Colecalciferol: instructions for use, price and reviews

Pharmacodynamics and pharmacokinetics

The substance accelerates the absorption of calcium in the digestive tract and activates the reabsorption of phosphorus in the renal tubules. Under the influence of this vitamin , normal formation of the bone skeleton and teeth occurs, and the correct bone structure is maintained. Colecalciferol increases the permeability of mitochondrial and cellular membranes on the intestinal epithelium, which greatly facilitates the transport of calcium cations and activates the processes of secondary absorption of phosphates. Stimulates ossification .

The drug is absorbed in the distal part of the small intestine in the presence of bile, then penetrates into the lymphatic system, into the general bloodstream and liver tissue. The substance is distributed throughout almost the entire body (liver, kidneys, skeletal muscles, adrenal glands, adipose tissue, myocardium), and has a high degree of binding to albumin and globulins .

The maximum concentration of the vitamin in the blood is observed 5 hours after ingestion. Then this indicator decreases slightly, but remains at a high level. Polar metabolites of the drug are concentrated in cell membranes, microsomes , nuclei and mitochondria . Metabolism occurs in the kidneys and liver with the formation of active metabolites.

The substance is excreted with bile into the intestines, where its derivatives can be reabsorbed or excreted from the body with feces.

Colecalciferol (vitamin D3)

Colecalciferol

or
cholecalciferol
(eng.
cholecalciferol
or
colecalciferol
) - vitamin D3. The most important vitamin for human physiology is from the group of vitamins D. Unlike most other vitamins, colecalciferol is synthesized in the human body. The provitamin of colecalciferol is 7-dehydrocholesterol. Colecalciferol regulates calcium-phosphorus metabolism in the body. It enhances the absorption of calcium and phosphates in the intestines, regulates their excretion by the kidneys, and also regulates the concentration of calcium in the blood plasma, normalizes the formation of teeth and bone skeleton in children, and helps in preserving bone structure.

Colecalciferol is absorbed in the distal part of the small intestine with the participation of bile, enters the lymphatic system, from where it enters the general bloodstream and the liver.

The daily requirement of vitamin D, including the total of colecalciferol, ergocalciferol (vitamin D2) and others, is, according to various sources, from 10 to 15 mcg.

Colecalciferol is a chemical substance

The chemical name of colecalciferol is (3beta,5Z,7E)-9,10-Secocholesta-5,7,10(19)-trien-3-ol. The gross formula is C27H44O. Soluble in vegetable oils, alcohol, insoluble in water. The colecalciferol molecule has the appearance of a steroid with an open window.

Colecalciferol is the international nonproprietary name of the drug

In the ATC, colecalciferol is classified in the group “A11 Vitamins”, subgroup “A11CC Vitamin D and its derivatives”.
The code for colecalciferol is A11CC05. Pharmacological group “Vitamins and vitamin-like products”. In addition, in the group “M05 Drugs for the treatment of bone diseases” it is included in the complex INN:

M05BB03 Alendronic acid and colecalciferol
M05BB04 Risedronic acid, calcium and colecalciferol, for sequential use
M05BB05 Alendronic acid, calcium and colecalciferol, for sequential use
M05BB07 Risedronic acid and colecalciferol
M05BB08 Zoledronic acid, calcium and colecalciferol, for sequential use
M05BB09 Ibandronic acid and colecalciferol
M05BX53 Strontium ranelate and colecalciferol

On the website GastroScan.ru in the “Literature” section there is a subsection “Vitamins”, containing articles addressing the use of vitamins.

Indications for use of colecalciferol

rickets, prevention and treatment

prevention of vitamin D deficiency in patients at high risk: malabsorption, chronic diseases of the small intestine, biliary cirrhosis of the liver, conditions after resection of the stomach and/or small intestine
maintenance therapy for osteoporosis
osteomalacia due to disorders of mineral metabolism in patients over 45 years of age, prolonged immobilization in case of injury, adherence to diets that exclude milk and dairy products
inadequate and unbalanced nutrition (including parenteral, vegetarian diet)
insufficient insolation
hypocalcemia
hypophosphatemia
alcoholism
liver failure, cirrhosis, obstructive jaundice
hypoparathyroidism and pseudohypoparathyroidism
persistent diarrhea
Crohn's disease
tropical sprue

Use of colecalciferol during pregnancy and breastfeeding

It has been established that when colecalciferol is taken in doses several times higher than the therapeutic dose, it penetrates into mother's milk.
Therefore, breastfeeding mothers should take it with caution, in the minimum required doses. Colecalciferol is FDA Category C for fetal risk use in pregnant women (animal studies have shown adverse effects on the fetus and there have been no adequate studies in pregnant women, but the potential benefits associated with use of this drug in pregnant women may justify it use despite the risk). It is known that long-term overdose of vitamin D during pregnancy can cause increased sensitivity to vitamin D in the fetus, suppression of parathyroid function, specific elf-like appearance syndrome, mental retardation, and aortic stenosis.

Colecalciferol and antacids containing aluminum salts

Most modern antacids contain one of the aluminum salts (aluminum hydroxide, algeldrate, aluminum phosphate, carbaldrate, aluminum acetoacetate, aloglutamol, aluminum glycinate and/or others). Long-term use of aluminum-containing antacids and/or their use in high doses can cause intoxication, accompanied by damage to bone tissue, brain and the development of nephropathy. It is assumed that aluminum directly disrupts the mineralization of bone tissue, has a toxic effect on osteoblasts, affects the function of the parathyroid glands and inhibits the synthesis of the active metabolite of the vitamin colecalciferol - calcitirol (Ushkalova E.A., Fadeenko G.D.).

Colecalciferol in medications and dietary supplements

Colecalciferol is used in three main dosage forms:

oily solution for oral administration
oral solution aqueous
oil solution for injection

and, as the only active ingredient, is found in the following medicines: Aquadetrim, Vigantol, Videchol solution in oil*, Vitamin D3 (GalenoPharm)*, Vitamin D3 BON*, Vitamin D3 aqueous solution*, D3-Droplet, Detriferol, Complivit Aqua D3,
as well as in dietary supplements: Detrimax, Vitamin D-3 Now Foods and others.

As a component of a complex active ingredient in the following medicines and dietary supplements:

“calcium carbonate + colecalciferol” - Calcium D3 Classic, Calcium D3 MIC, Complivit Calcium D3, Complivit Calcium D3 for babies, Complivit Calcium D3 forte, Calcium-D3 Nycomed, Calcium-D3 Nycomed Forte, Natekal 1000, Natekal D3, Revital Calcium D3 , Ideos*
“calcium carbonate + magnesium hydroxide + zinc sulfate + colecalciferol” - Osteokea
“alendronic acid + colecalciferol” - Ostalon Calcium-D, Fosavance, Fosavance forte
in multicomponent vitamin complexes: Vitrum* (various options), Duovit, Multi-Tabs (various options), Oligovit, Pikovit (various options), Vitamin and mineral complex from A to Zn (“Vitamins for adults”, Monte-vit premium) and many others
in combination with polyunsaturated omega-3 fatty acids: dietary supplement Fish oil with calcium and vitamin D3

Table 1.

Compositional composition and doses of vitamin D3 in some dietary supplements and medicines (Kodentsova V.M., Risnik D.V., RMZh No. 1 dated February 26, 2020).

The amount of colecalciferol (vitamin D3) in different versions of vitamin and mineral complexes of the same brand varies greatly. For example, in various types of Vitrum*:

Vitrum, Vitrum Kids, Vitrum Performance, Vitrum Prenatal, Vitrum Centuri, Vitrum Junior contain 400 IU (10 mcg) of colecalciferol in one tablet
Vitrum Beauty Lux, Vitrum Beauty Princess, Vitrum Baby, Vitrum Osteomag, Vitrum Teen - 200 IU (5 mcg)
Vitrum Beauty, Vitrum Beauty Elite - 67 IU (1.68 mcg)
Vitrum Antioxidant, Vitrum Vision, Vitrum Cardio Omega-3, Vitrum Lift-Skin Q10, Vitrum Memory, Vitrum Superstress do not contain colecalciferol

Note.
For drugs marked with an asterisk, registration in Russia has ended and there is no information about its renewal. In pharmacies, a number of them can be sold as dietary supplements. Trade names of colecalciferol drugs in the USA: Carlson D, D 1000 IU, D2000, D3, D400, Ddrops, Decara, Delta D3, D-Vita Drops, Enfamil D-Vi-Sol, Replesta, Thera-D 2000, Thera-D Rapid Repletion, Vitamin D3, D3-5, D3-50, Maximum D3, Liquid Vitamin D-3, Thera-D 4000, Replesta NX, Replesta Children's, Thera-D Sport.

Colecalciferol has contraindications, side effects and application features; consultation with a specialist is necessary.

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Indications for use

The medicine is prescribed:

for the prevention and treatment of hypovitaminosis and vitamin D deficiency;
for rickets , spasmophilia , osteoporosis , osteomalacia ;
patients with nephrogenic osteopathy ;
with unbalanced and inadequate nutrition (diet, including vegetarian, parenteral nutrition );
patients with hypocalcemia , hypophosphatemia ;
with insufficient insolation;
alcoholics;
for liver diseases, including cirrhosis and obstructive jaundice ;
patients with diseases of the digestive tract, persistent diarrhea , celiac enteropathy , tropical sprue , Crohn's disease , malabsorption ;
while taking barbiturates and mineral oils;
as a prophylactic agent during treatment with anticonvulsants, primidone , phenytoin ;
for postoperative, idiopathic hypoparathyroidism , tetany ;
patients with pseudohypoparathyroidism .

When is colecalciferol indicated?

Instructions for use contain a list of conditions and diseases for which colecalciferol is prescribed:

insufficient intake, absorption or complete absence of vitamin D in the body (for treatment and prevention);
increased need for vitamin D in the following pathologies: rickets and a tendency to convulsions against its background; insufficient mineralization of bone tissue; osteoporosis; skeletal damage due to renal failure; poor diet, including vegetarianism; insufficient exposure to sunlight; low calcium levels in the blood; cirrhosis of the liver or impairment of most of its functions; some diseases of the stomach and intestines; alcoholism; insufficient absorption of the substance in the intestine;
taking medications that depress the central nervous system and have a sedative effect;
taking medications to relieve seizures;
insufficient production of parathyroid hormone, including after surgery, due to hereditary osteodystrophy or unknown origin.

Contraindications

Colecalciferol is contraindicated for use:

in the presence of hypersensitivity reactions to the substance;
patients with hypercalciuria , hypercalcemia , calcium nephrourolithiasis ;
in large dosages in bedridden patients;
for hyperphosphatemia , renal osteodystrophy ;
patients with sarcoidosis ;
with an active form of pulmonary tuberculosis .

In what cases should you not take colecalciferol?

The substance is contraindicated in case of increased sensitivity to the substance, as well as:

persons with elevated calcium concentrations in the blood;
patients with intense excretion of calcium in the urine;
with urolithiasis;
when immobile for a long time (for vitamin D in large doses);
skeletal damage due to renal failure, accompanied by increased phosphate production;
with a systemic disease affecting internal organs, mainly the respiratory system (sarcoidosis);
with active pulmonary tuberculosis.

Side effects

Colecalciferol rarely causes adverse reactions. Most often, they occur due to drug abuse, with hypercalcemia or hypercalciuria .

However, during vitamin treatment the following may occur:

headaches , exacerbation of pulmonary tuberculosis ;
diarrhea , constipation, side effects from the digestive tract, nausea;
kidney irritation;
vomiting , disturbances in the functioning of the cardiovascular system, general weakness and irritability.

Overdose of the drug Colecalciferol, symptoms and treatment

Manifested by symptoms mainly caused by hypercalcemia, such as general weakness, headache, anorexia, nausea, vomiting, abdominal pain, diarrhea, constipation, dizziness, tinnitus, ataxia, arterial hypotension, drowsiness, depression, amnesia, disorientation, hallucinations , syncope, coma. Renal dysfunction may be accompanied by polyuria, polydipsia and albuminuria. Calcification of soft tissues, heart, blood vessels, kidneys and lungs is possible. Treatment is withdrawal of colecalciferol, bed rest, low-calcium diet, plenty of fluid intake, and taking laxatives. In case of severe hypercalcemia - intravenous administration of large quantities of isotonic sodium chloride solution, administration of furosemide or ethacrynic acid derivatives, calcitonin preparations, hemodialysis.

List of pharmacies where you can buy Colecalciferol:

Moscow
Saint Petersburg

Colecalciferol, instructions for use (Method and dosage)

The drug is prescribed for oral administration. At the same time, it is used in a daily dosage of 400 to 600 IU.

200 thousand IU are administered intramuscularly. Dosage depends on age and indications.

To treat spasmophilia , rickets and calcium deficiency in the body, 200 thousand IU is used every 7 days in combination with calcium salts for two weeks.

For osteomalacia and osteoporosis - 200 thousand IU, every 2 weeks, course of treatment - 3 months.

Use of the drug Colecalciferol

To prevent rickets, full-term infants starting from 2 weeks of life are prescribed 1–2 drops of oil solution (about 500 IU) per day. In special cases, such as premature babies, 1000 IU/day is prescribed. In the 2nd year of life, it may be necessary to prescribe colecalciferol in high doses, especially in winter. For the treatment of rickets, up to 5 drops are prescribed 3 times a day. Infants with spasmophilia are prescribed a dose of 10 drops 3 times a day. For the prevention of osteomalacia, adults are prescribed a dose of 1-2 drops per day, for the treatment of osteomalacia - up to 5 drops 3 times a day. The duration of treatment is determined individually. For the treatment of hypoparathyroidism and pseudohypoparathyroidism, 10,000 to 20,000 IU/day is prescribed. In this case, it is necessary to monitor the level of calcium in the blood every 3–6 months and dose adjustment depending on the data obtained.

Overdose

Symptoms of overdose also appear when the patient is hypersensitive to this substance. Observed: nausea, heart rhythm disturbances, headaches , vomiting, general weakness, weight loss, irritability, thirst, frequent urination, urolithiasis , anorexia , increased blood pressure , constipation, kidney disease.

Chronic poisoning with Colecalciferol leads to demineralization of bones, deposition of calcium salts in the heart, kidneys, lungs, and digestive tract; to disruption of the functioning of these organs, including death.

As therapy, the medication is discontinued and vitamin E , corticosteroids, magnesium, vitamin C , potassium, thiamine and retinol .

Drugs containing (Analogs)

Level 4 ATX code matches:
Etalfa

Dihydrotachysterol

Oksidevit

Tevabon

Alpha D3-Teva

Ergocalciferol

Aquadetrim

Vigantol

Medicines that contain this substance: Vigantol , Videhol solution in oil, Vitamin D3 100 SD/S dry , Vitamin D3 aqueous solution , Aquadetrim , Videhol , Vitamin D3 , Vitamin D3 BON , Cholecalciferol .

Calcium carbonate and Colecalciferol are included in the preparations: Revital Calcium D3 , Ideos , Calcium D3 Classic , Calcium-D3 Nycomed Forte , Complivit calcium D3 , Complivit calcium D3 forte , Revital Calcium D3 , Calcium + Vitamin D3 Vitrum , Calcium-D3 Nycomed , Calcium -D3-MIK , Complivit Calcium D3 for babies, Natekal D3 .

Vitamin D3 in combination with calcium carbonate and ascorbic acid is part of the drug Calcium SEDICO .

In combination with alendronic acid, Fosavance Forte tablets .

What is colecalciferol, what effect does it have?

The substance colecalciferol is better known as vitamin D3. In appearance, it is a white powder with crystals that are poorly soluble in water, it is poorly resistant to light, and dissolves well under the influence of ether, vegetable oil or chloroform.

Preparations with colecalciferol belong to the group of vitamins and vitamin-like drugs that regulate the metabolism of calcium and phosphorus.

The main beneficial functions of vitamin D3 in the body:

promotes high-quality absorption of calcium and phosphates in the intestinal lumen;
improves the reabsorption of phosphorus in the kidneys;
participates in the formation of bones and teeth;
maintains normal bone structure, improves bone mineralization;
supports the functioning of the parathyroid glands;
has a positive effect on the immune system by stimulating the production of lymphokines.

Due to a lack of cholecaciferol supplied with food, a disruption in the process of its absorption, as well as due to a lack of calcium and insufficient exposure to the sun, the following pathologies arise:

disruption of the process of supplying calcium to growing bones - in children during the neonatal period;
rickets – in young children during the period of active growth;

decreased bone strength – in adults;
limb cramps in women expecting a child;
osteoporosis – in women during menopause.