Amlodipine Alkaloid, tablets 5 mg 30 pcs

Pharmacotherapeutic group:

Slow calcium channel blocker
ATC:
C.08.C.A.01 Amlodipine

Pharmacodynamics:

A dihydropyridine derivative. It has antihypertensive, antianginal action. It blocks entering of calcium ions through cell membranes into smooth muscle cells of myocardium and vessels.

Antianginal action is caused by dilation of coronary and peripheral arteries and arterioles: in angina pectoris it reduces intensity of myocardial ischemia; dilation of peripheral arterioles reduces myocardial hypertension, reduces post-load of oxygen, reduces myocardial oxygen demand. By dilating the main coronary arteries and arterioles in the unchanged and ischemic areas of the myocardium increases the flow of oxygen to the myocardium (especially in vasospastic angina); prevents the development of coronary artery constriction (including that caused by smoking). In patients with angina a single daily dose increases exercise tolerance, slows down the development of angina and “coronary depression” segment S-T, reduces the frequency of angina attacks and nitroglycerin consumption.

It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to direct vasodilating effect on vascular smooth muscle. In arterial hypertension a single dose provides clinically significant BP reduction for 24 hours (in “lying” and “standing” positions). It does not cause a sharp decrease in BP, decreases exercise tolerance and LV ejection fraction. It reduces the degree of LV myocardial hypertrophy, has anti-atherosclerotic and cardioprotective effect in CHD. It does not increase the risk of death in patients suffering from CHF (III-IV class according to NYHA), against the background of digoxin, diuretics and ACE inhibitors therapy.

It has no effect on myocardial contractility and conduction, does not cause reflex increase of HR, inhibits platelet aggregation, increases glomerular filtration rate, has weak natriuretic effect. In diabetic nephropathy it does not increase the severity of microalbuminuria. It does not have adverse effects on metabolism and plasma lipids and is suitable for patients with concomitant bronchial asthma and diabetes.

Pharmacokinetics:

Absorption – slow, does not depend on food intake, is about 90%, bioavailability – 60-65%. The tCmax when taken orally is 6-12 hours. Css is formed in 7-8 days after continuous use. The volume of distribution is 21 l/kg. Binding with plasma proteins is 90-97%. It penetrates through the BBB.
Intensively (90%) metabolized in the liver to form inactive metabolites, has “first pass” effect through the liver. T1/2 averaged 35 hours. Total clearance is 500 ml/min.

T1/2 in patients with arterial hypertension-48 hours in elderly patients is increased up to 65 hours, in hepatic insufficiency – up to 60 hours, similar parameters of T1/2 increase are observed in severe CHF, in renal impairment – unchanged. In hemodialysis it is not eliminated.
Excreted by the kidneys-60% as metabolites, 10% unchanged, with the bile and intestine-20-25% as metabolites, as well as with breast milk.

Indications

Active ingredient

Composition

One tablet contains amlodipine (in the form of amlodipine besylate) 5,000 mg.

Auxiliary substances:

Lactose monohydrate,

Magnesium stearate,

Cellulosamicrocrystalline.

How to take, the dosage

Interaction

Special Instructions

Contraindications

High sensitivity to the drug and other dihydropyridine derivatives, severe arterial hypotension, collapse, unstable angina pectoris (except for Prinzmetal angina), pregnancy, lactation.

Arterial hypotension, aortic stenosis, chronic heart failure, liver failure, acute myocardial infarction (and within 1 month after), hypertrophic obstructive cardiomyopathy (HOCMP), sinus node weakness syndrome (SBMS) and mitral stenosis, age

Side effects

Overdose

Similarities