Testosterone Enanthate 250 mg/ml

Testosterone Enanthate 250 mg/ml (Testosterone) · ATC G03BA03

Androgen · long-acting ester

Each 1 ml contains Testosterone Enanthate 250 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

Androgen replacement therapy in conditions associated with a deficiency of endogenous testosterone, 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

Androgens enhance the anticoagulant response by reducing the concentration of vitamin K-dependent clotting factors; a clinically significant rise in INR and bleeding risk may occur, so more frequent INR monitoring and anticoagulant dose review by the prescriber are required.

Insulin and oral hypoglycaemic agents

Improved insulin sensitivity during androgen therapy may reduce insulin and oral antidiabetic requirements and precipitate hypoglycaemia; glycaemic monitoring is recommended when treatment is initiated or discontinued.

Ciclosporin

Androgens may inhibit the metabolism of ciclosporin, increasing plasma concentrations and the risk of nephrotoxicity; ciclosporin levels should be monitored.

Levothyroxine and thyroid function testing

Androgens lower thyroxine-binding globulin, decreasing total T4 and altering resin uptake of T3; free thyroid hormone concentrations and clinical thyroid status remain unchanged, but laboratory results may be misinterpreted.

Corticosteroids and corticotrophin

Concomitant use increases sodium and fluid retention, with additive risk of oedema, particularly in patients with cardiac or hepatic disease.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Androgens are teratogenic with respect to sexual differentiation and may masculinise a female foetus; pregnancy should be excluded before use in a woman and effective contraception maintained. Use is also contraindicated during breastfeeding, since androgens pass into milk and inhibit lactation.

Paediatric population

Not established for use in children. In prepubertal boys androgens can cause precocious sexual development, phallic enlargement and accelerated bone maturation with premature epiphyseal fusion and compromised adult height; radiological monitoring of bone age is required whenever androgens are prescribed before skeletal maturity.

Elderly

There is limited experience in older men and no evidence that androgens improve age-related decline; the risks of erythrocytosis, exacerbation of benign prostatic hyperplasia, urinary retention, sleep apnoea and cardiovascular events are increased. Prostate assessment and haematocrit measurement before and during treatment are advised.

Renal impairment

No dose recommendation can be made. Androgen-related sodium and water retention may worsen hypertension and oedema in renal impairment, and treatment should be discontinued if significant fluid retention develops. Caution is also required in patients with nephrotic syndrome or cardiac failure.

Hepatic impairment

Contraindicated in severe hepatic insufficiency and used only with caution and periodic monitoring of hepatic function in lesser degrees of impairment, since testosterone is extensively metabolised by the liver.

Athletes

Testosterone enanthate is an exogenous anabolic androgenic steroid prohibited at all times, in and out of competition, under section S1.1 of the WADA Prohibited List. Administration produces an adverse analytical finding on the carbon isotope ratio and steroid profile tests and remains detectable for a prolonged period. Treatment of a competing athlete requires an approved therapeutic use exemption.

Undesirable effects

Endocrine and reproductive system

Dose-dependent suppression of the hypothalamic-pituitary-gonadal axis, testicular atrophy, impaired spermatogenesis and reduced fertility, gynaecomastia and breast tenderness, prolonged or frequent erections and rarely priapism, prostatic enlargement

Blood and lymphatic system

Polycythaemia, raised haematocrit and haemoglobin requiring monitoring, hypercoagulability and thromboembolic events

Cardiovascular

Increased blood pressure, fluid retention and oedema, tachycardia; adverse remodelling of the left ventricle with prolonged supraphysiological exposure

Hepatobiliary

Increased alanine and aspartate aminotransferase and gamma-glutamyl transferase, cholestatic hepatitis and jaundice (uncommon with parenteral esters), hepatic adenoma and peliosis hepatis with prolonged high-dose use

Skin and subcutaneous tissue

Acne vulgaris including truncal acne, seborrhoea, hypertrichosis, androgenetic alopecia, injection-site pruritus and rash

Psychiatric

Altered libido, aggression and hostility, irritability, emotional lability, restlessness and insomnia; depressive symptoms, anhedonia and loss of libido during withdrawal

Musculoskeletal

Muscle cramps, myalgia, tendon discomfort; premature closure of the epiphyses if administered before skeletal maturity

General and injection site

Injection-site pain, swelling and induration, post-injection inflammation, sterile abscess; rare pulmonary oil microembolism presenting as cough, dyspnoea and urge to cough during or shortly after injection, and rare anaphylactic reactions

Overdose

Overdose with the intramuscular ester is not expected to be acutely life-threatening, but the depot nature of the formulation means that supraphysiological androgen concentrations, erythrocytosis, oedema, hypertension, priapism and psychiatric disturbance may persist for one to two weeks after the last injection. No specific antidote exists; treatment is discontinuation together with symptomatic and supportive care, including monitoring of haematocrit, blood pressure, hepatic enzymes and lipid profile, with venesection if erythrocytosis is severe. Extensive protein binding makes elimination by dialysis ineffective.

Pharmacodynamic properties

Pharmacotherapeutic group: androgens, 3-oxoandrosten (4) derivatives; ATC code G03B A03. Testosterone enanthate is the heptanoate ester of testosterone and functions as a depot prodrug, the liberated hormone acting as an agonist at the nuclear androgen receptor to regulate transcription of androgen-responsive genes. Its clinical activity in hypogonadism reflects restoration of androgenic effects (maintenance of the male genital tract, secondary sexual characteristics, libido and potency, sebaceous and hair follicle activity) together with anabolic effects on skeletal muscle protein synthesis, bone mineral density and erythropoiesis. Tissue-level activity is modified by pre-receptor metabolism, dihydrotestosterone formed by 5-alpha reductase acting as the more potent androgen in prostate and skin and oestradiol formed by aromatase mediating skeletal and metabolic effects; both metabolites, together with testosterone itself, contribute to negative feedback that suppresses pituitary LH and FSH release and hence endogenous testicular function.

Pharmacokinetic properties

Following deep intramuscular injection of the oily solution the ester is released from the depot and hydrolysed by tissue and plasma esterases to free testosterone; the seven-carbon enanthate chain gives an intermediate release rate, faster than cypionate and considerably slower than propionate. Serum testosterone reaches a supraphysiological maximum approximately 24 to 72 hours after injection and thereafter falls, approaching the lower end of the eugonadal range by around days 10 to 14; the apparent half-life after intramuscular administration is approximately 4.5 days and is governed by release from the depot rather than by clearance of testosterone itself, which has a plasma half-life of only 10 to 100 minutes. In the circulation about 98 % is bound, some 44 to 65 % to sex hormone-binding globulin and the remainder mainly to albumin. Elimination follows hepatic biotransformation by 5-alpha reduction, aromatisation via CYP19A1 and oxidative pathways including CYP3A4 to androsterone, etiocholanolone and other 17-ketosteroids, which are conjugated and excreted predominantly in urine (approximately 90 %), with a minor faecal component.

List of excipients

Refined oil carrier (vehicle for injection); benzyl alcohol 100 mg per 1 ml (co-solvent and antimicrobial preservative); butylated hydroxytoluene 0.2 mg per 1 ml (antioxidant); nitrogen (headspace overlay). The higher benzyl alcohol content relative to the 100 mg/ml and 200 mg/ml presentations is required to hold 250 mg of ester per millilitre in solution over the storage range.

Excipient warnings

This medicinal product contains 100 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 administered to premature babies or neonates because of the risk of severe adverse reactions including "gasping syndrome". Patients who are pregnant or breastfeeding, and patients with hepatic or renal impairment, should be assessed by the prescriber, since large amounts of benzyl alcohol may accumulate and cause metabolic acidosis. The product also contains butylated hydroxytoluene, which may cause local skin reactions or irritation of the eyes and mucous membranes. As an oil solution, it must not be given to 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 solution it must not be drawn into the same syringe as an aqueous injection.

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, which refers to the last day of that month.

After first opening

For single use only. Open the ampoule immediately before administration, withdraw the full contents and inject without delay; discard any residue — an opened ampoule must never be re-used or retained. From a microbiological point of view, the product should be used immediately. At 250 mg/ml the solution is close to saturation and crystals may separate at low storage temperatures; if crystallisation is seen, the unopened ampoule may be warmed to hand temperature and gently swirled until the solution is clear again before use. Do not use if the solution remains cloudy or contains visible particles after warming.

Storage

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

Container

1 ml of solution in a 1 ml one-point-cut ampoule of Type I neutral borosilicate glass (Ph. Eur. 3.2.1 / USP <660>), amber or clear according to the presentation, flame-sealed under a nitrogen overlay. Ten ampoules in a moulded tray within a serialised outer carton with the package leaflet; the carton carries a GS1 DataMatrix encoding GTIN, serial, lot and expiry, a human-readable serial and a scratch-off verification code. Pack size: 10 ampoules × 1 ml. Not all pack presentations may be marketed in every territory.

Disposal

Any unused medicinal product or waste material should be disposed of in accordance with local requirements. Opened ampoules, residual oil solution, needles and syringes must be placed directly into an approved sharps container for glass and needles; do not discard with domestic waste or into wastewater.

Pack

10 Ampoules × 1 ml

GTIN

05012345678900

Serial

4471 0928 6630 02

LOT

TE2509A

MFG

06 / 2026

EXP

06 / 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.