Retabolil (Solution) Instructions for Use

Marketing Authorization Holder

Gedeon Richter, Plc. (Hungary)

ATC Code

A14AB01 (Nandrolone)

Active Substance

Nandrolone (Rec.INN registered by WHO)

Dosage Form

Retabolil

Solution for intramuscular injection oil-based 50 mg/1 ml: amp. 1 pc.

Dosage Form, Packaging, and Composition

Solution for intramuscular injection oil-based of greenish-yellow color, transparent, with a characteristic odor, free from mechanical inclusions.

Excipients: benzyl alcohol, isopropanol, sunflower oil (for injections).

1 ml – ampoules of colorless glass (1) – plastic trays (1) – cardboard packs.

Clinical-Pharmacological Group

Anabolic steroid for systemic use – depot form

Pharmacotherapeutic Group

Anabolic steroid agent

Pharmacological Action

Retabolil is a synthetic derivative of testosterone, an anabolic drug of prolonged action (depot drug).

It stimulates protein synthesis in the body, causes retention of nitrogen, calcium, sodium, potassium, chlorides, and phosphorus, which leads to an increase in muscle mass and acceleration of bone growth, and retention of water in the body.

It has low androgenic activity.

Pharmacokinetics

Absorption and Distribution

Nandrolone decanoate is slowly released from the injection site into the bloodstream with a T_1/2 of 6 days.

In the blood, the ester is rapidly hydrolyzed to Nandrolone with a T_1/2 of less than 1 hour.

The overall T_1/2 for the combined process of hydrolysis, distribution, and elimination of nandrolone from plasma is 4.3 hours.

Metabolism and Excretion

Nandrolone is metabolized in the liver.

The metabolites excreted by the kidneys are 19-norandrosterone, 19-noretiocholanolone, and 19-norepiandrosterone.

Data on the pharmacological activity of these metabolites are not known.

Indications

• Osteoporosis of various origins;
• Cachexia of various etiologies;
• Impaired protein metabolism, increased catabolic processes that deplete the body’s resources (burns, trauma, surgical operations, radiation therapy, severe infectious diseases);
• Progressive muscular dystrophy;
• Progressive spinal muscular atrophy Werdnig-Hoffmann;
• Glomerulonephritis;
• Programmed hemodialysis in patients with chronic renal failure.

ICD codes

Dosage Regimen

Administer the drug via deep intramuscular injection only.

Determine the dose individually based on the patient’s condition and therapeutic response.

For adult patients, the average single dose is 25-50 mg administered once every 3-4 weeks.

In cases of severe renal impairment, including patients with uremia, administer a dose of 50 mg once per week.

For pediatric patients, calculate the dose based on body weight: administer 400 mcg/kg of body weight once every 3-4 weeks.

For geriatric patients or those with hepatic impairment, exercise caution and consider a reduced dosage; monitor liver function tests every 4 weeks.

Adjust the dosing interval or total dose for patients with concomitant cardiac failure, hypertension, or severe atherosclerosis.

In postmenopausal osteoporosis, a dose of 50 mg every 3-4 weeks may be used; monitor serum calcium levels.

For catabolic states such as severe burns or major surgery, a dose of 50 mg every 1-2 weeks may be required for a limited duration.

Do not exceed the recommended dosage or frequency of administration.

Monitor growth plate status in children via X-ray every 6 months to prevent premature epiphyseal closure.

Discontinue treatment immediately if signs of virilization in women or prostatic hyperplasia in men occur.

Adverse Reactions

When using Retabolil according to the recommended dosage regimen, the occurrence of adverse reactions is usually unlikely.

With prolonged use or in case of drug abuse, the following adverse reactions may occur.

In patients of both sexes

From the digestive system nausea, vomiting, loss of appetite, abdominal pain, burning sensation in the tongue, impaired liver function with jaundice, hepatonecrosis (dark stools, vomiting with blood, headache, feeling of discomfort, unpleasant liver odor from the mouth), hepatocellular carcinoma, peliosis hepatis (loss of appetite, dark urine, discoloration of stools, urticaria, pinpoint or macular hemorrhagic rashes on the skin and mucous membranes of the oral cavity and nose), cholestatic hepatitis (yellow coloration of the sclera and skin, pain in the right hypochondrium, dark urine, discoloration of stools), diarrhea, feeling of fullness in the stomach, flatulence,

From the reproductive system increase or decrease in libido,

From the skin acne (especially in women and in boys of pubertal age), increased skin vascularization.

From metabolism retention of nitrogen, sodium and water in the body, peripheral edema, hypercalcemia (especially in immobile patients and in women with breast cancer metastases).

Progression of atherosclerosis (increase in the concentration of low-density lipoproteins – LDL and decrease in the concentration of high-density lipoproteins – HDL), iron deficiency anemia, leukemoid syndrome (leukemia, pain in long tubular bones, hypocoagulation with a tendency to bleeding), increased secretion of sebaceous glands, chills, convulsions, sleep disturbance.

From the endocrine system suppression of gonadotropin secretion.

In women

From the endocrine system symptoms of virilization (hirsutism, alopecia, irreversible deepening of the voice, dys- and amenorrhea, suppression of ovarian function, clitoral enlargement, steroid acne, oily skin).

From metabolism: hypercalcemia (nausea, vomiting, increased fatigue).

In men

From the endocrine system in the prepubertal period – virilism (acne, penile enlargement, priapism, formation of secondary sexual characteristics), idiopathic skin hyperpigmentation, slowing or cessation of growth (calcification of the epiphyseal growth zones of tubular bones); in the postpubertal period – bladder irritation (increased frequency of urges), mastodynia, gynecomastia, priapism, oligospermia, decreased sexual function.

From the reproductive system in elderly patients – hyperplasia and/or carcinoma of the prostate gland.

Contraindications

• Hypersensitivity to any of the components of the drug;
• Pregnancy;
• Lactation;
• Nephrotic syndrome;
• Prostate cancer;
• Acute or chronic prostatitis;
• Breast cancer in men;
• Severe liver damage, hepatic failure in cancer patients or liver metastases;
• Breast cancer (with metastases in the presence of hypercalcemia);
• Hypercalcemia (including in the anamnesis).

With caution cardiac, hepatic and renal failure, arterial hypertension, severe atherosclerosis, myocardial infarction (including in the anamnesis), cerebrovascular accident, diabetes mellitus, prostatic hypertrophy, migraine, epilepsy, glaucoma in the anamnesis (anabolic steroids cause retention of sodium and fluid in the body), elderly age, convulsions (including in the anamnesis).

Due to androgenic activity, the drug is prescribed to women and children only if the expected therapeutic effect outweighs the possible risk.

Use in Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

The drug is contraindicated for use in severe liver damage, in hepatic failure in cancer patients or in patients with liver metastases.

In some cases, during the use of the drug, disturbances in the indicators of some functional liver tests are observed.

Therefore, liver function should be monitored every 4 weeks.

Use in Renal Impairment

The drug should be prescribed with caution to patients with renal failure.

Pediatric Use

Due to androgenic activity, the drug is prescribed to children only if the intended benefit outweighs the potential risk.

When using Retabolil in high doses during puberty, premature closure of growth zones and growth arrest are possible.

Geriatric Use

Data on the use of Retabolil in elderly patients are not provided.

Special Precautions

To achieve the optimal therapeutic effect during therapy with Retabolil, the patient should receive an adequate amount of proteins, fats, carbohydrates, vitamins, and minerals with food.

When using Retabolil in high doses during puberty, premature closure of growth zones and growth arrest are possible.

Acceleration of epiphyseal growth of tubular bones can be observed in children both during treatment and 6 months after discontinuation of the drug.

To monitor the condition of the epiphyseal growth zones of tubular bones in children and adolescents, their X-ray examination is recommended every 6 months.

During treatment with Retabolil, careful monitoring of intraocular pressure should be carried out.

During treatment, systematic monitoring of the blood concentration of calcium ions, cholesterol (especially in patients with concomitant cardiovascular pathology), hematocrit, hemoglobin, and serum phosphorus concentration is necessary.

In some cases, during the use of the drug, disturbances in the indicators of some functional liver tests are observed.

Therefore, liver function should be monitored every 4 weeks.

In patients with diabetes mellitus, Retabolil may cause an increase in glucose tolerance, thereby reducing the need for insulin or oral hypoglycemic agents.

If menstrual cycle disturbances occur and/or signs of virilization appear, treatment should be discontinued.

Use strictly as prescribed by a doctor to avoid complications.

Before starting and during treatment with the drug, it is necessary to perform a rectal control of the size of the prostate gland.

Abuse of medicines containing Nandrolone (when using high doses as an anabolic agent) can cause endocrine, metabolic and mental disorders.

The use of anabolic steroids to stimulate athletic performance can cause serious harm to health and is unacceptable!

The Retabolil solution may become cloudy under the influence of cold.

In this case, before use, the ampoule with the drug must be heated until the crystals dissolve.

Effect on the ability to drive vehicles and mechanisms

Does not affect the ability to drive vehicles and perform work associated with a high risk of injury.

Overdose

No data on overdose are available.

Symptoms intensification of the adverse effects described above.

Treatment symptomatic therapy.

There is no specific antidote.

Drug Interactions

Retabolil should be prescribed with caution during the use of antiplatelet agents and indirect anticoagulants (their effect may be enhanced), hypoglycemic drugs (their hypoglycemic effect may be enhanced).

Retabolil can be used as part of combination therapy with glucocorticosteroids, tuberculostatic and cytostatic drugs.

It weakens the effects of growth hormone and its derivatives (accelerates the mineralization of the epiphyseal growth zones of tubular bones).

Glucocorticoids and mineralocorticoids, corticotropin, sodium-containing medicines and sodium-rich food enhance (mutually) fluid retention in the body, increase the risk of edema, and increase the severity of acne eruptions.

Concomitant administration with hepatotoxic medicines increases the risk of impaired liver function.

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature of 15-25°C (59-77°F).

Shelf Life

The shelf life is 5 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.