Normodipine, tablets 5 mg 30 pcs

Normodipine has antianginal, hypotensive effect.

A slow calcium channel blocker, a dihydropyridine derivative, has antianginal and hypotensive effects. Binding to segments S6 of III and IV domains of alpha1-subunit of L-type calcium channel, it blocks calcium channels, decreases transmembrane transition of calcium ions into cell (more in vascular smooth muscle cells than in cardiomyocytes).

The antianginal action is caused by the dilation of coronary and peripheral arteries and arterioles: in angina pectoris it reduces myocardial ischemia; by dilation of peripheral arterioles it reduces myocardial perfusion, decreases cardiac preload, reduces myocardial oxygen demand.

Dilates coronary arteries and arterioles in unchanged and ischemic areas of the myocardium, increases oxygen supply to the myocardium (especially in vasospastic angina); prevents development of coronary artery spasm (including that caused by smoking). In patients with stable angina a single daily dose increases exercise tolerance, slows down the development of angina and “coronary” ST-segment depression, reduces the frequency of angina attacks and the use of nitroglycerin and other nitrates.

It has a long-term dose-dependent hypotensive effect. The hypotensive effect is due to a direct vasodilatory effect on the vascular smooth muscles. In arterial hypertension a single dose provides clinically significant reduction of BP during 24 hours (in “lying” and “standing” position of the patient).

Orthostatic hypotension when prescribing amlodipine is quite rare. It does not cause a decrease in exercise tolerance, left ventricular ejection fraction. It reduces the degree of left ventricular myocardial hypertrophy.

It does not influence myocardial contractility and conduction, does not cause reflex elevation of HR, inhibits platelet aggregation, increases glomerular filtration rate, has a weak natriuretic effect. It does not increase the severity of microalbuminuria in diabetic nephropathy.

It has no adverse effect on metabolism and concentration of plasma lipids and can be used for treatment of patients with bronchial asthma, diabetes mellitus and gout.

The time of onset of effect is 2-4 hours, the duration of effect is 24 hours.

Pharmacokinetics

Absorption

When taken orally it is slowly and almost completely absorbed from the gastrointestinal tract. Food intake has no effect on absorption. Cmax in plasma is reached after 6-9 h in both elderly and young patients. Average absolute bioavailability is 64%.

Distribution

The Css of amlodipine in plasma is reached after continuous use for 7-8 days.

The Vd is approximately 21 L/kg, indicating prevailing tissue distribution. It penetrates through the HEB and into the breast milk.

The binding to plasma proteins is 97%.

Metabolism

About 90% of amlodipine is biotransformed in the liver to form inactive metabolites.

Amlodipine is excreted from the body with urine (10% of dose – unchanged and 60% – as inactive metabolites) and in the feces (20-25% as metabolites). Excretion is biphasic, T1/2 averages 31-48 hours.

The total clearance of amlodiline is 7 ml/min/kg. Amlodipine is not eliminated by hemodialysis.

Pharmacokinetics in special clinical cases

The excretion of amlodipine is slower (T1/2 – 65 h) in elderly patients (older than 65 years) compared to younger patients, but these differences are not clinically relevant.

The prolonged T1/2 in patients with hepatic impairment suggests that long-term administration will result in higher cumulation of the drug in the body (T1/2 is up to 60 h).

The presence of renal impairment in a patient has no significant effect on the pharmacokinetics of amlodipine.

Indications

Active ingredient

Composition

Active ingredient:

amlodipine;

Associates:

magnesium stearate;

sodium carboxymethyl starch;

calcium hydrophosphate anhydrous;

MCC

How to take, the dosage

In the oral route, the initial dose for treatment of arterial hypertension and angina pectoris is 5 mg/day. The maximum daily dose is 10 mg once. For arterial hypertension, the maintenance dose may be 5 mg/day (1 tablet of 5 mg).

In elderly patients, the T1/2 of amlodipine may increase and creatinine clearance may decrease. No dose changes are required, but closer monitoring of patients is necessary.

Dose changes are not required when concomitantly prescribed with thiazide diuretics, β-adrenoblockers and ACE inhibitors.

Dose changes are not required in patients with renal impairment.

Interaction

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use

Similarities