Parykaltsytol | Zemplar capsules 1 mcg, 28 pcs.
Special Price
$105.73
Regular Price
$117.00
In stock
SKU
BID465660
Release form
Capsules
Capsules
Release form
Capsules
Packing
28 pcs.
Pharmacological action
Zemplar - a drug that regulates the exchange of calcium and phosphorus. Paricalcitol is a synthetic analogue of biologically active vitamin D (calcitriol), in the structure of which there are modifications of the side chain (D2) and ring A (19-nor). Paricalcitol selectively activates the vitamin D receptors in the parathyroid gland without increasing the activity of vitamin D receptors in the intestine and less actively affects bone resorption. Paricalcitol also activates calcium-sensitive receptors in the parathyroid glands, thereby reducing parathyroid hormone (PTH) levels by inhibiting parathyroid proliferation and decreasing PTH synthesis and secretion. It has a minimal effect on calcium and phosphorus levels and can directly affect bone cells. By correcting pathological levels of PTH and normalizing calcium and phosphorus homeostasis, it can prevent and treat bone diseases associated with impaired metabolism due to chronic kidney diseases.
Secondary hyperparathyroidism is characterized by an increase in the content of PTH, which is associated with an inadequate level of active vitamin D. This vitamin is synthesized in the skin and enters the body with food. Vitamin D is sequentially hydroxylated in the liver and kidneys and turns into an active form that interacts with vitamin D. receptors.
Indications
Prevention and treatment of secondary hyperparathyroidism developing in chronic kidney disease stage 3 and 4, as well as in patients with chronic kidney disease stage 5, undergoing hemodialysis or peritoneal dialysis.
Contraindications
giipervitaminosis D
hypercalcemia
co-administration with phosphates or vitamin D derivatives
children under 18 years of age (no clinical studies)
lactation period
hypersensitivity to any component of the drug.
Caution is advised to prescribe the drug concomitantly with cardiac glycosides.
Special instructions
Excessive suppression of PTH secretion can lead to increased serum calcium levels and decreased metabolic processes in bone tissue. To achieve physiological parameters, monitoring of the patient's condition and individual dose selection are necessary.
In the event of the development of clinically significant hypercalcemia in a patient taking calcium-containing phosphate binders, the dose of the latter should be reduced, or its reception should be interrupted.
At the initial dose selection or any change in it, serum calcium, phosphorus serum or plasma levels of IPTG should be determined at least every 2 weeks for 3 months after the start of treatment with paricalcitol in capsules or after changing the dose of paricalcitol, then monthly for 3 months, then - every 3 months.
There were no differences in efficacy or safety in patients 65 years of age or older.
Composition of
1 capsule contains paricalcitol 1 Ојg
Dosage and administration of
Initial dose of
There are two methods for selecting the initial dose of paricalcitol. In clinical studies, the maximum safe dose reached 40 mcg.
Selection of the initial dose by body weight
The recommended initial dose of paricalcitol is 0.04-0.1 mcg / kg (2.8-7 mcg).
Side effects of
Among the side effects in patients with chronic kidney disease of stages 3 and 4 treated with paricalcitol, skin rashes were most often observed (in 2% of patients).
All adverse events, both clinical and laboratory, the relationship of which with the use of paricalcitol could be characterized, at least as possible, are presented by organ systems and frequency of development. According to the frequency of development, they are divided into the following groups: very often (? 1/10), often (? 1/100, <1/10), infrequently (? 1/1000, <1/100), rarely (? 1/10 000, <1/1000), very rarely (<1/10 000), including isolated cases.
Adverse reactions in patients with chronic kidney disease stage 3 and 4, described in clinical trials
From the central nervous system: infrequently - dizziness.
From the digestive system: infrequently - perversion of taste, constipation, dry mouth, dyspepsia, gastritis, abnormal results of liver tests.
From the skin: often - a skin rash, infrequently skin itching, urticaria.
From the musculoskeletal system: infrequently - cramps in the muscles of the lower extremities.
Other: infrequently - allergic reactions.
Adverse reactions in patients with stage 5 chronic kidney disease described in a clinical trial of phase III
From the digestive system: often - anorexia, diarrhea, gastrointestinal disorders.
From the side of the central nervous system: often - dizziness.
From the skin: often - acne.
Other: often - pain in the mammary gland, hypercalcemia, hypocalcemia.
Adverse reactions, registered during post-marketing observations: Quincke's edema and laryngeal edema.
Drug interaction
In vitro results indicate that paricalcitol at concentrations up to 50 nM (21 ng / ml) (approximately 20 times higher than the concentrations observed after administration of the drug at the maximum dose studied) does not inhibit CYP3A, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 or CYP2E1. In experiments on a fresh hepatocyte culture, paricalcitol in concentrations up to 50 nM caused an increase in the activity of CYP2B6, CYP2C9 or CYP3A by less than 2 times, while under the influence of the inducers of these isoenzymes (positive control), it increased by 6-19 times. Therefore, paricalcitol should not inhibit or induce clearance of drugs that are metabolized by these enzymes.
The pharmacokinetic interaction between paricalcitol in capsules (16 μg) and omeprazole (40 mg orally) was investigated in a cross-sectional study in healthy volunteers. The pharmacokinetics of paricalcitol when it is taken with omeprazole does not change.
In healthy volunteers, Cmax of paricalcitol, when co-administered with ketoconazole, changes minimally, and AUC is approximately doubled. The average T1 / 2 of paricalcalcitol is 9.8 hours, with the concomitant use of ketoconazole - 17 hours. Caution should be exercised while prescribing paricalcitol and ketoconazole or other known CYP3A4 inhibitors.
Overdose
Symptoms: possible hypercalcemia, hypercalciuria and hyperphosphatemia, as well as a pronounced decrease in PTH secretion. The consumption of large amounts of calcium and phosphorus simultaneously with the use of paricalcitol can lead to similar disorders.
Treatment of acute accidental overdose of paricalcitol requires emergency care. If an overdose is detected after a relatively short time, you can induce vomiting or gastric lavage, which will help prevent further absorption of paricalcitol. If the drug has already passed through the stomach, the intake of liquid paraffin may contribute to its rapid elimination from the intestine. It is necessary to determine the serum concentration of electrolytes (especially calcium), the rate of excretion of calcium in the urine and evaluate changes in the ECG, which may be associated with hypercalcemia. Such monitoring is very important for patients receiving digitalis preparations. Stopping calcium supplements and following a low calcium diet, also shown in case of accidental overdose of the drug. Given the relatively short duration of action of paricalcitol, the above measures may be sufficient. For the treatment of severe hypercalcemia, it is possible to use drugs such as salts of phosphoric acids and GCS, as well as forced diuresis.
Storage conditions
The product should be stored out of the reach of children, at temperatures between 15 ° and 25 РC and must not be frozen.
Form of Treatment
kapsul
Capsules
Packing
28 pcs.
Pharmacological action
Zemplar - a drug that regulates the exchange of calcium and phosphorus. Paricalcitol is a synthetic analogue of biologically active vitamin D (calcitriol), in the structure of which there are modifications of the side chain (D2) and ring A (19-nor). Paricalcitol selectively activates the vitamin D receptors in the parathyroid gland without increasing the activity of vitamin D receptors in the intestine and less actively affects bone resorption. Paricalcitol also activates calcium-sensitive receptors in the parathyroid glands, thereby reducing parathyroid hormone (PTH) levels by inhibiting parathyroid proliferation and decreasing PTH synthesis and secretion. It has a minimal effect on calcium and phosphorus levels and can directly affect bone cells. By correcting pathological levels of PTH and normalizing calcium and phosphorus homeostasis, it can prevent and treat bone diseases associated with impaired metabolism due to chronic kidney diseases.
Secondary hyperparathyroidism is characterized by an increase in the content of PTH, which is associated with an inadequate level of active vitamin D. This vitamin is synthesized in the skin and enters the body with food. Vitamin D is sequentially hydroxylated in the liver and kidneys and turns into an active form that interacts with vitamin D. receptors.
Indications
Prevention and treatment of secondary hyperparathyroidism developing in chronic kidney disease stage 3 and 4, as well as in patients with chronic kidney disease stage 5, undergoing hemodialysis or peritoneal dialysis.
Contraindications
giipervitaminosis D
hypercalcemia
co-administration with phosphates or vitamin D derivatives
children under 18 years of age (no clinical studies)
lactation period
hypersensitivity to any component of the drug.
Caution is advised to prescribe the drug concomitantly with cardiac glycosides.
Special instructions
Excessive suppression of PTH secretion can lead to increased serum calcium levels and decreased metabolic processes in bone tissue. To achieve physiological parameters, monitoring of the patient's condition and individual dose selection are necessary.
In the event of the development of clinically significant hypercalcemia in a patient taking calcium-containing phosphate binders, the dose of the latter should be reduced, or its reception should be interrupted.
At the initial dose selection or any change in it, serum calcium, phosphorus serum or plasma levels of IPTG should be determined at least every 2 weeks for 3 months after the start of treatment with paricalcitol in capsules or after changing the dose of paricalcitol, then monthly for 3 months, then - every 3 months.
There were no differences in efficacy or safety in patients 65 years of age or older.
Composition of
1 capsule contains paricalcitol 1 Ојg
Dosage and administration of
Initial dose of
There are two methods for selecting the initial dose of paricalcitol. In clinical studies, the maximum safe dose reached 40 mcg.
Selection of the initial dose by body weight
The recommended initial dose of paricalcitol is 0.04-0.1 mcg / kg (2.8-7 mcg).
Side effects of
Among the side effects in patients with chronic kidney disease of stages 3 and 4 treated with paricalcitol, skin rashes were most often observed (in 2% of patients).
All adverse events, both clinical and laboratory, the relationship of which with the use of paricalcitol could be characterized, at least as possible, are presented by organ systems and frequency of development. According to the frequency of development, they are divided into the following groups: very often (? 1/10), often (? 1/100, <1/10), infrequently (? 1/1000, <1/100), rarely (? 1/10 000, <1/1000), very rarely (<1/10 000), including isolated cases.
Adverse reactions in patients with chronic kidney disease stage 3 and 4, described in clinical trials
From the central nervous system: infrequently - dizziness.
From the digestive system: infrequently - perversion of taste, constipation, dry mouth, dyspepsia, gastritis, abnormal results of liver tests.
From the skin: often - a skin rash, infrequently skin itching, urticaria.
From the musculoskeletal system: infrequently - cramps in the muscles of the lower extremities.
Other: infrequently - allergic reactions.
Adverse reactions in patients with stage 5 chronic kidney disease described in a clinical trial of phase III
From the digestive system: often - anorexia, diarrhea, gastrointestinal disorders.
From the side of the central nervous system: often - dizziness.
From the skin: often - acne.
Other: often - pain in the mammary gland, hypercalcemia, hypocalcemia.
Adverse reactions, registered during post-marketing observations: Quincke's edema and laryngeal edema.
Drug interaction
In vitro results indicate that paricalcitol at concentrations up to 50 nM (21 ng / ml) (approximately 20 times higher than the concentrations observed after administration of the drug at the maximum dose studied) does not inhibit CYP3A, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 or CYP2E1. In experiments on a fresh hepatocyte culture, paricalcitol in concentrations up to 50 nM caused an increase in the activity of CYP2B6, CYP2C9 or CYP3A by less than 2 times, while under the influence of the inducers of these isoenzymes (positive control), it increased by 6-19 times. Therefore, paricalcitol should not inhibit or induce clearance of drugs that are metabolized by these enzymes.
The pharmacokinetic interaction between paricalcitol in capsules (16 μg) and omeprazole (40 mg orally) was investigated in a cross-sectional study in healthy volunteers. The pharmacokinetics of paricalcitol when it is taken with omeprazole does not change.
In healthy volunteers, Cmax of paricalcitol, when co-administered with ketoconazole, changes minimally, and AUC is approximately doubled. The average T1 / 2 of paricalcalcitol is 9.8 hours, with the concomitant use of ketoconazole - 17 hours. Caution should be exercised while prescribing paricalcitol and ketoconazole or other known CYP3A4 inhibitors.
Overdose
Symptoms: possible hypercalcemia, hypercalciuria and hyperphosphatemia, as well as a pronounced decrease in PTH secretion. The consumption of large amounts of calcium and phosphorus simultaneously with the use of paricalcitol can lead to similar disorders.
Treatment of acute accidental overdose of paricalcitol requires emergency care. If an overdose is detected after a relatively short time, you can induce vomiting or gastric lavage, which will help prevent further absorption of paricalcitol. If the drug has already passed through the stomach, the intake of liquid paraffin may contribute to its rapid elimination from the intestine. It is necessary to determine the serum concentration of electrolytes (especially calcium), the rate of excretion of calcium in the urine and evaluate changes in the ECG, which may be associated with hypercalcemia. Such monitoring is very important for patients receiving digitalis preparations. Stopping calcium supplements and following a low calcium diet, also shown in case of accidental overdose of the drug. Given the relatively short duration of action of paricalcitol, the above measures may be sufficient. For the treatment of severe hypercalcemia, it is possible to use drugs such as salts of phosphoric acids and GCS, as well as forced diuresis.
Storage conditions
The product should be stored out of the reach of children, at temperatures between 15 ° and 25 РC and must not be frozen.
Form of Treatment
kapsul
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