Calcitriol (When ATH D05AX02)

When ATH:
D05AX02

Characteristic.

Calcitriol is the active form of vitamin D3. The white crystalline powder. It is soluble in methanol, ethanol, ethyl acetate. Soluble in organic solvents, is relatively insoluble in water. Sensitive to the action of air and light. Molecular weight 416,64.

Pharmacological action.
D-vitamin-like.

Application.

For systemic use: renal osteodystrophy genesis (in patients with renal insufficiency, incl. against the background of hemodialysis), postoperative and idiopathic hypoparathyroidism, psevdogipoparatireoz, Vitamin-D-zavisimыy rickets, gipofosfatemicheskiy vitamin-D-rezistentnыy rickets (natural phosphate diabetes), osteoporosis (postmenopauzny, senile and "steroid"), tetany (incl. Postoperative, Idiopathic).

For application to the skin: psoriasis (mild to moderate).

Contraindications.

Hypersensitivity. When administered systemically: hypercalcemia, renal osteodystrophy with hyperphosphatemia, гипервитаминоз D, pregnancy, lactation.

When applied topically: hypercalcemia and metabolic Ca2+, Related systems (supports) treatment of calcium homeostasis, pregnancy, lactation.

Restrictions apply.

For systemic use: atherosclerosis, pulmonary tuberculosis (active form), congestive heart failure, giperfosfatemiя, phosphate nefrourolitiaz, sarcoidosis or other granulomatosis, pregnancy, lactation, advanced age (can promote atherosclerosis), childhood (to 18 years).

For topical application,: childhood (to 12 years).

Pregnancy and breast-feeding.

Teratogenic effects. Research teratogenicity, performed in rabbits at doses 0,08 and 0,3 mg / kg (about 2 and 6 times higher than MRDC), shown, that all three offspring 15 gestational external and skeletal abnormalities. However, none of the 23 other litters (156 fruit) no significant abnormalities detected in comparison with control.

Studies in rats at doses up to 0,45 mg / kg (about 5 times higher than MRDC) They did not reveal the potential teratogenicity.

Nonteratogenic effects. In studies in rabbits, treated with calcitriol 7th to the 18th day of gestation at doses 0,3 ug / kg / day (about 6 times higher than MRDC), in 19% It marks the death of females, reduction in body weight in fetuses, decrease in the number of newborns, Lived 24 no. In studies of prenatal and postnatal development in rats the development of hypercalcemia was observed in offspring of females, receiving calcitriol at doses 0,08 or 0,3 ug / kg / day (approximately equal in 3 times higher than MRDC), hypercalcemia and hyperphosphatemia in females, receiving calcitriol at doses 0,08 or 0,3 ug / kg / day, and increased serum urea nitrogen in females, receiving calcitriol at a dose 0,3 ug / kg / day. In another study in the rat body weight in females was slightly reduced at doses of calcitriol 0,3 ug / kg / day (about 3 times higher than MRDC), inputted from the 7th to the 15th day of gestation.

Newborns of women, receiving calcitriol at doses of 17-36 mg / day (about 17 and 36 times higher than MRDC) during pregnancy, manifested mild hypercalcemia on the 2nd day of life returning to normal on the 3rd day.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies in pregnant women were not conducted).

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

In small amounts into breast milk of women (2,2±0,1) pg / ml.

Side effects.

Systemic effects. Symptoms of an overdose of vitamin D: hypercalcemia syndrome or calcium intoxication (depending on the severity and duration of hypercalcemia).

Early symptoms: weakness, prolonged headache, drowsiness, nausea, vomiting, dry mouth, constipation, myalgia, bone pain, metallic taste in mouth, decreased appetite, abdominal pain, thirst, increased frequency of urination, especially at night, or polyuria, arrhythmia.

Late symptoms: bone pain, polydipsia, anorexia, nocturia, conjunctivitis, pancreatitis, photophobia, rhinorrhea, itch, hyperthermia, decreased libido, increase in blood urea nitrogen, albuminuria, hypercholesterolemia, increase in liver transaminases (ALT IS), ectopic calcification, nephrocalcinosis, arterial hypertension, dystrophy (weakness, weight loss), violation of the sensitivity, degidratatsiya, apathy, retardation, urinary tract infection; rarely, psychosis. Allergic reactions (itch, rash, hives; very rarely is erythematous skin lesions).

In patients with normal renal function, chronic hypercalcemia may lead to an increase in serum creatinine.

When applied topically: dermatitis.

Cooperation.

Thiazide diuretics, calcium-containing drugs (high dose) — increase the risk of hypercalcemia; however, it may be therapeutically justified in elderly patients and high-risk groups, when it is necessary to assign the vitamin D or derivatives thereof, together with calcium; long-term therapy should be closely monitored in serum calcium concentration. Inductors of microsomal oxidation (incl. anticonvulsants, barbiturates, prymydon) accelerate metabolism and help to reduce the action of calcitriol. Cholestyramine, colestipol and mineral oils — reduce suction and reducyruut concentration in blood serum. Calcitriol increases absorption of phosphorus-containing drugs and the risk of hyperphosphataemia. Incompatible with vitamin D and its derivatives (increases the risk of hypervitaminosis D). Caution is required, while the appointment of cardiac glycosides, tk. and increased risk of arrhythmia due to the development of hypercalcemia. When long-term therapy of aluminum-containing antacids at the same time increased calcitriol levels of aluminum in the blood, which may lead to intoxication aluminum (especially in chronic renal failure). Against the backdrop of the simultaneous use of magnesium-containing antacids may develop gipermagniemii, especially in patients with chronic renal failure. Calcitriol with concomitant use of calcitonin, etidronovoy and Pamidronic acids may reduce their effect in the treatment of hypercalcemia. The addition of vitamin D in the treatment of glucocorticoids may be recommended when prolonged use.

Overdose.

Symptoms: increased severity of side effects is hypercalcemia, hypercalciuria, giperfosfatemiя.

Treatment: in case of accidental overdose-washing stomach, the appointment of an antiemetic (to prevent further absorption), for elimination of the drug in the faeces as a purgative used mineral oil. When developing gipercalziemii — discontinuations, diet low in calcium, observation of the patient to normalize the level of calcium in plasma. Further treatment can be resumed with a reduced dose of, or with an increased interval between doses. Acute hypercalcemia is hydration (to stimulate diuresis); with the increase of bone resorption-appointment of calcitonin (reduces serum calcium).

Dosing and Administration.

Inside, outwardly. The optimal daily dose is adjusted depending on the level kaltsiemii.

Inside, the initial dose is 0,25 mg / day. If clinical indicators do not improve within 2-4 weeks of treatment, the daily dose 0,25 micrograms to the average (0,5-1 g/day) and above at intervals of 2-4 weeks. When menopausal osteoporosis — on 0,25 g 2 once a day. In renal osteodystrophy: initial dose for adults is 0,25 mg / day, patients with normal or slightly reduced level of serum calcium is enough 0,25 micrograms a day, children — by 0.014-0.041 µg/kg/day. In liver disease initial dose may be increased to 0.1-0.2 micrograms / kg / day. When rickets and hypoparathyroidism: initial dose for adults is 0,25 mg / day (morning), children-0.01-0.1 mcg/kg. When phosphate diabetes shows phosphorus supplementation drugs.

Outwardly. The ointment is applied in a thin layer to the affected skin (on clean and dry skin) 2 once a day (in the morning and in the evening). The maximum dose - 30 g / day. Daily application of ointment should not be more than 35% skin. Average duration of treatment is 6 Sun, if necessary possibly longer treatment, as well as the use of the drug as maintenance therapy.

Precautions.

The dose should be calculated individually based on the patient's response (for the prevention of hypercalcemia). The effectiveness of treatment provided by the definition of an adequate daily dose of calcium, including, if necessary, changes in diet and taking medications or dietary supplements, containing calcium (some patients may avoid reducing the consumption of calcium supplements, and if the tendency towards hypercalcemia is to stop taking them). In elderly patients requires careful selection of individual dose (to prevent complications hypercalcemic).

Do not mix other medications Vitamin D, including derivatives thereof, eat food, fortified with vitamin D (butter, eggs, etc.).

During treatment should regularly monitor the level of calcium and inorganic phosphate in plasma and urine, especially in patients with renal osteodystrophy, and are on prolonged bed rest (particularly after surgery).

Patients with normal renal function should avoid dehydration by consuming plenty of fluids.

Monitoring of serum calcium levels during treatment should be carried out at least twice a week; If it exceeds the level of calcium in 1 mg / 100ml (250 mmol / l) compared to the norm is 9-11 mg/100 ml (2250-2750 Mmol / l), or with an increase in serum creatinine to 120 mmol / l or more stop taking the drug immediately. The resumption of treatment is allowed only after normalization of serum calcium levels using dose, reduced to 0,25 g.

When concomitant administration of barbiturates and anticonvulsants may require increased doses of calcitriol.

In the treatment of osteoporosis in the initial period of the calcium concentration in serum should be measured by 4 Sun, 3 and 6 Months, then control tests should be carried out at intervals 6 Months.

The risk of skin irritation increased when applying the ointment on your face. After applying the ointment should wash their hands. If you accidentally hit the ointment on the mucous membrane of eyes, mouth or nose must be thorough washing with warm water.

Cooperation

Active substanceDescription of interaction
PhenytoinFKV. Accelerates biotransformation (inductor mikrosomalynogo oxalate) and decreases the concentration in the blood.
PhenobarbitalFKV. Accelerates biotransformation (inductor mikrosomalynogo oxidized) and decreases the concentration in the blood.

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