Perindopril - Teva tablets p / o 10mg, No. 30

Arterial hypertension.

Chronic heart failure.

Prevention of recurrent stroke (combination therapy with indapamide) in patients with stroke or transient ischemic stroke.

Stable coronary artery disease: reducing the risk of cardiovascular complications in patients with stable coronary artery disease.

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

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 hypertension in 1 dose.

In case of impaired renal function, correction of the dosage regimen is required depending on the CC values.

1 tab.

Active ingredient: perindopril tosylate - 10 mg, which corresponds to perindopril - 6.79 mg

Excipients: lactose monohydrate - 143.924 mg, corn starch - 5.4 mg, sodium bicarbonate - 3.172 mg, pregelatinized corn starch - 14.4 mg, povidone K30 - 3.6 mg, magnesium stearate - 1.8 mg.

Shell composition: Opadray II green 85F210013 (partially hydrolyzed polyvinyl alcohol - 3.6 mg, titanium dioxide (E171) - 2.133 mg, macrogol 3350 (polyethylene glycol 3350) - 1.818 mg, talc - 1.332 mg, indigo carmine aluminum varnish (E132) - 0.0495 mg, aluminum varnish of brilliant blue dye (E133) - 0.0315 mg, iron dye yellow oxide (E172) - 0.018 mg, aluminum varnish of quinoline yellow dye (E104) - 0.018 mg).

A history of angioedema, simultaneous use with aliskiren and aliskiren-containing drugs in patients with diabetes mellitus or impaired renal function (GFR <60 ml / min / 1.73 m2), pregnancy, lactation, children and adolescence up to 18 years of age, hypersensitivity to perindopril, hypersensitivity to other ACE inhibitors.

Perindopril-Teva

Description:

Film-coated tablets of green color, round, biconvex, on one side - engraving '10', on the other - 'T'; cross-section - white or almost white core.

Ingredients: 1 tab.

Active ingredient: perindopril tosylate - 10 mg, which corresponds to perindopril - 6.79 mg

Excipients: lactose monohydrate - 143.924 mg, corn starch - 5.4 mg, sodium bicarbonate - 3.172 mg, pregelatinized corn starch - 14.4 mg, povidone K30 - 3.6 mg, magnesium stearate - 1.8 mg.

Shell composition: Opadray II green 85F210013 (partially hydrolyzed polyvinyl alcohol - 3.6 mg, titanium dioxide (E171) - 2.133 mg, macrogol 3350 (polyethylene glycol 3350) - 1.818 mg, talc - 1.332 mg, indigo carmine aluminum varnish (E132) - 0.0495 mg, aluminum varnish of brilliant blue dye (E133) - 0.0315 mg, iron dye yellow oxide (E172) - 0.018 mg, aluminum varnish of quinoline yellow dye (E104) - 0.018 mg).

Clinical and pharmacological group: ACE inhibitor

Pharmaco-therapeutic group: ACE inhibitor

pharmachologic effect

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 the release of renin and a direct decrease in aldosterone secretion. Due to the vasodilating effect, it reduces the OPSS (afterload), the pressure of wedging in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases cardiac output and exercise tolerance.

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

In clinical studies, with the use of perindopril (monotherapy or in combination with a diuretic), a significant reduction in the risk of recurrent stroke (both ischemic and hemorrhagic), as well as the risk of fatal or disabling strokes has been shown; major cardiovascular complications, including myocardial infarction, incl. fatal; dementia associated with stroke; severe cognitive impairment. These therapeutic benefits were noted in both hypertensive and normal blood pressure patients, regardless of age, gender, presence or absence of diabetes mellitus, and type of stroke.

It was shown that against the background of the use of perindopril tert-butylamine at a dose of 8 mg / day (equivalent to 10 mg of perindopril arginine) in patients with stable coronary artery disease, there is a significant decrease in the absolute risk of complications provided for by the main criterion of effectiveness (mortality from cardiovascular diseases, the incidence of non-fatal myocardial infarction). and / or cardiac arrest followed by successful resuscitation) by 1.9%. In patients who had previously undergone myocardial infarction or coronary revascularization, the absolute risk reduction was 2.2% compared with the placebo group.

Perindopril is used both as monotherapy and as fixed combinations with indapamide and amlodipine.

Pharmacokinetics

After oral administration, perindopril is rapidly absorbed from the gastrointestinal tract. Cmax is achieved after 1 hour. Bioavailability is 65-70%.

In the process of metabolism, perindopril is biotransformed with the formation of an active metabolite - perindoprilat (about 20%) and 5 inactive compounds. Cmax of perindoprilat in plasma is achieved between 3 and 5 hours after administration. The binding of perindoprilat to blood plasma proteins is insignificant (less than 30%) and depends on the concentration of the active substance. The Vd of free perindoprilat is close to 0.2 L / kg.

Does not cumulate. Re-admission does not lead to cumulation 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 hour.

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

In elderly patients, as well as in renal and heart failure, the excretion of perindoprilat is slowed down.

Indications

Arterial hypertension.

Chronic heart failure.

Prevention of recurrent stroke (combination therapy with indapamide) in patients with stroke or transient ischemic stroke.

Stable coronary artery disease: reducing the risk of cardiovascular complications in patients with stable coronary artery disease.

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

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 hypertension in 1 dose.

In case of impaired renal function, correction of the dosage regimen is required depending on the CC values.

Side effect

From the hematopoietic system: eosinophilia, decreased hemoglobin and hematocrit, thrombocytopenia, leukopenia / neutropenia, agranulocytosis, pancytopenia, hemolytic anemia in patients with congenital glucose-6-phosphate dehydrogenase deficiency.

From the side of metabolism: hypoglycemia, hyperkalemia, reversible after drug withdrawal, hyponatremia.

From the nervous system: paresthesia, headache, dizziness, vertigo, sleep disturbances, mood lability, drowsiness, fainting, confusion.

From the senses: visual impairment, tinnitus.

From the side of the cardiovascular system: an excessive decrease in blood pressure and associated symptoms, vasculitis, tachycardia, palpitations, heart rhythm disturbances, angina pectoris, myocardial infarction and stroke, possibly due to an excessive decrease in blood pressure in high-risk patients.

From the respiratory system: cough, shortness of breath, bronchospasm, eosinophilic pneumonia, rhinitis.

From the digestive system: constipation, nausea, vomiting, abdominal pain, taste disturbance, dyspepsia, diarrhea, dryness of the oral mucosa, pancreatitis, hepatitis (cholestatic or cytolytic).

On the part of the skin and subcutaneous fat: skin itching, rash, photosensitivity, pemphigus, increased sweating.

Allergic reactions: angioedema, urticaria, erythema multiforme.

From the musculoskeletal system: muscle spasms, arthralgia, myalgia.

From the urinary system: renal failure, acute renal failure.

Reproductive system disorders: erectile dysfunction.

General reactions: asthenia, chest pain, peripheral edema, weakness, fever, falls.

On the part of laboratory parameters: an increase in the activity of hepatic transaminases and bilirubin in the blood serum, an increase in the concentration of urea and creatinine in the blood plasma.

Contraindications for use

A history of angioedema, simultaneous use with aliskiren and aliskiren-containing drugs in patients with diabetes mellitus or impaired renal function (GFR <60 ml / min / 1.73 m2), pregnancy, lactation, children and adolescence up to 18 years of age, hypersensitivity to perindopril, hypersensitivity to other ACE inhibitors.

Application during pregnancy and lactation

Perindopril is contraindicated during pregnancy and lactation (breastfeeding).

Application for impaired renal function

In case of impaired renal function, correction of the dosage regimen is required depending on the CC values.

Application in children

Contraindicated in childhood.

special instructions

Carefullyperindopril should be used for bilateral renal artery stenosis or renal artery stenosis of a solitary kidney; kidney failure; systemic connective tissue diseases; therapy with immunosuppressants, allopurinol, procainamide (risk of developing neutropenia, agranulocytosis); reduced BCC (taking diuretics, diet with salt restriction, vomiting, diarrhea); angina pectoris; cerebrovascular diseases; renovascular hypertension; diabetes mellitus; chronic heart failure IV functional class according to NYHA classification; simultaneously with potassium-sparing diuretics, potassium preparations, potassium-containing substitutes for table salt, with lithium preparations; with hyperkalemia; surgery / general anesthesia; hemodialysis using high-flow membranes; desensitizing therapy; LDL apheresis;condition after kidney transplantation; aortic stenosis / mitral stenosis / hypertrophic obstructive cardiomyopathy; in patients of the black race.

Cases of arterial hypotension, fainting, stroke, hyperkalemia and impaired renal function (including acute renal failure) have been reported in predisposed patients, especially when used simultaneously with drugs that affect the RAAS. Therefore, double blockade of the RAAS as a result of the combination of an ACE inhibitor with an angiotensin II receptor antagonist or aliskiren is not recommended.

Before starting treatment with perindopril, a study of renal function is recommended for all patients.

During treatment with perindopril, kidney function, the activity of liver enzymes in the blood should be regularly monitored, and peripheral blood tests should be performed (especially in patients with diffuse connective tissue diseases, in patients receiving immunosuppressive drugs, allopurinol). Patients with sodium and fluid deficiency need to correct water-electrolyte disturbances before starting treatment.

Drug interactions

The risk of developing hyperkalemia increases with the simultaneous use of perindopril with other drugs that can cause hyperkalemia: aliskiren and aliskiren-containing drugs, potassium salts, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs, heparin, immunosuppressive drugs, or such as triplets.

When used simultaneously with aliskiren in patients with diabetes mellitus or impaired renal function (GFR <60 ml / min), the risk of hyperkalemia, deterioration of renal function and an increase in the incidence of cardiovascular morbidity and mortality increases (this combination is contraindicated in patients of these groups).

Simultaneous use with aliskiren in patients without diabetes mellitus or renal dysfunction is not recommended, because possible increased risk of hyperkalemia, deterioration of renal function and increased incidence of cardiovascular morbidity and mortality.

In the literature, it has been reported that in patients with established atherosclerotic disease, heart failure, or diabetes mellitus with target organ damage, concomitant therapy with an ACE inhibitor and an angiotensin II receptor antagonist is associated with a higher incidence of hypotension, syncope, hyperkalemia, and deterioration of renal function (including acute renal failure) compared with the use of only one drug that affects the RAAS. Double blockade (for example, when an ACE inhibitor is combined with an angiotensin II receptor antagonist) should be limited to individual cases with careful monitoring of renal function, potassium and blood pressure.

Concomitant use with estramustine may increase the risk of side effects such as angioedema.

With the simultaneous use of lithium and perindopril preparations, a reversible increase in the concentration of lithium in the blood serum and associated toxic effects are possible (this combination is not recommended).

Simultaneous use with hypoglycemic drugs (insulin, hypoglycemic drugs for oral administration) requires special care, because ACE inhibitors, incl. perindopril, can enhance the hypoglycemic effect of these drugs up to the development of hypoglycemia. As a rule, this is observed in the first weeks of simultaneous therapy and in patients with impaired renal function.

Baclofen enhances the antihypertensive effect of perindopril; with simultaneous use, a dose adjustment of the latter may be required.

In patients receiving diuretics, especially those that remove fluids and / or salts, at the beginning of therapy with perindopril, there may be an excessive decrease in blood pressure, the risk of which can be reduced by discontinuing the diuretic, replacing fluid or salt loss before starting therapy with perindopril, and using perindopril in low the initial dose with its further gradual increase.

In chronic heart failure, in the case of diuretics, perindopril should be used in a low dose, possibly after reducing the dose of a potassium-sparing diuretic used simultaneously. In all cases, renal function (creatinine concentration) should be monitored in the first weeks of using ACE inhibitors.

The use of eplerenone or spironolactone in doses from 12.5 mg to 50 mg / day and ACE inhibitors (including perindopril) in low doses: in the treatment of heart failure II-IV functional class according to NYHA classification with left ventricular ejection fraction <40% and previously used ACE inhibitors and 'loop' diuretics, there is a risk of developing hyperkalemia (with a possible fatal outcome), especially if the recommendations for this combination are not followed. Before using this combination, you must make sure that there is no hyperkalemia and renal dysfunction. It is recommended to regularly monitor the concentration of creatinine and potassium in the blood - weekly in the first month of treatment and monthly thereafter.

The simultaneous use of perindopril with NSAIDs (acetylsalicylic acid in a dose that has an anti-inflammatory effect, COX-2 inhibitors and non-selective NSAIDs) can lead to a decrease in the antihypertensive effect of ACE inhibitors. The simultaneous use of ACE inhibitors and NSAIDs can lead to deterioration of renal function, including the development of acute renal failure, and an increase in serum potassium, especially in patients with reduced renal function. Use this combination with caution in elderly patients. Patients should receive an adequate amount of fluid; it is recommended to carefully monitor renal function, both at the beginning and during treatment.

The antihypertensive effect of perindopril can be enhanced by concomitant use with other antihypertensive drugs, vasodilators, including short-acting and prolonged-acting nitrates.

The simultaneous use of gliptins (linagliptin, saxagliptin, sitagliptin, vitagliptin) with ACE inhibitors (including perindopril) may increase the risk of angioedema due to suppression of dipeptidylpeptidase IV activity by gliptin.

The simultaneous use of perindopril with tricyclic antidepressants, antipsychotics and general anesthetics can lead to an increase in the antihypertensive effect.

Sympathomimetics may weaken the antihypertensive effect of perindopril.

When using ACE inhibitors, incl. perindopril, in patients receiving iv gold preparation (sodium aurothiomalate), a symptom complex was described, in which there were facial flushing, nausea, vomiting, arterial hypotension.

Release form / dosage:

Film-coated tablets, 2.5 mg, 5 mg, 10 mg.

Packaging:

30 tablets in a white polypropylene container with a polyethylene lid with a desiccant insert equipped with a polyethylene stopper with first opening control. 1 container with instructions for use in a cardboard box with first opening control.

Storage conditions:

Store at a temperature not exceeding 25 ? C. Keep out of the reach of children!

Shelf life:

2 years.

Do not use after the expiration date.

Terms of dispensing from pharmacies:

On prescription