Perindopril

Izvarino Pharma, Russia

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$11 - $13
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Product Overview

Composition

1 tablet contains perindopril erbumine 

pharmachologic effect

Perindopril is an ACE inhibitor (interacts with zinc ions in the ACE molecule and causes its inactivation). Perindopril acts through its active metabolite, perindoprilat. Eliminates the vasoconstrictor effect of angiotensin II, increases the concentration of bradykinin and vasodilator prostaglandins (ACE converts inactive angiotensin I into angiotensin II, which has a vasoconstrictor effect, and also causes the degradation of bradykinin and prostaglandins, which have vasodilating activity); reduces production and release

aldosterone, inhibits the release of norepinephrine from the endings of sympathetic nerve fibers and the formation of endothelin in the vascular wall. A decrease in the formation of angiotensin II is accompanied by an increase in the activity of blood plasma renin (due to inhibition of negative feedback). The suppression of ACE is accompanied by an increase in the activity of both the circulating and tissue kallikrein-kinin system, as well as the prostaglandin system.

Promotes the restoration of the elasticity of large arterial vessels (reducing the formation of excess subendothelial collagen), reduces the pressure in the pulmonary capillaries, with prolonged administration reduces the severity of left ventricular myocardial hypertrophy and interstitial fibrosis, normalizes the isoenzyme profile of myosin; normalizes heart function.

Reduces preload and afterload (reduces systolic and diastolic blood pressure (BP) in the lying and standing positions), filling pressure of the left and right ventricles, total peripheral vascular resistance (OPSS); increases the minute blood volume (IOC) and the cardiac index, does not increase the heart rate (HR) (in patients with chronic heart failure (CHF), moderately decreases the heart rate), increases regional blood flow in the muscles. Increases the concentration of high density lipoproteins, in patients with hyperuricemia, reduces the concentration of uric acid. Increases renal blood flow, does not change the glomerular filtration rate.

Indications

Arterial hypertension. 
Chronic heart failure.

Contraindications

Hypersensitivity to perindopril and other components of Perindopril or other ACE inhibitors, a history of angioneurotic edema during therapy with ACE inhibitors, hereditary or idiopathic angioedema, pregnancy, lactation, age up to 18 years (efficacy and safety have not been established).

Carefully:

Aortic valve stenosis, hypertrophic obstructive cardiomyopathy, cerebro- and cardiovascular diseases (including cerebral circulation insufficiency, coronary heart disease, coronary insufficiency - the risk of developing an excessive decrease in blood pressure and concomitant ischemia).

Severe autoimmune systemic diseases of the connective tissue (including systemic lupus erythematosus, scleroderma), inhibition of bone marrow hematopoiesis while taking immunosuppressants (increasing the likelihood of developing neutropenia).

Renovascular hypertension, bilateral stenosis of the renal arteries, stenosis of an artery of a single kidney, condition after kidney transplantation (risk of renal impairment and agranulocytosis), chronic renal failure (especially accompanied by hyperkalemia), hyperkalemia, sodium-restricted diet, conditions accompanied by a decrease in blood volume (including diarrhea, vomiting, taking diuretics), diabetes mellitus, old age, surgery (general anesthesia).

Side effects

The frequency of side effects is estimated on the basis of: often - 1-10%; rarely - 0.1-1%; extremely rare, including individual messages - less than 0.1%.

From the side of the cardiovascular system: often - an excessive decrease in blood pressure and associated symptoms, rarely - arrhythmia, angina pectoris, myocardial infarction and stroke.

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

On the part of the respiratory system: often - "dry" cough, difficulty breathing; rarely - bronchospasm, rhinorrhea.

From the digestive system: often - nausea, vomiting, abdominal pain, change in taste, diarrhea or constipation, dry mouth, decreased appetite, cholestatic jaundice, pancreatitis, intestinal edema.

From the side of the central nervous system: often - headache, asthenia, fatigue, dizziness, ringing in the ears, visual disturbances, muscle cramps, paresthesia; rarely - decreased mood, insomnia; extremely rarely - confusion.

Allergic reactions: often - skin rash, itching; rarely - urticaria, angioedema; extremely rare - exudative erythema multiforme.

Laboratory indicators: often - hypercreatininemia, proteinuria, hyperkalemia; hyperuricemia; rarely (with prolonged use in high doses) - neutropenia, leukopenia, hypoglobinemia, thrombocytopenia, decreased hematocrit; extremely rarely - agranulocytosis, pancytopenia, increased activity of "liver" enzymes, hyperbilirubinemia, hemolytic anemia (against the background of glucose-6-phosphate dehydrogenase deficiency).

Others: increased sweating, impaired sexual function.

Interaction

Increases the severity of the hypoglycemic action of insulin and sulfonylurea derivatives.
Baclofen, tricyclic antidepressants, antipsychotic drugs (neuroleptics), saluretics enhance the hypotensive effect and increase the risk of orthostatic hypotension (additive effect).

Antacids reduce the bioavailability of ACE inhibitors.

Glucocorticosteroids, non-steroidal anti-inflammatory drugs reduce the severity of the hypotensive effect (fluid and electrolyte retention).

Potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium supplements increase the risk of hyperkalemia. The simultaneous use of drugs that can cause hyperkalemia and ACE inhibitors is not recommended, except in cases of severe hypokalemia (control of serum potassium).

With simultaneous use with lithium preparations, it is possible to slow down its excretion from the body (regular monitoring of the lithium content in the blood is necessary).

Diuretics, drugs for general anesthesia and muscle relaxants, ethanol increase the risk of developing an excessive decrease in blood pressure. The risk of developing clinically pronounced arterial hypotension can be reduced by stopping diuretics a few days before starting treatment with perindopril.

Myelotoxic drugs - increased myelotoxic action.

How to take, course of administration and dosage

Perindopril is taken orally, in the morning, before meals.
The initial dose for the treatment of arterial hypertension is 4 mg / day, if necessary (after 1 month) the dose can be increased to 8 mg / day in one dose.

When prescribing ACE inhibitors to patients receiving diuretic therapy, there may be a sharp decrease in blood pressure, for the prevention of which it is recommended to stop taking diuretics 2-3 days before the intended start of Perindopril therapy or to prescribe the drug in lower doses - 2 mg 1 time per day.

In patients with renovascular hypertension, the initial dose is 2 mg once a day. If necessary, the subsequent dose may be increased.

In elderly patients, therapy should be started with a dose of 2 mg per day, and then, if necessary, gradually increase it up to a maximum dose of 8 mg per day.

Treatment of patients with chronic heart failure in combination with a non-potassium-sparing diuretic and / or digoxin is recommended to start under close medical supervision. Perindopril is prescribed in an initial dose of 2 mg once a day, in the morning.
In the future, after 1-2 weeks of therapy, the dose of the drug can be increased to 4 mg 1 time per day.

In patients with impaired renal function, the dose of the drug should be selected taking into account the degree of renal failure: depending on creatinine clearance.

With a creatinine clearance of more than 60 ml / min - 4 mg perindopril per day. With a creatinine clearance of 30-60 ml / min - 2 mg once a day; with creatinine clearance 15-30 ml / min - 2 mg every other day; patients on hemodialysis (creatinine clearance less than 15 ml / min.) - 2 mg per day of dialysis.

Patients with impaired liver function do not need dose changes.

Overdose

Symptoms: decreased blood pressure, shock, stupor, bradycardia, electrolyte disturbances, renal failure. 

Treatment: gastric lavage, the use of enterosorbents, restoration of water-electrolyte balance, intravenous administration of 0.9% sodium chloride solution. In the case of a pronounced decrease in blood pressure, the patient must be given a horizontal position with raised legs.

Hemodialysis is effective (do not use highly permeable polyacrylonitrile membranes). With the development of bradycardia, atropin. In severe cases, temporary implantation of a pacemaker is indicated. It is necessary to control and correct the vital functions of the body.

Special instructions

The risk of developing arterial hypotension and / or renal failure while taking the drug increases with significant loss of sodium and water (strict salt-free diet, and / or taking diuretics, diarrhea, vomiting) or stenosis of the renal arteries (blockade in these situations of the renin-angiotensin system can lead , especially at the first intake of the drug and during the first 2 weeks of treatment, to a sudden decrease in blood pressure and the development of chronic renal failure). Before starting and during therapy, it is recommended to determine the concentration of creatinine, electrolytes and urea (within 1 month).

In patients with arterial hypertension already receiving diuretic therapy, it is necessary to stop taking them (3 days before the start of the appointment of Perindopril) and, if necessary, add them to the treatment again.

In patients with chronic heart failure receiving diuretic therapy, if possible, their dose should also be reduced a few days before the start of admission.

In patients at risk, especially with chronic heart failure in the stage of decompensation, elderly patients, as well as patients with initially low blood pressure, impaired renal function, or receiving large doses of diuretics, the drug should be started under the supervision of medical personnel.

In patients on hemodialysis, the use of polyacrylonitrile membranes should be avoided (anaphylactoid reactions may develop). It is necessary to stop taking it before the upcoming surgical treatment for 12 hours and warn the anesthesiologist about taking the drug.

Release form

Pills.

Storage conditions

Store in a dry, out of reach of children, protected from light at a temperature not exceeding 25 ° C.

Shelf life

2 years.

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