Methandrostenolone 10 mg

Methandrostenolone 10 mg (Metandienone (methandrostenolone)) · ATC A14AA03

Anabolic steroid · oral 17α-methylated

Each tablet contains Methandrostenolone 10 mg.

For the full list of excipients, see section 6.1.

Tablet for oral administration.

Therapeutic indications

Short-course anabolic therapy under close medical supervision.

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

Anticoagulant activity is markedly enhanced through reduced synthesis of clotting factors and displacement from binding sites, with a risk of haemorrhage; INR must be monitored and the anticoagulant dose reduced accordingly.

Insulin and oral antidiabetic agents

Requirements may fall as glucose tolerance changes; conversely fluid retention and weight gain may confound glycaemic control, so monitoring is necessary.

Corticosteroids and corticotrophin

Additive fluid retention and increased risk of oedema and acne.

Hepatotoxic medicinal products and alcohol

Additive risk of cholestasis and hepatocellular injury; concurrent use should be avoided where possible.

Antihypertensive agents and diuretics

Efficacy may be reduced by androgen-induced sodium and water retention, requiring adjustment of antihypertensive therapy.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Virilisation of a female foetus may occur, and the strongly oestrogenic metabolite adds further theoretical risk; use in breastfeeding is not recommended as excretion in milk cannot be excluded.

Paediatric population

Not recommended. Androgens advance bone age disproportionately and may cause irreversible premature epiphyseal fusion with loss of final adult height, together with precocious virilisation.

Elderly

Caution is required because of the risk of prostatic hypertrophy, unmasking of occult prostatic carcinoma, fluid retention and cardiac decompensation; prostatic and cardiovascular assessment is advised before treatment.

Hepatic impairment

Contraindicated in hepatic tumours and in significant hepatic impairment. Liver function tests should be performed at baseline and periodically, and treatment discontinued if cholestasis or a sustained rise in transaminases develops.

Cardiac, renal and hypertensive patients

Sodium and water retention may aggravate cardiac failure, hypertension or renal dysfunction; regular monitoring of weight, blood pressure and electrolytes is required.

Athletes

Methandrostenolone is an exogenous anabolic androgenic steroid prohibited at all times, in and out of competition, under class S1.1a of the WADA Prohibited List. Its urinary metabolites are detectable for an extended period and its use will result in an adverse analytical finding.

Undesirable effects

Hepatobiliary disorders

Dose-related cholestatic jaundice, raised transaminases, alkaline phosphatase and bilirubin, peliosis hepatis and hepatic adenoma with prolonged administration

Reproductive system and breast disorders

Gynaecomastia and breast tenderness (reflecting conversion to 17alpha-methyloestradiol), oligospermia, testicular atrophy, priapism; in women, menstrual disturbance and clitoral enlargement

Metabolism and nutrition disorders

Sodium and water retention with oedema and weight gain, hypertension, impaired glucose tolerance

Investigations

Pronounced fall in HDL-cholesterol with rise in LDL-cholesterol, raised haematocrit and haemoglobin, suppressed serum LH, FSH and testosterone

Skin and subcutaneous tissue disorders

Acne vulgaris, seborrhoea, striae, hirsutism in women, androgenetic alopecia

Psychiatric disorders

Increased aggression and irritability, mood swings, hypomania, insomnia, depressive symptoms after discontinuation

Musculoskeletal and connective tissue disorders

Premature epiphyseal closure in adolescents, tendon and ligament strain, muscle cramp

Cardiac and vascular disorders

Left ventricular hypertrophy, hypertension, and an increased atherogenic risk attributable to the adverse lipid profile

Overdose

Acute overdosage is unlikely to be life-threatening and typically presents with nausea, vomiting, headache, oedema and gynaecomastia; sustained excessive exposure produces cholestatic jaundice, polycythaemia, hypertension and marked lipid disturbance. No specific antidote exists; treatment is withdrawal of the product with symptomatic and supportive management, including monitoring of liver function, haematocrit and blood pressure.

Pharmacodynamic properties

Methandrostenolone (metandienone) is an anabolic androgenic steroid, the delta-1 dehydrogenated analogue of 17alpha-methyltestosterone. It acts as an agonist at the nuclear androgen receptor, promoting nitrogen retention, protein synthesis in skeletal muscle and erythropoiesis, with a modest anabolic bias over androgenic activity. Introduction of the 1,2 double bond reduces affinity for sex hormone binding globulin and slows 5alpha-reduction, but the molecule remains a substrate for aromatase, being converted to 17alpha-methyloestradiol, a potent and slowly cleared oestrogen; this accounts for the pronounced oestrogenic profile of the agent. As with all exogenous androgens, hypothalamic-pituitary-gonadal feedback suppression reduces endogenous testosterone secretion and spermatogenesis.

Pharmacokinetic properties

Methandrostenolone is rapidly and almost completely absorbed after oral administration, the 17alpha-methyl substituent conferring resistance to hepatic 17beta-hydroxysteroid dehydrogenase and hence oral bioavailability. Plasma protein binding is high but affinity for sex hormone binding globulin is low, leaving a comparatively large free fraction. Metabolism is hepatic and extensive, comprising 6beta-hydroxylation, 17-epimerisation to 17-epimetandienone, aromatisation of the A-ring to 17alpha-methyloestradiol and reduction of the 3-keto group; metabolites are excreted in urine chiefly as glucuronide conjugates. The elimination half-life of the parent compound is short, of the order of 3 to 6 hours, although hydroxylated and epimeric metabolites remain detectable in urine for considerably longer.

List of excipients

Lactose monohydrate (direct-compression grade), microcrystalline cellulose (PH-102), sodium starch glycolate (type A), colloidal anhydrous silica, magnesium stearate. Uncoated, scored tablet; no film-coat or colouring agent is applied. 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; a tablet pressed out of the blister should be taken immediately. A tablet divided at the score line for a half dose should be used at the next administration and not stored loose.

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 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

05012345678918

Serial

1074 8529 6307 18

LOT

MD2704D

MFG

06 / 2027

EXP

06 / 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.