osteotriol

General characteristics. Structure:

Active agent: calcitriol - 0,25 mkg or 0,5 mkg;
excipients: butylated hydroxyanisole, butylated hydroxytoluene, the fractioned coconut oil.
Structure of a cover of the capsule: gelatin, glycerin of 85%, sorbitol of 70%, titanium dioxide (Е 171), quinolinic yellow WS (Е 104), Patent blue V of 85% (capsule of 0,5 mkg).

Description
Capsules of 0,25 mkg: Oval, elastic, soft gelatin capsules of yellow color, with a text black 0,25 paint. Capsules of 0,5 mkg: Oval, elastic, soft gelatin capsules of green color with a text black 0,5 paint.

Pharmacological properties:

Calcitriol - 1.25α(OH) a 2D3-active metabolite of D3 vitamin having all properties of natural D3 vitamin. Considerably surpasses natural D3 vitamin in biological activity. Calcitriol increases absorption of calcium in intestines, its reabsorption in kidneys, promotes a mineralization of bones. Besides, calcitriol participates in growth and a differentiation of cells of a bone, and also in neuromuscular transmission maintenance, functioning of cross-striped muscles, modulates immune responses. The mechanism of effect of calcitriol is connected with interaction with the specific receptors localized in a cellular kernel (the genomic mechanism) and also on a plasma membrane of target cells (not genomic mechanism). Effect of drug is followed by normalization of reduced absorption of calcium in intestines, its reabsorption in kidneys and increase in concentration in a blood plasma, suppression of secretion of parathyroid hormone. At its use decrease an ostealgia and muscles, the skeleton mineralization improves.

Pharmacokinetics. After intake it is quickly soaked up in intestines. The maximum concentration in blood serum is reached in 4-6 hours. In blood contacts specific plasma proteins. Gets through a placental barrier and it is allocated in breast milk. Biotransformation of drug proceeds with formation of a number of the metabolites having in various degree the expressed activity of D3 vitamin. The elimination half-life makes 3-6 h, however because of high lipophilicity drug and its metabolites can partially collect in fatty tissue in this connection pharmacological action can will remain to 3-5 days. It is removed with bile and, partially, is exposed to enterohepatic recirculation. At the patients who are on a hemodialysis, concentration in blood serum is reduced, and its maximum concentration is reached through longer span.

Indications to use:

Renal osteodystrophy at a chronic renal failure (especially at the patients who are on a hemodialysis). Post-menopausal, senile and steroid osteoporosis. Postoperative hypoparathyrosis, idiopathic hypoparathyrosis and pseudohypoparathyroidism.

Route of administration and doses:

Capsules accept inside, washing down with water.
Renal osteodystrophy (patients on dialysis)
At patients with the normal and a little reduced level of calcium in blood serum drug is usually used in a dose 0,25 mkg / дн. every other day.
In case of lack of satisfactory effect it is possible to increase a dose on 0,25 mkg with an interval of 2-4 weeks.
As a rule, the dosage of 0,5-1 mkg a day provides necessary clinical effect.
Post-menopausal, senile and steroid osteoporosis
On 0,25 mkg 2 times a day, are long.
Hypoparathyrosis
Treatment begin with a dose 0,25 mkg, once a day in the morning. If necessary the dose can be increased with an interval of 2-4 weeks or by 0,25 mkg to 0,5-1 mkg/day.

Features of use:

During treatment by Osteotriol it is not necessary to appoint other drugs of vitamin D, including its derivatives. It is also not necessary to use in a significant amount the foodstuff enriched with vitamin D (butter, eggs and др).
During treatment it is regularly necessary to control the level of calcium and inorganic phosphates in a blood plasma and urine, especially at the patients with a renal osteodystrophy and also who are on a long bed rest (in particular, after operation).
For the purpose of the prevention of a hypercalcemia Osteotriol's dosage is calculated proceeding from reaction of the patient to drug and is selected individually. Efficiency of treatment is provided with definition of an adequate daily dose of calcium, including, if necessary, changes in a diet, and also reception containing calcium-additives or drugs. Thanks to improvement of absorption of calcium in a GIT some patients receiving calcitriol can manage the lowered consumption of drugs of calcium, and in some cases (at a tendency to a hypercalcemia) to do without their reception.
Observation of calcium level in serum at least two times a week throughout the drug use period is necessary. In case of exceeding of level of calcium in serum on 1 mg / 100 ml (250 μмоль/л), in comparison with the accepted standard - 9-11 mg / 100 ml (2250 - 2750 μмоль/л), or increases in level of creatinine in blood serum to 120 μмоль/л from above, Osteotriol's reception has to be immediately stopped. Resuming of treatment is allowed only after normalization of level of calcium in serum within admissible normative range with use of the drug dose reduced by 0,25 mkg. At co-administration of barbiturates or anticonvulsant drugs increase in a dosage of calcitriol can be required. During an initial stage of treatment of osteoporosis measurement of concentration of calcium in blood serum and creatinine in 4 weeks, 3 months and 6 months is necessary. Upon termination of this period it is necessary to carry out check analyses of these indicators at an interval of 6 months.
The patients with normal function of kidneys accepting Osteotriol need to avoid dehydration, monitoring sufficient intake of liquid.

Use during pregnancy
Osteotriol's use during pregnancy is possible only if the estimated advantage for mother exceeds possible risk for a fruit.

Side effects:

Drug is well transferred, seldom causes side effects. In some cases at Osteotriol's reception the hypercalcemia, a hypercalcuria which symptoms are nausea, vomiting, a lock, an abdominal pain, anorexia, slackness, a headache, drowsiness and apathy can be observed. At patients with normal function of kidneys the chronic hypercalcemia can lead to increase in creatinine of blood serum.
Emergence of the specified effects demonstrates exceeding of a dosage. The probability of emergence of a hypercalcemia is higher at patients with a renal failure, a hyper parathyroidism or being on a hemodialysis. In very exceptional cases (especially in the presence of a hypercalcemia and a hyperphosphatemia) calcification of soft tissues can develop.

Interaction with other medicines:

At simultaneous use of Osteotriol with drugs of a foxglove the risk of development of arrhythmia increases, and with the drugs containing magnesium (for example, antacids) - the risk of development of a gipermagniyemiya in this connection the specified means should not be appointed by the patient who is on a hemodialysis receiving Osteotriol increases.
Use of the medicines which are inductors of liver enzymes (Phenytoinum, phenobarbital, etc.), can cause strengthening of metabolism of drug and decrease in concentration of calcitriol in blood serum in this connection at simultaneous use of Osteotriol and the specified drugs more raised calcitriol doses can be required.
Colestyraminum can reduce intestinal absorption of fat-soluble vitamins and, including, calcitriol.
Osteotriol's use together with thiazide diuretics can increase risk of development of a hypercalcemia.
At Osteotriol's use because of risk of a hypercalcemia co-administration of other drugs of vitamin D and its derivatives is not allowed.

Contraindications:

The diseases which are followed by a hypercalcemia and a hyperphosphatemia, a hypervitaminosis of D.
Hypersensitivity to drug, and also to other drugs of vitamin D. The lactation period - Children's age

Precautionary measures
With care drug is used at a heart and renal failure, a phosphatic nephrolithiasis, a sarcoidosis, etc. granulomatoza. From patients of advanced age the prevention of hyper calcemic complications requires especially careful individual selection of a dosage.

Overdose:

Symptoms of acute poisoning: anorexia, headache, vomiting, locks.
Symptoms of chronic poisoning: dystrophy (weakness, loss of weight, disorder of sensitivity, fever with thirst, a polyuria, dehydration, apathy, infections of urinary tract, the calcification centers in internals.
Treatment
At accidental overdose: carrying out a gastric lavage or use of vomitive for the prevention of further absorption of drug. At development of a hypercalcemia therapy by Osteotriol needs to be stopped, to appoint a diet with the lowered content of calcium and to keep the patient under observation of the doctor before normalization of concentration of calcium in a blood plasma. After that therapy can be resumed or using the lowered dose, or same, but at big intervals of administration of drug. In case of an acute hypercalcemia the hydration for the purpose of a call at the patient whenever possible of a diuresis is necessary. At increase in a bone resorption the calcitonin promotes decrease in calcium in serum.

Storage conditions:

List B. At a temperature not above +30 °C in the place, unavailable to children. Period of validity 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules on 0,25 mkg or 0,5 mkg.
Packaging:
Capsules on 0,25 mkg: 30 capsules (3 blisters on 10 capsules in everyone) with the application instruction in a cardboard pack.
30 capsules or 100 capsules in a plastic bottle with the application instruction in a cardboard pack.
Capsules on 0,5 mkg: 30 capsules (3 blisters on 10 capsules in everyone) with the application instruction in a cardboard pack.
30 capsules in a plastic bottle with the application instruction in a cardboard pack.