Amlodipine, tablets 5 mg 20 pcs

Dihydropyridine derivative, has antianginal and hypotensive effect.

Binding to segment S6 of III and IV domains of L-type calcium channel alpha 1-subunit, it blocks calcium channels, reduces transmembrane transition of calcium ions into the cell (more in vascular smooth muscle cells than in cardiomyocytes).

Antianginal action is due to the expansion of peripheral and coronary arteries and arterioles.

With angina reduces the severity of myocardial ischemia, expanding the peripheral arterioles, reduces total peripheral vascular resistance (reduces the post-load on the heart) without causing

reflexive increase in heart rate, which helps to reduce energy consumption; reduces myocardial oxygen demand.

By dilating coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases the flow of oxygen to the myocardium in vasospastic angina; prevents the development of coronary spasm (including that caused by smoking).

In patients with angina a single daily dose of amlodipine increases time to the onset of the first ischemic episode during exercise, prevents the development of an angina attack and

“ischemic” ST-segment depression (by 1 mm) during exercise, reduces the frequency of angina attacks and consumption of nitroglycerin and other nitrates.

Hypotensive effect is due to direct vasodilating effect on vascular smooth muscle. It has a long-term dose-dependent hypotensive effect.

In arterial hypertension a single daily dose of amlodipine provides clinically significant reduction of arterial pressure (BP) for 24 hours (in “lying” and “standing” positions).

It does not cause sharp decrease of BP and left ventricular ejection fraction. Does not affect myocardial contractility and conduction. It reduces the degree of myocardial hypertrophy of the left ventricle.

In patients with coronary heart disease (CHD) (including coronary atherosclerosis with lesion of one vessel and up to stenosis of 3 or more arteries and atherosclerosis of carotid arteries), who had myocardial infarction,

percutaneous transluminal angioplasty of the coronary arteries (TLAP) or suffering from angina pectoris, use of amlodipine prevents the development of carotid intima-media thickening, reduces mortality Pharmacokinetics

Absorption. After oral administration, amlodipine is well absorbed in the gastrointestinal tract. Food intake has no effect on absorption of amlodipine.

Maximum concentration in blood serum is reached 6-12 hours after intake. Bioavailability is 60-65%. Average volume of distribution is 21 l/kg body weight. Binding with plasma proteins is 90-97%. The drug penetrates through the blood-brain barrier.

Metabolism and excretion. Amlodipine undergoes slow but significant metabolism (90%) in liver with formation of inactive metabolites, has low hepatic clearance (effect of “primary passage” through liver).

The half-life is on average 35 hours (varies from 35 to 50 hours), which corresponds to the prescription of the drug once a day. Total clearance is 500 ml/min.

Stable equilibrium concentration in plasma is reached after 7-8 days of therapy. It is excreted by the kidneys (10% unchanged, 60% as metabolites), in the bile and intestines – 20-25% as metabolites, and with the breast milk.

In hemodialysis it is not eliminated.

In elderly patients, patients with hepatic insufficiency and severe CHF the half-life is increased to 60-65 hours; in renal function disorders it does not change.

Indications

Active ingredient

Composition

1 tablet contains:

The active ingredient:

Amlodipine – 5,000 mg or 10,000 mg (in the form of amlodipine besylate – 6.934 mg or 13.869 mg);

Auxiliary substances:

Prosolv [microcrystalline cellulose 98%, colloidal silicon dioxide 2%] – 111.066 mg or 222.131 mg,

Pregelatinized starch – 30,000 mg or 60,000 mg

Magnesium stearate – 2,000 mg or 4,000 mg.

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How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose

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