Jintropine^® (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Profit-Pharm LLC (Russia)

Manufactured By

Genescience Pharmaceuticals, Co. Ltd. (China)

ATC Code

H01AC01 (Somatropin)

Active Substance

Somatropin (Rec.INN registered by WHO)

Dosage Forms

	Jintropine®	Lyophilisate for preparation of solution for subcutaneous administration 4 IU: vial 5 pcs. in a set with solvent and disposable syringes; vial 20 pcs.; vial 10 or 50 pcs. in a set with solvent
		Lyophilisate for preparation of solution for subcutaneous administration 10 IU: vial 5 pcs. in a set with solvent and disposable syringes; vial 20 pcs.; vial 10 or 50 pcs. in a set with solvent

Dosage Form, Packaging, and Composition

Lyophilisate for preparation of solution for subcutaneous administration as a mass or powder white or white with a yellowish tint; supplied solvent is a colorless, transparent liquid without odor.

Excipients: glycine, sucrose, methionine, sodium hydrogen phosphate, polysorbate 80, sodium dihydrogen phosphate monohydrate.

Solvent water for injections – 1 ml.

Glass vials (5) in a set with solvent (amp. 1 ml 5 pcs.) and disposable syringes (5 pcs.) – cardboard packs.
Glass vials (10) in a set with solvent (amp. 1 ml 10 pcs.) – cardboard packs.
Glass vials (20) – cardboard packs.
Glass vials (50) in a set with solvent (amp. 1 ml 50 pcs.) – cardboard packs.

Lyophilisate for preparation of solution for subcutaneous administration as a mass or powder white or white with a yellowish tint; supplied solvent is a colorless, transparent liquid without odor.

Excipients: glycine, sucrose, methionine, sodium hydrogen phosphate, polysorbate 80, sodium dihydrogen phosphate monohydrate.

Solvent water for injections – 1 ml.

Glass vials (5) in a set with solvent (amp. 1 ml 5 pcs.) and disposable syringes (5 pcs.) – cardboard packs.
Glass vials (10) in a set with solvent (amp. 1 ml 10 pcs.) – cardboard packs.
Glass vials (20) – cardboard packs.
Glass vials (50) in a set with solvent (amp. 1 ml 50 pcs.) – cardboard packs.

Clinical-Pharmacological Group

Recombinant somatropin

Pharmacotherapeutic Group

Somatotropic hormone

Pharmacological Action

The drug Jintropine^® is a genetically engineered somatotropic hormone.

It stimulates skeletal and somatic growth and also has a pronounced effect on metabolic processes.

It stimulates the growth of skeletal bones by acting on the epiphyseal plates of long bones and bone metabolism.

It contributes to the normalization of body structure by increasing muscle mass and reducing body fat mass.

In patients with growth hormone deficiency and osteoporosis, replacement therapy leads to the normalization of mineral composition and bone density.

It increases the number and size of muscle, liver, thymus, gonads, adrenal glands, and thyroid gland cells.

It stimulates the transport of amino acids into the cell and protein synthesis, reduces cholesterol levels by affecting the lipid and lipoprotein profile.

It suppresses insulin release.

It promotes the retention of sodium, potassium, and phosphorus.

It increases body weight, muscle activity, and physical endurance.

Pharmacokinetics

Absorption and Distribution

The absorption of somatropin after subcutaneous administration is 80%, C_max in blood plasma is reached in 3-6 hours. It penetrates into well-perfused organs.

Metabolism and Excretion

It is metabolized in the kidneys and liver. V_d of somatropin is 0.49-2.11 l/kg. It is excreted by the kidneys and with bile (including 0.1% unchanged). T_1/2 after subcutaneous administration is 3-5 hours.

Indications

• Growth retardation in children due to insufficient secretion of growth hormone, in gonadal dysgenesis (Turner syndrome), in chronic renal failure (decrease in kidney function by more than 50%) in the prepubertal period;
• In adults with confirmed congenital or acquired growth hormone deficiency as replacement therapy.

ICD codes

Dosage Regimen

Jintropine^® is administered subcutaneously, slowly, once a day, usually at night. The injection sites should be changed to prevent the development of lipoatrophy.

It is recommended to dissolve the contents of the vial in 1 ml of the supplied solvent, based on the calculated dose. To do this, draw up the solvent with a syringe and inject it into the vial with the drug through the stopper. Gently swirl until the contents of the vial are completely dissolved. Vigorous shaking is not acceptable. The prepared solution is stored in the vial for no more than two weeks at a temperature from 2°C (35.6°F) to 8°C (46.4°F).

Doses are selected individually, taking into account the severity of growth hormone deficiency, body weight or body surface area, and effectiveness during therapy.

In children with insufficient secretion of growth hormone, a dose of 25-35 mcg/kg/day (0.07-0.1 IU/kg/day) is recommended, which corresponds to 0.7-1 mg/m²/day (2-3 IU/m²/day). Treatment should be started as early as possible and continued until puberty and/or until bone growth zones are closed. Treatment may be discontinued upon achieving the desired result.

In Turner syndrome, in chronic renal failure in children accompanied by growth retardation, a dose of 50 mcg/kg/day (0.14 IU/kg/day) is recommended, which corresponds to 1.4 mg/m²/day (4.3 IU/m²/day). If growth dynamics are insufficient, dose adjustment may be required.

In growth hormone deficiency in adults, the initial dose is 0.15-0.3 mg/day (which corresponds to 0.45-0.9 IU/day) with a subsequent increase, depending on the effect.

When titrating the dose, the level of insulin-like growth factor I (IGF-I) in the blood serum can be used as a control indicator. The maintenance dose is selected individually but generally does not exceed 1 mg/day, which corresponds to 3 IU/day.

Elderly patients are recommended lower doses.

Adverse Reactions

Possible increase in intracranial pressure (headache, nausea, vomiting, visual impairment), decreased thyroid function, hyperglycemia, leukemoid reactions, epiphysiolysis of the femoral head, fluid retention with the development of peripheral edema, arthralgia, myalgia, tunnel syndrome. Symptoms are usually transient, dose-dependent, and may require dose reduction.

Allergic reactions: skin rash, itching.

Rarely formation of antibodies to the drug with a decrease in its effectiveness.

Local reactions hyperemia, swelling, pain, itching, lipoatrophy at the injection site.

The following side effects are described in the literature with the use of the drug Somatropin: weakness, fatigue, gynecomastia, optic disc edema (usually observed within the first 8 weeks of treatment, most common in patients with Turner syndrome), pancreatitis (abdominal pain, nausea, vomiting), otitis media and hearing impairment (in patients with Turner syndrome), hip subluxation in children (limping, pain in the hip and knee), acceleration of growth of a pre-existing nevus (possible malignancy), progression of scoliosis (in patients with excessively rapid growth), increase in the blood levels of inorganic phosphate, parathyroid hormone and alkaline phosphatase activity.

Contraindications

• Malignant neoplasms;
• Active brain tumors;
• Urgent conditions (including conditions after heart, abdominal surgery, acute respiratory failure);
• Pregnancy;
• Breastfeeding period (breastfeeding should be discontinued during treatment);
• Hypersensitivity to the components of the drug.

With caution the drug should be prescribed for diabetes mellitus, intracranial hypertension, hypothyroidism.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Pediatric Use

In children with insufficient secretion of growth hormone, a dose of 25-35 mcg/kg/day (0.07-0.1 IU/kg/day) is recommended, which corresponds to 0.7-1 mg/m²/day (2-3 IU/m²/day). Treatment should be started as early as possible and continued until puberty and/or until bone growth zones are closed. Treatment may be discontinued upon achieving the desired result.

In Turner syndrome, in chronic renal failure in children accompanied by growth retardation, a dose of 50 mcg/kg/day (0.14 IU/kg/day) is recommended, which corresponds to 1.4 mg/m²/day (4.3 IU/m²/day). If growth dynamics are insufficient, dose adjustment may be required.

Geriatric Use

Elderly patients are recommended lower doses.

Special Precautions

During treatment with Jintropine^®, adjustment of the doses of hypoglycemic drugs in patients with diabetes mellitus may be required, latent hypothyroidism may manifest, and in patients receiving thyroxine, signs of hyperthyroidism may appear.

During treatment, it is necessary to monitor the condition of the fundus, especially in the presence of symptoms of intracranial hypertension. Optic nerve edema requires discontinuation of the drug.

Detection of limping during somatropin therapy requires careful observation.

It is necessary to change the sites of subcutaneous injections due to the possibility of developing lipoatrophy.

Overdose

Acute overdose may initially lead to hypoglycemia and then to hyperglycemia. In chronic overdose, signs and symptoms characteristic of an excess of human growth hormone may be observed – the development of acromegaly and/or gigantism, as well as the development of hypothyroidism, a decrease in the level of cortisol in the blood serum.

Treatment: discontinuation of the drug, symptomatic therapy.

Drug Interactions

Corticosteroids reduce the stimulating effect of somatropin on growth processes.

The effectiveness of the drug (regarding final height) can also be affected by concomitant therapy with other hormones, such as gonadotropin, anabolic steroids, estrogens, and thyroid hormones.

Storage Conditions

The drug should be stored in a light-protected place at a temperature from 2°C (35.6°F) to 8°C (46.4°F). Do not freeze.

The prepared solution should be stored at a temperature from 2°C (35.6°F) to 8°C (46.4°F) for 2 weeks.

Keep out of reach of children.

Shelf Life

Shelf life – 2 years. Do not use the drug after the expiration date.

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.