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

Kolekaltsiferol - inactive form of the vitamin D₃. Biologically active forms of vitamins D - alfacalcidol (1α-hydroxycholecalciferol) and calcitriol (1,25-dihydroxycholecalciferol) are the products of hydroxylation of cholecalciferol (provitamin D of animal origin) or ergocalciferol (provitamin D of vegetable origin). Vitamin D activation requires sunlight (ultraviolet component) and a normal level of hydroxylase activity in the liver and kidneys. Kidney diseases (most often), liver and insolation deficiency reduce the synthesis of active forms of vitamin D. Deficiency of vitamin D in childhood leads to a delay in the closure of the fontanel fetuses and teething, deformation of bones, muscle weakness; develops rickets (osteomalacia in adults).Vitamin D deficiency in adults (a consequence of chronic kidney and gastrointestinal diseases, menopause and others) is also manifested by a decrease in bone strength (osteoporosis), bone fractures even under normal loads. Vitamin D metabolites activate the synthesis of transport calcium-binding protein in intestinal mucosa cells, this transporter provides absorption of calcium and phosphorus in the intestine, as well as calcification of bone tissue.

Stimulation of absorption of Ca2 + and phosphorus from the small intestine (necessary element for absorption, utilization of Ca2 +, calcification process). Regulation of phosphorus-calcium metabolism (along with parathyroid hormone and calcitonin), stimulation of calcium mobilization from the bone. Binding of active metabolites to receptors, initiation of calcium-binding protein synthesis, enhancement of reabsorption in distal tubules of the kidneys, increase in bone tissue capture, maintenance of normal Ca2 + concentration in extracellular fluid.

Pharmacokinetics:

Absorption is more complete and rapid than ergocalciferol. Connection with plasma proteins - specific α-globulin (for transport) (vitamin D₃binding protein for colcalciferol). Depot: liver, fat depots.Biotransformation (sequential in 2 stages) in the liver and kidneys. Elimination by the kidneys and with feces.

Indications:

Hypo-and vitamin vitamin D deficiency (prophylaxis and treatment), a state of increased vitamin D demand: rickets, spasmophilia, osteomalacia, osteoporosis, nephrogenic osteopathy, inadequate and unbalanced nutrition (including parenteral, vegetarian diet), insolation, hypocalcaemia, hypophosphatemia, alcoholism, hepatic insufficiency, cirrhosis, mechanical jaundice, gastrointestinal diseases (gluten enteropathy, persistent diarrhea, tropical sprue, Crohn's disease), malabsorption; taking barbiturates, mineral oils, anticonvulsants (including phenytoin, primidon); hypoparathyroidism (postoperative, idiopathic, tetany), pseudohypoparathyroidism.

ICD-10

IV.E20-E35.E21.3 Hyperparathyroidism, unspecified

IV.E20-E35.E21.2 Other forms of hyperparathyroidism

IV.E20-E35.E21.1 Secondary hyperparathyroidism, not elsewhere classified

IV.E20-E35.E21.0 Primary hyperparathyroidism

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

IV.E50-E64.E55.9 Vitamin D deficiency, unspecified

IV.E50-E64.E55 Insufficiency of vitamin D

IV.E50-E64.E55.0 Rickets active

XIII.M80-M85.M83.9 Osteomalacia in adults, unspecified

XIII.M80-M85.M83.8 Other osteomalacia in adults

XIII.M80-M85.M83.5 Other medicinal osteomalacia in adults

XIII.M80-M85.M83.3 Osteomalacia in adults due to malnutrition

XIII.M80-M85.M83.2 Osteomalacia due to malabsorption

XIII.M80-M85.M83.1 Older osteomalacia

XIII.M80-M85.M83.0 Postpartum osteomalacia

XIII.M80-M85.M83 Osteomalacia in adults

XIII.M86-M90.M90.2 * Osteopathy in other infectious diseases classified elsewhere

XIII.M86-M90 Other osteopathies

XVIII.R25-R29.R29.0 Tetany

Contraindications:

Hypersensitivity, hypercalcemia, hypercalciuria, calcium nephrourolythiasis, long-term immobilization (large doses), renal osteodystrophy with hyperphosphatemia, sarcoidosis, active form of pulmonary tuberculosis.

Carefully:

Chronic heart failure, atherosclerosis, chronic renal failure, nephrourolythiasis in the anamnesis.

Pregnancy and lactation:

The category of FDA recommendations is C.

Problems with the administration of therapeutic doses are not recorded. It should not be prescribed in pregnancy in high doses (has a teratogenicaction). With caution in lactation. During pregnancy and during breastfeeding, the dose of vitamin D₃ should not exceed 600 IU per day.

Dosing and Administration:

Inside, intramuscularly. Dosing regimen is individual, depending on the indications and age of the patient.

Osteoporosis and osteopenia are a combination with vitamin K, a course of 24 months. Secondary hyperparathyroidism is a course of 8 weeks with calcium.

Side effects:

Headache, gastrointestinal disorders, kidney irritation, exacerbation of the tuberculous process in the lungs.

Overdose:

With hypersensitivity and overdose, hypercalcemia, hypercalciuria and symptoms caused by heart rhythm disturbances, nausea, vomiting, headache, weakness, irritability, weight loss, severe thirst, frequent urination, formation of kidney stones, nephrocalcinosis, calcification of soft tissues , anorexia, arterial hypertension, constipation, renal insufficiency.

With chronic poisoning - demineralization of bones, calcium deposition in the kidneys, blood vessels, heart, lungs, intestines, organ dysfunction, which can lead to death.

Treatment: elimination of colcalciferol, administration of corticosteroids, vitamin E, preparations of magnesium, potassium, ascorbic acid, retinol, thiamine.

Interaction:

With simultaneous use with anticonvulsant drugs, rifampicin, colestyramine, absorption of colcalciferol decreases.

When used simultaneously with cardiac glycosides, the toxic effect of cardiac glycosides may be increased (the risk of heart rhythm disturbances increases).

With simultaneous use with thiazide diuretics, the risk of hypercalcemia increases.

Special instructions:

In case of prophylactic use, it is necessary to bear in mind the possibility of overdose, especially in children (do not prescribe more than 10-15 mg per year). During treatment, it is mandatory to monitor the calcium levels in the blood and urine (especially when combined with thiazide diuretics). Long-term use in high doses leads to chronic hypervitaminosis D₃. It should be borne in mind that the sensitivity to vitamin D in different patients is individual and in a number of patients the intake of even therapeutic doses can cause hypervitaminosis phenomena.The sensitivity of newborns to vitamin D may be different, some of them may be sensitive even to very low doses. In children receiving vitamin D for a long period of time, the risk of growth retardation increases. For prevention of hypovitaminosis D, a balanced diet is most preferable. Newborns who are breastfed, especially those born to mothers with dark skin and / or who have been exposed to insolation, have a high risk of vitamin D deficiency.

In the elderly, the need for vitamin D may increase due to a decrease in vitamin D absorption, a decrease in the ability of the skin to synthesize provitamin D₃, a decrease in the time of insolation, an increase in the incidence of renal failure.

Instructions

Kolekaltsiferol (Colecalciferolum)