Fluoxymesterone 10 mg

Fluoxymesterone 10 mg (Fluoxymesterone) · ATC G03BA01

Androgen · oral 17α-methylated

Each film-coated tablet contains Fluoxymesterone 10 mg.

For the full list of excipients, see section 6.1.

Tablet for oral administration.

Therapeutic indications

Androgen therapy where a potent oral androgen is preferred, 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, acenocoumarol)

Anticoagulant effect is potentiated, with a marked fall in prothrombin activity and risk of bleeding; more frequent INR monitoring and dose reduction of the anticoagulant are required.

Insulin and oral antidiabetic agents

Glucose tolerance may improve and insulin sensitivity increase, so hypoglycaemia can occur unless antidiabetic therapy is reassessed.

Corticosteroids and corticotrophin

Additive sodium and water retention with increased risk of oedema, particularly in patients with cardiac or hepatic disease.

Other hepatotoxic medicinal products (for example methotrexate, azole antifungals, isoniazid) and alcohol

Additive hepatocellular and cholestatic injury; liver function should be monitored.

Ciclosporin

Reduced hepatic clearance of ciclosporin with raised trough concentrations and increased nephrotoxicity.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Androgens cross the placenta and cause virilisation of a female foetus; excretion into breast milk and suppression of lactation cannot be excluded. Women of childbearing potential must use effective contraception during treatment.

Paediatric population

Use only under specialist endocrinological supervision. Androgens accelerate skeletal maturation disproportionately to linear growth and may cause irreversible premature epiphyseal closure and reduced final height; bone age should be monitored radiologically at intervals.

Elderly

Increased risk of prostatic hypertrophy, occult prostatic carcinoma, polycythaemia and fluid retention. Digital rectal examination, prostate-specific antigen and haematocrit should be assessed before and during treatment.

Hepatic impairment

Contraindicated in severe hepatic impairment. Because the 17alpha-alkyl group predisposes to cholestasis and peliosis hepatis, liver function tests are required at baseline and periodically; treatment must be stopped if jaundice or a persistent rise in transaminases occurs.

Renal impairment and cardiac disease

Sodium and water retention may precipitate or worsen oedema, hypertension and cardiac failure; caution and monitoring of weight, blood pressure and electrolytes are required.

Athletes

Fluoxymesterone is an exogenous anabolic androgenic steroid listed in class S1.1a of the WADA Prohibited List and is prohibited in and out of competition. Use will produce an adverse analytical finding; athletes subject to anti-doping regulation must not be treated with this product other than under a granted therapeutic use exemption.

Undesirable effects

Hepatobiliary disorders

Cholestatic jaundice, raised serum transaminases and bilirubin, peliosis hepatis, hepatic adenoma and, with prolonged high-dose use, hepatocellular carcinoma

Endocrine disorders

Suppression of gonadotrophins with reduced endogenous testosterone, oligospermia and testicular atrophy in men; virilisation in women (hirsutism, deepening of the voice, clitoral enlargement, menstrual irregularity), some features being irreversible

Investigations

Marked reduction in HDL-cholesterol with increased LDL-cholesterol, suppressed thyroxine-binding globulin, polycythaemia and raised haematocrit

Reproductive system and breast disorders

Priapism and excessive sexual stimulation, gynaecomastia, prostatic hypertrophy and acceleration of pre-existing prostatic carcinoma in older men

Skin and subcutaneous tissue disorders

Acne, seborrhoea, hirsutism, male-pattern hair loss

Metabolism and nutrition disorders

Sodium and water retention with oedema, hypercalcaemia (notably in patients treated for metastatic breast carcinoma)

Psychiatric disorders

Irritability, aggression, mood lability, insomnia, depressed mood on withdrawal

Musculoskeletal and connective tissue disorders

Premature epiphyseal closure in adolescents, muscle cramp

Overdose

Acute overdosage is expected to produce nausea, vomiting, headache, oedema and, on repeated excessive exposure, cholestatic jaundice and virilisation. There is no specific antidote; management consists of withdrawal of the medicinal product, supportive care and monitoring of liver function, electrolytes and haematocrit.

Pharmacodynamic properties

Fluoxymesterone is an androgen and anabolic steroid (ATC G03BA01), chemically 9-fluoro-11beta-hydroxy-17alpha-methyltestosterone. It is an agonist at the nuclear androgen receptor; the ligand-receptor complex binds androgen response elements in target-cell DNA and modulates transcription of genes governing male secondary sexual characteristics, nitrogen retention and erythropoiesis. The 9-fluoro and 11beta-hydroxy substitutions confer high androgenic potency relative to methyltestosterone while rendering the molecule essentially resistant to aromatisation, so oestrogenic effects are less prominent than with methyltestosterone. Like all exogenous androgens it suppresses hypothalamic gonadotrophin-releasing hormone and pituitary LH/FSH secretion, reducing endogenous testosterone production and spermatogenesis.

Pharmacokinetic properties

Fluoxymesterone is absorbed from the gastrointestinal tract and, being 17alpha-alkylated, resists complete first-pass hepatic degradation, giving useful oral activity. It circulates extensively bound to plasma proteins, with lower affinity for sex hormone binding globulin than unmodified testosterone. Metabolism is hepatic, principally by 11-oxidation to 11-ketofluoxymesterone and by 6beta-hydroxylation, with conjugation to glucuronides and sulphates; the 17alpha-methyl group prevents oxidation at C-17 and accounts for the prolonged hepatic exposure characteristic of this class. Elimination is predominantly renal as conjugated metabolites; the reported elimination half-life is approximately 9 hours.

List of excipients

Tablet core: lactose monohydrate, maize starch, povidone K30, croscarmellose sodium, colloidal anhydrous silica, magnesium stearate. Film-coat: hypromellose 6 cP, macrogol 6000, talc, titanium dioxide (E171). 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 film-coated tablet, that is to say essentially sodium-free.

Incompatibilities

Not applicable. Compatibility with vehicles for extemporaneous dispersion has not been studied; the film-coated tablet should be swallowed whole and not crushed or dispersed.

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 do not remove or discard the desiccant canister; 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 containing a desiccant canister, closed with a child-resistant, tamper-evident polypropylene cap over an induction-sealed liner. Pack size: 50 film-coated tablets in one bottle per serialised carton. The carton carries the GS1 DataMatrix, human-readable serial and the scratch-off 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

05012345678917

Serial

9630 7418 5296 17

LOT

FM2703C

MFG

05 / 2027

EXP

05 / 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.