Kalchek pills 10mg №10×3

Name:
Kalchek. Forms of release Tablets. INNAmlodipine. FTGBmkk. Composition Each 5 mg tablet contains: Active substance: amlodipine 5 mg (as amlodipine besylate 6.93 mg). Excipients: corn starch 66.72 mg, calcium hydrogen phosphate 150.88 mg, talc 2.0 mg, colloidal silicon dioxide 2.0 mg, sodium carboxymethyl starch 0.24 mg, magnesium stearate 1.0 mg. Each 10 mg tablet contains: Active substance: amlodipine 10 mg (as amlodipine besylate 13.92 mg). Excipients: corn starch 101.1 mg, calcium hydrogen phosphate 235.7 mg, talc 3.5 mg, colloidal silicon dioxide 3.0 mg, sodium carboxymethyl starch 0.5 mg, magnesium stearate 2.0 mg.
Description:
Round, flat tablets with bevelled edges, from white to almost white, scored on one side. Pharmacotherapeutic group Slow calcium channel blocker (BMCC). ATX code: С08СА01 Pharmacological action Pharmacodynamics Dihydropyridine derivative is a blocker of “slow” calcium channels of the II generation, has antianginal and hypotensive effect. By binding to dihydropyridine receptors, it blocks calcium channels, reduces the transmembrane transition of calcium ions into the cell (to a greater extent into vascular smooth muscle cells than into cardiomyocytes). The antianginal effect is due to the expansion of the coronary and peripheral arteries and arterioles: in angina pectoris, it reduces the severity of myocardial ischemia; expanding peripheral arterioles, reduces total peripheral vascular resistance, reduces afterload on the heart, reduces myocardial oxygen demand. By expanding the main coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, it increases the supply of oxygen to the myocardium (especially with vasospastic angina); prevents the development of constriction of the coronary arteries (including those caused by smoking). In patients with angina pectoris, a single daily dose increases the time of exercise, slows down the development of angina pectoris and “ischemic” depression of the ST segment (by 1 mm), reduces the frequency of angina attacks and the consumption of nitroglycerin. It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilating effect on vascular smooth muscle. With arterial hypertension, a single dose provides a clinically significant decrease in blood pressure for 24 hours (in the position of the patient “lying” and “standing”). Does not cause a sharp decrease in blood pressure, reduce exercise tolerance, left ventricular ejection fraction. Reduces the degree of left ventricular myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effects in coronary heart disease. It does not affect myocardial contractility and conduction, does not cause a reflex increase in heart rate, inhibits platelet aggregation, increases glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria. It has no adverse effects on metabolism and plasma lipids. The onset of the effect is 2-4 hours, the duration of the effect is 24 hours. Pharmacokinetics After oral administration, amlodipine is slowly absorbed from the gastrointestinal tract. The average absolute bioavailability is 64%, the maximum concentration in blood serum is observed after 6-9 hours. Equilibrium concentration is reached after 7 days of therapy. Food does not affect the absorption of amlodipine. The mean volume of distribution is 21 l/kg of body weight, which indicates that most of the drug is in the tissues, and relatively less in the blood. Most of the drug in the blood (95%) binds to plasma proteins. Amlodipine undergoes slow but extensive metabolism (90%) in the liver with the formation of inactive metabolites, has a “first pass” effect through the liver. Metabolites do not have significant pharmacological activity. After a single oral administration, the half-life (T1 / 2) averages 35 hours. About 60% of the ingested dose is excreted by the kidneys mainly in the form of metabolites, 10% – unchanged, and 20-25% – through the intestines, as well as in breast milk. In patients with arterial hypertension T1 / 2 – 48 hours, in elderly patients (over 65 years old), the excretion of amlodipine is slowed down (T1 / 2 – 65 hours) compared with young patients, but this limit has no clinical significance. In patients with hepatic insufficiency, an extension of T1 / 2 is expected, and with long-term administration, the accumulation of the drug in the body will be higher (T1 / 2 up to 60 hours). Renal failure does not significantly affect the kinetics of amlodipine. The drug penetrates the blood-brain barrier. It is not removed by hemodialysis. Indications for use Arterial hypertension (monotherapy or in combination with other antihypertensive agents; Treatment of stable angina pectoris, vasospastic angina pectoris (Prinzmetal’s angina pectoris). Dosage and administration In arterial hypertension and angina pectoris, the usual initial dose of amlodipine is 5 mg once a day, which can be increased to a maximum a dose of 10 mg, depending on the individual response of the patient.Dose adjustment of amlodipine with simultaneous use of thiazide diuretics, beta-blockers or angiotensin-converting enzyme inhibitors is not required.Use in the elderly The drug is recommended to be used in usual doses.Identical doses of amlodipine were well tolerated as young and elderly patients Use in children The safety and efficacy of amlodipine when used in children has not been established Use in patients with impaired liver function See section Special instructions and precautions sti when applied. Use in Renal Insufficiency Amlodipine can be used in the usual doses for the treatment of such patients. Changes in the concentration of amlodipine in plasma do not correlate with the degree of impaired renal function. Amlodipine is not removed during dialysis. Contraindications Amlodipine is contraindicated in patients who have shown hypersensitivity to dihydropyridines, amlodipine or any of the auxiliary components of the drug, in patients with severe arterial hypotension, in a state of shock (including cardiogenic shock), with obstruction of the outflow tract of the left ventricle (severe aortic stenosis), hemodynamically unstable heart failure caused by acute myocardial infarction. Special instructions and precautions for use Use in patients with heart failure The drug should be used with caution in patients with heart failure. In a long-term placebo-controlled study in patients with severe heart failure (NYHA functional class III-IV) of non-ischemic etiology, the incidence of pulmonary edema was higher in the amlodipine-treated group compared to the placebo group. Calcium channel blockers, including amlodipine, should be used with caution in patients with congestive heart failure as they may increase the risk of future cardiovascular events and mortality. Use in patients with impaired liver function In patients with impaired liver function, the half-life of amlodipine is prolonged and the AUC values are higher. Recommendations for dosage in this category of patients have not been developed, therefore, it is necessary to start taking the drug with the lowest doses of the permissible range, being careful both at the very beginning of treatment and when increasing the dose of the drug. Patients with severe hepatic impairment require slow dose titration and close monitoring. Use in elderly patients In elderly and younger people, the time required to achieve the maximum concentration of amlodipine in blood plasma is almost the same. The drug is recommended to be used in normal doses. The same doses of amlodipine were well tolerated by both young and elderly patients. In the elderly, there was a tendency to reduce the clearance of amlodipine, which leads to an increase in AUC (area under the concentration-time curve) and half-life. As expected, in patients of various age groups suffering from congestive heart failure, there was an increase in AUC and half-life of the drug. Therefore, in the elderly, increasing the dose of the drug should be carried out with caution. Pregnancy and breastfeeding The safety of amlodipine during pregnancy and breastfeeding has not been established. In animal studies, reproductive toxicity has been reported at high doses. Thus, the use of amlodipine during pregnancy is recommended only in cases where there is no safer alternative, and the risk associated with the disease itself outweighs the possible harm to the mother and fetus. A decision should be made to discontinue nursing mothers taking the drug or stop breastfeeding, based on the importance of taking the drug to the mother or the benefits of breastfeeding. Side effects The following are the adverse reactions observed during treatment with amlodipine. The frequency of adverse reactions was determined as follows: very often (≥ 1/10), often (≥ 1/100 and < 1/10), infrequently (≥ 1/1000 and < 1/100), rarely (≥ 1/10 000, and < 1/1000), very rare (< 1/10,000). Blood and lymphatic system disorders: very rarely - leukopenia, thrombocytopenia. Immune system disorders: very rarely - allergic reactions. Metabolic and nutritional disorders: very rarely - hyperglycemia. Mental disorders: infrequently - insomnia, mood changes, depression; rarely - confusion. Nervous system disorders: often - drowsiness, dizziness, headache (especially at the beginning of treatment); infrequently - tremor, dysgeusia, fainting, hypoesthesia, paresthesia; very rarely - hypertension, peripheral neuropathy. On the part of the organ of vision: infrequently - visual disturbances, including diplopia. On the part of the organ of hearing and labyrinth disorders: infrequently - tinnitus. Heart disorders: often - palpitations; very rarely - myocardial infarction, arrhythmia (including bradycardia, ventricular tachycardia and atrial fibrillation). Vascular disorders: often - hot flashes; infrequently - arterial hypotension; very rarely - vasculitis. Disorders from the respiratory system, chest organs, mediastinum: infrequently - dyspnea, rhinitis; very rarely - cough. Gastrointestinal disorders: often - abdominal pain, nausea; infrequently - vomiting, dyspepsia, changes in bowel function (including diarrhea and constipation), dry mouth; very rarely - pancreatitis, gastritis, hypertrophic gingivitis. Liver and biliary tract disorders: very rarely - hepatitis, jaundice, increased activity of liver enzymes, mostly consistent with cholestasis. Skin and subcutaneous tissue disorders: infrequently - alopecia, purpura, discoloration of the skin, hyperhidrosis, itching, rash, exanthema; very rarely - angioedema, erythema multiforme, urticaria, exfoliative dermatitis, Steven-Johnson syndrome, Quincke's edema, photosensitization. Musculoskeletal and connective tissue disorders: often - swelling of the ankle joint; infrequently - arthralgia, myalgia, muscle spasms, back pain. On the part of the genital organs and the mammary gland: infrequently - impotence, gynecomastia. General disorders and disorders at the injection site: infrequently - chest pain, asthenia, pain, malaise Effect on the results of laboratory and instrumental studies: infrequently - weight gain, weight loss. There were isolated cases of development of extrapyramidal syndrome. Overdose Symptoms: marked decrease in blood pressure, tachycardia, excessive peripheral vasodilation (risk of severe and persistent arterial hypotension, including the development of shock and death). Treatment: In some cases, gastric lavage, administration of activated charcoal (especially in the first 2 hours after an overdose), maintenance of the function of the cardiovascular system, control of indicators of heart and lung function, elevation of the limbs, control of circulating blood volume and diuresis can be effective in some cases. To restore vascular tone - the use of vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the effects of blockade of calcium channels - intravenous administration of calcium gluconate. Since amlodipine is highly protein bound, hemodialysis is unlikely to be effective. Interaction with other drugs and other forms of interaction Amlodipine has been safely used in conjunction with thiazide diuretics, alpha-blockers, beta-blockers, angiotensin-converting enzyme inhibitors, long-acting nitrates, sublingual nitroglycerin, non-steroidal anti-inflammatory drugs, antibiotics and oral hypoglycemic drugs. The results of in vitro studies using human plasma indicate that amlodipine does not affect protein binding of the drugs tested (digoxin, phenytoin, warfarin and indomethacin). Simvastatin: Co-administration of multiple doses of amlodipine 10 mg with simvastatin 80 mg resulted in a 77% increase in simvastatin exposure compared to simvastatin alone. It is recommended to limit the dose of simvastatin in patients taking amlodipine to 20 mg per day. GRAPEFRUIT JUICE: Simultaneous single oral administration of 240 ml of grapefruit juice and 10 mg of amlodipine in 20 healthy volunteers did not significantly affect the pharmacokinetics of amlodipine. In this study, it was not possible to study the effect of the genetic polymorphism of CYP3A4 (the main enzyme responsible for the metabolism of amlodipine). Taking amlodipine with grapefruit or grapefruit juice is not recommended, since the bioavailability and, accordingly, the hypotensive effect of amlodipine may increase. CYP3A4 INHIBITORS: Co-administration of diltiazem 180 mg and amlodipine 5 mg in elderly patients (69-87 years) resulted in a 57% increase in systemic exposure to amlodipine. Simultaneous administration with erythromycin in healthy volunteers (aged 18 to 43 years) did not lead to a significant change in the systemic exposure of amlodipine (22% increase in AUC). Although the clinical significance of these data is unclear, pharmacokinetic changes can be clearly expressed in the elderly. Strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir) may increase amlodipine concentrations to a greater extent than diltiazem. Amlodipine should be used with caution in combination with CYP3A4 inhibitors. CYP3A4 stimulants: There are no data on the effect of CYP3A4 stimulants on amlodipine. Simultaneous use of CYP3A4 stimulants (eg, rifampicin, St. John's wort) may lead to a decrease in amlodipine plasma concentrations. Amlodipine should be used with caution in combination with CYP3A4 stimulants. In the studies below, there were no significant changes in the pharmacokinetics of both amlodipine and other drugs while taking it. Special studies: the effect of other drugs on amlodipine CIMETIDINE: the simultaneous use of amlodipine and cimetidine was not accompanied by a change in the pharmacokinetics of amlodipine. ALUMINUM / MAGNESIUM (antacid): A single dose of aluminum / magnesium containing antacids with amlodipine did not significantly affect the pharmacokinetics of amlodipine. SILDENAFIL: A single dose of sildenafil at a dose of 100 mg in patients with essential hypertension had no effect on the pharmacokinetic parameters of amlodipine. With the combined use of amlodipine and sildenafil, both drugs had an independent hypotensive effect. DANTROLENE (infusion): when administered intravenously with verapamil and dantrolene, animals developed ventricular fibrillation and fatal cardiovascular failure, accompanied by hyperkalemia. Due to the risk of hyperkalemia, it is recommended that concomitant administration of calcium channel blockers such as amlodipine be avoided in patients at risk of developing malignant hyperthermia or for the treatment of malignant hyperthermia. Special Studies: Effects of Amlodipine on Other Medicinal Products ATORVASTATIN: Repeated use of amlodipine 10 mg and atorvastatin 80 mg was not associated with significant changes in the steady-state pharmacokinetics of atorvastatin. DIGOXIN: Serum levels and renal clearance of digoxin did not change when amlodipine was co-administered with digoxin in healthy volunteers. ETHANOL (alcohol): with a single and repeated use at a dose of 10 mg, amlodipine did not significantly affect the pharmacokinetics of ethanol. WARFARIN: Amlodipine did not affect changes in prothrombin time induced by warfarin. CIKLOSPORIN: No drug interaction studies have been conducted with cyclosporine and amlodipine in healthy volunteers or other populations other than renal transplant patients. In various studies conducted in patients after kidney transplantation, it was found that the combined use of amlodipine and cyclosporine has an effect on the minimum concentration of cyclosporine, ranging from 0 to an average increase of 40%. In kidney transplant patients taking amlodipine, monitoring of ciclosporin concentrations should be considered. The hypotensive effect of amlodipine enhances the hypotensive effect of other drugs that lower blood pressure. Effect on laboratory test results: Not known. Influence on the ability to drive a car and mechanisms There were no reports of the effect of amlodipine on driving or working with mechanisms. However, in some patients, drowsiness and dizziness may occur mainly at the beginning of treatment. If they occur, the patient should refrain from driving and working with mechanisms Storage conditions Store at a temperature not exceeding 25 ° C. Keep out of the reach of children. Shelf life 3 years. Do not use after the expiry date stated on the package. Conditions for dispensing from pharmacies By prescription. Buy Kalchek tablets 10mg No. 10x3 Price for Kalchek tablets 10mg No. 10x3