Trenbolone Enanthate 200 mg/ml

Trenbolone Enanthate 200 mg/ml (Trenbolone)

Anabolic–androgenic steroid · long-acting ester

Each 1 ml contains Trenbolone 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 therapy with an extended release profile, under close medical supervision.

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

Vitamin K antagonists (warfarin, acenocoumarol)

Potentiation of anticoagulation with elevated INR; the long depot means the interaction develops gradually and persists for weeks after the last dose, so anticoagulant monitoring must extend well beyond discontinuation.

Corticosteroids

Trenbolone antagonises glucocorticoid-receptor signalling and may reduce the efficacy of corticosteroid treatment; concurrent mineralocorticoid-mediated sodium retention may aggravate oedema and hypertension.

Insulin and oral antidiabetic agents

Modified glucose handling with risk of hypoglycaemia; because exposure is continuous rather than intermittent, antidiabetic requirements may need sustained rather than transient adjustment.

Antihypertensive agents

Blood-pressure control may be lost during continuous trenbolone exposure, requiring review of antihypertensive therapy by the prescriber.

Hepatotoxic medicinal products and alcohol

Additive risk of hepatic injury over the prolonged exposure period; periodic liver function testing is warranted.

Use in special populations

Pregnancy and breastfeeding

Contraindicated. Trenbolone is a potent androgen and progestogen capable of virilising a female foetus, and the long depot maintains exposure for weeks after the last dose, so pregnancy must be excluded and effective contraception used well beyond discontinuation. Breastfeeding should be discontinued.

Paediatric population

Contraindicated. Sustained high-potency androgen exposure carries a substantial risk of premature epiphyseal closure with permanent loss of adult height and of precocious virilisation; no paediatric data exist.

Elderly

Not recommended. Continuous exposure amplifies the cardiovascular burden — hypertension, tachycardia, ventricular hypertrophy and severe HDL suppression — and may stimulate benign prostatic hyperplasia or occult prostate carcinoma. Cardiovascular, haematological and prostatic assessment are required if use is nevertheless considered.

Renal impairment

Contraindicated in significant renal impairment. Sustained hypertension, sodium retention and reported alterations in renal function markers make deterioration likely, and the depot cannot be withdrawn if it occurs; renal function and blood pressure should be monitored throughout.

Hepatic impairment

Contraindicated in severe hepatic impairment; caution in lesser degrees of impairment, where reduced clearance compounds an already protracted exposure. Liver function should be monitored at intervals during treatment.

Athletes

Prohibited at all times, in and out of competition, under class S1.1 of the WADA Prohibited List. The analytical targets are the urinary metabolites epitrenbolone and trendione; with a long-acting depot the detection window extends for many months after the final injection, and use will result in an adverse analytical finding.

Undesirable effects

Endocrine

Sustained suppression of luteinising hormone, follicle-stimulating hormone and endogenous testosterone with slow recovery after discontinuation; hyperprolactinaemia; persistently subphysiological estradiol, since the molecule does not aromatise

Cardiovascular

Sustained hypertension, tachycardia, markedly reduced aerobic capacity and exercise tolerance, left ventricular hypertrophy with continued exposure, severe adverse shift in the atherogenic lipid profile

General and injection site

Persistent nocturnal sweating throughout the dosing interval, fatigue; injection site pain, induration and nodule formation associated with the larger oil volume and co-solvent content of a long-ester depot

Psychiatric

Chronic insomnia, irritability, aggression, anxiety and emotional lability sustained across the dosing interval; depressed mood during the protracted withdrawal phase

Reproductive system and breast

Loss of libido and erectile dysfunction, oligospermia and impaired fertility, testicular atrophy; progestogen- and prolactin-mediated gynaecomastia in the absence of oestrogenic conversion; virilisation in women, which may be irreversible

Musculoskeletal and connective tissue

Arthralgia and reduced joint comfort attributable to chronically low estradiol; muscle cramp; tendon strain in the setting of rapidly increased strength

Investigations

Pronounced fall in high-density lipoprotein cholesterol with rise in low-density lipoprotein cholesterol, elevated haematocrit and haemoglobin, raised transaminases, altered renal function markers

Respiratory, thoracic and mediastinal

Transient cough and chest tightness immediately after intramuscular injection; exertional dyspnoea during treatment

Overdose

Overdose does not produce an acute toxic syndrome but an intensified and, critically, a prolonged pharmacological effect — hypertension, tachycardia, drenching sweats, insomnia, agitation and marked gonadotrophin suppression — which may persist for several weeks because the enanthate depot continues to release drug and cannot be retrieved. There is no antidote and dialysis is ineffective given the high protein binding. Treatment is symptomatic and supportive, with cardiovascular and hepatic monitoring maintained until concentrations decline.

Pharmacodynamic properties

Pharmacotherapeutic group: anabolic steroids, 19-nortestosterone (estrene) derivatives. The active moiety is trenbolone, 17-beta-hydroxyestra-4,9,11-trien-3-one, delivered here on a long heptanoate (enanthate) ester. Trenbolone binds the androgen receptor with an affinity several times that of testosterone and drives sustained increases in muscle protein synthesis and nitrogen retention. Its 4,9,11-triene structure prevents aromatisation, so no estradiol is generated from the parent steroid, and renders it a poor substrate for 5-alpha reductase. Beyond the androgen receptor, trenbolone is a high-affinity progesterone-receptor agonist and a glucocorticoid-receptor ligand with antiglucocorticoid, anticatabolic activity, reducing cortisol-mediated protein degradation. Because the enanthate ester maintains near-continuous receptor occupancy between doses, these progestogenic, antiglucocorticoid and gonadotrophin-suppressive actions are expressed continuously rather than in the peaks and troughs seen with the acetate.

Pharmacokinetic properties

The seven-carbon enanthate ester is markedly more lipophilic than the acetate and is released slowly from the intramuscular oil depot, hydrolysis by plasma and tissue esterases then liberating free trenbolone. Onset is correspondingly slower, with serum concentrations rising over several days, and the apparent terminal half-life is of the order of 7 to 10 days, governed by depot release rather than by clearance of the parent steroid. Trenbolone is highly bound to plasma proteins, chiefly albumin, and has negligible affinity for sex hormone-binding globulin. Hepatic metabolism yields 17-alpha-trenbolone (epitrenbolone) and trendione, conjugated as glucuronides and sulfates and eliminated in urine and faeces. Accumulation occurs over successive doses until steady state is reached, and, importantly, both pharmacological and adverse effects persist for weeks after the final injection because the depot cannot be withdrawn.

List of excipients

Benzyl benzoate 200 mg (co-solvent, required to hold 200 mg of the ester in solution at room temperature), benzyl alcohol 50 mg (antimicrobial preservative and co-solvent), butylated hydroxytoluene 0.15 mg (antioxidant, protecting the oxidation-sensitive trienone system of the active substance), refined oil carrier of vegetable origin q.s. to 1 ml. Compounding, sterile filtration and filling are carried out under a nitrogen blanket, and the ampoule headspace is nitrogen-overlaid. All excipients comply with the current Ph. Eur. / USP–NF monographs.

Excipient warnings

This medicinal product contains 200 mg benzyl benzoate and 50 mg benzyl alcohol in each 1 ml. Benzyl alcohol may cause allergic reactions. It must not be given to premature or newborn infants and may cause toxic reactions and anaphylactoid reactions in infants and children up to 3 years old; use with caution in patients with hepatic or renal impairment because of the risk of accumulation and metabolic acidosis. Benzyl benzoate may cause local irritation at the injection site. The product also contains a refined oil carrier of vegetable origin; it must not be used in patients with a known hypersensitivity to vegetable oils.

Incompatibilities

In the absence of compatibility studies, this medicinal product must not be mixed with other medicinal products. As a benzyl benzoate-containing oil solution it is not miscible with aqueous injections or infusion fluids, must not be diluted, and should not be drawn up through administration sets or components incompatible with benzyl benzoate.

Shelf life

36 months from the date of manufacture in the unopened container. Do not use after the expiry date (EXP) printed on the ampoule and the carton.

After first opening

Single-dose ampoule — for immediate use only. Inspect the solution visually before administration; use only if it is clear, free from visible particles and the ampoule is intact. A slight yellow colour is characteristic of the active substance. Because this is a concentrated, co-solvented oil solution, allow the ampoule to reach room temperature before withdrawal and inject slowly and deeply into the muscle. Withdraw and administer the dose immediately after opening; no in-use shelf life has been established and any residual solution must be discarded. Do not retain a part-used ampoule.

Storage

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

Container

Colourless (transparent) or amber Type I glass ampoule (Ph. Eur. / USP Type I borosilicate), one-point-cut, containing 1 ml of sterile oil solution for injection, sealed under a nitrogen overlay. Pack size: 10 ampoules × 1 ml in a serialised outer carton with the package leaflet; the carton bears a GS1 DataMatrix, a human-readable serial and a scratch-off verification code. Primary packaging is sourced and controlled to ISO 15378. Keep the ampoules in the outer carton in order to protect them from light.

Disposal

Any unused medicinal product or waste material should be disposed of in accordance with local requirements. The ampoule is for single use: discard the opened ampoule and any residual solution immediately after the dose has been withdrawn. Glass ampoules, needles and syringes must be placed directly into an approved puncture-resistant sharps container and must not be recapped or returned to the carton.

Pack

10 Ampoules × 1 ml

GTIN

05012345678913

Serial

9061 3310 4482 13

LOT

TB2613M

MFG

01 / 2027

EXP

01 / 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.