Drostanolone Propionate 100 mg/ml

Drostanolone Propionate 100 mg/ml (Drostanolone)

Anabolic–androgenic steroid · short-acting ester

Each 1 ml contains Drostanolone Propionate 100 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 short-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

Oral anticoagulants of the coumarin type

Enhancement of the anticoagulant response with prolongation of prothrombin time and INR and an increased bleeding risk; close coagulation monitoring is required when drostanolone propionate is started, adjusted or stopped, the more so because its short half-life makes exposure fluctuate between injections.

Insulin, sulfonylureas and other oral antidiabetics

Improved insulin sensitivity may lower blood glucose and increase the risk of hypoglycaemia, requiring reassessment of antidiabetic therapy by the prescriber.

Corticosteroids and corticotrophin

Additive fluid and sodium retention with an increased likelihood of oedema, particularly in patients with cardiac, hepatic or renal disease.

Tamoxifen and other anti-oestrogens

Pharmacodynamic overlap at mammary tissue; the historical palliative use of drostanolone propionate in breast carcinoma involved anti-oestrogenic activity, and concurrent administration offers no additional oestrogen blockade while adding androgenic burden.

Hepatotoxic medicinal products (for example methotrexate, isoniazid, high-dose paracetamol)

Potential for additive hepatic injury; monitoring of liver function is advisable during concomitant use.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Placental transfer of androgens may virilise a female foetus. Effective contraception is required in women of childbearing potential, and breastfeeding should be discontinued, as excretion into milk and effects on the infant are not established.

Paediatric population

Not recommended in children and adolescents. Androgens hasten epiphyseal maturation and may cause premature epiphyseal closure with permanent reduction of adult height, as well as precocious sexual development; skeletal age monitoring is required if use is unavoidable.

Women

Androgenic adverse reactions occur at lower exposures in women, and voice deepening, clitoral enlargement and androgenetic alopecia may be irreversible even after discontinuation. Treatment should be withdrawn at the first sign of virilisation.

Elderly

Increased susceptibility to prostatic hyperplasia, urinary obstruction and cardiovascular adverse effects. Contraindicated in carcinoma of the prostate or of the male breast; prostate assessment, haematocrit and blood pressure should be reviewed periodically.

Hepatic and renal impairment

Contraindicated in severe hepatic impairment; in lesser degrees of impairment, exposure may be prolonged and liver function should be monitored. In renal impairment, fluid and sodium retention may aggravate oedema, hypertension and cardiac failure.

Athletes

Prohibited in and out of competition under class S1.1a (exogenous anabolic androgenic steroids) of the World Anti-Doping Agency Prohibited List. Use will produce an adverse analytical finding; although the propionate ester clears more quickly than long-chain esters, urinary metabolites remain detectable for a prolonged period. Use by athletes subject to anti-doping rules is permissible only under a granted therapeutic use exemption.

Undesirable effects

General disorders and administration site conditions

Injection site pain, tenderness, erythema and induration, which are more frequent than with longer esters because of the higher injection frequency and the irritant propionate moiety; local inflammatory nodules, rarely sterile abscess; very rarely post-injection cough or dyspnoea consistent with pulmonary oil microembolism

Endocrine

Suppression of luteinising hormone and follicle-stimulating hormone, reduced endogenous testosterone, testicular atrophy, oligospermia and reduced fertility; in women, virilisation with hirsutism, deepening of the voice (frequently irreversible), clitoromegaly, menstrual disturbance and amenorrhoea

Skin and subcutaneous tissue

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

Investigations and metabolism

Reduction in high-density lipoprotein cholesterol with an increase in low-density lipoprotein cholesterol, suppressed sex hormone-binding globulin, modest sodium and fluid retention, decreased thyroxine-binding globulin producing altered total thyroid hormone assays without true thyroid dysfunction

Cardiovascular

Hypertension, palpitations, peripheral oedema; with prolonged high exposure, left ventricular hypertrophy

Blood and lymphatic system

Increased haemoglobin and haematocrit, erythrocytosis, increased blood viscosity

Hepatobiliary

Occasional transient elevations of serum transaminases; serious hepatic reactions such as cholestasis, peliosis hepatis and hepatic neoplasia are uncommon with this non-17-alpha-alkylated parenteral ester, in contrast to 17-alpha-alkylated oral androgens

Psychiatric

Irritability, aggression, emotional lability, restlessness and insomnia; depressive symptoms and loss of libido following withdrawal

Overdose

A single excessive injection is not expected to cause serious acute toxicity, the presentation being an intensification of androgenic effects together with pronounced local reaction at the injection site. Repeated excessive administration leads to virilisation, erythrocytosis, dyslipidaemia, hypertension and suppression of the hypothalamic-pituitary-gonadal axis. There is no specific antidote; treatment is withdrawal of the product with symptomatic and supportive care, and recovery of biochemical parameters is generally more rapid than with long-acting esters owing to the short half-life.

Pharmacodynamic properties

Drostanolone propionate is the short-chain propionate ester of drostanolone (2-alpha-methyl-5-alpha-dihydrotestosterone), an androstane-derived anabolic-androgenic steroid. After hydrolysis of the ester, drostanolone binds with high affinity to the androgen receptor and initiates transcription of androgen-responsive genes, producing nitrogen retention, increased skeletal muscle protein synthesis and the expected androgenic actions on skin, pilosebaceous units and the reproductive tract. The 2-alpha-methyl group protects the 3-keto function from reductive inactivation, while the saturated A-ring precludes aromatisation, so no oestrogenic metabolites are formed; drostanolone additionally exerts a weak anti-oestrogenic effect on mammary tissue, which is the basis of the historical use of drostanolone propionate as a palliative hormonal agent in advanced breast carcinoma in postmenopausal women. Gonadotrophin secretion is suppressed by negative feedback, with consequent reduction of endogenous testosterone production.

Pharmacokinetic properties

The propionate ester is only three carbons long, so release from the intramuscular oil depot is comparatively rapid: serum concentrations of free drostanolone rise within hours, peak at approximately 24 to 36 hours and decline over the following 2 to 3 days, giving a sharper concentration profile and a shorter duration of action than the enanthate ester and requiring correspondingly more frequent administration as determined by the prescriber. Hydrolysis to drostanolone and propionic acid is effected by non-specific esterases in plasma and tissue. Plasma protein binding is high, of the order of 98%, chiefly to sex hormone-binding globulin and albumin. Drostanolone is not aromatised and is not a substrate for 5-alpha-reductase; it undergoes hepatic reduction by 3-alpha- and 3-beta-hydroxysteroid dehydrogenases, 17-beta-oxidation and subsequent glucuronide and sulfate conjugation, with predominantly urinary excretion. The apparent elimination half-life is approximately 1.5 to 2 days.

List of excipients

Benzyl alcohol (E 1519) 20 mg (co-solvent and antimicrobial preservative), refined oil carrier q.s. to 1 ml. The oil carrier is a light pharmacopoeial refined vegetable oil for parenteral use complying with the current Ph. Eur./USP monograph. No antioxidant and no benzyl benzoate co-solvent are required at this strength, the active being fully soluble in the oil carrier at 100 mg/ml.

Excipient warnings

This medicinal product contains 20 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. 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. Being an oil solution it is immiscible with aqueous injections and infusion fluids; it must not be diluted, combined in one syringe with other injections, or administered intravenously. For deep intramuscular injection only.

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. Withdraw and administer the dose immediately after opening. Discard any residual solution in an opened ampoule; opened ampoules must never be retained for a later dose or pooled with other ampoules. Before use, check that the solution is clear, colourless to pale yellow and free from visible particles.

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, fusion-sealed. Ten ampoules per moulded tray in a printed folding carton with the package leaflet, the carton carrying a GS1 DataMatrix (GTIN, batch, expiry, unique serial) and a scratch-off verification panel. Primary packaging components are 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. Ampoules — whole or broken — together with needles and syringes must be placed directly into an approved rigid sharps container. Do not discard glass with domestic waste and do not empty the oil solution into drains or wastewater.

Pack

10 Ampoules × 1 ml

GTIN

05012345678902

Serial

3152 6678 9041 22

LOT

DP2602B

MFG

02 / 2026

EXP

02 / 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.