Calcitonin - instructions for use, dose, side effects, contraindications

The drug suppresses osteoclast activity by acting on specific receptors, reduces the rate of bone turnover to the normal level in conditions with increased rate of resorption, such as osteoporosis, it possesses analgesic activity with pain of bone origin, increases the excretion of calcium in urine, phosphorus and sodium (due reducing their tubular reabsorption), and reduces excretion of hydroxyproline. It reduces the level of biochemical markers of bone turnover, such as serum C-telopeptides and bone isoenzyme of alkaline phosphatase, increases bone mineral density in lumbar vertebrae, maintains the mineral density in the femur. Calcitonin reduces gastric and exocrine pancreatic secretion.

Pharmacokinetics:

When administered intranasally, it is rapidly absorbed through the nasal mucosa, and its C_max in the plasma is reached within the first hour. Bioavailability with intranasal application is 3-5% in relation to the bioavailability of the drug used parenterally. Half-life is 16-43 minutes. With repeated prescriptions of the drug, no cumulation of the active substance was noted.

In parenteral administration, the bioavailability is about 70%, C_max in the plasma is reached within the first hour. Apparent V_d is 0.15-0.3 l / kg. Binding to plasma proteins - 30-40%. Up to 95% of calcitonin and its metabolites are excreted in the urine, with only 2% in unchanged form. Half-life is about 1 hour with intramuscular injection and 1-1.5 hours - with subcutaneous injection.

Indications:

Osteoporosis: primary osteoporosis - postmenopausal osteoporosis (both early and late stages), senile osteoporosis in women and men; secondary osteoporosis, in particular caused by therapy with glucocorticoids or immobilization;

Bone pain associated with osteolysis and / or osteopenia;

Paget's disease (deforming osteitis);

Hypercalcemia and hypercalcemic crisis, caused by the following factors: osteolysis caused by malignant tumors (carcinoma of the breast, lungs, kidneys, myeloma), hyperparathyroidism, immobilization, vitamin D intoxication, both for relief of chronic conditions and for chronic treatment of chronic conditions pores, until the effect of specific therapy of the underlying disease appears;

Neurodystrophic diseases (synonyms: algoneurodystrophy or Zudeck's disease), caused by various etiological and predisposing factors, such as posttraumatic painful osteoporosis, reflex degeneration, humerus syndrome, causalgia, drug neurotrophic disorders;

Acute pancreatitis (as part of combination therapy).

ICD-10

XXI.Z80-Z99.Z85.1 In a personal history, a malignant neoplasm of the trachea, bronchi, and lung

II.C50.C50 Malignant neoplasm of breast

II.C64-C68.C64 Malignant neoplasm of kidney, except for renal pelvis

II.C81-C96.C90.0 Multiple myeloma

IV.E20-E35.E21 Hyperparathyroidism and other disorders of the parathyroid [parathyroid] gland

IV.E65-E68.E67.3 Hypervitaminosis D

XI.K80-K87.K85 Acute pancreatitis

XIII.M80-M85.M81.0 Postmenopausal osteoporosis

XIII.M80-M85.M81.2 Osteoporosis caused by immobility

XIII.M80-M85.M81.4 Medicinal osteoporosis

XIII.M86-M90.M88 Paget's disease (bones) [deforming osteitis]

XIII.M86-M90.M89.0 Algoneurodroystrophy

XIII.M86-M90.M89.5 Osteolysis

Contraindications:

Hypersensitivity, pregnancy, breast-feeding, children's age.

Carefully:No data.

Pregnancy and lactation:

Clinical data on the safety of the use of calcitonin preparations during pregnancy is not available. In this regard, it is not recommended to use the drug in pregnant women. It is not known whether calcitonin preparations penetrate breast milk, so it is recommended to stop breastfeeding during the treatment period.

The category of FDA recommendations is C.

Dosing and Administration:

For parenteral administration

When osteoporosis - subcutaneously or intramuscularly at a daily dose of 50-100 IU daily or every other day (depending on the severity of the disease).

When bone pain associated with osteolysis and / or osteopenia - subcutaneously, intramuscularly or intravenously drip daily in a daily dose of 100-200 IU. The dose should be adjusted taking into account the patient's response to treatment.

When Paget's disease - subcutaneously or intramuscularly at a daily dose of 100 IU daily or every other day.

The duration of treatment is at least 3 months; if necessary, it can be more. The dose should be adjusted taking into account the patient's response to treatment.

Emergency treatment of hypercalcemic crisis - intravenously infuzionalno for at least 6 hours in a daily dose of 5-10 IU / kg body weight in 500 ml of saline. It is also possible to use an intravenous, slow, jet infusion in which the daily dose should be divided into 2-4 injections throughout the day.

Long-term treatment for chronic hypercalcemia - subcutaneously or intramuscularly daily in a daily dose of 5-10 IU / kg in 1 or in 2 injections. The dosage regimen should be adjusted taking into account the dynamics of the patient's clinical state and biochemical parameters.

When neurodegenerative diseases - subcutaneously or intramuscularly in a daily dose of 100 IU for 2-4 weeks. It is possible to continue treatment with the introduction of 100 IU every other day for up to 6 weeks, depending on the dynamics of the patient's condition.

When acute pancreatitis (as part of combined conservative treatment) - intravenously drip in a dose of 300 IU (in physiological saline) for 24 hours to 6 consecutive days.

For intranasal administration

When osteoporosis - daily dose of 200 IU per day. In order to prevent progressive loss of bone mass at the same time with the use of the drug in the form of a dosed nasal spray, the administration of adequate doses of calcium and vitamin D is recommended. Treatment should be carried out for a long time.

When pain in bones associated with osteolysis and / or osteopenia - daily in a daily dose of 200-400 IU. A daily dose of 200 IU can be administered at a time. Higher doses should be divided into several injections. The dose should be adjusted to meet the individual needs of the patient.

When Paget's disease - daily in a daily dose of 200 IU. In some cases, at the beginning of treatment, a dose of 400 IU per day may be required, administered in several administrations. The duration of treatment is at least 3 months.

When neurodegenerative diseases - 200 IU per day (per administration) daily for 2-4 weeks. It is possible to administer 200 IU every other day for up to 6 weeks, depending on the dynamics of the patient's condition.

The introduction of intranasal drugs is recommended to be performed in the nasal passages alternately.

Side effects:

Local: very often - rhinitis (including dryness in the nasal cavity, edema and congestion in the nasal mucosa, sneezing, allergic rhinitis), nonspecific symptoms from the nose (for example, soreness, papules, excoriations, bad odor, irritation, erythema) ; often - ulcerative rhinitis, sinusitis, nosebleeds. These phenomena are usually poorly expressed (about 80% of all reports) and require discontinuation of treatment in less than 5% of cases.

System: often - hot flashes, dizziness, headache, nausea, diarrhea, abdominal pain, pain in the bones and muscles, pharyngitis, fatigue, perversion of taste; sometimes - arterial hypertension, vomiting, joint pain, cough, flu-like symptoms, edema (face, limbs, generalized edema), visual disturbances.

Reactions of hypersensitivity can manifest generalized skin reactions, hot flashes, swelling (face, limbs, generalized edema), increased blood pressure, joint pain, itching.There are reports of anaphylactoid type reactions and of individual cases of anaphylactic shock.

Systemic adverse events are less common with intranasal than with parenteral calcitonin.

Overdose:

Symptoms: for parenteral use - nausea, vomiting, hot flashes and dizziness are dose-dependent. With an overdose of calcitonin with intranasal use, it is possible to develop hypocalcemia with symptoms such as paresthesia, muscle twitching.

Treatment: conduct symptomatic therapy, with the development of hypocalcemia, the administration of calcium gluconate is recommended.

Interaction:

Not described.

Special instructions:

Because the calcitonin is a peptide, there is a possibility of occurrence of systemic allergic reactions. There are reports of allergic reactions, including individual cases of anaphylactic shock, so if suspected of increased sensitivity to calcitonin before the start of treatment should be done skin tests.

Use in Pediatrics

Experience with children is limited, and therefore it is not possible to give recommendations for this age group.

Impact on the ability to drive vehicles and manage mechanisms

Given the possibility of dizziness, as well as increased blood pressure, it is impossible to exclude the possibility of adverse effects of the drug on the rate of reactions. When using the drug, it is advisable to take care when driving a car and controlling the mechanisms.

Instructions

Calcitonin (Calcitoninum)