Amlodipin-Zdorovye of the tab. of 10 mg No. 10Õ3/tab. 5 of mg No. 10х3

General characteristics. Structure:

Main physical and chemical properties: tablets on 5 mg – color, white or white with a creamy shade, a ploskotsilindricheky form with a facet; tablets on 10 mg – color, white or white with a creamy shade, a ploskotsilindricheky form with risky and a facet; 1 tablet contains an amlodipin of a besilat in terms of 100% substance and амлодипин 5 mg or 10 mg; excipients: cellulose microcrystallic, sodium of a kroskarmelloz, lactose monohydrate, calcium hydrophosphate anhydrous, silicon dioxide colloid anhydrous, calcium stearate.

Pharmacological properties:

Pharmacodynamics. The selection blocker of "slow" calcium channels with preferential action on vessels; derivative dihydropyridine. The mechanism of action is caused by linkng with dihydropyridinic receptors, blocking of "slow" calcium channels, inhibition of transmembrane current of calcium in cells of unstriated muscles of heart and vessels (more in smooth muscle cells of vessels, than in cardiomyocytes). Has anti-hypertensive and anti-anginal effect. Anti-hypertensive action is caused by direct vazodilatiruyushchy impact on unstriated muscles of arterial vessels and the subsequent decrease in the general peripheric resistance of vessels. Thanks to the slow beginning of action and the prolonged effect provides a smooth and long lowering of arterial pressure. At patients with arterial hypertension reception of 1 times a day is followed by clinically significant dozozavisimy lowering of arterial pressure in situation both "lying", and "standing" within a day.

Anti-anginal action is caused by expansion of coronary and peripheral arteries and decrease in the general peripheric resistance of vessels (afterload) without change of heart rate. Prevents development of a spasm of coronary arteries (Printsmetal's stenocardia or vasospastic stenocardia). At patients with stenocardia regular reception of an amlodipin increases tolerance to an exercise stress. At the patients with cardiovascular diseases who had a myocardial infarction, through skin transluminal angioplasty of coronary arteries or having stenocardia, амлодипин prevents development of a thickening erotic-medii of carotid arteries, considerably reduces a lethality from the cardiovascular reasons, a myocardial infarction, stroke, transluminal angioplasty of coronary arteries, aortocoronary shunting; leads to decrease in hospitalization concerning unstable stenocardia and progressing of chronic heart failure, reduces the frequency of the interventions directed to recovery of a coronary blood-groove.

Has no significant effect on contractility and conductivity of a myocardium, does not cause reflex increase in heart rate, slows down aggregation of thrombocytes, raises a glomerular filtration rate, has a weak natriuretic effect. At a diabetic nephropathy does not increase expressiveness of a microalbuminuria. Does not exert any adverse impact on a metabolism and concentration of lipids of plasma. Amlodipin has the big duration of action, it is possible to appoint it 1 time a day. The therapeutic effect develops in 2 – 4 h after reception, action duration – about 24 h.

Pharmacokinetics. After use it is inside soaked up slowly, but almost completely (reception with food does not change absorption). Bioavailability makes 60 – 80%. The maximum concentration in plasma is reached in 6 - 12 h after reception. Communication with proteins of plasma – 90 – 98%. It is well distributed in an organism (distribution volume – 21 l/kg). Constant concentration in a blood plasma is reached for 7 – 8 day of treatment. Gets through a blood-brain barrier and into breast milk. Slowly, but it is intensively metabolized in a liver; about 90% turn into small and inactive derivatives of pyridine; has small effect of "the first passing". The elimination half-life after a single dose varies from 31 to 48 h, at repeated reception makes about 45 h. The general clearance makes 7 ml / минкг (patients with body weight have 60 kg – 25 l/h, elderly patients have –19 l/h). Elimination is carried out by kidneys (about 60% – in the form of metabolites, about 10% – in not changed look) and with bile (20 – 25% in the form of metabolites). It is allocated with breast milk. Is not removed at a hemodialysis.

At patients with arterial hypertension the elimination half-life makes about 48 h, at patients 65 years are more senior – increases to 65 h, at a liver failure and at heavy chronic heart failure – to 60 h. Lengthening of an elimination half-life testifies to a possibility of cumulation of drug at its long appointment. Insufficiency of function of kidneys has no significant effect on pharmacokinetics of an amlodipin.

Indications to use:

Arterial hypertension, stable stenocardia or vasospastic stenocardia (Printsmetal's stenocardia).

Route of administration and doses:

Appoint the adult in 1 times a day, irrespective of meal, washing down with enough water (up to 100 ml).

The initial daily dose usually makes 5 mg, if necessary increase in 7 – 10 days (taking into account reaction of the patient) to a daily dose of 10 mg is possible. A maintenance dose at arterial hypertension – 5 mg a day.

At an angina of exertion and vasospastic stenocardia appoint 5 – 10 mg in a daily dose; for prevention of attacks of stenocardia – 10 mg a day.

For patients thin, low growth, elderly, with an abnormal liver function the initial daily dose makes 2,5 mg (use drugs of an amlodipin with a possibility of dosing of 2,5 mg).

At a renal failure, co-administration with thiazide diuretics, adrenoblockers and inhibitors of an angiotensin-converting enzyme change of the mode of a drug dosing is not required.

Features of use:

It is not recommended to apply at children and teenagers up to 18 years due to the lack of sufficient clinical data. With care apply at an abnormal liver function, a syndrome of weakness of a sinus node (the expressed bradycardia, tachycardia), dekompensirovanny chronic heart failure, slight or moderate hypotension, an aortal stenosis, a mitral stenosis, a hypertrophic cardiomyopathy (especially obstructive), a diabetes mellitus, at advanced age.

During treatment it is necessary to control arterial pressure daily;

to exercise regular control of body weight and consumption of sodium; purpose of the corresponding diet. Maintenance of hygiene of teeth and regular consultations of the stomatologist (prevention of morbidity, bleeding and a hyperplasia of gums) is necessary.

For Amlodipin not characteristic the syndrome of "cancellation", however before the termination of treatment recommends a gradual dose decline. Amlodipin does not change in a blood plasma of potassium concentration, triglycerides, the general cholesterol, lipoproteids of low density, uric acid, creatinine and an urea nitrogen.

Use during pregnancy and feeding by a breast. Drug is contraindicated at pregnancy (safety of use is not established). In need of use during feeding by a breast it is necessary to stop feeding.

Influence on ability to manage vehicles or to work with difficult mechanisms. During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions as drug can cause dizziness and drowsiness (especially in an initiation of treatment).

 

Side effects:

From cardiovascular system: heartbeat, an asthma, the expressed lowering of arterial pressure, a vasculitis, rushes of blood to the person; seldom – stenocardia, a myocardial infarction, arrhythmias (fibrillation of auricles and ventricular tachycardia); very seldom – development or aggravation of heart failure, premature ventricular contraction.

From the central nervous system: headache, dizziness, increased fatigue, drowsiness, change of mood, spasm; seldom – an adynamy, a loss of consciousness, decrease in sensitivity to irritants, nervousness, paresthesias, a tremor, вертиго, sleeplessness, a depression; very seldom – an ataxy, apathy, agitation, amnesia.

From the alimentary system: nausea, vomiting, pains in epigastriums, a hyperbilirubinemia; seldom – increase in level of hepatic transaminases, an abnormal liver function, jaundice, pancreatitis, dryness in a mouth, a meteorism, a lock or diarrhea, a hyperplasia of gums; very seldom – gastritis, increase in appetite.

From urinogenital system: peripheral hypostases (anklebones and feet); seldom – sexual disturbances (including decrease in a potentiality), a pollakiuria, painful desires on an urination, a nocturia; very seldom – a dysuria, a polyuria.

From a musculoskeletal system: seldom – an arthralgia, arthrosis, a mialgiya (at prolonged use); very seldom – a myasthenia.

From integuments: very seldom – a xerodermia, an alopecia, dermatitis, a purpura, skin discoloration.

Allergic reactions: seldom – skin rash (including erythematic, makulopapulezny, a small tortoiseshell), an itch.

From an organ of sight: vision disorders, conjunctivitis, diplopia, eye pain; seldom – a xerophthalmia; very seldom – accommodation disturbance.

Others: seldom – диспноэ, a gynecomastia, a lithemia, a body increase/degrowth, thrombocytopenia, a leukopenia, a hyperglycemia, a sonitus, a dorsodynia, nasal bleeding, the increased sweating; very seldom – a cold clammy sweat, cough, rhinitis, a parosmiya, disturbance of flavoring feelings.

Interaction with other medicines:

Concentration of an amlodipin in blood is increased by inhibitors of a microsomal oxidation (the risk of development of side effects increases), reduce – inductors of a microsomal oxidation. The hypotensive effect of an amlodipin is weakened by non-steroidal anti-inflammatory drugs, especially indometacin (a delay of sodium and blockade of synthesis of prostaglandins kidneys), - adrenostimulyator, estrogen (a sodium delay), sympathomimetics; strengthen – Amiodaronum, quinidine, 1 adrenoblockers, neuroleptics and other blockers of calcium channels.

The hypotensive and anti-anginal effect of an amlodipin is strengthened by thiazide and "loopback" diuretics, - adrenoblockers, verapamil, inhibitors of an angiotensin-converting enzyme and nitrates.

Effects of an amlodipin reduce calcium drugs. The procaineamide, quinidine and other means causing lengthening of an interval of QT strengthen negative dromotropic effect and can increase risk of considerable lengthening of an interval of QT.

Amlodipin strengthens manifestations of side effect of drugs of lithium (nausea, vomiting, diarrhea, an ataxy, a tremor, a sonitus).

In blood grapefruit juice can slightly increase concentration of an amlodipin, however it is not followed by clinically significant lowering of arterial pressure.

Contraindications:

Hypersensitivity to an amlodipin or other derivatives of dihydropyridine, to auxiliary components of drug; heavy arterial hypotension (systolic arterial pressure <90 mm of mercury.), a collapse, cardiogenic shock, unstable stenocardia, the expressed stenosis of the mouth of an aorta, the pregnancy period, the feeding period a breast, age up to 18 years (efficiency and safety of use are not established).

Overdose:

Symptoms: excessive lowering of arterial pressure, reflex tachycardia, excessive peripheral vazodilatation. Treatment: to give to the patient a prone position with the raised legs. A gastric lavage, purpose of absorbent carbon (especially in the first 2 h after overdose), at a considerable lowering of arterial pressure – maintenance of functions of cardiovascular system, continuous monitoring of function of heart and lungs, control of volume of the circulating blood and a diuresis. For recovery of a tone of vessels – purpose of vasoconstrictors (in the absence of contraindications to their use). Symptoms of blockade of calcium channels are reduced by intravenous administration of calcium of a gluconate. The specific antidote is absent. The hemodialysis is inefficient.

Storage conditions:

To store in the dry, protected from light place at a temperature from 8 °C to 25 °C. To store in the place, unavailable to children.

Period of validity – 3 years.

Issue conditions:

According to the recipe

Packaging:

Tablets on 5 mg or 10 mg No. 10, No. 103, No. 30 in blisters in a box.