Perindopril

General characteristics. Structure:

Active ingredient: 2 mg, 4 mg or 8 mg of a perindopril.

Pharmacological properties:

Pharmacodynamics. APF inhibitor. Is pro-medicine of which in an organism the active metabolite периндоприлат is formed. Believe that the mechanism of anti-hypertensive action is connected with competitive inhibition of activity of APF which leads to reduction in the rate of transformation of angiotensin I into the angiotensin II which is powerful vasoconstrictive substance. Reduction of concentration of angiotensin II is resulted by secondary increase in activity of a renin of plasma due to elimination of negative feedback at release of a renin and direct decrease in secretion of Aldosteronum. Thanks to vasodilating action, reduces OPSS (afterload), jamming pressure in pulmonary capillaries (preloading) and resistance in pulmonary vessels; increases the minute volume of heart and tolerance to loading.

The hypotensive effect develops within the first hour after reception of a perindopril, reaches a maximum by the 4-8th o'clock and proceeds during 24 h.

Pharmacokinetics. After intake perindoprit quickly it is absorbed from a GIT. Cmax is reached in 1 h. Bioavailability makes 65-70%.

In the course of metabolism perindoprit it biotransformirutsya with formation of an active metabolite - a perindoprilata (about 20%) and 5 inactive connections. Cmax of a perindoprilat in plasma is reached between 3 and 5 h after reception. Linkng of a perindoprilat with proteins of a blood plasma insignificant (less than 30%) also depends on concentration of active agent. Vd of a free perindoprilat is close to 0.2 l/kg.

Does not kumulirut. Repeated reception does not lead to cumulation and T1/2 corresponds to the period of its activity.

At inclusion in food time metabolism of a perindopril is slowed down.

T1/2 of a perindopril makes 1 h Perindoprilat is brought from an organism by kidneys; T1/2 of its free fraction makes 3-5 h.

At elderly patients, and also at renal and heart failure removal of a perindoprilat is slowed down.

Indications to use:

Arterial hypertension, chronic heart failure.

Route of administration and doses:

Initial dose - 1-2 mg/days in 1 reception. Maintenance doses - 2-4 mg/days at congestive heart failure, 4 mg (is more rare - 8 mg) - at arterial hypertension in 1 reception.

At renal failures correction of the mode of dosing depending on KK values is required.

Features of use:

Use at pregnancy and feeding by a breast. Perindopril is contraindicated to use at pregnancy and in the period of a lactation (breastfeeding).

Use at renal failures. At renal failures correction of the mode of dosing depending on KK values is required.

Use for children. It is contraindicated at children's age.

Special instructions. With care to apply at a renal failure and heavy arterial hypertension.

Before an initiation of treatment perindoprily the research of function of kidneys is recommended to all patients.

During treatment perindoprily it is regularly necessary to control function of kidneys, activity of liver enzymes in blood, to carry out analyses of peripheral blood (especially at patients with diffusion diseases of connecting fabric, at patients who receive immunodepressive means, Allopyrinolum). Patients with deficit of sodium and liquid before an initiation of treatment need to carry out correction of water and electrolytic disturbances.

During treatment perindoprily it is impossible to carry out a hemodialysis with use of polyacrylonitrile membranes (the risk of emergence of anaphylactic reactions is increased).

Perindopril it is necessary to apply with care along with drugs which can cause increase in level of potassium in blood (indometacin, cyclosporine). Simultaneous use with kaliysberegayushchy diuretics and drugs of potassium is not recommended.

Side effects:

From respiratory system: dry cough is possible.

From the alimentary system: the dispeptic phenomena, dryness in a mouth, taste disturbances.

From TsNS: headache, sleep disorders and/or moods, dizziness; in some cases - spasms.

From system of a hemopoiesis: hemoglobin lowering of the level (especially in an initiation of treatment); seldom - decrease in number of erythrocytes and/or thrombocytes.

From kidneys: reversible increase in level of creatinine and uric acid.

Allergic reactions: Quincke's disease, skin rash, itch, erythema.

Others: sexual frustration.

Interaction with other medicines:

At simultaneous use with anti-hypertensive means, muscle relaxants, means for anesthesia strengthening of anti-hypertensive action is possible.

At simultaneous use with loopback diuretics, thiazide diuretics strengthening of anti-hypertensive action is possible. The expressed arterial hypotension, especially after reception of the first dose of diuretic, apparently, arises at the expense of a hypovolemia which leads to tranzitorny strengthening of hypotensive effect of a perindopril. The risk of a renal failure increases.

At simultaneous use with sympathomimetics reduction of anti-hypertensive action of a perindopril is possible.

At simultaneous use with tricyclic antidepressants, antipsychotic means (neuroleptics) the risk of development of postural hypotension increases.

At simultaneous use with indometacin anti-hypertensive action of a perindopril, apparently, owing to inhibition under the influence of NPVS of synthesis of prostaglandins decreases (which as believe, play a part in development of hypotensive effect of APF inhibitors).

At simultaneous use with insulin, hypoglycemic means derivative sulphonylurea development of a hypoglycemia due to increase in tolerance to glucose is possible.

At simultaneous use with kaliysberegayushchy diuretics (including with Spironolactonum, Triamterenum, amiloride), the potassium drugs, substitutes of salt and dietary supplement to food containing potassium development of a hyperpotassemia (especially at patients with renal failures) is possible since APF inhibitors reduce the maintenance of Aldosteronum that leads to a potassium delay in an organism against the background of restriction of removal of potassium or its additional receipt in an organism.

At simultaneous use from lithium a carbonate reduction of removal of lithium from an organism is possible.

Contraindications:

Quincke's disease in the anamnesis, pregnancy, a lactation, children's age, hypersensitivity to a perindopril.

Issue conditions:

According to the recipe

Packaging:

On 10, 20, 30, 50, 60 or 90 pieces of tablets in strip packagings and cardboard packs.