Somatropin: all details you need

Biosoma; Genotropin; Dzhintropin; Kreskormon; Norditropin (Norditropin NordiLet, PenSet Norditropin, Norditropin simplex); Rastan; Saizen; Growth Hormone; somatropin; Humatrop.

Somatropin – preparations of pituitary human growth hormone. Growth hormone – somatropin – a powerful metabolic hormone influences on lipid metabolism, carbohydrate and protein. It has an anabolic effect and stimulates growth. As in adults, and children maintain normal structure of the body, stimulating the growth of muscles, promotes the metabolism of body fat, increases strength, energy and subjective well-being. It is used for replacement therapy. Children: Growth hormone deficiency in the body (pituitary dwarfism, pituitary dwarfism); Turner’s syndrome; kidney failure in children in pre-adolescent, accompanied by growth retardation. In adults: a pronounced growth hormone deficiency with known hypothalamic-pituitary pathology; pronounced growth hormone deficiency with manifestation in childhood. It is also used in osteoporosis and immunodeficiency syndromes, accompanied by weight loss. Details

Active-active substance:

Somatropin / Somatropin.

Dosage Forms:

The lyophilisate (freeze-dried powder, the dry matter) for solution for injection (ampoules, vials, cartridges).

Complete solution for injection (in cartridges).

The pre-filled multidose disposable pen for repeated injections.

Somatropin (growth hormone)

Properties / Action:

Somatropin – preparations of pituitary human growth hormone. Growth hormone – somatropin – a powerful metabolic hormone influences on lipid metabolism, carbohydrates and proteins; It has anabolic and growth stimulating effect.

Growth hormone is a polypeptide containing 191 amino acid residues and has a molecular weight of about 22.125 kDa.

DNA recombinant somatropin for injection is a polypeptide hormone produced by recombinant DNA technology (e.g., synthesized strain of Escherichia coli, which has been modified by the addition of human growth hormone gene). The amino acid sequence of the recombinant growth hormone is identical to that of human growth hormone produced by the pituitary gland.

Effects of growth hormone induced directly by itself or indirectly via the synthesis and release of IGF-1 (IGF-1 / insulin-like growth factor / somatomedin-C). Somatropin treatment of children with growth hormone deficiency increases the concentration of their IGF-1 and IGF-binding protein-3 IRFSB.

Somatropin stimulates linear growth in children who do not have enough of normal endogenous growth hormone in children with short stature and gonadal dysgenesis associated with Turner’s syndrome or chronic renal insufficiency. Read more

As in adults, and children somatropin maintains a normal body composition, stimulating muscle growth and promoting fat metabolism. In adult patients with growth hormone deficiency growth hormone reduces fat mass, increases muscle mass and strength, energy, and subjective well-being.

It is shown that growth hormone and / or human growth hormone of pituitary origin have the following effects:

  1. exhibits anabolic effect (stimulates the transport of amino acids into cells and promotes protein synthesis), counteracts the catabolism;
  2. It stimulates the growth of the skeleton, bones;
  3. causes an increase in the number and size of muscle cells;
  4. increases body weight;
  5. It causes a delay in the body of nitrogen, mineral salts (calcium, phosphorus and sodium) and liquid;
  6. stimulates the absorption of calcium from the gastrointestinal tract;
  7. stimulates lipolysis, it causes a decrease in fat accumulation, reduces the flow of triglycerides in the fat depots (especially sensitive to somatropin visceral adipose tissue);
  8. It causes an increase in fatty acids in plasma concentration;
  9. increases blood sugar (initially reduces sensitivity to insulin, which can be retrieved later or even improved due to the beneficial effects of growth hormone on body cytoarchitectonics).
  • Effect of growth hormone on skeletal growth. Somatropin stimulates skeletal growth in patients with growth hormone deficiency. A notable increase in body length after administration of growth hormone due to their influence on the growth plates of long bones. The concentration of IGF-1, which may play a role in skeletal growth in serum of children with growth hormone deficiency is low, but it increases the treatment somatropin. In patients with growth hormone deficiency and osteoporosis somatropin prolonged treatment leads to recovery of the mineral composition and bone density. Somatropin activates the synthesis of chondroitin sulfate and collagen, increases the excretion of hydroxyproline. There has also been an increase in average concentration of serum alkaline phosphatase.
  • Effect of growth hormone on cell growth and physical performance. It has been shown that short children with deficient endogenous growth hormone less skeletal muscle cells than in healthy children. somatropin treatment leads to an increase in both the number and size of skeletal muscle cells, increases muscle strength and physical endurance. Somatropin also increases cardiac output, but the mechanism of this effect is not yet known. A role it can play in reducing the total peripheral vascular resistance (SVR). Furthermore, Somatropin causes an increase in the number and size of liver cells, thymus gland, gonads, adrenal gland and thyroid.
  • Effect of growth hormone on protein metabolism. Linear growth is partly accelerated by increasing the synthesis of cellular proteins. Initiation of treatment is somatropin nitrogen retention, which manifests itself in lowering its excretion in the urine and blood urea nitrogen in serum.
  • Effect of growth hormone on carbohydrate metabolism. Children with hypopituitarism are bouts of fasting hypoglycemia, which are in the treatment of somatropin. Somatropin increases insulin levels and can cause hyperglycemia, but the fasting blood glucose level is typically not altered.
  • Effect of growth hormone on lipid metabolism. In patients with growth hormone deficiency growth hormone administration leads to a mobilization of lipids, decrease body fat stores and increase in fatty acids in plasma concentration. Somatropin stimulates LDL receptors in the liver, and acts on lipid and lipoprotein profile in serum. The whole purpose of growth hormone in patients with growth hormone deficiency leads to a decrease in serum LDL and apolipoprotein B. You may also experience a decrease in total cholesterol levels.
  • Effect of growth hormone on mineral metabolism. Lack of growth hormone associated with a reduction in the blood plasma volume and tissue fluid. Both of these figures are rising rapidly after the start of somatropin therapy. Somatropin causes sodium retention, potassium and phosphorus. In patients with growth hormone deficiency after somatropin treatment increases the concentration of inorganic phosphate in the blood serum. The loss of calcium (acceleration of renal release) is offset by an increase in its absorption in the digestive tract; Serum calcium levels were not significantly changed.
  • Effect of growth hormone on the mental status. In patients with growth hormone deficiency may be violated mental ability and mental status. Somatropin increases vitality, improves memory and affect the balance of neurotransmitters in the brain.

Somatropin not possess toxic, mutagenic and carcinogenic effects.

Pharmacokinetics:

Approximately 80% of growth hormone is absorbed into the systemic circulation following subcutaneous injection. The absolute bioavailability appears the same for both male and female persons. Maximum plasma concentration is reached after 3.6 hours. After subcutaneous injection at 0.1 IU / kg, the maximum concentration is 13-35 ng / mL. It is metabolized in the liver. The half-life is 3-4 hours. Displayed through the intestines. Details

Indications:

Somatropin is used for replacement therapy in children and adults:

Somatropin is used in children:

growth hormone deficiency in the body (pituitary dwarfism, pituitary dwarfism); children with growth retardation due to growth hormone deficiency;

Prior to the use of somatropin diagnosis should be confirmed by functional assays pituitary gland condition. Stimulation of growth is only possible as long as there was no closure of growth zones.

Turner syndrome, confirmed by chromosome analysis;

A characteristic feature of Turner’s syndrome is low growth and gonadal dysgenesis. The reason for growth retardation in these patients is not known until the end. Growth hormone secretion is normal to about 9 years, then in most cases decreases.

kidney failure in children in pre-adolescent, accompanied by growth retardation;

For growth inhibition in these patients can result in the following factors: renal osteo-dystrophy, anemia, acidosis, malnutrition. However, it is believed to be the main cause disturbances in the system are: growth hormone / insulin-like growth factor-1 (IGF-1). Conservative treatment of renal insufficiency should not be interrupted in connection with the appointment of somatropin. During treatment with somatropin should be monitored renal function.

Somatropin is used in adults:

pronounced growth hormone deficiency with known hypothalamic-pituitary pathology proven by two provocative tests;

If you find during adulthood as a result of hypothalamic-pituitary insufficiency of growth hormone deficiency may be associated with a deficit of more of a hormone (except for prolactin), on which adequate replacement therapy prior to initiating therapy somatropin should be assigned.

pronounced growth hormone deficiency with manifestation in childhood;

Revealed in childhood growth hormone deficiency should be confirmed again before the start of somatropin replacement therapy.

osteoporosis;

Immunodeficiency syndromes accompanied by weight loss.

Dosage and administration:

Somatropin may be appointed only by doctors with special training in the treatment of growth hormone deficiency.

Preparations of recombinant somatropin are designed for subcutaneous or intramuscular administration. The dry substance is dissolved in the supplied solvent. The resulting solution should be clear and free of suspended particles. For each administration of growth hormone is necessary to use a sterile needle.

Some drugs are also used special somatropin injection device (injector Genotropin Pen 16 Genotropin; syringe pen NordiPen for Norditropin simplex; injector Humatro Pins II for the Humatropa etc.).

Applied dose of somatropin are individual and depend on weight, body surface area, patient’s response to treatment.

Preference is given daily by subcutaneous injection in the evening.

To prevent the development of lipoatrophy somatropin injection site should be varied.

Somatropin treatment should be started with the main recommended doses.

Basic recommended dose of growth hormone:

Growth hormone deficiency in children (dysplasia with insufficient secretion of growth hormone):

The recommended weekly dose of somatropin is 0.5-0.7 IU / kg body weight or 12-16 IU / m ^ 2 body surface area, which is spread on 6-7 s / c injection.

Somatropin subcutaneously administered at 0.07-0.1 IU / kg (0,025-0,035 mg / kg), 6-7 times a week, or 2.3 IU / m ^ 2 body surface (0.7-1.0 mg / m ^ 2) 6-7 times a week.

Somatropin intramuscularly appoint 0,14-0,2 U / kg 3 times a week, or 4.6 IU / m ^ 2 body surface 3 times per week.

It reported on the use and higher doses of somatropin.

Turner Syndrome:

Daily subcutaneous administration of higher dosages as compared with growth hormone deficiency in children: Somatropin administered subcutaneously at 0.14 IU / kg (0.045-0.050 mg / kg) 7 times a week (1.0 IU / kg per week) or 4.3 IU / m ^ 2 (1.4 mg / m ^ 2) 7 times a week (30 IU / m ^ 2 per week).

Chronic renal failure in children, accompanied by growth retardation:

Daily subcutaneous administration of higher dosages as compared with growth hormone deficiency in children: Somatropin administered subcutaneously at 0.14 IU / kg (0.045-0.050 mg / kg) 7 times a week (1.0 IU / kg per week) or 4.3 IU / m ^ 2 (1.4 mg / m ^ 2) 7 times a week (30 IU / m ^ 2 per week).

In case of insufficient growth rate may be needed higher doses. After 6 months of treatment may require dose adjustment somatropin.

Adults with growth hormone deficiency:

Somatropin dose is adjusted individually. It is recommended to begin treatment with low doses of 0,018 IU / kg (0.006 mg / kg or 0,45-0,9 IU / day) per day, gradually increasing the dose at monthly intervals, to a maximum of 0.036 U / kg (0.012 mg / kg) in a day. When selecting a dose somatropin take into account the clinical effect of adverse reactions and determining the level of IGF-1 in blood serum, which may serve koiteriaem adequacy dose. More elderly patients typically require a lower dose of Somatropin. Somatropin maintenance dose varies from patient to patient, but rarely exceeds 1.0 mg / day (equivalent to 3.0 IU / day).

The maximum dose of growth hormone replacement therapy is 0.1 mg / kg (0.3 IU / kg) and injected 3 times per week.

Overdose:

Acute overdose of somatropin may first lead to hypoglycemia, subsequently replaced by hyperglycemia.

Chronic overdose of somatropin can theoretically occur symptoms characteristic of endogenous growth hormone excess: gigantism and acromegaly.

In these cases, a removal of the drug.

Contraindications:

  • any signs of tumor growth, cancer (anti-tumor therapy should be completed prior to the start of somatropin therapy, intracranial tumor should be inactive, when the signs of regrowth of the tumor administration of somatropin should be discontinued);
  • idiosyncrasy (including a history of hypersensitivity) growth hormone;
  • closure of epiphyseal growth zones of long bones (not designated as a growth promoter for children);
  • patients in critical condition, urgently develop as a result of open heart surgery or abdominal cavity, multiple trauma and acute respiratory failure;
  • pregnancy and lactation (at the time of treatment should abandon breastfeeding);
  • kidney transplant (in children with chronic renal insufficiency treatment should be discontinued).

Application of pregnancy and breastfeeding:

Somatropin is contraindicated in pregnancy and lactation.

Although the description of the clinical cases of growth hormone during pregnancy and there is currently no proven safety of treatment with growth hormone during pregnancy. Thus, Somatropin is contraindicated during pregnancy, and therapy should be interrupted in case of pregnancy in a patient.

We should not forget about the possibility of release of growth hormone from the mother’s milk.