Turinabol 10 mg

Turinabol 10 mg (4-Chlorodehydromethyltestosterone (chlorodehydromethyltestosterone; no INN has been assigned))

Anabolic steroid · oral, chlorinated non-aromatising

Each tablet contains 4-Chlorodehydromethyltestosterone 10 mg.

For the full list of excipients, see section 6.1.

Tablet for oral administration.

Therapeutic indications

Anabolic therapy where a mild, non-aromatising oral agent is preferred, 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 effect is enhanced with prolongation of prothrombin time and risk of haemorrhage; INR must be monitored and the anticoagulant dose adjusted at initiation and withdrawal.

Insulin and oral antidiabetic agents

Insulin sensitivity may increase and glucose-lowering requirements fall; blood glucose should be monitored and antidiabetic therapy adjusted.

Corticosteroids and corticotrophin

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

Hepatotoxic medicinal products (including methotrexate, azole antifungals, isoniazid) and alcohol

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

Lipid-lowering therapy (statins, fibrates)

The severe androgen-induced suppression of HDL-cholesterol is not corrected by lipid-lowering therapy and may mask assessment of cardiovascular risk; lipid monitoring is required in any patient on concomitant treatment.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. The compound crosses the placenta and can virilise a female foetus; it must not be used during pregnancy or breastfeeding, and women of childbearing potential require effective contraception.

Paediatric population

Not recommended. Androgens advance skeletal maturation disproportionately to linear growth and may cause irreversible premature epiphyseal closure 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, polycythaemia and cardiovascular decompensation; prostatic examination, prostate-specific antigen and haematocrit should be assessed before and during treatment.

Hepatic impairment

Contraindicated in significant hepatic impairment and in hepatic tumours. As a 17alpha-alkylated androgen it carries the class risk of cholestasis and peliosis hepatis; liver function tests are required at baseline and periodically, and treatment stopped if jaundice or a persistent transaminase rise occurs.

Renal impairment and cardiovascular disease

Sodium and water retention may aggravate oedema, hypertension or cardiac failure; the severe HDL-cholesterol suppression makes use inadvisable in established ischaemic heart disease or familial dyslipidaemia.

Athletes

Chlorodehydromethyltestosterone 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. Its long-term metabolites are detectable in urine for months after the last administration and stored samples may be reanalysed retrospectively, so any use will lead to an adverse analytical finding.

Undesirable effects

Hepatobiliary disorders

Raised transaminases and bilirubin, cholestatic jaundice, peliosis hepatis and hepatic adenoma with prolonged administration

Investigations

Pronounced suppression of HDL-cholesterol with elevation of LDL-cholesterol, reduced sex hormone binding globulin, suppressed serum LH, FSH and testosterone, raised haematocrit

Endocrine and reproductive disorders

Oligospermia and testicular atrophy in men with prolonged suppression of the hypothalamic-pituitary-gonadal axis; in women, hirsutism, deepening of the voice, clitoral enlargement and menstrual disturbance. Gynaecomastia is not expected, the compound being non-aromatising

Skin and subcutaneous tissue disorders

Acne, seborrhoea, androgenetic alopecia, hirsutism

Psychiatric disorders

Irritability, aggression, mood lability, insomnia, depressive symptoms after withdrawal

Cardiac and vascular disorders

Hypertension, left ventricular hypertrophy and an increased atherogenic risk related to the adverse lipid profile

Musculoskeletal and connective tissue disorders

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

Metabolism and nutrition disorders

Modest sodium and water retention, altered glucose tolerance

Overdose

Acute overdosage is of low acute toxicity and may cause nausea, headache and oedema, while repeated excessive exposure produces hepatic dysfunction, marked dyslipidaemia, polycythaemia and virilisation in women. There is no specific antidote; management is withdrawal of the product with symptomatic and supportive care, including monitoring of liver function, haematocrit and lipid profile.

Pharmacodynamic properties

Chlorodehydromethyltestosterone (4-chloro-17alpha-methylandrosta-1,4-dien-17beta-ol-3-one) is a 17alpha-alkylated anabolic androgenic steroid, structurally the 4-chloro analogue of methandrostenolone. It acts as an agonist at the nuclear androgen receptor, promoting nitrogen retention and protein synthesis with a moderate anabolic and comparatively low androgenic effect. The chlorine substituent at C-4 sterically blocks the aromatase reaction, so the compound is non-aromatising and produces no oestrogenic activity, and it also impedes 5alpha-reduction, limiting conversion to more androgenic metabolites. Affinity for sex hormone binding globulin is low. As with all exogenous androgens, administration suppresses hypothalamic and pituitary gonadotrophin release with consequent reduction of endogenous testosterone secretion and of spermatogenesis.

Pharmacokinetic properties

The compound is well absorbed after oral administration and, being 17alpha-alkylated, resists hepatic first-pass inactivation at C-17. Plasma protein binding is high with low affinity for sex hormone binding globulin, leaving a relatively large free fraction. Hepatic metabolism proceeds by 6beta-hydroxylation, 16-hydroxylation, reduction of the 3-keto group and 17-epimerisation, together with a characteristic dehydrogenation and D-ring rearrangement that yields long-term metabolites such as 4-chloro-18-nor-17beta-hydroxymethyl-17alpha-methylandrosta-4,13-dien-3-one; metabolites are excreted in urine as glucuronide conjugates. The plasma elimination half-life of the parent compound is of the order of 16 hours, whereas the long-term metabolites remain detectable in urine for many weeks to months after the last dose.

List of excipients

Lactose monohydrate, maize starch, gelatin (granulation binder, of bovine origin), talc, colloidal anhydrous silica, magnesium stearate. Uncoated tablet manufactured by aqueous granulation. All excipients comply with the current Ph. Eur. or USP-NF monograph; the gelatin is sourced against the Ph. Eur. general chapter on minimising the risk of transmitting animal spongiform encephalopathy agents.

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 gelatin of bovine origin, which may be relevant to patients who avoid materials of animal origin.

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 remain in the intact blister until the moment of administration; a tablet pressed out of the blister should be taken immediately and not returned to the pack.

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 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

05012345678926

Serial

9852 7630 5418 26

LOT

TU2712M

MFG

02 / 2028

EXP

02 / 2031

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.