INSTRUCTIONS FOR MEDICAL USE
COSTAPHEROL
Trade name of the drug: Costaferool
Active substance (INN): Cholecalciferol
Dosage form: Oral drops.
Contents:
1 ml of the solution contains:
Active substance: Cholecalciferol – 15 000 ME
Excipients: macrogol glycerylcyanoleate, sucrose, sodium hydrophosphate dodecahydrate, citric acid monohydrate, anise flavoring, benzyl alcohol, purified water.
Description: colorless, transparent or slightly opalescent liquid with aniseed odor.
Pharmacotherapeutic group: Vitamins.
ATX code:A11CC05
Pharmacological properties
Pharmacodynamics
Aqueous solution of vitamin D3 is better absorbed than the oil-based solution (which is important when used in premature babies). After oral administration, colecalciferol is absorbed in the small intestine. It is metabolized in the liver and kidneys. Half-life of colocalciferol from blood is several days and may be prolonged in case of renal insufficiency. The drug penetrates through the placental barrier and into the mother’s milk. It is excreted with urine and feces.
Pharmacokinetics
Vitamin D3 is an active anti-rachitis factor. The most important function of vitamin D is to regulate calcium and phosphate metabolism, which promotes mineralization and skeletal growth. Vitamin D3 is a natural form of vitamin D, which is formed in the human skin by the action of sunlight. It plays an essential role in the absorption of calcium and phosphate from the intestine, in the transport of mineral salts and in the calcification of bones, and regulates the excretion of calcium and phosphate by the kidneys. The concentration of calcium ions acts on a number of important biochemical processes responsible for maintaining muscle tone in the skeletal muscles, in conducting nerve excitement, and in the process of blood clotting. Vitamin D is also involved in the immune system by affecting the production of lymphokines.
Indications for use
- Prevention and treatment of vitamin D deficiency
- Prevention and treatment of rickets
- Prevention and treatment of rickets-like diseases (inherited tubulopathies)
- Hypocalcemic tetany
- Osteomalacia and metabolic disorders of the bones (such as hypoparathyreosis and pseudohypoparathyreosis)
- Complex treatment of osteoporosis, including postmenopausal
Dosage and administration
The drug is taken orally with a small amount of liquid. One drop contains about 500 ME of vitamin D3.
The drug is used in the following dosages:
Prophylactic doses:
- Premature infants from 3-4 weeks of life, up to 2-3 years of age with proper care and sufficient exposure to fresh air: 500-1000 ME (1-2 drops) per day;
- Premature infants, from 7-10 days of age, twins, infants in poor living conditions: 1000-1500 ME (2-3 drops) per day. In summertime, the dose may be limited to 500 ME (1 drop) per day.
- Pregnant women: a daily dose of 500 ME (1 drop)/day of vitamin D3, for the duration of pregnancy, or 1000 ME (2 drops) /day, starting at 28 weeks of pregnancy.
- In postmenopausal period 500-1000 IU (1-2 drops) per day are prescribed.
Therapeutic doses:
- For rickets: 2000-5000 ME (4-10 drops) daily, depending on the severity of rickets (I, II or III) and the course variant, for 4-6 weeks, under careful monitoring of the clinical condition and the examination of biochemical parameters (calcium, phosphorus, alkaline phosphatase) of blood and urine. It should be started with 2000 ME for 3-5 days. Then, if tolerated well, the dose is increased to an individual therapeutic dose (usually 3000 ME). The dose of 5000 ME is prescribed only in case of marked bone changes.
If necessary, after a one-week break, the treatment can be repeated.
Treatment is continued until a clear therapeutic effect is achieved, followed by a prophylactic dose of 500 to 1500 ME/day.
- In the treatment of rickets-like diseases: 20,000-30,000 ME per day (40-60 drops) depending on the age, body weight and severity of the disease, under the control of biochemical blood and urine tests. The course of treatment is 4-6 weeks. The treatment is carried out under the supervision of a doctor.
- In the complex treatment of postmenopausal osteoporosis: 500-1000 ME (1-2 drops) per day.
The dosage is usually prescribed taking into account the amount of vitamin D coming from food.
Side effects
Not observed when used in the recommended doses.
In case of rare individual hypersensitivity to vitamin D3 or as a result of using too high doses for a long period, hypervitaminosis D3 may occur:
- loss of appetite, nausea, vomiting
- Headaches, muscle and joint pains.
- constipation, dry mouth, and polyuria
- mental disorders, including depression, weight loss, increased calcium levels in blood and excretion of calcium in urine
- Renal stone formation and calcification of soft tissues.
Contraindications
- hypervitaminosis D
- High calcium levels in blood and urine
- calcium kidney stones
- sarcoidosis
- Hypersensitivity to drug components, especially benzyl alcohol
- In case of hepatic or renal impairment
Drug interactions
Antiepileptic agents, rifampicin, cholestyramine reduce the reabsorption of vitamin D3. Simultaneous use with thiazide diuretics increases the risk of hypercalcemia.
Simultaneous use with cardiac glycosides may increase their toxic effect (increased risk of cardiac arrhythmias).
Cautions
Avoid overdose.
Individual provision of a certain need should take into account all possible sources of this vitamin. Too high doses of vitamin D3 administered for long periods or shock doses can cause chronic hypervitaminosis D3. Determination of the child’s daily vitamin D requirement and method of administration should be determined by the physician individually and adjusted each time during periodic examinations, especially in the first months of life.
Use with caution in immobilized patients.
Do not use calcium preparations in high doses simultaneously with vitamin D3. Treatment is carried out under periodic monitoring of calcium levels in blood and urine. Caution is necessary when prescribing the drug to elderly people because calcium deposition in the body increases in this category of people.
Pregnancy and lactation
It is not recommended to use high doses of vitamin D3 during pregnancy because of possible teratogenic action in case of overdose.
Caution should be exercised when prescribing vitamin D3 for breastfeeding women, since the drug taken in high doses by the mother may cause overdose symptoms in the child.
Effect on the ability to drive vehicles and maintain mechanical equipment
No effect
Overdose
Symptoms of overdose: decreased appetite, nausea, vomiting, constipation, restlessness, thirst, polyuria, diarrhea, intestinal colic. Frequent symptoms are headache, muscle and joint pain, mental disorders, including depression, stupor, ataxia and progressive weight loss. Renal dysfunction develops with albinuria, erythrocyturia and polyuria, increased potassium loss, hypostenuria, nycturia and increased blood pressure. In severe cases there may be corneal clouding, less often edema of the optic nerve papilla, iris inflammation up to cataract development. Kidney stones may form, calcification of soft tissues, including blood vessels, heart, lungs and skin may occur. Rarely cholestatic jaundice develops.
Treatment: Discontinue use of the drug. Consult a doctor. Take plenty of fluids. If necessary, hospitalization may be required.
Form of production
Oral drops 15 000 IU/ml in 10 ml, 20 ml, 30 ml in dropper bottles, vials.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25°C. Keep out of the reach of children!
Shelf life
2 years. Do not use after the expiration date.
Conditions of dispensing from pharmacies
Released without a prescription.