Pharmacological properties of the drug Retabolil
Nandrolone (17β-hydroxyestr-4-en-3-one decanoate) is a testosterone derivative. Unlike testosterone, it has a more pronounced androgenic effect (data obtained during studies on receptors, as well as in preclinical and clinical studies). Nandrolone stimulates human erythropoiesis, as indicated by an increase in the number of red blood cells, an increase in the level of hematocrit and hemoglobin. This effect is used therapeutically to treat anemia caused by bone marrow hypoplasia or decreased erythropoietin production as a result of chemotherapy. If the recommended doses are observed, androgenic effects (for example, virilization) are rarely observed. Nandrolone does not contain a C17 α-alkyl group, which is associated with impaired liver function and the development of cholestasis. Pharmacokinetics. Nandrolone decanoate is slowly released from the injection site and enters the bloodstream. The half-life is 6 days. The ester is quickly converted in the blood to nandrolone with a half-life of ≤1 hour. The total time of hydrolysis of nandrolone decanoate, its distribution and excretion is 4.3 hours. Nandrolone is metabolized in the liver. Nandrolone metabolites (19-norandrosterone, 19-noretiocholanolone and 19-norepiandrosterone) are detected in urine. Their pharmacological activity is unknown.
Retabolil 50 mg/ml No. 1 solution for intravenous oil.
Instructions for medical use of the drug RETABOLIL Trade name Retabolil International nonproprietary name Nandrolone Dosage form oil solution for injection Composition One 1 ml ampoule contains the active substance - nandrolone decanoate 50 mg excipients: benzyl alcohol, isopropyl alcohol, sunflower oil for injection Description Yellow transparent oil particle-free solution. Pharmacotherapeutic group Anabolic steroid drugs - esters ATC code A14AB01 Pharmacological properties Pharmacokinetics Nandrolone decanoate is slowly released from the injection site and enters the blood. The half-life is 6 days. The ester is quickly converted in the blood to nandrolone with a half-life of ≤ 1 hour. The total time for hydrolysis of nandrolone decanoate, distribution and excretion of nandrolone is 4.3 hours. Nandrolone is metabolized in the liver. Nandrolone metabolites - 19-norandrosterone, 19-noretiocholanolone and 19-norepiandrosterone, are determined in the urine. Their pharmacological activity is unknown. Pharmacodynamics Retabolil is a synthetic derivative of testosterone. Unlike testosterone, it has a more pronounced anabolic and less pronounced androgenic effect. Promotes the synthesis of nucleic acids, proteins, causes retention of nitrogen, calcium, sodium, potassium, chloride and phosphate. Activates reparative processes in epithelium, bone and muscle tissues. Retabolil stimulates the production of erythropoietin and stimulates erythropoiesis, provides protection of the bone marrow from the inhibitory effects of cytotoxic agents, which, with the simultaneous use of iron supplements, manifests itself as an antianemic effect. When recommended doses are followed, androgenic effects (eg, virilization) are rare. Indications for use - convalescence after severe injuries, intoxication, infectious diseases, extensive surgical interventions - anemia as a result of chronic renal failure (as part of complex therapy) Method of administration and dosage Anemia: weekly, intramuscularly - women 100 mg - men 200 mg. The therapeutic effect is individual. Treatment should be discontinued if there is no therapeutic effect after 3-6 months. applications. After a corresponding improvement in the blood picture or its normalization, the dose should be gradually reduced under regular monitoring of hematological parameters. Deterioration in performance during dose reduction or after completion of treatment may be an indication for resumption of treatment. Convalescence: 50 mg every 3-4 weeks, intramuscularly, deep into the muscle. Side effects - burning sensation in the tongue, heartburn, loss of appetite, nausea, vomiting - cholestasis, jaundice - suppression of gonadotropin secretion - peripheral edema - increased vascularization of the skin - hypercalcemia - virilization in women (acne, hirsutism, male pattern baldness, irreversible decrease in tone voices, menstrual irregularities, clitoral hypertrophy) - in men - suppression of testicular function, oligospermia, gynecomastia - hypocoagulation with a tendency to bleeding - slowing or cessation of growth - hypertrophy and/or prostate carcinoma Contraindications - children and adolescents under 18 years of age - pregnancy , lactation period - prostate hypertrophy or carcinoma - breast carcinoma in men - hypersensitivity to any of the components of the drug - edema syndrome Drug interactions When prescribed simultaneously with antidiabetic drugs, indirect anticoagulants - coumarin derivatives, antiplatelet agents, caution should be exercised due to the possible enhancing the effect of these drugs. When used simultaneously with glucocorticoids, mineralocorticoids, corticotropin, sodium-containing saline solutions; Food rich in sodium increases fluid retention in the body. Special instructions Do not exceed recommended doses. When prescribing the drug, women should weigh the benefits and harms of treatment due to the androgenic effect of the drug. The drug is prescribed with caution for myocardial dysfunction, hypertension, impaired liver and kidney function, epilepsy, migraine and glaucoma (including a history of it). During treatment, it is recommended to monitor intraocular pressure due to possible retention of sodium and water in the body. Changes in liver function (for example, bromsulfthalein levels) are possible, so after a 4-week course of treatment it is recommended to monitor its function. Before starting treatment and further, during it, a rectal examination of the prostate should be performed regularly. In case of diabetes mellitus, the dosage of antidiabetic drugs should be reconsidered. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms. The effect of the drug on the abilities necessary to drive vehicles and working machines has not been studied. Overdose Symptoms: severe endocrine, metabolic and mental adverse reactions develop. Treatment: symptomatic. Release form and packaging 1 ml of oil solution for injection in a colorless glass ampoule. 1 ampoule in plastic form, in a cardboard box with attached instructions for use. Storage conditions Store at temperatures from +15 °C to +25 °C, protected from light. Keep out of the reach of children! Shelf life: 5 years. Do not use the drug after the expiration date. Conditions for dispensing from pharmacies By prescription 1103 Budapest, st. Gemrei 19-21, Hungary
Use of the drug Retabolil
Anemia. Adults: intramuscularly, men 200 mg once a week, women 100 mg once a week. The therapeutic effect is individual. Treatment should be discontinued if there is no therapeutic effect after 3-6 months of use. After a corresponding improvement in the blood picture or its normalization, the dose should be gradually reduced, regularly monitoring hematological parameters. Deterioration in performance during dose reduction or after completion of treatment may be an indication for resumption of treatment. The period of convalescence. Adults: 50 mg every 3-4 weeks, IM deep into the muscle.
Side effects of the drug Retabolil
in male and female patients: heartburn, loss of appetite, vomiting, burning sensation of the tongue, suppression of gonadotropin secretion, cholestasis, jaundice; retention of nitrogen, sodium and water in the body; swelling, increased vascularization of the skin, hypercalcemia (especially in patients on bed rest and women with metastatic breast cancer). In women: symptoms of virilization (acne, hirsutism, male pattern baldness, irreversible decrease in voice tone, menstrual irregularities, clitoral hypertrophy). In men: suppression of testicular function, oligospermia, gynecomastia.
Retabolil
When using the drug Retabolil according to the recommended dosage regimen, side effects are usually unlikely. With long-term use or in case of abuse of the drug, the following side effects may occur:In patients of both sexes; nausea, vomiting, loss of appetite, abdominal pain, burning sensation in the tongue, impaired liver function with jaundice, hepatonecrosis (dark stool, vomiting blood, headache, discomfort, bad liver odor), hepatocellular carcinoma, peliosis of the liver (loss of appetite, dark urine, discoloration of stool, urticaria, pinpoint or macular hemorrhagic rashes on the skin and mucous membranes of the mouth and nose), cholestatic hepatitis (yellow discoloration of the sclera and skin, pain in the right hypochondrium, dark urine, discoloration of stool), diarrhea , feeling of fullness in the stomach, flatulence, increased or decreased libido, acne (especially in women and puberty boys). Retention of nitrogen, sodium and water in the body, peripheral edema, increased vascularization of the skin, hypercalcemia (especially in immobile patients and women with metastases of breast cancer) may be observed. Progression of atherosclerosis (increased concentration of low-density lipoproteins - LDL and decreased concentration of high-density lipoproteins - LH1VH1), iron deficiency anemia, leukemoid syndrome (leukemia, pain in long bones, hypercoagulation with a tendency to bleeding), increased secretion of the sebaceous glands, chills, seizures, sleep disturbance.
Suppression of the secretion of gonadotropic hormones.
In women: symptoms of virilization (hirsutism, alopecia, irreversible decrease in voice, dys- and amenorrhea, suppression of ovarian function, clitoral enlargement, steroid acne, oily skin), hypercalcemia (nausea, vomiting, fatigue).
In men: in the prepubertal period - virilism (acne, penis enlargement, priapism, formation of secondary sexual characteristics), idiopathic hyperpigmentation of the skin, slowdown 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; elderly – prostate hyperplasia and/or carcinoma.
Special instructions for the use of the drug Retabolil
Prescribing the drug to children is contraindicated! Do not exceed recommended doses. When prescribing the drug, women should evaluate the benefit/harm ratio due to the androgenic effect of the drug. The drug is prescribed with caution in case of impaired myocardial function, hypertension (arterial hypertension), impaired liver and kidney function, epilepsy, migraine and glaucoma (including a history). During treatment, it is recommended to monitor intraocular pressure due to possible retention of sodium and water in the body. Changes in liver function tests (for example, bromsulfalein test) are possible, so after a 4-week course of treatment it is recommended to monitor liver function. Before and during treatment, a rectal examination of the prostate gland should be performed regularly. In case of diabetes mellitus, the dosage of antidiabetic drugs should be reconsidered. In case of a progressive malignant tumor, adjustment of therapy is necessary taking into account the results of renal tests and the patient’s condition. Use during pregnancy and breastfeeding: contraindicated. Effect on the ability to drive vehicles or operate complex machinery: no studies have been conducted.
