Amlodipin

General characteristics. Structure:

Active ingredient: 3,73 mg of an amlodipin of a besilat (in terms of амлодипин 2,5 mg); 7,450 (5 mg); 14,908 mg (10 mg).

Excipients of an amlodipin: cellulose microcrystallic, calcium phosphate double-base (anhydrous), sodium glikolit starch, magnesium stearate.

Hypotensive and antiarrhythmic medicine.

Pharmacological properties:

Pharmacodynamics. The selection blocker of calcium channels of the II class. Anti-hypertensive action is caused by the direct weakening impact on unstriated muscles of vessels. It is supposed that anti-anginal action of an amlodipin is connected with its ability to expand peripheral arterioles; what leads to reduction of OPSS, reflex tachycardia at the same time does not arise. Decrease in need of a myocardium for oxygen and energy consumption by a cardiac muscle results. On the other hand, амлодипин, apparently, causes expansion of coronary arteries of large caliber and coronary arterioles of both intact, and ischemic sites of a myocardium. It provides intake of oxygen to a myocardium at spasms of coronary arteries.

Pharmacokinetics. After intake it is slowly absorbed from a GIT (irrespective of meal), bioavailability makes 60–65%, _Cmax in blood is observed in 6–12 h. Concentration of stable balance in plasma is reached in 7–8 days after constant reception. Has the high volume of distribution — about 20 l/kg and well contacts proteins — more than 95%. It is metabolized in a liver with formation of inactive metabolites. Less than 10% of a dose 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 GEB. _T1/2 makes 35–45 h, patients with arterial hypertension have 48 h, elderly patients have 65 h, at a liver failure — to 60 h, at a renal failure — does not change. Is not removed at a hemodialysis.

Indications to use:

Arterial hypertension (in the form of monotherapy and in a combination with thiazide diuretics, APF inhibitors, alpha and beta adrenoblockers); stable and unstable stenocardia (including Printsmetal's stenocardia).

Route of administration and doses:

Accept inside irrespective of meal, washing down with enough water.

At arterial hypertension амлодипин appoint 2.5 mg/days in an initial dose; for prevention of attacks of stenocardia - 5 mg/days. The recommended maintenance dose at arterial hypertension and stenocardia - 5 mg/days. If necessary the daily dose can be increased to 10 mg.

It is not recommended to exceed an initial daily dose at patients with an abnormal liver function, patients of advanced age and at patients with reduced body weight.

The maximum daily dose - 10 mg. At simultaneous use of thiazide diuretics, beta adrenoblockers or APF inhibitors of correction of the mode of dosing of an amlodipin it is not required.

Features of use:

With care apply at abnormal liver functions, at a stenosis of the mouth of an aorta, at chronic heart failure. To patients with renal failures, and also to patients of advanced age of a dose decline it is not required. Use of an amlodipin for treatment of patients with the dilatatsionny (not ischemic) cardiomyopathy which is followed by a severe form of chronic heart failure is possible.

Clinical data on use of an amlodipin at children are absent.

Safety of use of an amlodipin at pregnancy and in the period of a lactation is not established. Use is possible only when the estimated advantage for mother exceeds potential risk for a fruit or the child.

Side effects:

From outside to a cardiovascular sistemy:serdtsebiyenia, asthma, excessive decrease in the ABP, syncope, vasculitis, hypostases of anklebones and feet, inflows; seldom - disturbances of a cordial rhythm (bradycardia, ventricular tachycardia, an atrial flutter), thorax pains, orthostatic hypotension.

From TsNS and peripheral nervous system: dizziness, headache, drowsiness, increased fatigue; seldom - an adynamy, change of mood, a spasm, a mialgiya, a vision disorder, paresthesias.

From the alimentary system: dyspepsia phenomena, nausea, abdominal pains; seldom - increase in activity of hepatic transaminases, the jaundice (caused by an intra hepatic cholestasia), a hyperplasia of gums, pancreatitis, a food faddism, dryness in a mouth.

From system of a hemopoiesis: seldom - thrombocytopenia, a leukopenia.

Dermatological reactions: skin rash, itch; seldom - a multiformny erythema, skin discoloration.

Others: seldom - a gynecomastia, impotence, increase of an urination, увеличние / decrease in body weight.

Interaction with other medicines:

At simultaneous use of an amlodipin with other anti-hypertensive drugs strengthening of hypotensive action is possible; with means for an inhalation anesthesia - strengthening of hypotensive action is possible; with lithium drugs - manifestations of a neurotoxicity, including nausea, vomiting, diarrhea, an ataxy, trembling and/or a sonitus are possible; with sympathomimetics - decrease in hypotensive action is possible.

Indometacin and other NPVS can reduce hypotensive action of an amlodipin, suppressing synthesis of prostaglandins in kidneys and/or causing a liquid delay.

Simultaneous use of an amlodipin and digoxin does not change the level of concentration of digoxin in blood serum and renal clearance of digoxin.

Combined use of an amlodipin and Cimetidinum does not change pharmacokinetics of an amlodipin.

Co-administration of an amlodipin significantly did not change effect of warfarin to a prothrombin time at healthy male volunteers.

At combined use with drugs of lithium manifestation of a neurotoxicity is possible.

Contraindications:

The expressed arterial hypotension. Hypersensitivity to dihydropyridine derivatives.

Overdose:

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

Treatment: 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 recovery of a tone of vessels — purpose of vasoconstrictive drugs (in the absence of contraindications to their use); for elimination of effects of blockade of calcium channels — in/in introduction of a gluconate of calcium. The hemodialysis is inefficient.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above +25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 20 or 30 tablets in banks polymeric. One bank together with a leaf insert in a pack.

On 10 tablets in a blister strip packaging. 2 or 3 blister strip packagings together with a leaf insert in a pack.