Stamlo tablets 10mg №10×2

Name:
10 mg tablet
Description:
5 mg tablets White or almost white flat round tablets with bevelled edges, inscription “5” on one side and with a separating strip on the other. Tablets 10 mg: White or almost white flat round tablets with bevelled edges, inscribed “10” on one side and with a separating strip on the other. The main active ingredient Amlodipine Release form 10 tablets in an aluminum foil strip, 2 or 3 strips are packed in a cardboard box with instructions for use. Dosage 10 mg Pharmacological action Amlodipine is a long-acting calcium channel blocker from the group of dihydropyridine derivatives. Amlodipine selectively inhibits the current of calcium ions across the membrane into the smooth muscle cells of the heart and blood vessels, with a predominant effect on the muscle fibers of the vessels. The antihypertensive effect is due to a direct effect on the smooth muscle fibers of peripheral arterioles, which leads to a decrease in peripheral vascular resistance and a decrease in blood pressure. Exercising angina: in this group of patients, amlodipine causes a decrease in total peripheral vascular resistance (afterload), which leads to a decrease in myocardial oxygen demand at any level of exercise. Vasospastic angina: amlodipine prevents vasospasm and restores blood flow in the coronary arteries and arterioles when exposed to calcium, epinephrine potassium, serotonin, and thromboxane AI analog in experimental animals and in human coronary vessels in vitro. Elimination of coronary spasm determines the effectiveness of amlodipine in vasospastic (variant and Prinzmetal’s angina) angina pectoris. Pharmacokinetics After taking a therapeutic dose of amlodipine, the maximum plasma concentration of the drug is reached within 6-12 hours. Absolute bioavailability is 60 – 90%. Plasma protein binding is high – 90%. The drug is extensively metabolized by the liver, 10% is excreted unchanged and 60% in the form of inactive metabolites in the urine. The equilibrium concentration of the drug in plasma is established on the 7th-8th day of daily continuous intake. The half-life is 30 – 50 hours. In patients with moderate and severe heart failure, an increase in AUC is noted. . Pregnancy and lactation. Severe arterial hypotension. Aortic stenosis Chronic heart failure of non-ischemic etiology (NYHA class III-IV) Liver failure Acute myocardial infarction (within 1 month after) Hypertrophic cardiomyopathy Sick sinus syndrome Precautions Progressive angina and / or myocardial infarction: Rare in patients with predominantly severe obstruction coronary arteries, there was an increase in the duration and / or severity of angina attacks or the development of acute myocardial infarction at the beginning of therapy with calcium channel blockers or during a dose increase. Chronic heart failure: Calcium channel blockers should be used with caution in patients with heart failure. However, the likelihood of side effects being correlated with survival or mortality has not been reported with amlodipine in patients with heart failure receiving continuous maintenance doses of ACE inhibitors, digoxin, and diuretics. Use in patients with hepatic impairment: Amlodipine is metabolized primarily by the liver. In patients with insufficient liver function, the plasma half-life of amlodipine increases to 56 hours, so therapy should be started with a minimum dose of 2.5 mg 1 time per day, with caution when prescribing the drug to patients with severe impairment of function. Use in patients with renal insufficiency: The pharmacokinetics of amlodipine does not significantly depend on the degree of renal insufficiency, therefore, there is no need for individual dose selection in patients with renal insufficiency. Use in Elderly Patients: Elderly patients should be dosed with caution. Usually, therapy begins with a minimum dose due to the higher incidence of complications from the liver, kidneys, cardiovascular system, the presence of concomitant pathology and the use of other drugs in this group of patients. In elderly patients, the clearance of amlodipine is reduced, this leads to an AUC of up to 40-60% approximately, so a dose of 2.5 mg is recommended. Use during pregnancy and lactation: The safety and efficacy of amlodipine during pregnancy and lactation have not been studied, so the use is not indicated. Use in the treatment of hypertensive crisis: The safety and efficacy of amlodipine in the treatment of hypertensive crisis has not yet been confirmed. With angina pectoris, it is recommended to avoid abrupt discontinuation of the drug due to the risk of worsening the course of the disease. During treatment, it is necessary to control body weight and be observed by a dentist (to prevent soreness, bleeding and gum hyperplasia). Influence on the ability to drive a car and use machinery: although the experience of clinical use of the drug has shown that amlodipine does not affect the speed of reaction and the ability to concentrate, it is recommended to be careful when driving and working with mechanisms. Interactions with other drugs Amlodipine has been safely used 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 agents. 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 inhibitors of CYP3A4 (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 administration of CYP3A4 stimulants (for example, rifampicin, St. John’s wort) can lead to a decrease in plasma concentrations of amlodipine. 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: unknown. Contraindications Identified allergy to amlodipine. Pregnancy and lactation. Severe arterial hypotension. Aortic stenosis Chronic heart failure of non-ischemic etiology (III-IV class according to NYHA) Liver failure Acute myocardial infarction (within 1 month after) Hypertrophic cardiomyopathy Sick sinus node syndrome Composition Active substance: aml o dipine besylate, equivalent to 5 or 10 mg of amlo dipine. Auxiliary ingredients: microcrystalline cellulose (PH 102), anhydrous calcium hydrogen phosphate, sodium starch glycolate (type A), magnesium stearate, anhydrous colloidal silicon dioxide. Overdose Available data suggest that significant overdose may lead to excessive peripheral vasodilation and possibly reflex tachycardia. Cases of severe and persistent arterial hypotension, including those with the development of shock and death, have been described. The use of activated charcoal in healthy volunteers immediately or within 2 hours after taking amlodipine 10 mg led to a significant delay in the absorption of the drug. In some cases, gastric lavage may be effective. Clinically significant arterial hypotension caused by an overdose of amlodipine requires active measures aimed at maintaining the function of the cardiovascular system, including monitoring of indicators of the heart and lungs, elevated position of the limbs, and control of circulating blood volume and diuresis. To restore vascular tone and blood pressure, it may be useful to use a vasoconstrictor drug, if there are no contraindications to its appointment. To reverse the effects of calcium channel blockade, intravenous calcium gluconate may be helpful. Since amlodipine is highly protein bound, hemodialysis is unlikely to be effective. Side effects The most common adverse reactions reported with amlodipine were drowsiness, dizziness, headache, palpitations, hot flashes, abdominal pain, nausea, ankle swelling, edema, and fatigue. The table below shows the adverse reactions observed during treatment with amlodipine. The frequency of development of adverse reactions was determined as follows: very often (> 1/10); often (>1/100 and <1/10); infrequently (> 1/1000 and <1/100); rarely (>1/10000 and <1/1000); very rarely (<1/10000). Within each frequency group, adverse reactions are listed in order of decreasing severity. Storage conditionsKeep in a dry, dark place at temperatures up to 25°C. 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