Vero-amlodipin

General characteristics. Structure:

Acting substance: амлодипин (in the form of a bezilat) 5 mg or 10 mg;
excipients: potato starch, lactose, cellulose microcrystallic, magnesium stearate, calcium stearate.

Description: tablets of color, white or white with a cream shade, the easy mramornost is allowed.

Pharmacological properties:

Pharmacodynamics. Derivative dihydropyridine. Possesses anti-hypertensive, anti-anginal action. Blocks receipt of calcium ions through cellular membranes in smooth muscle cells of a myocardium and vessels.
The mechanism of hypotensive action is caused by the direct weakening impact on unstriated muscles of vessels. The anti-anginal effect of drug is caused by ability to expand peripheral arterioles that leads to decrease in the general peripheric vascular resistance. Reduction of load of heart leads to decrease in need of a myocardium for oxygen. Under the influence of drug due to expansion of coronary arteries intake of oxygen in a myocardium (increases especially at vasospastic stenocardia).

Does not exert adverse impact on a metabolism and lipids of a blood plasma, has anti-atherosclerotic, antitrombotichesky activity, raises a glomerular filtration rate, possesses a weak natriuretic effect. At a diabetic nephropathy does not increase expressiveness of a microalbuminuria.

Pharmacokinetics. After intake the maximum concentration of drug in blood in 6 - 12 hours is slowly absorbed from digestive tract (90%) irrespective of meal. Concentration of stable balance of drug in a blood plasma is reached in 7–8 days after its constant reception. Distribution volume — about 20 l/kg; bioavailability — 60–65%, communication with proteins of a blood plasma — more than 95%. A drug elimination half-life — 35–45 hours that allows to appoint it once a day. It is metabolized generally in a liver with formation of inactive metabolites. Less than 10% of the dose accepted inside are removed in not changed look, about 60% are excreted by kidneys in the form of inactive metabolites; 20–25% are removed in the form of metabolites with bile and through intestines, and also with breast milk. Gets through a blood-brain barrier. The elimination half-life at patients with arterial hypertension — 48 hours, at elderly patients increases till 65 o'clock, at a liver failure — till 60 o'clock, at a renal failure — does not change. At a hemodialysis is not removed.

Indications to use:

Aterialny hypertensia (in the form of mono - and a combination therapy);
stable stenocardia and vasospastic stenocardia.

Route of administration and doses:

Initial dose: as an antihypertensive — 2,5 mg (especially thin and elderly patient, the patient with an abnormal liver function and as a part of complex therapy); as anti-anginal means — 5 mg (it is recommended to elderly patients and patients with an abnormal liver function). At arterial hypertension and stenocardia — 5 mg a day. If necessary the daily dose can be increased to 10 mg a day. The maximum daily dose — 10 mg. Any correction of a dose of Vero-amlodipin at simultaneous use of thiazide diuretics, beta adrenoblockers or APF inhibitors is not required.

Features of use:

 During treatment control of body weight and a diet, especially sodium consumption, maintenance of hygiene of teeth and frequentation of the stomatologist (prevention of morbidity, bleeding and growth of gums) is necessary.

Experience of use for children is absent. Does not exert impact on ability of control of motor transport and moving mechanisms.

Side effects:

 From cardiovascular system: heartbeat, an asthma, the expressed lowering of arterial pressure, a faint, a vasculitis, hypostases (puffiness of anklebones and feet), is rare — disturbances of a rhythm (bradycardia, ventricular tachycardia, an atrial flutter), thorax pain, orthostatic hypotension.

 From the central nervous system: dizziness, a headache, "inflows" of blood to the person, drowsiness, the increased fatigue, is rare — change of mood, an adynamy, myotonia, a mialgiya, a vision disorder, paresthesias.

 From digestive tract: dispeptic frustration, nausea, abdominal pains; seldom: the increase in level of "hepatic" transaminases and jaundice (caused by a cholestasia), pancreatitis, a food faddism, dryness in a mouth, change of the mode of defecation.

 From integuments: allergic reactions (skin rash, itch); seldom: multiformny exudative erythema, skin discoloration.

 From other bodies: seldom — a gynecomastia, decrease in a potentiality, a polylithemia, a hyperplasia of gums, increase/decrease in body weight, thrombocytopenia, a leukopenia, an arthralgia, extremity pain (at prolonged use).

Interaction with other medicines:

Let's combine with thiazide diuretics, alpha and beta adrenoblockers, APF inhibitors, nitrates, non-steroidal anti-inflammatory drugs, antibiotics, hypoglycemic drugs for intake. Inhibitors of a microsomal oxidation increase concentration in plasma, strengthening risk of development of side effects, and inductors of microsomal enzymes of a liver reduce.

Simultaneous use of Amlodipin and digoxin does not change the level of concentration of digoxin in blood serum and renal clearance of digoxin; Cimetidinum — does not change Amlodipin's pharmacokinetics; warfarin — did not change action to a prothrombin time at zdorovykhmuzhchin-volunteers. Hypotensive effect non-steroidal anti-inflammatory drugs, especially indometacin (a delay of sodium and blocking of synthesis of prostaglandins kidneys) weaken, sympathomimetics and estrogen (a sodium delay). Means for inhalation anesthesia (derivatives of hydrocarbons), Amiodaronum, quinidine, blockers of "slow" calcium channels can strengthen hypotensive effect. At combined use with drugs of lithium manifestation of a neurotoxicity is possible.

Thiazide and "loopback" diuretics, beta adrenoblockers, verapamil, APF inhibitors and nitrates increase anti-anginal and hypotensive action.

Contraindications:

- hypersensitivity to an amlodipin and other derivatives of dihydropyridine;
- heavy arterial hypotension, age up to 18 years (efficiency and safety are not established).

With care: appoint to patients with an abnormal liver function and kidneys, chronic heart failure of II and III degrees, a sick sinus syndrome (the expressed bradycardia, tachycardia), an aortal and mitral stenosis, a hypertrophic cardiomyopathy with obstruction of an output path of a left ventricle, an acute myocardial infarction (and  within 1 month after), slight and moderate arterial hypotension, advanced age.

Overdose:

Symptoms: the expressed lowering of arterial pressure, tachycardia, an excessive peripheral vazodilatation.

Treatment: a gastric lavage, purpose of absorbent carbon, maintenance of function of cardiovascular system, monitoring of indicators of cardiac performance and lungs, sublime position of extremities, control of volume of the circulating blood and a diuresis. For a vosstnovleniye of a tone of vessels — use of vasoconstrictive drugs (in the absence of contraindications to their use); for elimination of effects of blockade of calcium channels — intravenous administration of a gluconate of calcium. The hemodialysis is not effective.

Storage conditions:

List B. In dry, protected from light and the place, unavailable to children. A period of validity - 2 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,005 g and 0,01 g. On 10 tablets in a blister strip packaging. On 10 or 30 tablets in bank of orange glass. Each can, 1 or 3 blister strip packagings with the application instruction in a pack.