Perindopril - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Perindopril is an inhibitor of the angiotensin-converting enzyme. ACE provides the conversion of angiotensin I into a vasoconstrictor substance, angiotensin II. In addition, the ACE destroys bradykinin, which has vasodilator action. Thus, inhibition of ACE causes the antihypertensive and vasodilating effects of the drug, which is used to treat hypertension of any severity.

Pharmacokinetics:Absorption in the gastrointestinal tract is rapid, the maximum concentration of the drug is detected after 1 hour. Poorly penetrates the blood-brain barrier. The connection with plasma proteins is about 60%. In the liver, biotransformation to the active metabolite - perindoprilata (20% of the total absorbed amount) occurs. Elimination by the kidneys. The half-life of perindopril from the blood plasma is 50-60 min. With chronic renal failure, the elimination time increases. Perindopril and its active metabolite - perindoprilat, are removed during hemodialysis.

Indications:

Arterial hypertension (monotherapy or as part of combination therapy).
Chronic heart failure
Cardiac ischemia
Prevention of complications in patients who have had previous myocardial infarction or coronary revascularization.
Prevention of recurrent stroke (in combination with indapamide) in patients who have previously suffered a stroke or transient cerebral circulation disorder according to the ischemic type.

ICD-10

IV.E00-E07.E05 Thyrotoxicosis [hyperthyroidism]

IX.I10-I15.I10 Essential [primary] hypertension

IX.I10-I15.I15 Secondary Hypertension

IX.I20-I25.I21.9 Acute myocardial infarction, unspecified

IX.I20-I25.I25 Chronic ischemic heart disease

IX.I30-I52.I50.9 Heart failure, unspecified

IX.I60-I69.I64 Stroke not specified as a hemorrhage or infarction

Contraindications:

Hypersensitivity to perindopril, auxiliary components, other ACE inhibitors (possible angioedema).
Idiopathic hereditary edema of Quincke.
Pregnancy, breastfeeding.
Simultaneous administration of aliskiren or aliskiren-containing drugs in patients with diabetes mellitus or renal dysfunction
Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption syndrome.
Children under 18 years.

Carefully:

Chronic renal failure.
Stenosis of the renal arteries (especially - with a single functioning kidney)
Systemic diseases of connective tissue (systemic lupus erythematosus, scleroderma).
Angina pectoris, atherosclerosis, cerebrovascular diseases.
Renovascular hypertension.
Diabetes.
Severe chronic heart failure IV functional class.
Hypertrophic obstructive cardiomyopathy.
Simultaneous reception of antidepressants, allopurinol, procainamide (risk of neutropenia, agranulocytosis).
Surgery / general anesthesia.
Hemodialysis using high-flow membranes.
Condition after kidney transplantation.
Reduction of the volume of circulating blood with diuretics, vomiting, diarrhea.
A diet with sodium intake restriction, hyperkalemia.
Elderly age.
Patients of the Negroid race (the risk of angioedema development is higher).

Pregnancy and lactation:Category of recommendations FDA is not defined. Contraindicated in pregnancy and breastfeeding. If taking the drug is vital, then breastfeeding should be stopped for the period of treatment.

Dosing and Administration:

The drug is taken orally 1 time per day in the morning before eating.

The initial dose is 2 mg per day, then after a month, if necessary, the dose can be increased to 4-8 mg per day. The dose is determined individually, based on the state of kidney function, the general condition of the patient. The maximum daily dose is 8 mg.

Side effects:

Quincke edema, skin rash
Hypotension
Dry non-productive cough
Headache, chest pain
Unusual fatigue
Nausea, taste disorder, diarrhea
Pancreatitis, hepatotoxic action
Hyperkalemia
Neutropenia, agranulocytosis

Overdose:

Symptoms: marked decrease in blood pressure (orthostatic hypotension), dizziness, anxiety, cough, fainting, tachycardia, in severe cases - bradycardia.

Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy. In severe cases, hemodialysis is indicated.

Interaction:

Alcohol, diuretics, drugs that reduce blood pressure increase the hypotensive effect of perindopril.

Donor blood (if stored for more than ten days), ciclosporin, potassium-sparing diuretics, potassium-containing preparations, salt substitutes with simultaneous application with perindopril can cause hyperkalemia, therefore, frequent determination of potassium concentration in blood serum is necessary.

NSAIDs (especially indomethacin), estrogens, adrenomimetics weaken the hypotensive effect of perindopril.

Oral hypoglycemic agents together with perindopril increase hypoglycemic effect.

The use of lithium drugs simultaneously with perindopril increases the concentration of lithium in the blood (pharmacokinetic monitoring).

The drugs that depress the bone marrow together with perindopril increase the risk of developing neutropenia and / or agranulocytosis with a fatal outcome.

Special instructions:

During treatment with the drug it is necessary to control blood pressure, kidney function, volume of circulating blood, potassium concentration in blood plasma. Patients with diabetes should monitor blood glucose levels.

With caution apply to patients who manage motor vehicles and engage in potentially hazardous activities that require concentration and speed of psychomotor reactions.

Instructions

Perindopril (Perindoprilum)