Amlodipin

General characteristics. Structure:

Active agent: амлодипин (in the form of a bezilat) 10 mg; 5 mg.

Pharmacological properties:

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; it 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. At intake it is absorbed from a GIT slowly and almost completely, Cmax in a blood plasma is reached during 6-9 h. Linkng with proteins makes 95-98%. Is exposed to the minimum metabolism at the first passing through a liver and to slow, but considerable hepatic metabolism with formation of metabolites with insignificant pharmacological activity.
T1/2 averages 35 h and at arterial hypertension can increase on average to 48 h, at elderly patients - to 65 h and at abnormal liver functions - to 60 h. It is removed mainly in the form of metabolites: 59-62% - kidneys, 20-25% - through intestines.

Indications to use:

Arterial hypertension (including as a part of a combination therapy), stable stenocardia, unstable stenocardia, Printsmetal's stenocardia.

Route of administration and doses:

For adults at intake the initial dose makes 5 mg of 1 times/days. If necessary the dose can be increased.
Maximum dose: at intake - 10 mg/days.

Features of use:

With care apply at abnormal liver functions and kidneys, at a stenosis of the mouth of an aorta. It is not required to patients of advanced age of a dose decline.
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 in pediatrics are absent.

Side effects:

- From cardiovascular system: peripheral hypostases, tachycardia, hyperemia of integuments; at use in high doses - arterial hypotension, arrhythmias, short wind.
- From the alimentary system: nausea, abdominal pains; seldom - a hyperplasia of gums.
- From TsNS and a peripheral nervous system: headache, fatigue, drowsiness, dizziness; at prolonged use - paresthesia.
- Allergic reactions: skin rash, itch.
- Other: at prolonged use - extremity pain.

Interaction with other medicines:

At simultaneous use of an amlodipin and blockers of calcium channels strengthening of hypotensive action is possible.
At simultaneous use of sympathomimetics, estrogen reduction of anti-hypertensive action owing to a sodium delay in an organism is possible.
At simultaneous use of means for an inhalation anesthesia strengthening of hypotensive effect is possible.
At simultaneous use of Amiodaronum strengthening of anti-hypertensive action is possible.
At simultaneous use of lithium of a carbonate manifestations of a neurotoxicity are possible (including nausea, vomiting, diarrhea, an ataxy, trembling and/or a sonitus).
At simultaneous use орлистат reduces anti-hypertensive action of an amlodipin that can lead to substantial increase of the ABP, development of hypertensive crisis.
At simultaneous use of indometacin and other NPVS reduction of anti-hypertensive action of an amlodipin owing to oppression of synthesis of prostaglandins in kidneys and liquid delays under the influence of NPVS is possible.
At simultaneous use of quinidine strengthening of anti-hypertensive action is possible.

Contraindications:

The expressed arterial hypotension, hypersensitivity to dihydropyridine derivatives.

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

Use at abnormal liver functions
With care apply at abnormal liver functions.

Use at renal failures
With care apply at renal failures.

Use for elderly patients
It is not required to patients of advanced age of a dose decline.

Use for children
Clinical data on use of an amlodipin in pediatrics are absent.

Overdose:

There are no data.

Storage conditions:

To store in the dry place far from direct sunshine, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets of 10 mg: 30 pieces.