TEVA #Vitamins_and_minerals #Vitamins #Vitamin_D #HEALTH_CARE
Pharmacological properties
Pharmacodynamics. Alpha d3-teva is a highly effective active metabolite of vitamin d3 that regulates calcium and phosphorus metabolism. Alfacalcidol (1-alpha hydrocholecalciferol) is rapidly converted to calcitriol (1,25-dihydrocholecalciferol, d-hormone) in the liver. Calcitriol is one of the main metabolites of cholecalciferol (vitamin d3) in maintaining calcium and phosphorus homeostasis. alpha d3-teva is transformed into 1,25-dihydrocholecalciferol (d-hormone) and thus increases its level in the blood. this causes an increase in the absorption of calcium and phosphorus in the intestine, an increase in their reabsorption in the kidneys, an increase in bone mineralization, and a decrease in the level of parathyroid hormone in the blood. in patients with age-related disorders of 1-alpha-hydroxylation in the kidneys, the intake of alpha-d3-teva contributes to the sufficient formation of calcitriol, which neutralizes the deficiency of d-hormone. Alpha d3-teva restores a positive calcium balance, as a result of which the intensity of bone resorption decreases, which helps to reduce the incidence of fractures. increases bone mineral density. With the course of use of the preparation, a decrease in the severity of bone and muscle pain associated with a violation of phosphorus-calcium metabolism is noted, coordination of movements and maintenance of balance improves, muscle strength increases, as a result of which the frequency of falls decreases.
Pharmacokinetics. After oral administration, Alpha D3-Teva is rapidly absorbed in the gastrointestinal tract. The time to reach Cmax of the preparation in blood plasma is 8-18 hours. The onset of action is after 6 hours, the duration of action is up to 48 hours.
In the liver, alfacalcidol is rapidly transformed into calcitriol (1,25-dihydrocholecalciferol, D-hormone). A smaller part of the preparation is transformed into bone tissue.
Unlike natural vitamin D3, the biotransformation of the preparation does not occur in the kidneys, which makes it possible to use it in patients with renal pathology.
Indications
Postmenopausal osteoporosis. osteoporosis associated with glucocorticoid treatment. softening of bones in old age (osteomalacia) as a result of insufficient absorption, for example, in the case of malabsorption and postgastrectomy syndrome. to significantly reduce the incidence of falls in the elderly. with hypoparathyroidism or hypophosphatemic (vitamin d-resistant) rickets / osteomalacia, additional therapy with alpha d3-teva may be indicated if the plasma calcium level is 2.2 mmol / l. diseases accompanied by impaired 1-alpha hydroxylation in the kidneys, which, in turn, cause disorders of vitamin d metabolism (for example, renal osteodystrophy with a decrease in calcium absorption and a plasma calcium level of 2.2 mmol / l (8.8 mg / 100 ml), which can occur as a result of impaired renal function without or with dialysis, as well as in the beginning with a condition after kidney transplantation).
Application
Inside. the capsule should be swallowed whole, washed down with plenty of water. the dose and duration of therapy are determined by the doctor individually and depend on the nature of the disease and the effectiveness of therapy. in some cases, the preparation is used throughout life.
Unless otherwise prescribed by a doctor, the initial dose for adults is 1 μg of alfacalcidol (4 capsules of 0.25 μg, or 2 capsules of 0.5 μg, or 1 capsule of 1 μg) daily. Patients with more severe bone disease are prescribed higher doses: 1-3 mcg of alfacalcidol (4-12 capsules of 0.25 mcg, or 2-6 capsules of 0.5 mcg, or 1-3 capsules of 1 mcg) daily.
Children over the age of 6 years with a body weight of ≥20 kg who can swallow a capsule - 1 μg / day (except in cases of renal osteodystrophy).
For patients with hypoparathyroidism, the dose should be reduced after reaching normal blood calcium levels (2.2–2.6 mmol / L; 8.8–10.4 mg / 100 ml), or when the product of plasma calcium • phosphate concentrations is 3.5-3.7 (mmol / l).
Alpha D3-Teva capsules 0.25 mcg. If the daily dose is 0.5 mcg of alfacalcidol, take 1 capsule in the morning and in the evening every day. If the daily dose is 1 mcg of alfacalcidol, take 2 capsules in the morning and in the evening every day.
Alpha D3-Teva capsules, 0.5 mcg. If the daily dose is 0.5 mcg, take 1 capsule daily in the evening. If the daily dose is 1-3 mcg of alfacalcidol (2-6 capsules of 0.5 mcg), it must be divided in half and taken one half in the morning and the other half in the evening.
Alpha D3-Teva capsules 1 mcg. If the daily dose is 1 mcg of alfacalcidol, take 1 capsule in the evening every day. If the daily dose is 3 mcg of alfacalcidol, take 1 capsule in the morning and 2 capsules of Alpha D3-Teva in the evening.
Contraindications
Hypersensitivity to alfacalcidol, peanuts, soy or any other components of the preparation; hypersensitivity to vitamin d and manifestations of vitamin d intoxication; plasma calcium level 2.6 mmol / l; the product of calcium concentrations • plasma phosphate 3.7 (mmol / l); alkalosis with a ph level of venous blood of 7.44 (lactate alkalosis syndrome, burnett syndrome); metastatic calcification; hypersensitivity to analogs of vitamin d.
Side effects
If the dose of alfacalcidol is not adjusted, an increase in the level of calcium in the blood is possible, which disappears when the dose is reduced or the preparation is temporarily discontinued. signs of a possible increase in blood calcium levels - fatigue, gastrointestinal disorders (vomiting, heartburn, abdominal pain, nausea, epigastric discomfort, constipation, diarrhea), anorexia, dry mouth, moderate muscle pain, bone pain, joints, weight loss, polyuria, increased sweating, headache, thirst, vertigo, increased levels of calcium and phosphate in the urine, nephrocalcinosis, hypersensitivity reactions, including pruritus, rashes, urticaria.
During therapy with alfacalcidol, adverse reactions may occur, which in frequency are defined as very often (≥1 / 10), often (≥1 / 100 to 1/10), infrequently (≥1 / 1000 to 1/100), rarely (≥ 1/10 000 to 1/1000), very rare (1/10 000), unknown (impossible to establish from the available data).
Often: hypercalcemia *, hypercalciuria.
Rarely: hyperphosphatemia, in order to prevent which the patient can be prescribed inhibitors of phosphate absorption (such as aluminum compounds); tachycardia, weakness, headache, dizziness, drowsiness.
Very rarely, including isolated cases: heterotopic calcification (cornea and blood vessels), which disappears after preparation withdrawal; a slight increase in HDL in blood plasma. In patients with severe renal impairment, hyperphosphatemia may develop; allergic skin reactions (itching) and anaphylactic shock, the latter can be caused by the peanut butter that is part of the preparation.
Unknown: hypersensitivity.
* Hypercalcemia is also associated with reactions such as hyperkaliuria, ectopic calcification, kidney and heart damage.
Special instructions
Alfacalcidol should not be administered to patients with hypercalcemia.
The preparation is prescribed with caution:
patients prone to hypercalcemia, especially with urolithiasis;
patients who are simultaneously using cardiac glycosides or digitalis preparations, since hypercalcemia can lead to arrhythmias in such patients.
During the period of use of the preparation, it is necessary to regularly (at least 1 time in 3 months) monitor the level of calcium in the blood plasma and urine, monitor the development of the therapeutic effect and, if necessary, adjust the dose of alfacalcidol in order to avoid the development of hypercalcemia and hypercalciuria. In the presence of biochemical signs of normalization of the bone structure (normalization of the ALP content in the blood plasma), a corresponding decrease in the dose of Alpha D3-Teva is necessary, which avoids the development of hypercalcemia. Hypercalcemia or hypercalciuria can be eliminated by discontinuing the preparation and reducing calcium intake until its plasma concentration normalizes. Typically, this period is 1 week. Then therapy can be continued, starting at half of the last dose applied.
During therapy with alfacalcidol, plasma phosphate levels should be monitored to reduce the risk of ectopic calcification.
Adding vitamin D to the diet can be harmful to individuals who are already receiving adequate amounts of it from food and sunlight, since the difference between therapeutic and toxic concentration is very small.
Since alfacalcidol is the most active form of vitamin D, there is reason to expect the greatest risk of toxicity from its intake, however, its effects are quickly reversible if the intake is discontinued.
Alfacalcidol increases the absorption of calcium and phosphate in the intestine, therefore, in patients with renal insufficiency, their plasma concentrations should be monitored.
It is necessary to monitor the clinical manifestations of hypo- or hypercalcemia in elderly patients, especially in the presence of concomitant renal or cardiac pathology.
Early symptoms of hypercalcemia include polyuria; polydipsia; weakness, headache, nausea, constipation; dry mouth; muscle and bone pain; metallic taste in the mouth.
The medicinal product contains soybean oil. If the patient is allergic to peanuts or soy, the preparation is not recommended.
During pregnancy and breastfeeding. Although it has not been proven to have a negative effect on the fetus or infant, the preparation should not be used during pregnancy and lactation.
Due to the possible risk of developing persistent hypercalcemia, which can cause delayed physical and mental development, supravalvular aortic stenosis, retinopathy in infants, an overdose of a vitamin D analogue during pregnancy should be avoided.
The use of alfacalcidol during breastfeeding may increase the level of calcitriol in breast milk. Given this, the preparation is not used during breastfeeding.
Children. It is used in children over the age of 6 years with a body weight of ≥20 kg, who can swallow the capsule.
The ability to influence the reaction rate when driving or working with other mechanisms. The effect of the preparation on the ability to drive vehicles and work with complex mechanisms has not been identified, but the possibility of such adverse reactions as drowsiness and dizziness should be taken into account.
Interactions
In the treatment of osteoporosis, alpha d3-teva can be prescribed in combination with antiresorptive preparations of different groups and estrogens. the effect of alfacalcidol enhances the simultaneous use of estrogens in women during the pre- and postmenopausal period.
Vitamin D and its derivatives should not be used concomitantly with Alpha D3-Teva due to the possibility of additive interactions and an increased risk of hypercalcemia.
With the simultaneous use of Alpha D3-Teva with digitalis preparations, the risk of arrhythmia increases.
With simultaneous use with barbiturates, anticonvulsants (for example, carbamazepine, phenobarbital, phenytoin and primidone) and other preparations that activate enzymes of microsomal oxidation in the liver, it is necessary to take Alpha D3-Teva in a higher dose.
GCS can also reduce the effect of vitamin D.
The absorption of alfacalcidol is reduced when it is used with cholestyramine, colestipol, sucralfate, antacids with a high aluminum content. Alpha D3-Teva and aluminum-based antacids cannot be used simultaneously, the interval between doses should be at least 2 hours.
With the simultaneous use of Alpha D3-Teva and magnesium-based antacids, the risk of developing hypermagnesemia increases.
With the simultaneous use of calcium preparations, thiazide diuretics, the risk of developing hypercalcemia increases.
Rifampicin and isoniazid may reduce the effectiveness of vitamin D.
Overdose
With a single overdose (25-30 mcg) of alfacalcidol, no harm to health was detected. subsequent cases of alfacalcidol overdose may cause hypercalcemia.
Symptoms: anorexia, weakness, lethargy, dizziness, headache, nausea, dry mouth, constipation, diarrhea, heartburn, vomiting, abdominal pain, bone pain, increased sweating, drowsiness, itching, tachycardia. Perhaps the appearance of polyuria, polydipsia, nocturia, thirst, proteinuria with impaired renal function, weight loss.
Treatment: stop taking the preparation. Depending on the severity of hypercalcemia, you can follow a calcium-free or low-calcium diet, drink fluids, carry out dialysis, use loop diuretics, GCS and calcitonin. In acute overdose, a positive effect is possible with gastric lavage and / or the use of mineral oil (which helps to reduce absorption and increase excretion of the preparation in the feces). There are no specific antidotes for alfacalcidol.
Storage conditions
In a tightly closed container at a temperature not exceeding 25 ° C.
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