Pharmacological properties

Pharmacodynamics. d3 vitamin is an active antirachitic factor. the most important function of d3 vitamin is regulation of metabolism of calcium and phosphates that promotes the correct mineralization and growth of a skeleton.

_{3 Vitamin D} is a natural form of vitamin D which is formed at animals and the person. In comparison with _{2 vitamin D} it is characterized by higher activity (for 25%).

_{3 Vitamin D} it is necessary for functioning of an epithelial body, intestines, kidneys and skeletal system. Plays an essential role in absorption of calcium and phosphates from intestines, in transport of mineral salts and in the course of calcification of bones, regulates discharge of calcium and phosphates kidneys. Concentration of calcium ions influences a number of the important biochemical processes causing support of a tone of skeletal muscles participates in carrying out nervous excitement and affects blood clotting. _{3 vitamin D} also participates in functioning of the immune system, influences production of lymphokines.

Lack of _{3 vitamin D} in food, decrease in its absorption, deficiency in calcium and also lack of exposure on sunlight during rapid growth of the child lead to development of rickets, and at adults — to osteomalacy, at pregnant women is to emergence of symptoms of a tetany and further to disturbance of formation of adamantine substance of tooth at children.

to Women in the period of a menopause who have osteoporosis in connection with hormonal violations needs to raise a dose of _{3 vitamin D} .

Pharmacokinetics

Absorption. Water solution of _{3 vitamin D} is better soaked up, than oil. Premature children have an insufficient formation and intake of bile in intestines that breaks absorption of vitamins B a type of oil solutions. After oral administration, cholecalciferol is absorbed in a small intestine.

Distribution. Gets through a placental barrier and into breast milk.

Metabolism. It is metabolized in a liver and kidneys, turning into an active metabolite — calcitriol which connects to carrier protein and is transported to target organs (intestines, bones, kidneys). The half-life period in blood is several days and can be prolonged in case of a disease of kidneys.

Removal. It is removed with urine and a stake.

_{3 Vitamin D} participates in regulation of exchange of phosphorus and calcium in an organism in 6 h after administration of drug.

After intake of _{3 vitamin D} already in 48 h notes substantial increase of level of cholecalciferol in blood plasma.

Indication

Prevention of rickets at children. prevention of deficiency of vitamin D in groups of high risk, at malabsorption (chronic diseases of a small intestine, biliary cirrhosis, a state after a resection of a stomach and/or a small intestine). treatment of rickets and osteomalacy. the supporting treatment of osteoporosis.

Use

Drug is used orally.

1 ml of solution. 1 drop contains about 500 ME of cholecalciferol ( _{3 vitamin D} ). Precisely to measure a medicine dose, it is necessary to hold during a nakapyvaniye a bottle at an angle 45 °.

Usual dose for prevention of rickets at the full-term children aged from 4 weeks till 1 year with the correct leaving and sufficient stay under the influence of sunlight makes 1 drop (about 500 ME of _{3 vitamin D} ) in day, at premature — 2 drops (about 1000 ME of _{3 vitamin D} ) in day. During the solar summer period of year it is possible to limit a dose to 1 drop (about 500 ME of _{3 vitamin D} ) in day. During second or third lives there can be a need for further prescribing of _{3 vitamin D} , especially in winter time.

to Children of chest age of a drop is added to a spoon of milk or porridge. It is not recommended to add a drop to a small bottle or to a plate as at the same time it is impossible to guarantee reception of all dose. Children of advanced age and adults take the medicament with a water spoon.

Duration of administration of medicament is defined by the doctor.

At treatment of rickets and osteomalacy the dose makes 2–10 drops (about 1000-5000 ME of _{3 vitamin D} ) in day. Treatment duration — 1 year.

At maintenance therapy of osteoporosis the dose makes 2–6 drops (about 1000-3000 ME of _{3 vitamin D} ) in day.

Prevention of deficiency of vitamin D in groups of high risk — 1–2 drops (about 500–1000 ME of _{3 vitamin D} ) in day.

malabsorption Prevention — 6–10 drops (about 3000-5000 ME of _{3 vitamin D} ) in day.

At application of doses over 1000 ME of _{3 vitamin D} in day and also at long administration of medicament it is necessary to control calcium level in blood plasma.

Contraindication

Hypersensitivity to medicine components. d hypervitaminosis, the increased calcium level in blood and urine, an urolithiasis, a sarcoidosis, a renal failure, a nephrolithiasis.

in treatment of children aged up to 4 weeks because of possible emergence of hypersensitivity to benzyl alcohol.

Side effects

Side reactions, as a rule, do not develop at use of medicine in the recommended doses.

in case of individual hypersensitivity to _{3 vitamin D} which is noted seldom, or in case of application of too high doses during the long period can be shown a vitamin D hypervitaminosis.

from digestive system: loss of appetite, nausea, vomiting, constipations, dryness in a mouth.

from nervous system: headache, violations of mentality, depression.

from an urinary system: increase in level of calcium in blood and/or in urine, an urolithiasis and calcification of fabrics, a polyuria.

from skin: allergic reactions, including urticaria, rash, itch.

from a musculoskeletal system: muscular and articulate pain.

Other effects: degrowth of a body.

Determining by

need for d3 vitamin, it is necessary to consider all possible sources of this vitamin.

Too high doses of _{3 vitamin D} which are applied it is long, or shock doses can be the cause of a chronic hypervitaminosis of D ₃ .

a way of reception it is necessary to Determine by

daily need of the child for _{3 vitamin D} and individually, reconsidering every time at periodic researches of the patient, especially in the first months of life.

With care to use medicament in treatment of the immobilized patients accepting thiazide diuretics, foxglove glycosides and also to patients with a nephrolithiasis, heart diseases.

not to apply

along with medicine of high doses of calcium.

to

during treatment recommends control of level of calcium, phosphates and glucose in blood plasma and in urine.

Use during pregnancy and feeding by a breast. The chronic overdose (a hypercalcemia, transplacental penetration of metabolites of _{3 vitamin D} in a fruit) which arises at long intake of _{3 vitamin D} in the doses exceeding recommended can cause defects of physical fetation, an aorta stenosis.

_{3 Vitamin D} gets into breast milk therefore during feeding by a breast medicament should be used only on doctor's orders.

Children. Apply at children aged from 4 weeks

Ability to influence speed of response at control of vehicles or other mechanisms. There are no messages about negative impact of medicine on ability to drive the car or to work with other mechanisms for today. However at control of vehicles or other mechanisms it is recommended to observe extra care because of possible side reactions from nervous system.

Interaction

Antiepileptic means, especially Phenytoinum and phenobarbital and also rifampicin, Neomycinum, Colestyraminum, liquid paraffin reduce effect of d3 vitamin.

Concomitant use from tiazida increases risk of a hypercalcemia.

Use along with cardiac glycosides can strengthen their toxic action (risk of development of violations of a heart rhythm increases).

Ketokonazol can reduce biosynthesis and catabolism 1.25 (IT) of ₂ - cholecalciferol.

Co-administration of _{3 vitamin D} with metabolites or analogs of vitamin D perhaps only in exceptional cases and only with control of level of calcium in blood plasma.

Overdose

Symptoms: toxic symptoms because of sharp poisoning are shown seldom, more often at newborns and at children after application 100,000 me or more vitamin D in day.

At overdose the weakness, lack of appetite, nausea, vomiting, a lock, concern, thirst, a polyuria, hyperacidity of a stomach, diarrhea, intestinal colic develop. The increased sweating, dizziness, arrhythmia are possible.

Frequent symptoms are muscle and joints pain, a headache, a depression, violations of mentality, an ataxy, a stupor and the progressing degrowth of a body. The renal failure with the albuminuria, an erythrocyturia and a polyuria raised by potassium loss, a hyposthenuria, a nocturia and increase in pressure of blood of average degree develops.

can appear In hard cases turbidity of a cornea, is more rare — hypostasis of a nipple of an optic nerve, inflammation of an iris of the eye up to development of a cataract.

concrements in kidneys, lime application in kidneys, soft tissues, such as blood vessels, heart, lungs and skin Can be formed.

cholestatic jaundice Seldom develops.

Treatment: medicament withdrawal, a bed rest, a diet with the low content of calcium, the use of a large amount of liquid, use of depletive, at a considerable hypercalcemia — in/in introduction of a large amount of isotonic solution of sodium of chloride, introduction of furosemide or derivatives of Acidum etacrynicum, GKS, calcitonin medicines, carrying out a hemodialysis.

Specific antidote.

Storage conditions

At a temperature not above 25 °C. after opening of a bottle to store with densely closed cover in the fridge (at a temperature from 2-8 °C) no more than 6 months