Perindopril, pills 8mg 30pcs

Composition

of perindopril 8 mg

Pharmacological action

An ACE inhibitor. It is a prodrug from which the active metabolite perindoprilat is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I to angiotensin II, which is a powerful vasoconstrictor. As a result of a decrease in the concentration of angiotensin II, a secondary increase in plasma renin activity occurs due to the elimination of negative feedback during renin release and a direct decrease in aldosterone secretion. Due to its vasodilating action, it reduces OPSS (afterload), jamming pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases the minute volume of the heart and load tolerance.

The hypotensive effect develops within the first hour after taking perindopril, reaches a maximum by 4-8 hours and continues for 24 hours.

After oral use, perindopril is rapidly absorbed from the gastrointestinal tract. Cmax is reached after 1 h. Bioavailability is 65-70%.

During metabolism, perindopril is biotransformed to form the active metabolite perindoprilate (about 20%) and 5 inactive compounds. Cmax of plasma perindoprilat is reached between 3 and 5 hours after use. Binding of perindoprilat to plasma proteins is insignificant (less than 30%) and depends on the concentration of the Active ingredient. The Vd of free perindoprilate is close to 0.2 l / kg.

It doesn’t accumulate. Repeated use does not lead to accumulation and T1/2 corresponds to the period of its activity.

When taken with food, the metabolism of perindopril slows down.

T1 / 2 of perindopril is 1 h.

Perindoprilat is excreted by the kidneys; T1 / 2 of its free fraction is 3-5 hours.

In elderly patients, as well as in patients with renal and heart failure, the elimination of perindoprilat slows down.

Indications

Arterial hypertension, chronic heart failure.

Contraindications

A history of angioedema, pregnancy, lactation, childhood, hypersensitivity to perindopril.

Use during pregnancy and lactation

Perindopril is contraindicated for use during pregnancy and lactation (breastfeeding).

Use in patients with impaired renal function

In case of impaired renal function, the dosage regimen should be adjusted depending on the values of creatinine clearance.

Use in children

Contraindicated in childhood.

Side effects

Respiratory system disorders:  possible dry cough.

From the digestive system:  dyspeptic symptoms, dry mouth, taste disorders.

From the central nervous system:  headache, sleep and/or mood disorders, dizziness; in some cases – convulsions.

From the hematopoietic system:  decreased hemoglobin levels (especially at the beginning of treatment); rarely, a decrease in the number of red blood cells and / or platelets.

From the side of the kidneys:  reversible increase in creatinine and uric acid levels.

Allergic reactions:  angioedema, skin rash, pruritus, erythema.

Other services:  sexual disorders.

Interaction

When used concomitantly with antihypertensive agents, muscle relaxants, and anesthetics, it is possible to increase the antihypertensive effect.

When used concomitantly with loop diuretics, thiazide diuretics, it is possible to increase the antihypertensive effect. Severe hypotension, especially after taking the first dose of a diuretic, appears to occur due to hypovolemia, which leads to a transient increase in the hypotensive effect of perindopril. The risk of impaired renal function increases.

When used concomitantly with sympathomimetics, the antihypertensive effect of perindopril may be reduced.

When used concomitantly with tricyclic antidepressants, antipsychotic drugs (neuroleptics), the risk of postural hypotension increases.

When used concomitantly with Indometacin, the antihypertensive effect of perindopril decreases, apparently due to the inhibition of prostaglandin synthesis under the influence of NSAIDs (which are believed to play a role in the development of the antihypertensive effect of ACE inhibitors).

When used concomitantly with insulin, hypoglycemic agents and sulfonylureas, hypoglycemia may develop due to increased glucose tolerance.

When used concomitantly with potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes, and dietary supplements containing potassium, hyperkalemia may develop (especially in patients with impaired renal function), since ACE inhibitors reduce the content of aldosterone, which leads to potassium retention in the body against the background of limiting the excretion of potassium or its additional intake into the body.

When used concomitantly with lithium carbonate, it is possible to reduce the excretion of lithium from the body.

How to take, course of use and dosage

The initial dose is 1-2 mg / day in 1 dose. Maintenance doses – 2-4 mg / day for congestive heart failure,4 mg (less often-8 mg ) – for arterial hypertension in 1 reception.

In case of impaired renal function, the dosage regimen should be adjusted depending on the values of creatinine clearance.

Special instructions

Use with caution in patients with renal insufficiency and severe arterial hypertension.

Before starting treatment with perindopril, all patients are recommended to study renal function.

During treatment with perindopril, kidney function, liver enzyme activity in the blood should be regularly monitored, and peripheral blood tests should be performed (especially in patients with diffuse connective tissue diseases, in patients who receive immunosuppressive agents, allopurinol). Patients with sodium and fluid deficiencies should have their water and electrolyte disorders corrected before starting treatment.

During treatment with perindopril, hemodialysis using polyacrylonitrile membranes should not be performed (the risk of anaphylactic reactions is increased).

Perindopril should be used with caution simultaneously with drugs that may cause an increase in blood potassium levels (Indometacin, cyclosporine). Concomitant use with potassium-sparing diuretics and potassium supplements is not recommended.

Active ingredient

Perindopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as directed by your doctor

Indications

Heart failure, Hypertension, Heart attack and stroke prevention, Angina