Drostanolone Enanthate 200 mg/ml

Drostanolone Enanthate 200 mg/ml (Drostanolone)

Anabolic–androgenic steroid · long-acting ester

Each 1 ml contains Drostanolone Enanthate 200 mg in a sterile oil carrier.

For the full list of excipients, see section 6.1.

Solution for injection in a single-use glass ampoule for deep intramuscular use.

Therapeutic indications

Anabolic–androgenic therapy where a long-acting drostanolone ester is preferred, as determined by a physician.

Posology and method of administration

Deep intramuscular injection as directed by a physician. Not for intravenous use. Rotate injection sites. Dose and interval are individualised by the prescriber.

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)

Androgens potentiate the anticoagulant effect by reducing procoagulant factor concentrations and altering clotting factor turnover; prothrombin time and INR may rise markedly with an increased risk of haemorrhage, and anticoagulant dosage requires reassessment by the prescriber.

Insulin and oral antidiabetic agents

Anabolic androgens improve peripheral insulin sensitivity and lower blood glucose, which may unmask hypoglycaemia and reduce antidiabetic requirements; glycaemic monitoring is warranted at initiation and on withdrawal.

Corticosteroids and corticotrophin (ACTH)

Additive sodium and fluid retention, increasing the risk of oedema and aggravation of hypertension or cardiac failure, particularly in patients with impaired cardiac or renal function.

Ciclosporin and other calcineurin inhibitors

Androgens may increase ciclosporin blood concentrations with a corresponding rise in the risk of nephrotoxicity; trough concentration monitoring is advised during concomitant use.

5-alpha reductase inhibitors (finasteride, dutasteride)

No attenuation of the androgenic effects of drostanolone is to be expected, since the molecule is already 5-alpha-reduced and is not a substrate for the enzyme; concurrent use does not protect against androgenic adverse reactions.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Androgens cross the placenta and may cause virilisation of a female foetus, including clitoral hypertrophy and labial fusion. Women of childbearing potential should use effective contraception. Excretion into human milk and effects on the breast-fed infant have not been established, and breastfeeding is not recommended during treatment.

Paediatric population

Not recommended. Androgens accelerate skeletal maturation disproportionately to linear growth and may cause premature closure of the epiphyses with irreversible loss of adult height, together with precocious virilisation. Where treatment is nevertheless considered essential, growth and bone age must be monitored radiologically at intervals determined by the prescriber.

Elderly

Elderly male patients may be at increased risk of benign prostatic hyperplasia and of unmasking occult prostatic carcinoma. Periodic assessment of prostate status, haematocrit and blood pressure is appropriate; androgens are contraindicated in known carcinoma of the prostate or of the male breast.

Renal impairment

Use with caution. Sodium and water retention may precipitate or worsen oedema, hypertension and cardiac failure. No specific pharmacokinetic data are available in renal impairment; dosage and interval remain as determined by the prescriber, with monitoring of weight, blood pressure and electrolytes.

Hepatic impairment

Contraindicated in severe hepatic impairment. In mild to moderate impairment, reduced hepatic metabolism may prolong exposure; liver function should be monitored. The hepatic risk profile of this non-17-alpha-alkylated parenteral ester is nonetheless substantially lower than that of 17-alpha-alkylated oral androgens.

Athletes

Drostanolone is prohibited in sport at all times, in and out of competition, under class S1.1a (exogenous anabolic androgenic steroids) of the World Anti-Doping Agency Prohibited List. Administration will result in an adverse analytical finding; the enanthate depot gives a urinary detection window of many weeks after the final injection. Athletes subject to anti-doping regulation must not use this product other than under a granted therapeutic use exemption.

Undesirable effects

Endocrine

Dose-dependent suppression of luteinising hormone and follicle-stimulating hormone with reduced endogenous testosterone production, testicular atrophy, oligospermia or azoospermia and impaired fertility; in women, virilisation with hirsutism, irreversible deepening of the voice, clitoral enlargement, menstrual irregularity, amenorrhoea and breast atrophy

Skin and subcutaneous tissue

Acne, seborrhoea and oily skin, androgenetic alopecia, hirsutism, increased sweating

Investigations and metabolism

Decreased high-density lipoprotein cholesterol, increased low-density lipoprotein cholesterol, reduced sex hormone-binding globulin, mild sodium and water retention (less marked than with aromatisable androgens), decreased thyroxine-binding globulin with altered total thyroid hormone measurements

Cardiovascular

Hypertension, peripheral oedema; with prolonged high exposure, left ventricular hypertrophy and impaired diastolic function

Blood and lymphatic system

Increased haemoglobin and haematocrit, polycythaemia with attendant increase in blood viscosity and thromboembolic risk

Hepatobiliary

Transient increases in aspartate and alanine aminotransferase; because drostanolone is not 17-alpha-alkylated and is given parenterally, cholestatic jaundice, peliosis hepatis and hepatic tumours are rare in comparison with 17-alpha-alkylated oral androgens

Psychiatric and nervous system

Irritability, aggression, mood lability, anxiety, insomnia, headache; depressed mood and loss of libido during withdrawal of prolonged therapy

General disorders and administration site conditions

Injection site pain, induration, erythema and inflammatory nodules attributable to the oily carrier; rarely sterile abscess; very rarely cough, dyspnoea and transient chest discomfort immediately after injection consistent with pulmonary oil microembolism

Overdose

Acute overdose with a single excessive intramuscular dose is unlikely to give rise to life-threatening effects and usually manifests only as an exaggeration of the known androgenic reactions. Sustained excessive exposure produces virilisation, polycythaemia, adverse lipid changes, hypertension and profound suppression of endogenous testosterone secretion. No specific antidote exists; management consists of withdrawal of the product together with symptomatic and supportive measures, with haematological, hepatic, lipid and endocrine monitoring until parameters normalise, which may take several weeks given the long depot half-life.

Pharmacodynamic properties

Drostanolone enanthate is the enanthate (heptanoate) ester of drostanolone, 2-alpha-methyl-5-alpha-dihydrotestosterone, an anabolic-androgenic steroid of the androstane series. The parent steroid acts as a competitive agonist at the intracellular androgen receptor; the ligand-receptor complex translocates to the nucleus and modulates transcription of androgen-responsive genes, promoting nitrogen retention and protein synthesis in skeletal muscle while exerting androgenic effects on skin, hair follicles and the reproductive tract. The 2-alpha-methyl substituent hinders inactivation by 3-hydroxysteroid dehydrogenase and confers high androgen receptor affinity; because the A-ring is already saturated, drostanolone is not a substrate for aromatase and produces no oestrogenic metabolites, and it exhibits weak anti-oestrogenic activity at breast tissue, the property that underlay the historical use of drostanolone esters in advanced breast carcinoma in postmenopausal women. Like all androgens it suppresses hypothalamic-pituitary-gonadal function through negative feedback on luteinising hormone and follicle-stimulating hormone secretion.

Pharmacokinetic properties

Following deep intramuscular injection of the oily solution, the ester forms a depot from which drostanolone enanthate is released slowly into the circulation and hydrolysed by non-specific plasma and tissue esterases to free drostanolone and enanthic acid; absorption from the depot is rate-limiting, so the observed disposition follows flip-flop kinetics. Peak serum concentrations of the free steroid are reached approximately 3 to 5 days after administration and clinically relevant concentrations persist for 10 to 14 days. Drostanolone is extensively bound to plasma proteins (of the order of 98%), predominantly to sex hormone-binding globulin, for which 5-alpha-reduced androgens have high affinity, and to albumin. It is not a substrate for aromatase or for 5-alpha-reductase; metabolism is hepatic, by 3-alpha- and 3-beta-hydroxysteroid dehydrogenase reduction, 17-beta-oxidation and hydroxylation, with urinary excretion of glucuronide and sulfate conjugates. The apparent terminal half-life is approximately 5 to 10 days.

List of excipients

Benzyl alcohol (E 1519) 30 mg (co-solvent and antimicrobial preservative), butylated hydroxytoluene (E 321) 0.1 mg (antioxidant), nitrogen (headspace overlay), refined oil carrier q.s. to 1 ml. The oil carrier is a pharmacopoeial refined vegetable oil for parenteral use, meeting the acid-value, peroxide-value and unsaponifiable-matter limits of the current Ph. Eur./USP monograph.

Excipient warnings

This medicinal product contains 30 mg benzyl alcohol in each 1 ml ampoule. Benzyl alcohol may cause allergic reactions and local irritation at the injection site. It must not be given to newborn infants (up to 4 weeks of age) and should not be used for more than one week in infants and children under 3 years of age without medical advice, because of the risk of severe adverse reactions including metabolic acidosis and gasping syndrome. Ask a doctor or pharmacist for advice if you are pregnant or breast-feeding, or if you have liver or kidney impairment, since large volumes of benzyl alcohol may accumulate. This medicinal product also contains a refined vegetable oil carrier; rare hypersensitivity reactions to vegetable oils used as injection vehicles have been reported, and it must not be used in patients with known hypersensitivity to the oil carrier.

Incompatibilities

In the absence of compatibility studies, this medicinal product must not be mixed with other medicinal products. As an oil-based solution it is immiscible with aqueous injections and infusion fluids and must not be diluted, co-administered in the same syringe, or added to an infusion line. For deep intramuscular injection only — it must not be given intravenously.

Shelf life

36 months from the date of manufacture in the unopened container. Do not use after the expiry date stated on the ampoule and carton; the expiry date refers to the last day of that month.

After first opening

Single-use ampoule. The solution is intended for immediate use after opening: withdraw the dose and administer without delay. Any solution remaining in an opened ampoule must be discarded and must never be retained, pooled or re-used, as the presentation contains no preservative system validated for multiple withdrawals. Inspect visually before use — the solution should be clear, free from visible particles and free from crystalline deposit. Crystallisation may occur if the product has been stored below the stated temperature; if crystals are seen the ampoule must be discarded.

Storage

Store below 25 °C. Protect from light. Do not freeze. Keep ampoules in the outer carton until use.

Container

Clear or amber USP/Ph. Eur. Type I borosilicate glass one-point-cut ampoule, 1 ml nominal fill, sealed by fusion under a nitrogen headspace. Ten ampoules are held in a moulded tray within a printed folding carton together with the package leaflet. The carton bears a GS1 DataMatrix encoding GTIN, batch, expiry and unique serial number, plus a scratch-off verification panel. Primary packaging components are sourced and controlled under ISO 15378. Pack size: 10 ampoules × 1 ml.

Disposal

Any unused medicinal product or waste material should be disposed of in accordance with local requirements. Opened and unopened ampoules, needles and syringes must be placed immediately into an approved rigid sharps container; broken glass must not be discarded with domestic waste. The oil solution must not be emptied into drains or wastewater.

Pack

10 Ampoules × 1 ml

GTIN

05012345678901

Serial

2041 5567 8830 11

LOT

DE2601A

MFG

01 / 2026

EXP

01 / 2029

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.