Stanozolol 10 mg

Stanozolol 10 mg (Stanozolol) · ATC A14AA02

Anabolic steroid · oral, non-aromatising

Each tablet contains Stanozolol 10 mg.

For the full list of excipients, see section 6.1.

Tablet for oral administration.

Therapeutic indications

Anabolic therapy and management of selected conditions such as hereditary angioedema, 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

Anticoagulant effect is markedly potentiated, in part through reduced plasma fibrinogen and altered clotting factor synthesis; the anticoagulant dose usually requires substantial reduction with frequent INR monitoring.

Insulin and oral antidiabetic agents

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

Corticosteroids and corticotrophin

Additive sodium and water retention with increased risk of oedema and acne.

Androgen-suppressing or hepatotoxic medicinal products and alcohol

Concurrent hepatotoxins compound the cholestatic and hepatocellular risk of this 17alpha-alkylated agent; combined use should be avoided and liver function monitored.

Ciclosporin

Impaired hepatic metabolism raises ciclosporin concentrations with increased risk of nephrotoxicity.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Stanozolol may virilise a female foetus and must not be used in pregnancy; where it is used for hereditary angioedema in women of childbearing potential, effective contraception is required and treatment is not to be continued during breastfeeding.

Paediatric population

Use only under specialist supervision, for example in hereditary angioedema in a child, with six-monthly radiological monitoring of bone age; androgens accelerate epiphyseal maturation and may irreversibly reduce final adult height.

Elderly

Increased risk of prostatic hypertrophy and occult prostatic carcinoma in older men, and of fluid retention aggravating hypertension or cardiac failure; prostatic and cardiovascular status should be reviewed before and during treatment.

Hepatic impairment

Contraindicated in significant hepatic impairment or hepatic tumours. Long-term prophylactic use in hereditary angioedema requires periodic liver function testing and consideration of hepatic imaging, since peliosis hepatis and hepatic adenoma have been reported in this setting.

Patients with hereditary angioedema and dyslipidaemia

Stanozolol causes a particularly severe fall in HDL-cholesterol; lipid profile should be assessed at baseline and periodically, and the lowest effective maintenance exposure sought in patients requiring long-term prophylaxis, as determined by the prescriber.

Athletes

Stanozolol 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 hydroxylated metabolites are routinely detected in urine and use will result in an adverse analytical finding.

Undesirable effects

Hepatobiliary disorders

Raised transaminases, cholestatic jaundice, peliosis hepatis and hepatic adenoma with prolonged treatment; liver function abnormalities are common in patients on long-term prophylaxis

Investigations

Severe reduction in HDL-cholesterol with elevation of LDL-cholesterol, reduced sex hormone binding globulin, reduced plasma fibrinogen, raised haematocrit

Endocrine disorders

Virilisation in women, including hirsutism, deepening of the voice, clitoral enlargement and menstrual disturbance, which are the principal dose-limiting effects in hereditary angioedema; suppression of gonadotrophins and endogenous testosterone in men

Musculoskeletal and connective tissue disorders

Muscle cramp, tendon and ligament injury, premature epiphyseal closure in patients with incomplete skeletal maturation

Skin and subcutaneous tissue disorders

Acne, seborrhoea, androgenetic alopecia, hirsutism

Metabolism and nutrition disorders

Sodium and water retention with oedema, changes in glucose tolerance

Psychiatric disorders

Irritability, aggression, mood lability, sleep disturbance

Reproductive system and breast disorders

Priapism and altered libido in men, oligospermia; gynaecomastia is not expected as the compound does not aromatise

Overdose

Overdosage would be expected to cause nausea, oedema, headache and, with repeated excessive exposure, hepatic dysfunction, severe dyslipidaemia and virilising effects in women. There is no specific antidote; treatment consists of withdrawal of the product with symptomatic and supportive care, including assessment of liver function and lipid profile.

Pharmacodynamic properties

Stanozolol (ATC A14AA02) is a 17alpha-alkylated anabolic steroid derived from dihydrotestosterone, distinguished by a pyrazole ring fused to positions 2 and 3 of the A-ring in place of the 3-keto group. It is an androgen receptor agonist with a high anabolic-to-androgenic ratio and, because the A-ring is heterocyclic and saturated, it is not a substrate for aromatase and produces no oestrogenic activity. It is licensed in some territories for the long-term prophylaxis of attacks of hereditary angioedema, where it raises plasma concentrations of C1-esterase inhibitor and C4 and reduces the frequency and severity of attacks, and it has been used for its fibrinolytic and profibrinolytic properties, reducing plasma fibrinogen and increasing fibrinolytic activity. It lowers sex hormone binding globulin and, as a 17alpha-alkylated agent, causes hepatotoxicity and a particularly severe suppression of HDL-cholesterol.

Pharmacokinetic properties

Stanozolol is well absorbed after oral administration, the 17alpha-methyl group conferring resistance to hepatic 17beta-hydroxysteroid dehydrogenase and thus oral activity. Plasma protein binding is high while affinity for sex hormone binding globulin is low, and circulating concentrations of that globulin are themselves reduced by treatment. Metabolism is hepatic and proceeds mainly by hydroxylation of the steroid nucleus and the pyrazole ring to 3'-hydroxystanozolol, 16beta-hydroxystanozolol and 4beta-hydroxystanozolol, followed by glucuronidation; the pyrazole ring is resistant to the usual A-ring reductive pathways. Excretion is predominantly urinary as conjugated hydroxylated metabolites, and the plasma elimination half-life after oral administration is approximately 9 hours, though metabolites remain detectable in urine for a considerably longer period.

List of excipients

Lactose monohydrate, maize starch, pregelatinised maize starch, talc, colloidal anhydrous silica, magnesium stearate. Uncoated tablet compressed from a geometrically diluted low-dose blend; 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.

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 cold-formed blister until the moment of administration; a tablet pressed out of the blister should be taken immediately, as the tablets are protected from moisture only by the sealed pocket.

Storage

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

Container

Cold-formed aluminium/aluminium (Alu/Alu) push-through blister, 10 tablets per blister strip, selected for the moisture protection required by a low-dose formulation. 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

05012345678923

Serial

6529 4307 2185 23

LOT

ST2709J

MFG

11 / 2027

EXP

11 / 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.