Amlodipine 10mg tabs 50 pcs Medisorb

Description

Composition
Active substance:
1 tablet contains: amlodipine besylate (calculated as amlodipine) 14 mg (10 mg) ;.
Excipients:
Lactose monohydrate (milk sugar) 128 mg; povidone (polyvinylpyrrolidone) 6 mg; calcium carbonate, 40 mg; Potato starch 10 mg; Calcium stearate 2 mg.
Description:
Tablets white or white color with kremovatam ploskotsilindricheskoy form chamfered.
Product form:
Tablets 10 mg. 10 tablets in blisters. 20, 30, 50 or 100 tablets per polymeric jars. Each bank or 1, 2, 3, 5, 10 contour cell packages together with instructions for use placed in a pile of cardboard.
Contraindications
-Increased sensitivity amlodipine and other dihydropyridine derivatives, as well as auxiliary substances forming part of the formulation; – severe hypotension (systolic blood pressure less than 90 mmHg…); – severe aortic, mitral stenosis; – hypertrophic obstructive cardiomyopathy with obstruction of the outflow tract of the left ventricle; – hemodynamically unstable heart failure after myocardial infarction; – Shock, including cardiogenic shock; – lactose intolerance, lactase deficiency and glucose-galactose malabsorption; – up to age 18 years.
Precautions prescribed to patients with liver failure, CHF nonischemic etiology class III-IV, unstable angina, acute myocardial infarction (and for 1 month. Afterwards), while receiving isoenzyme inhibitors and inducers of CYP3A4. As for the appointment of other BCCI should be careful while taking amlodipine in patients with sick sinus syndrome, hypotension.
Dosage
10 mg
Indications
Arterial hypertension (in both monotherapy and in combination with other antihypertensive agents). stable angina pectoris and vasospastic angina (Prinzmetal’s angina) (both in monotherapy and in combination with other antianginal drugs).
Interaction with other drugs
It can be expected that inhibitors of microsomal oxidation will increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes – reduce.
Cimetidine: the simultaneous use of amlodipine with cimetidine pharmacokinetics of amlodipine is not changed.
Grapefruit juice: simultaneous single dose of 240 ml grapefruit juice, and 10 mg amlodipine inwardly not accompanied by a significant change in the pharmacokinetics of amlodipine. Unlike other BCCI amlodipine clinically significant interaction (III BCCI generation) was not detected in the combined use with nonsteroidal anti-inflammatory drugs (NSAIDs), including: with indomethacin.
Erythromycin: a joint application increases the maximum concentration (Cmax) of amlodipine in younger patients by 22%, and the elderly – 50%. May increase antianginal and hypotensive action BCCI when combined with thiazide and “loop” diuretics, verapamil, ACE inhibitors, beta-blockers and nitrates, as well as strengthening their hypotensive effect when combined with alpha 1-blockers, neuroleptics.
With simultaneous use of amlodipine and simvastatin marked increase in AUC and Cmax of simvastatin in plasma of 1.3 and 1.4 times, respectively without changing the lipid-lowering effect of simvastatin. With simultaneous use of amlodipine and simvastatin 80 mg increases the risk of myopathy.
Isoflurane: can lead to a marked decrease in blood pressure when used in patients undergoing treatment BCCI, particularly dihydropyridine derivatives. Although the study of amlodipine negative inotropic action is usually not observed, nevertheless, some BCCI may increase the severity of the negative inotropic effects of antiarrhythmic agents causing the lengthening of the interval QT (e.g. amiodarone and quinidine).
Antiviral agents (ritonavir) increase the plasma concentrations of BCCI, including amlodipine.
Calcium: can reduce the effect of BCCI.
In a joint application with lithium BCCI drugs may enhance their neurotoxicity symptoms (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus).
Amlodipine in vitro did not affect the degree of binding to plasma proteins blood digoxin, phenytoin, warfarin and indomethacin.
Aluminum / magnesium-containing antacids: their single dose has no significant effect on the pharmacokinetics of amlodipine.
Sildenafil: single dose of 100 mg sildenafil in patients with essential hypertension have not effect on the pharmacokinetic parameters of amlodipine.
Atorvastatin: re-use of amlodipine 10 mg and atorvastatin 80 mg is not accompanied by a significant change in the pharmacokinetics of atorvastatin. Digoxin: while amlodipine with digoxin in healthy subjects, serum concentrations and renal clearance of digoxin are not changed.
Ethanol (alcoholic beverages): with a single and repeated administration in a dose of 10 mg amlodipine had no significant effect on the pharmacokinetics of ethanol.
Warfarin: amlodipine does not affect changes in prothrombin time induced by warfarin. Cyclosporine: amlodipine does not cause significant changes in the pharmacokinetics of cyclosporine.
Overdose
Symptoms: marked reduction of blood pressure with possible development of reflex tachycardia and excessive peripheral vasodilation (there is a probability of occurrence of severe and persistent hypotension, including the development of shock and death).
Treatment: The purpose of activated carbon (especially in the first 2 hours after the overdose), gastric lavage (in some cases), giving elevated position lower extremities low headboard active subtree-zhanie function of the cardiovascular system, monitoring of parameters of the heart and lungs, control for the circulating blood volume and diuresis.
To restore vascular tone and blood pressure, if no contraindications, requires the use of vasoconstrictors. To eliminate the use of calcium channel blockade intravenous administration of calcium gluconate. Since amlodipine is largely associated with serum proteins – hemodialysis is not effective.
pharmachologic effect
Pharmacological group:
BCCI (blocker “slow” calcium channel).
Pharmacodynamics:
Amlodipine – dihydropyridine derivative. Communicating with the dihydropyridine receptor blocking “slow” calcium channels, transmembrane calcium inhibits smooth transition into the heart and vascular cells (mainly – in the vascular smooth muscle cells than cardiac myocytes). It has hypotensive and antianginal effects. The mechanism of the antihypertensive action of amlodipine is due to a direct relaxing effect on vascular smooth muscle cells.
Amlodipine reduces myocardial ischemia following two ways: 1. Increase peripheral arterioles and thus, reduces the total peripheral resistance (afterload), while the heart rate remains virtually unchanged, which leads to lower energy consumption and myocardial oxygen demand. 2. Extends the coronary and peripheral arteries and arterioles, both in normal and in ischemic areas of the myocardium, which increases the supply of oxygen to the myocardium in patients with vasospastic angina (Prinzmetal’s angina), and prevents the development of coronary spasm caused by smoking. Patients with hypertension single daily dose provides a reduction in blood pressure (BP) for 24 hours (as in the “lying” and “standing”). Due to the slow onset of action am lodipin does not cause a sharp decrease in blood pressure. In patients with angina single daily dose increases the run time of exercise, retards the development of the next attack of angina and ST segment depression (1 mm) due to physical exertion, reduces the frequency of angina attacks and the consumption of nitroglycerin and other nitrates.
Use in patients with coronary heart disease (CHD)
In patients with cardiovascular disease (including coronary atherosclerosis with a lesion of the vessel and to the stenosis 3 or more arteries and carotid atherosclerosis), myocardial infarction, percutaneous transluminal angioplasty of coronary arteries (TLO) or angina, the use of the drug prevents the development of intima-media thickening of carotid arteries significantly reduces mortality from cardiovascular causes, myocardial infarction, stroke, TLO, aorto-coronary bypass, leads to a decrease in the number of hospitals tions for unstable angina and progression of chronic heart failure (CHF), reduces the frequency of interventions aimed at restoring coronary blood flow.
Use in patients with heart failure
The drug does not increase the risk of death or development of complications and death in patients with chronic heart failure III-IV functional class (classification NYHA) during therapy with digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors. In patients with chronic heart failure III-IV functional class on classification NYHA nonischemic etiology when using the drug there is a possibility of pulmonary edema. The drug does not appear to have any adverse effect on metabolism and lipid concentration in blood plasma.
Pharmacokinetics:
Suction. After ingestion of therapeutic doses of amlodipine is well absorbed, reaching maximum plasma concentrations in 6-12 hours after administration. Absolute bioavailability is 64-80%. The volume of distribution is approximately 21 l / kg. Communication with the plasma proteins is approximately 97.5%. Food intake does not affect absorption of amlodipine, amlodipine penetrates the blood-brain barrier. Biotransformation / elimination. The half-life (T1 / 2) from the blood plasma is about 35-50 hours, which corresponds to the destination of the drug once a day. Total clearance – 0.43 L / h / kg. A stable equilibrium plasma concentration achieved after 7-8 days of continuous use of amlodipine, it is metabolized in the liver to inactive metabolites; 10% of the parent drug and 60% of the metabolites eliminated via the kidneys. Excretion in breast milk is unknown. During hemodialysis is not removed.
Use in patients with hepatic insufficiency and chronic heart failure.
Patients with liver failure and severe CHF insufficiency T1 / 2 is increased to 56-60 hours.
Use in patients with renal insufficiency.
T1 / 2 from blood plasma in patients with renal failure is increased to 60 hours. Changing amlodipine plasma concentration does not correlate with the degree of renal impairment.
Use in elderly patients.
Older time required for maximum concentration of amlodipine in plasma, and its value, practically do not differ from those in younger patients. Elderly patients suffering from heart failure, there was a trend to decrease amlodipine clearance, which leads to an increase in the area under the concentration-time curve (AUC) and the T1 / 2 to 65 hours.
Pregnancy and breast-feeding
Safety of the drug during pregnancy and breastfeeding has not been established, therefore use during pregnancy is possible only when the benefits to the mother outweigh the risks to the fetus and newborn. For the period of breastfeeding are advised to stop taking the drug either, or breast-feeding (data for amlodipine excretion in breast milk are not available). In applying the BCCI some patients experienced biochemical changes in the head of spermatozoa. In a preclinical study in rats were found negative effects on fertility in male rats.
Conditions of supply of pharmacies
Prescription.
side effects
The frequency of side effects was evaluated as follows: very often (> 1/10); common (> 1/100,
special instructions
When treating arterial hypertension amlodipine may be used in combination with a thiazide diuretic, alpha- and beta-blockers, ACE inhibitors, long-acting nitrates, nitroglycerin sublingual, NSAIDs, antibiotics and hypoglycemic agents for oral administration. For the treatment of angina pectoris, amlodipine may be administered as a monotherapy or in combination with other antianginal drugs, including patients refractory to treatment with nitrates and / or beta-blockers in adequate doses. The use of amlodipine is not recommended in patients with unstable angina except Prinzmetal’s angina. In patients with chronic heart failure III-IV NYHA functional class classification, while taking amlodipine was an increase in the incidence of pulmonary edema. Amlodipine does not exert any adverse effect on metabolism and plasma lipids and can be used in the treatment of patients with bronchial asthma, diabetes and gout. Amlodipine may be used in those cases where the patient is prone to vasospasm / vasoconstriction.
Patients with low weight, small stature patients and patients with severe hepatic dysfunction may require a smaller dosage.
During treatment, the need to control the body weight and observation of the dentist and oral hygiene compliance (to prevent pain, bleeding and gingival hyperplasia).
The efficacy and safety of amlodipine use in hypertensive crisis has not been established. Despite the lack of BCCI syndrome “cancel”, discontinuation of treatment with amlodipine is desirable to conduct, gradually reducing the dose of the drug.
Effects on ability to drive and operate machinery
Although patients receiving amlodipine any negative impact on the ability to drive vehicles and work with non-observed mechanisms, however, due to the possible excessive reduction in blood pressure, development of dizziness, drowsiness and other side effects should be careful in these situations, especially at the beginning of treatment and if you change the dosing regimen.
Storage conditions
In a dry, dark place at a temperature not higher than 25 C. Keep out of reach of children.
Dosing and Administration
Inside, once a day, washing down the necessary volume of water (100 mL).
When hypertension and angina the usual initial dose is 5 mg, depending on the individual response of the patient it can be increased to the maximum daily dose – 10 mg.
Use in elderly patients.
Recommended for use in normal doses, changes in dose are required.
Use in patients with impaired hepatic function.
Despite the fact that the T1 / 2 of the drug, as well as all the BCCI, is increased in patients with this pathology, any change of dosage of the drug in patients with impaired liver function is usually not necessary (see. Section “Special Instructions”).
The use in renal failure.
It is recommended to use conventional doses but must take into account the possible slight increase in T1 / 2.
Changes in drug dosing regimen while the use of thiazide diuretics, beta-blockers or ACE inhibitors is not required.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist