cholestatic injury; liver function tests should be repeated periodically.

Ciclosporin

Reduced clearance with raised ciclosporin concentrations and increased risk of nephrotoxicity.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Oxandrolone may cause virilisation of a female foetus and is not to be used during breastfeeding; women of childbearing potential should use effective contraception during treatment.

Paediatric population

Where used in children under specialist supervision, for example in growth failure or after severe burns, bone age must be monitored radiologically at six-monthly intervals because androgen-induced advance of skeletal maturation may persist after the product is stopped and compromise final height.

Elderly

Increased risk of prostatic hypertrophy and occult prostatic carcinoma in older men, together with a greater susceptibility to fluid retention; prostatic and cardiovascular assessment is advised before treatment.

Hepatic impairment

Contraindicated in hepatic tumours and significant hepatic impairment. Liver function tests should be obtained at baseline and periodically; treatment must be stopped if cholestatic jaundice or a persistent rise in transaminases occurs.

Renal impairment and cardiac failure

A substantial fraction of the dose is excreted unchanged in urine, so exposure may be increased in renal impairment; sodium and water retention may aggravate oedema, hypertension or cardiac failure and requires monitoring of weight and blood pressure.

Athletes

Oxandrolone is prohibited at all times, in and out of competition, as an exogenous anabolic androgenic steroid under class S1.1a of the WADA Prohibited List; use will result in an adverse analytical finding.

Undesirable effects

Hepatobiliary disorders

Raised transaminases, cholestatic jaundice, and with prolonged use peliosis hepatis and hepatic adenoma; hepatic effects are generally less frequent than with more potent 17alpha-alkylated agents but are not absent

Investigations

Marked reduction in HDL-cholesterol with increase in LDL-cholesterol, raised haematocrit, altered thyroid function test results through suppression of thyroxine-binding globulin

Endocrine disorders

Suppression of gonadotrophins with reduced endogenous testosterone and oligospermia in men; in women, hirsutism, deepening of the voice, clitoral enlargement and menstrual irregularity, which may be irreversible

Musculoskeletal and connective tissue disorders

Premature epiphyseal closure and reduced final adult height in children, muscle cramp

Skin and subcutaneous tissue disorders

Acne, seborrhoea, male-pattern hair loss, hirsutism

Metabolism and nutrition disorders

Sodium and water retention with oedema, hypercalcaemia, changes in glucose tolerance

Psychiatric disorders

Insomnia, excitation, irritability, depressed mood

Reproductive system and breast disorders

Priapism, changes in libido, prostatic enlargement in older men

Overdose

Acute overdosage is of low acute toxicity and may produce nausea, vomiting, oedema and headache; repeated excessive exposure leads to hepatic dysfunction, adverse lipid changes and virilisation in women. No antidote is available and treatment is symptomatic and supportive, with discontinuation of the product and monitoring of hepatic function and lipid profile.

Pharmacodynamic properties

Oxandrolone (ATC A14AA08) is a synthetic anabolic steroid derived from dihydrotestosterone in which the C-2 carbon of the A-ring is replaced by oxygen, giving a 2-oxa-17alpha-methyl-5alpha-androstane structure. It is an androgen receptor agonist with a high anabolic-to-androgenic ratio, promoting nitrogen retention, protein anabolism and lean tissue accrual with relatively little virilising activity; it is used as an adjunct to promote weight gain after extensive surgery, chronic infection or trauma, and to offset the protein catabolism of prolonged corticosteroid therapy. Because the A-ring is oxygen-substituted and already saturated, oxandrolone is neither aromatised to oestrogens nor a substrate for 5alpha-reductase, so oestrogenic effects do not occur. It is nevertheless 17alpha-alkylated and retains the class risks of hepatotoxicity and marked suppression of HDL-cholesterol, albeit generally to a lesser degree than more potent oral agents.

Pharmacokinetic properties

Oxandrolone is rapidly and well absorbed after oral administration, the 2-oxa substitution and 17alpha-methyl group together conferring high metabolic stability. Plasma protein binding is high, of the order of 94 to 97 per cent. In contrast to other members of the class, oxandrolone undergoes comparatively little hepatic biotransformation and a substantial proportion of the dose, in the region of a quarter to a third, is excreted unchanged in the urine; the remainder is eliminated as 17-epimeric and hydroxylated metabolites and their conjugates. The elimination half-life in adults is approximately 9 to 10 hours and is shorter in children.

List of excipients

Lactose monohydrate, maize starch, pregelatinised maize starch, hypromellose 6 cP (granulation binder), croscarmellose sodium, colloidal anhydrous silica, magnesium stearate. Uncoated, scored tablet manufactured by aqueous granulation. All excipients comply with the current Ph. Eur. or USP-NF monograph.

Excipient warnings

This medicine contains lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine. 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 blister. Do not use after the expiry date printed on the carton and blister foil.

After first opening

No in-use shelf life applies to the blister presentation. Tablets should be left in the intact blister until the moment of administration. Where the score line is used to give a half dose, the remaining half should be used at the next administration and not stored beyond 24 hours outside the blister.

Storage

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

Container

Push-through blister of PVC/PVdC film sealed to hard-tempered aluminium foil, 10 tablets per blister strip. Pack size: 100 scored, uncoated tablets (10 strips) per serialised, tamper-evident 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 blisters and empty packaging should be returned to the point of supply for controlled disposal.

Pack

100 Tablets

GTIN

05012345678921

Serial

4307 2185 9630 21

LOT

OX2707G

MFG

09 / 2027

EXP

09 / 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.