Hypernik - instructions for use, doses, side effects, contraindications

Active substance: perindopril erbumine	2 mg	4 mg
Excipients: microcrystalline cellulose	22.5 mg	45 mg
aerosil (silicon dioxide colloidal)	0.45 mg	0.90 mg
milk sugar (lactose)	40.95 mg	81.90 mg
corn starch	22.75 mg	45.5 mg
polyvinylpyrrolidone (povidone)	0.45 mg	0.90 mg
magnesium stearate	0.90 mg	0.180 mg

Description:Tablets are white or white with a yellowish tint of color, flat-cylindrical shape with a bevel (for a dosage of 2 mg) and with a facet and a risk (for a dosage of 4 mg).

Pharmacotherapeutic group:Angiotensin-converting enzyme inhibitor (ACE)

ATX: & nbsp

Perindopril

Pharmacodynamics:

ACE inhibitor. Suppression of ACE leads to a decrease in angiotensin II in the blood plasma, resulting in a decrease in the secretion of aldosterone. Perindopril acts through its active metabolite perindoprilata. Eliminates the vasoconstrictive effect of angiotensin and increases the concentration of bradykinin and vasodilator prostaglandins (ACE converts inactive angiotensin I to angiotensin II, which has a vasoconstrictive effect, and also causes bradykinin and prostaglandin to degrade with vasodilating activity); reduces the production and release of aldosterone,suppresses the release of norepinephrine from the endings of sympathetic nerve fibers. and the formation of endothelin in the vessel wall. Reduction of the formation of angiotensin II is accompanied by an increase in the activity of renin of the blood plasma (due to the inhibition of negative feedback). Suppression of ACE is accompanied by an increase in the activity of both circulating and tissue kallikrein-kinin system, while the system of prostaglandins is also activated. Helps restore the elasticity of large arteries(reducing the formation of excessive amounts of subendothelial collagen), reduces pressure in the pulmonary capillaries, with long-term administration reduces the severity of myocardial hypertrophy of the left ventricle and interstitial fibrosis, normalizes the isozyme profile of myosin; normalizes the work of the heart. Reduces preload and postload (reduces systolic and diastolic blood pressure in the "lying" and "standing!"), the filling pressure of the left and right ventricles, OPSS (total peripheral resistance of blood vessels), increases the IOC (minute volume of circulation)and cardiac index without changes in heart rate (heart rate) (in patients with CHF (chronic heart failure), moderately reduces heart rate, strengthens, regional blood flow in muscles).

Increases the concentration of HDL (high-density lipoproteins), in patients with hyperuricemia reduces the concentration of uric acid. Increases renal blood flow, does not change the rate of glomerular filtration. In patients with CHF causes a significant decrease in severity clinical signs of heart failure, increases exercise tolerance (according to the veloergometric test), does not reliably reduce

HELL. After oral administration of an average single dose, the maximum hypotensive effect is achieved after 4-6 hours and persists for 24 hours. Stabilization of the hypotensive effect is observed after 1 month of therapy and persists for a long time time. The termination of treatment is not accompanied by the development of the "withdrawal" syndrome.

Pharmacokinetics:

Absorption is 25%, bioavailability is 65-70%. The time to reach the maximum concentration in the blood plasma - 1h, perindoprilata - 3-4 hours.

In the process of metabolism, 20% is transformed into an activemetabolite perindoprilat (taking perindopril after meals reduces the proportion of

perindoprilata - has no significant clinical significance); The rest is in 5 inactive connections. T1 / 2 (half-life) perindopril - 1 hour. The relationship between perindoprilata and blood plasma proteins is insignificant, with ACE less than 30% (depending on concentration). Volume of distribution of free perindoprilat - 0.2 l / kg Perindoprilat is excreted by the kidneys, T1 / 2 free fraction of the metabolite -

3-5 hours Dissociation of perindoprilat, associated with ACE, is slow. Therefore, the "effective" T1 / 2 is 25 hours. Repeated administration of perindopril does not lead to its cumulation, and T1 / 2 perindoprilata with repeated admission corresponds to the period of its activity.

The excretion of perindoprilat is slowed in elderly patients, as well as in patients with CHF and CRF (chronic renal failure) (in the latter, carry out depending on the clearance of creatinine). The dialytic clearance of perindopril is 70 ml / min.

In patients with liver cirrhosis, the liver clearance of perindopril decreases by a factor of 2, while the total amount of perindoprilat formed does not change and correction of the dosing regimen is not required.

Indications:Arterial hypertension; chronic heart failure.

Contraindications:

Hypersensitivity to perindopril and other components of the drug or other ACE inhibitors, angioedema in the anamnesis in the background therapy with ACE inhibitors, hereditary or idiopathic angioedema, pregnancy, lactation, age under 18 (efficacy and safety not established).

Carefully:

Stenosis of the aortic valve, hypertrophic obstructive cardiomyopathy, cerebrovascular diseases, (including cerebral circulatory insufficiency, ischemic heart disease, coronary insufficiency, the risk of excessive reduction of blood pressure and concomitant ischemia.

Heavy autoimmune systemic diseases of connective tissue (including systemic lupus erythematosus, scleroderma), oppression of bone marrow hematopoiesis against immunosuppressant therapy (increased probability of neutropenia development).

Renovascular hypertension, bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney, condition after kidney transplantation (risk of renal and agranulocytosis)chronic renal failure (especially accompanied by hyperkalemia), hyperkalemia, a diet with sodium restriction, conditions accompanied by a decrease in the volume of circulating blood (including diarrhea, vomiting, diuretics), diabetes, elderly age, surgical intervention (general anesthesia).

Pregnancy and lactation:Perindopril is contraindicated in pregnancy and lactation (breastfeeding).

Dosing and Administration:

Inside, in the morning, before eating.

The initial dose for the treatment of hypertension is 4 mg / day, if necessary (after 1 month) the dose can be increased to 8 mg / day in one session.

With the appointment of ACE inhibitors, patients who are receiving diuretic therapy may experience a sharp reduction in blood pressure, for the prevention of which it is recommended to stop taking diuretics 2-3 days before the proposed initiation of hypernal therapy or to prescribe the drug at lower doses - 2 mg once a day.

In patients with renovascular hypertension, the initial dose is 2 mg 1 time per day. If necessary, the dose may be increased later.

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

Treatment of patients with heart failure in combination with a non-potassium-sparing diuretic and / or digoxin is recommended to begin under careful medical control, Hypernik should be administered at 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 once a 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 the creatinine clearance. With KK 30-60 ml / min - 2 mg once a day; with QC 15-30 ml / min - 2 mg every other day; patients; on hemodialysis (QC less than 15 ml / min) - 2 mg per day of dialysis. With SC more than 60 ml / min 4 mg per day. When Hypernika is prescribed to patients with impaired liver function, no dose changes are required.

Side effects:

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

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

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

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

From the central nervous system: often - headache, asthenia, increased - fatigue, dizziness, ringing in ears, visual impairment, muscle cramps, paresthesia; rarely - decreased mood / insomnia; very rarely confusion.

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

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

Other: increased sweating, violation of sexual function.

Overdose:

Symptoms: marked decrease in blood pressure, shock, stupor, bradycardia, electrolyte disorders (hyperkalemia, hyponatremia), renal failure.

Treatment: gastric lavage, restoration of water-electrolyte intravenous administration of 0.9% sodium chloride solution. When a marked decrease in the blood pressure of the patient should be placed horizontally, lifting his legs up. Effective hemodialysis (do not use - high permeability polyacrylonitrile membranes). With the development of bradycardia - atropine, an artificial pacemaker may be required.

Interaction:

Increases the severity of hypoglycemic action of insulin and sulfonylurea derivatives.

Baclofen, tricyclic antidepressants, antipsychotic medicinal drugs (antipsychotics), saluretics strengthen the hypotensive effect and increase the risk of development, orthostatic hypotension (additive effect), antacids reduce the bioavailability of ACE inhibitors.

GCS (glucocorticosteroids), NSAIDs (non-steroidal anti-inflammatory drugs) reduce the severity of hypotensive action (fluid retention and electrolytes).

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

When used simultaneously with lithium preparations, it is possible to slow it down excretion from the body (regular monitoring of the lithium content in the blood is necessary). Diuretics, medicines for general anesthesia and muscle relaxants, Ethanol increases the risk of excessive blood pressure lowering. The risk of developing clinically pronounced arterial hypotension can be reduced by stopping diuretics a few days before the start of treatment with perindopril.

Special instructions:

The risk of developing arterial hypotension and / or renal insufficiency on the background of taking the drug increases with a significant loss of sodium and water (a strict salt-free diet and / or diuretics, diarrhea, vomiting) or stenosis, renal arteries (blockade in these situations of the renin-angiotensin system drive,especially at the first intake of the drug and during the first 2 weeks of treatment, to a sudden decrease in blood pressure and development of chronic renal failure).

Before and during the therapy it is recommended to determine the concentration of creatinine, electrolytes and urea (within 1 month).

In patients with hypertension who are already receiving diuretic therapy, it is necessary to stop taking them (3 days before the appointment of Hypernika) and, if necessary, add to the treatment in the future again.

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

In patients at risk, especially with chronic heart failure in the stage of decompensation, elderly patients, and patients with initially low blood pressure, impaired renal function or receiving large doses of diuretics, the beginning of the drug should be controlled.

Patients on hemodialysis should avoid using polyacrylonitrile membranes (possibly the development of anaphylactoid reactions).

It is necessary to stop taking before the forthcoming surgical treatment for 12 hours and warn an anesthesiologist about taking the drug.

Effect on the ability to drive transp. cf. and fur:In connection with the danger of developing arterial hypotension and dizziness, inhibitors. ACE should be cautiously prescribed to persons managing motor vehicles and engaged in activities requiring increased attention and rapid motor reaction.

Form release / dosage:

Tablets 2 mg and 4 mg.

Packaging:

For 7 or 10 tablets in a contour mesh package. 30 tablets per jar orange glass.

Each can or 2 contour packs of 7 tablets, or 3 contourcell packs of 10 tablets together with instructions for use in a pack of cardboard.

Storage conditions:List B. In a dry, protected from light and out of reach of children, at a temperature of no higher than 25 ° C.

Shelf life:

2 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001805

Date of registration:16.11.2011 / 13.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp17.04.2017

Illustrated instructions

Instructions

Hypernica (Gypernik)