Amlokardin

General characteristics. Structure:

Active agent: 5 mg or 10 mg of an amlodipin (in the form of a besilat) in 1 tablet.

Excipients: calcium hydrophosphate dihydrate, potato starch, starch 1500, calcium stearate, silicon dioxide colloid anhydrous, microcrystallic cellulose.

Pharmacological properties:

Pharmacodynamics. Amlodipin is the dihydropyridinic antagonist of calcium ions (a blocker of "slow" calcium channels) of the II generation. Blocks a transmembrane flow of calcium ions preferential in cells of unstriated muscles of vessels, and also in cardiomyocytes. Has anti-anginal and hypotensive effect. The mechanism of anti-hypertensive action is caused by the direct weakening impact on unstriated muscles of vessels. Thanks to the slow beginning of action and the prolonged effect does not cause the expressed arterial hypotension, providing at a single dose in days clinically significant smooth lowering of arterial pressure (ABP).

Amlodipin has anti-anginal effect due to expansion of peripheral arterioles and reduction of an afterload by heart, expansions of coronary vessels in not changed and in ischemic zones of a myocardium. Reduces degree of a hypertrophy of a myocardium of a left ventricle. Slows down aggregation of thrombocytes. Increases glomerular filtering, slightly raises a natriuresis and a diuresis. Unlike dihydropyridinic antagonists of calcium of the first generation амлодипин practically does not increase the level of catecholamines in a blood plasma and does not stimulate a renin-angiotenzinovuyu system.

Pharmacokinetics. It is slowly soaked up after intake. Meal does not influence absorption of an amlodipin. The maximum concentration in a blood plasma is reached in 6 - 12 h. Absolute bioavailability makes 64 - 80%.

At constant reception equilibrium concentration is created in 7 - 8 days. Distribution volume – 21 l/kg. Communication with proteins of plasma – 90 - 97%.

Amlodipin biotransformiruyetsya in a liver with formation of inactive metabolites. The elimination half-life averages 35 - 50 h. The general clearance makes 7 ml/min. It is excreted with urine as in an invariable look (10%), and in the form of metabolites (60%).

At elderly patients 65 years removal of an amlodipin are more senior it is slowed down (T1/2 - 65 h) in comparison with young patients, however the difference has no clinical value.

At patients with a liver failure lengthening of T1/2 to 60 h is noted (it is supposed that at long appointment cumulation of drug in an organism will be higher). Similar parameters of increase T1/2 are observed also at heavy chronic heart failure. At a renal failure of essential changes of pharmacokinetics of an amlodipin it is noted. At a hemodialysis is not removed.

Indications to use:

Arterial hypertension (monotherapy or in a combination with other hypotensive medicines), stenocardia stable and vasospastic (Printsmetala), including at patients, resistant to therapy by nitrates or beta adrenoblockers.

Route of administration and doses:

Inside, once, irrespective of meal. An initial dose - 5 mg/days. If necessary in 7 – 8 days the dose is raised to maximum - 10 mg/days. The maximum therapeutic effect develops within 8 weeks.

Features of use:

With care to apply in operating time to drivers of vehicles and people whose profession is connected with the increased concentration of attention (in an initiation of treatment dizziness and drowsiness are possible).

Side effects:

From cardiovascular system and blood: often peripheral hypostases (anklebones and feet), dermahemia of the person, heartbeat; seldom - disturbances of a rhythm (bradycardia, ventricular tachycardia, an atrial flutter), thorax pain, hypotension (including orthostatic); very seldom – development or aggravation of heart failure, premature ventricular contraction, migraine.

From a nervous system and sense bodys: fatigue, headache, dizziness, drowsiness; seldom - fatigue, an adynamy, change of mood, a vision disorder.

From urinogenital system: seldom – a pollakiuria, painful desires on an urination, a nocturia, disturbance of sexual function (including decrease in a potentiality), very seldom a dysuria, a polyuria.

From the alimentary system: nausea, vomiting, pains in epigastriums; seldom – the increase in level of hepatic transaminases, jaundice (caused by a cholestasia), pancreatitis, dryness in a mouth, a meteorism, a hyperplasia of gums, a lock or diarrhea; very seldom – gastritis, increase in appetite.

From respiratory system: seldom - an asthma.

From a musculoskeletal system: seldom - an arthralgia, a mialgiya, paresthesia and extremity pain (at prolonged use).

From integuments: rashes, an itch, it is rare - a mnogoformny erythema.

Others: seldom - a hyperplasia of gums, a gynecomastia.

Interaction with other medicines:

Inhibitors of a microsomal oxidation increase concentration of an amlodipin in a blood plasma (strengthening risk of development of side effects), and inductors of microsomal enzymes – reduce.

The hypotensive effect of medicine is weakened by NPVP, especially indometacin (at the expense of a delay of sodium and blockade of synthesis of prostaglandins kidneys), alpha адреномиметики, sympathomimetics are oestrogenic (at the expense of a sodium delay).

Thiazide and loopback diuretics, beta adrenoblockers, verapamil, APF inhibitors and nitrates strengthen anti-anginal and hypotensive effects of medicine.

Amiodaronum, quinidine, alfa1-adrenoblockers, antipsychotic drugs (neuroleptics) can strengthen hypotensive effect of medicine.

At simultaneous use with drugs of lithium strengthening of manifestations of their neurotoxicity (nausea, vomiting, diarrhea, an ataxy, a tremor, a sonitus) is possible.

Drugs of calcium can reduce effects of medicine.

The procaineamide, quinidine and other medicines causing lengthening of an interval of QT strengthen a negative inotropic effect and can increase risk of considerable lengthening of an interval of QT.

Amlokardin does not exert impact on pharmacokinetic parameters of digoxin and warfarin.

The pharmacokinetics of medicine does not change at co-administration with Cimetidinum.

Contraindications:

Hypersensitivity (including to other dihydropyridines), arterial hypotension (less than 90 mm hg), cardiogenic shock, an acute myocardial infarction, pregnancy, the lactation period.

Restrictions to use. Unstable stenocardia, the expressed aortal stenosis, heart failure, chronic heart failure of the III-IV Art., an abnormal liver function, age up to 18 years (safety and efficiency of use are not defined).

Overdose:

Symptoms: an excessive peripheral vazodilatation, the expressed and long decrease in the ABP, tachycardia.

Treatment: a gastric lavage, purpose of absorbent carbon, giving to the patient of horizontal position with the raised legs, monitoring of indicators of cardiac performance and lungs, control of the volume of the circulating blood (VCB) and a diuresis; a symptomatic and maintenance therapy, in/in administration of liquids, a gluconate of calcium, a dopamine, Phenylephrinum. The hemodialysis is not effective.

Storage conditions:

In the place protected from light and moisture, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use medicine after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

In a blister strip packaging No. 10, in packaging No. 10 x 3.