Perindopril

Description overdue on 07/22/2014

• Latin name: Perindopril
• ATC code: C09AA04
• Active substance: Perindopril erbumine (Perindopril erbumine)
• Manufacturer: Minskinterkaps (Belarus)

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Perindopril, instructions for use (method and dosage)
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• Synonyms
• Babies
• With alcohol
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

Perindopril in the form of tablets   It comprises:

• perindopril erbumine   (acting as a main active ingredient) - 4 mg;
• milk sugar (lactose);
• microcrystalline cellulose (MCC);
• Valium or primelloza sodium;
• magnesium stearate.

Product form

Perindopril - the drug, which is very popular, like the skilled professionals and among the population without medical or pharmaceutical education, but, apart from his peers (combined with funds Indapamide . Arginine   or other active ingredients), it has only one release form.

Perindopril Tablets   white or close to white color flat cylindrical form with a characteristic chamfered on one side. The preparation is supplied in blisters made of aluminum foil, or PVC, calculated on 10 units, or a polymer with a bank 10 or 30 tablets. Packed in a cardboard box 1 or 3 contour cell plate or a polymer bank with detailed instructions for use.

Pharmacological action

Perindopril - pharmaceutical preparation, which belongs to the group   angiotensin-converting enzyme . Due to chemical reaction of the catalyst with zinc ions, is its complete inactivation. As a result of these influences is inhibited the conversion of angiotensin I in angiotensin II, which has vasoconstrictor action   (due to the narrowing of the vascular bed increases blood pressure). Inhibition of ACE accompanied impact on   kallikrein-kinin system   and prostaglandins   - Increasing their circulating and tissue concentrations.

The active metabolite of perindopril influence the natural hormones   human body. Reduced products aldosterone   (the result of interaction with the renin-angiotensin-aldosterone system, kidneys), inhibits the release of noradrenaline   from sympathetic nerve endings and education endothelin an inner layer of the vessel wall. All these changes strengthen hypotensive action pharmaceutical, allowing, as they say, " attack on all fronts ", Which entails sustained reduction in blood pressure.

The drug has some degree of protective properties   - It promotes the Perindopril regenerative restoration of elasticity of major blood vessels of the arterial bed. The mechanism of the pharmacological effect is in reducing the amount of excess collagen occupying subendothelial layer structure. Thus, great vessels become stronger in a physiological sense, and may be more responsive to the change from the blood pressure.

Cardiac Effects   ACE inhibitors are to reduce pre and post load on the myocardium (reduced total peripheral vascular resistance and blood volume of inflows), allowing normal operation of muscular body, increases its effectiveness - minute blood volume increases without increasing heart rate. Peripheral tissues and organs to improve their trophism and Regional blood flow That affects the state of the entire body of the patient undergoing conservative treatment.

If the muscle pump is subject to such pathology as congestive heart failure , The degree of clinical symptoms of the nosological unit decreases. Exercise tolerance on the contrary, is growing rapidly. Clinical studies were conducted using a bicycle stress test, which confirmed the accuracy of therapeutic effects in the treatment of chronic heart disease.

Pharmacodynamics and pharmacokinetics

The drug is used orally Then 25 percent of the components absorbed from the cavity of the gastrointestinal tract. Bioavailability is 65-70 percent. An interesting and even more unusual is the time to reach maximum plasma concentration. The greatest number of inactive substances reaches 1 hour, and biologically active perindoprilat , A metabolite of the active ingredient in the internal medium of an organism (such form metabolized to about 20 percent of perindopril) exhibits its extreme ability to only 3-4 hours after drug administration.

Capable of perindoprilat   bound to plasma proteins Blood marginally and angiotensin-converting enzyme   (slightly less than 30 percent of the active fraction). The volume of distribution of free metabolite - 0, 2 L / kg. Provided metabolite primarily by the kidneys with a half-life of 3-5 hours. The part that is associated with ACE deployed very slowly, which prolongs the period of the effective half-life of 25 hours. Cumulation active substance is observed (the number perindoprilat and its half-life does not change with repeated administration of the drug).

Active excretion of existing product sharing can be slow at physiological wear renal unit at seniors   or chronic heart   and renal failure Because a strict adjustment is required based on the dose level CK   (continuous diagnostic tests during the course of treatment, if the patient falls into this risk group). The dialysis clearance   70 ml per minute.

Indications

Indications are narrow-profile hospital for therapeutic due to the specificity of the therapeutic effect of the drug Perindopril:

• arterial hypertension ;
• congestive heart failure ;
• renovascular hypertension etiology;
• prevention of re- stroke   or after a stroke transient ischemic attack ;
• stable coronary artery disease .

Contraindications

• Individual hypersensitivity, acquired or hereditary intolerance to the constituent components of the pharmaceutical preparation or the entire group of inhibitors angiotensin converting enzyme ;
• period pregnancy ;
• lactation or breast-feeding ;
• angioedema   hereditary or idiopathic origin;
• the medicament is not used in pediatric patients (before age 18 years).

We should also note that there are a number of pathological conditions, when the use of the drug Perindopril is not completely safe and It requires continuous diagnostic monitoring   for all sorts of indicators of an organism with a therapeutic environment of a hospital. The list consists of the following diseases:

• aortic   or mitral stenosis ;
• constrictive pericarditis ;
• leukopenia ;
• severe autoimmune connective tissue disease entities (in particular systemic lupus erythematosus   or scleroderma );
• hyponatremia ;
• the presence of transplanted donor kidney;
• hypertrophic cardiomyopathy ;
• thrombocytopenia ;
• cerebrovascular diseases;
• obliterating atherosclerosis   or narrowing of the blood vessels of different origin (especially the channel supplying the heart muscle);
• bilateral stenosis of afferent arterioles of the kidneys;
• hyperkalemia ;
• moderate or severe stage renal failure ;
• dehydration   and exsicosis .

Side effects

Perindopril is extremely active pharmaceuticals as, besides the therapeutic effects, shows The incidence of adverse reactions   during treatment. It is 1-10 percent of all cases of conservative therapy. Side effects of the components can take the form of violations of various systems of the body:

• Alimentary tract : Nausea, vomiting, indigestion, dry mouth, diarrhea , Decreased appetite, cholestatic jaundice . Pancreatic inflammation . enteric edema .
• On the side Cardiovascular Excessive lowering of blood pressure with the development of orthostatic hypotension, arrhythmia . angina . stroke   and myocardial infarction .
• On the side urinary system : Reduction of the functional capacity of the kidneys,   acute renal failure .
• Respiratory : "dry cough . rhinorrhea , Difficulty free of inhalation and exhalation, eosinophilic pneumonia , Bronchospasm.
• On the side CNS : headache . asthenia . dizziness , Fatigue, imbalance sleep and wakefulness , Depressed mood, periodic tinnitus , Disorders of the visual system, and muscle cramps paresthesia .
• Allergic reactions: itching   or rash, hives . angioedema , Exudative erythema .
• With other systems: increased sweating,   sexual dysfunction .
• Changes in laboratory parameters - hypercreatininemia, gipogemoglobinemiya . thrombocytopenia . proteinuria . hyperkalemia . hyperuricemia . neutropenia . leukopenia ( agranulocytosis ) pancytopenia , And the percentage increase in liver enzymes, hemolytic anemia against deficiency of glucose-6-phosphate dehydrogenase.

Perindopril, instructions for use (method and dosage)

Pharmaceutical drug use orally   at one time (1 per day). Treatment usually begins with a start of dosage of 1-2 mg per day. Further, depending on the indication for treatment and instructions for use of perindopril is somewhat different:

• at Congestive heart failure   conservative reorganization continued optimal dose of 2-4 mg per day;
• arterial hypertension   It can be treated with higher amounts received medication for this pathology using 4-8 mg per day, increasing the dosage should take place gradually, within 3-4 weeks;
• renovascular hypertension   treatable at 2 mg per day;
• stroke prevention carried out by a special scheme: first knock 2 mg for 2 weeks and then 4 mg per day, still the same length of time;
• therapy stable coronary heart disease   It begins with a starting dose of 4 mg per day for 2 weeks and then received the drug quantity increased to 8 mg per day.

Overdose

There are significant clinical cases of overdose pharmaceutical preparation, which usually manifests itself in the following list of symptoms:

• excessive reduction of blood pressure;
• shock ;
• stupor ;
• bradycardia ;
• electrolyte imbalance;
• renal failure .

Specific antagonist for the drug angry pharmaceutical products does not exist. When this complex adverse effects of treatment, which is accompanied by increased plasma concentrations of active components used symptomatic therapy . Effective health following steps:

• gastric lavage ;
• horizontal position with the raised lower end to restore blood pressure;
• application enterosorbents ;
• Correction fluid and electrolyte balance isotonic sodium chloride ;
• atropine   the development of bradycardia;
• Effective use of Hemodialysis   (not recommended the use of highly permeable polyacrylonitrile membranes);
• especially during severe pathological picture overdose can be used implantation of an artificial pacemaker heart.

Cooperation

Perindopril is an extremely active pharmaceuticals (in this parameter, even listed in List B of the International Register of Medicinal Products), therefore, he has a long list of interactions of a different nature. First of all, we should note production which enhances the hypotensive effect of ACE inhibitor (excessive lowering blood pressure can lead to orthostatic hypotension or acute cerebrovascular insufficiency)

• means which is used to anesthesia ;
• muscle relaxants ;
• anti-hypertensive drugs of any mechanism of action;
• loop and thiazide diuretics ;
• tricyclic antidepressants;
• a group of antipsychotic drugs;
• organic nitrates ;
• non-selective monoamine reuptake inhibitors.

The opposite effect, ie, reduction in the hypotensive effect, may cause Indomethacin .

Complex application of perindopril with such pharmaceuticals as potassium-sparing diuretics . digitalis glycosides   and means on the basis of potassium (e.g., active supplements) increase the risk of hyperkalemia   and flowing all of the symptoms of the disease state.

We should also mention the interaction with Nimodipine As well as clinically important heart rhythm disturbances and increased myocardial insufficiency with concomitant use of drugs in medical therapy.

Also should be cautious in patients with diabetes Because Perindopril increases symptoms sugar lowering effect of antidiabetic drugs. Accordingly, there is a risk of hypoglycemia   and Coma As its consequences.

Terms of sale

The drug is classified as a potent and is listed in Schedule B of the International Registry of pharmaceuticals, because the sale of perindopril is carried out only by the assurance of a personal signature and seal of the doctor receptor Form.

Storage conditions

Saves Perindopril should be dry, place inaccessible to children, which is protected from direct sunlight. Temperature conditions optimal storage should not exceed 25 degrees Celsius.

Shelf life

2 years.

Cautions

When using the ACE inhibitor perindopril in particular, there is a risk of hypotension . headache . dizziness   and disorders of the visual abilities, because in the period of medical treatment is to abandon self-management vehicles or other activities that require attention, speed and precision motor responses.

Analogs of perindopril

Match code ATC 4th level:

• Monopril
• Renitek
• Charter
• Fozikard
• Amprilan
• Ramipril
• Prestarium
• Perineva
• Capoten
• Berlipril
• Akkupro
• Diroton
• Enap
• Enalapril

The drug is a pharmaceutical group angiotensin-converting enzyme Because technically all drugs given subunit classification antihypertensive agents can be used as analogs of perindopril. Most often when individual contraindications therapeutic effect is replaced by the following medications: Gipernik . Stopress . Noliprel . A Prestarium . Perineva . Prestancia .

Separately, it is noted that Perindopril, due to its latitude and therapeutic effects of pharmacological action, are used to create richly   combined pharmaceutical formulations . The most popular among this series are:

• Perindopril PLUS indapamide - A drug, wherein the therapeutic effects of perindopril supplemented diuretic component. New active component blocks the reabsorption of sodium ions, chlorine and water, selectively inhibits the activity of calcium channels and decreases total peripheral vascular resistance. A positive feature of the combination of pharmaceutical agents is well marked hypotensive effect, which is independent of the position of the body in space and the patient's age. Also, the effect of this drug is not accompanied by reflex tachycardia .
• Indapamide Perindopril Richter   - A strengthened form of the previous analogue. Effect of the drug is maintained for 24 hours, and persistent therapeutic effects occur in less than a month of conservative treatment. It should be emphasized that the cessation of drug rehabilitation when using this form of the drug is not accompanied by withdrawal syndrome Which sometimes takes extremely seriously.
• Perindopril arginine   - A kind unique drug, as composite components antihypertensive augmented conditionally essential amino acid, the primary role of which is to be the source of NO-synthase in the preparation of endogenous nitric oxide. The latter is very active in terms of pathophysiological mediator of the body. In this context, the most important is its vasodilatory capacity and the regulatory impact on the smooth muscle tone. Thus, the hypotensive effect of the drug covers a much larger mechanism than pure Perindopril. It should be noted that this drug combination can not extend the list of side effects application since arginine is part of the natural metabolism of the human organism.
• Amlodipine Perindopril   - A pharmaceutical preparation, which includes another blocker of slow calcium channels - derivative dihydropyridine . In addition to the antihypertensive effect Amlodipine has also antianginal as contacting with the dihydropyridine receptor, the transmembrane current reduces calcium in the smooth muscle cells in coronary and peripheral channel. This mechanism of action and produced its effects put the drug in the first place among peers at perindopril indications for treatment of coronary heart disease and angina pectoris in particular.
• Perindopril-Mick   - Belarusian analogue of the domestic pharmaceutical. A key feature is the use of it tretbutilaminovoy salt of perindopril   (in the traditional form of the drug is used with the compound erbumine ). Due to this fact, the drug reduces the pressor effect on the vascular wall (including adrenergic ), Which manifests itself as angioprotective action. It should also be noted that the therapeutic effects of the combination applies to peripheral tissues to a greater extent - they are sensitized to insulin and therefore glucose metabolism occurs with greater intensity.

Synonyms perindopril

Synonyms pharmaceutical preparation: Perinpress . Pfizer . Perindopril erbumine . Perindopril tert-butylamine . Perinidid .

Babies

The drug is not used in pediatric patients below 18 years.

With alcohol

During the course of the conservative drug therapy should be   completely eliminate

During pregnancy and lactation

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