Testosterone Propionate 100 mg/ml

Testosterone Propionate 100 mg/ml (Testosterone) · ATC G03BA03

Androgen · short-acting ester

Each 1 ml contains Testosterone 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

Androgen replacement therapy where a short-acting 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

Androgens potentiate anticoagulation through reduced clotting factor synthesis, and prothrombin time or INR may increase; the short ester's rapid onset and offset make swings in anticoagulant response more likely, so monitoring should be intensified at the start and end of treatment.

Insulin and oral antidiabetic agents

Enhanced insulin sensitivity may reduce hypoglycaemic drug requirements and cause hypoglycaemia; glucose monitoring is advised.

Corticosteroids and corticotrophin

Additive fluid and sodium retention, increasing the risk of oedema and hypertension, particularly in cardiac or hepatic disease.

Oxyphenbutazone

Concurrent administration with androgens has been reported to increase plasma oxyphenbutazone concentrations.

Propranolol

Androgens increase the clearance of propranolol, which may reduce beta-blocker exposure and attenuate its clinical effect.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Exogenous androgens may virilise a female foetus and there is no justification for use in pregnancy; effective contraception is required in women of childbearing potential. Use during breastfeeding is contraindicated because androgens enter milk and suppress lactation.

Paediatric population

Not indicated in children; safety and efficacy have not been established. Androgen exposure before completion of growth accelerates epiphyseal maturation and may result in premature fusion and reduced adult stature, and may induce precocious virilisation.

Elderly

Limited data are available in patients over 65 years. Older men have a higher background risk of prostatic disease, erythrocytosis, urinary obstruction and cardiovascular events; prostate examination, prostate-specific antigen and haematocrit should be evaluated before and during treatment.

Hepatic impairment

Contraindicated in severe hepatic insufficiency; in mild to moderate impairment testosterone clearance may be reduced and hepatic function should be monitored periodically.

Renal impairment and cardiac failure

Caution is required, since androgen-induced sodium and water retention may precipitate oedema and decompensation; treatment should be stopped if clinically significant fluid retention develops.

Athletes

Testosterone propionate is prohibited in and out of competition under class S1.1 of the WADA Prohibited List. Although its short half-life shortens the period of elevated serum testosterone, urinary steroid-profile and isotope-ratio methods detect exogenous testosterone well beyond that period, and use will result in an adverse analytical finding. A therapeutic use exemption is required for any athlete under anti-doping jurisdiction.

Undesirable effects

General disorders and injection site

Injection-site pain, burning and tenderness lasting one to several days, local erythema, swelling and induration — more frequent and more intense than with longer esters because of the higher molar ester load and frequency of administration; sterile abscess, and rarely pulmonary oil microembolism with cough and dyspnoea immediately after injection

Endocrine and reproductive system

Suppression of LH, FSH and endogenous testosterone, testicular atrophy, oligospermia and reduced fertility, gynaecomastia, increased frequency of erections and rarely priapism, prostatic hyperplasia with raised prostate-specific antigen

Blood and lymphatic system

Erythrocytosis with increased haematocrit and haemoglobin, increased blood viscosity and thromboembolic risk

Cardiovascular

Hypertension, sodium and water retention with peripheral oedema, palpitations

Skin and subcutaneous tissue

Acne (often prominent early because of rapidly rising androgen levels), seborrhoea, oily skin, hirsutism, male-pattern hair loss

Psychiatric

Increased or fluctuating libido, irritability, aggression, mood swings that may track the peaks and troughs of the short ester, insomnia, anxiety; depressed mood on discontinuation

Hepatobiliary and investigations

Elevated transaminases, reduced HDL-cholesterol and increased LDL-cholesterol, suppressed sex hormone-binding globulin; rarely cholestatic jaundice

Immune system

Hypersensitivity reactions to the preparation or its oily carrier, including rash, urticaria and, very rarely, anaphylactoid reaction

Overdose

Overdose is unlikely to be life-threatening; the short half-life of the propionate ester means that excessive androgen concentrations and their consequences — oedema, hypertension, priapism, agitation — subside comparatively rapidly, generally within a few days of stopping administration. There is no specific antidote and management is symptomatic and supportive, with monitoring of blood pressure, haematocrit and hepatic function. Because of high plasma protein binding, dialysis does not accelerate elimination.

Pharmacodynamic properties

Pharmacotherapeutic group: androgens, 3-oxoandrosten (4) derivatives; ATC code G03B A03. Testosterone propionate is the short-chain propionic acid ester of testosterone; after esterase hydrolysis the released hormone acts through the nuclear androgen receptor, and the resulting change in gene transcription underlies development and maintenance of the male genital tract, secondary sexual characteristics, libido, spermatogenesis, muscle protein accretion, bone mineralisation and erythropoiesis. Because of the short ester chain, serum concentrations rise and fall rapidly, so androgen exposure is pulsatile rather than sustained, which produces earlier onset of effect and a shorter carry-over after withdrawal than the medium and long esters. As with all testosterone preparations, activity is amplified in androgen-dependent tissues by 5-alpha reduction to dihydrotestosterone and diversified by aromatisation to oestradiol, and administration suppresses gonadotrophin secretion and endogenous testicular steroidogenesis.

Pharmacokinetic properties

After intramuscular injection into the oily depot the propionate ester is hydrolysed rapidly by non-specific esterases, giving a fast rise in serum testosterone with a maximum within approximately 12 to 24 hours of administration. The apparent half-life is approximately 20 hours (about 0.8 days), the shortest of the commonly used testosterone esters, and concentrations return towards baseline within roughly 48 to 72 hours, so that frequent administration at intervals determined by the prescriber is needed to maintain steady androgen exposure. Testosterone is approximately 98 % bound in plasma to sex hormone-binding globulin and albumin. Clearance is hepatic, by 5-alpha reduction, aromatisation and oxidative metabolism to androstenedione and 17-ketosteroids, followed by glucuronide and sulphate conjugation and predominantly urinary excretion, with a small faecal fraction.

List of excipients

Light refined oil carrier of low viscosity (vehicle for injection); benzyl alcohol 9 mg per 1 ml (antimicrobial preservative and co-solvent); nitrogen (headspace overlay). At 100 mg/ml the ester is readily soluble, so no benzyl benzoate co-solvent and no antioxidant are required; the thinner vehicle is chosen to keep injection volumes comfortable for the frequent dosing this ester implies.

Excipient warnings

This medicinal product contains 9 mg benzyl alcohol in each 1 ml ampoule. Benzyl alcohol may cause allergic reactions. 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 before repeated administration, since benzyl alcohol may accumulate and cause metabolic acidosis. As an oil solution, the product 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, and must not be combined in one syringe with aqueous injections.

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. The ampoule is opened immediately before administration; withdraw and inject the contents in a single operation and discard any remainder. An opened ampoule must not be stored for a subsequent dose, even where the dosing interval is short. From a microbiological point of view, the product should be used immediately after opening. Inspect before use and administer only a clear, particle-free solution.

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, filled under a nitrogen overlay. Ten ampoules in a moulded tray within a serialised outer carton with the package leaflet, the carton bearing 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. Because dosing is frequent, patients and clinics should be provided with an approved sharps container: opened ampoules, residual solution, needles and syringes go into that container immediately after use and never into domestic waste or wastewater.

Pack

10 Ampoules × 1 ml

GTIN

05012345678911

Serial

8821 0035 4417 90

LOT

TP2611K

MFG

11 / 2026

EXP

11 / 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.