Amlessa (perindopril tert-butylamine) tablets 4 mg/10 mg. №30

active substances: perindopril tert-butylamine and amlodipine;

1 tablet contains 4 mg of perindopril tert-butylamine (corresponding to 3.34 mg of perindopril) and 10 mg of amlodipine (corresponding to 13.870 mg of amlodipine besylate);

excipients: microcrystalline cellulose; pregelatinized starch; sodium starch glycolate; calcium chloride, hexahydrate; sodium bicarbonate; colloidal anhydrous silicon dioxide; magnesium stearate.

Tablets.

The main physical and chemical properties:

4 mg/10 mg: white or almost white, capsule-shaped, biconvex, scored on one side of the tablet.

Combined preparations of angiotensin-converting enzyme inhibitors. ACE inhibitors in combination with calcium antagonists. ATX code C09B B04.

The rate and degree of absorption of perindopril and amlodipine as monopreparations in the composition of the drug Amlessa do not differ significantly.

Perindopril

Perindopril is an angiotensin-converting enzyme (ACE) inhibitor, which converts ACE. The converting enzyme, or kinase, is an exopeptidase that allows the conversion of angiotensin I to angiotensin II and also causes the breakdown of the vasodilator agent bradykinin to form an inactive heptapeptide. Inhibition of ACE activity leads to a decrease in the concentration of angiotensin II in the blood plasma, which is accompanied by an increase in the activity of renin in the plasma (by inhibiting the negative assessment of renin release) and a decrease in the secretion of aldosterone. Since ACE blocks bradykinin, inhibiting the activity of this enzyme leads to an increase in the activity of the circulating and local kallikrein-kinin system and, thereby, to the activation of the prostaglandin system.

Perindopril in the body turns into an active metabolite – perindoprilat. Other metabolites do not show inhibition of ACE activity in vitro.

Amlodipine

Amlodipine is an antagonist of calcium ions, which blocks the influx of calcium ions through the membranes to the smooth muscle cells of the myocardium and blood vessels. The mechanism of the hypotensive effect of amlodipine is caused by a direct effect on vascular smooth muscles. The exact mechanism of action of amlodipine in angina has not been established, but it is known that amlodipine reduces myocardial ischemia in two ways.

Amlodipine dilates peripheral arterioles and thus reduces the total peripheral resistance (afterload) against which the heart works. Reducing the load on the heart leads to a decrease in energy consumption and myocardial oxygen demand.

The mechanism of action of amlodipine may also involve dilation of the major coronary arteries and coronary arterioles. This expansion increases the oxygen supply to the myocardium in patients with Prinzmetal’s angina. In patients with arterial hypertension, dosing once a day provides a clinically significant reduction in blood pressure (both in standing and supine positions) throughout the entire 24-hour interval.

In patients with angina pectoris, taking amlodipine 1 time per day prolongs the total active time, the time to the onset of angina pectoris, and the time to depression of the 1 mm ST segment. Amlodipine reduces the frequency of angina pectoris and reduces the need to take nitroglycerin tablets.

Arterial hypertension and/or coronary heart disease (if treatment with perindopril and amlodipine is necessary).

• hypersensitivity to perindopril (or to any other ACE inhibitors), to amlodipine (or to other dihydropyridines) or to any auxiliary substance of the drug;
• angioedema in the anamnesis after the use of any ACE inhibitors;
• idiopathic or hereditary angioedema;
• severe arterial hypotension;
• shock, including cardiogenic shock;
• obstruction of the outflow tract of the left ventricle (for example, severe stenosis of the aorta);
• unstable angina pectoris;
• heart failure after an acute myocardial infarction (within the first 28 days);
• pregnant women or women who plan to become pregnant;
• simultaneous use with drugs containing the active ingredient aliskiren, in patients with diabetes or in patients with renal failure (glomerular filtration rate < 60 ml/min/1.73 m2)