AMLODIPINE

Active material: Amlodipine
When ATH: C08CA01
CCF: Kalьcievыh channel blocker
ICD-10 codes (testimony): I10, I15, i20, I20.1, i25
When CSF: 01.03.02
Manufacturer: HEMOFARM A.D. (Serbia)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills from white to almost white, round, flat, with beveled edges.

Excipients: silicate microcrystalline cellulose, pre-gelatinized starch, magnesium stearate.

10 PC. – blisters (2) – packs cardboard.

Pharmacological action

Selective calcium channel blocker class II. The antihypertensive effect is due to a direct relaxing effect on vascular smooth muscle.. Expected, that the antianginal effect of amlodipine is due to its ability to dilate peripheral arterioles; this leads to a decrease in OPSS, reflex tachycardia does not occur. As a result, there is a decrease in myocardial oxygen demand and energy consumption by the heart muscle.. On the other hand, amlodipine, apparently, causes expansion of large-caliber coronary arteries and coronary arterioles as intact, and ischemic areas of the myocardium. This ensures the supply of oxygen to the myocardium during spasms of the coronary arteries..

Pharmacokinetics

When taken orally, it is absorbed from the gastrointestinal tract slowly and almost completely., C_max plasma levels reached within 6-9 no. Protein binding is 95-98%. Undergoes minimal first-pass metabolism and slow, but significant hepatic metabolism with the formation of metabolites with negligible pharmacological activity.

T_1/2 averages 35 h and with arterial hypertension can increase on average up to 48 no, elderly patients – to 65 h and with violations of liver function – to 60 no. Write mainly in the form of metabolites: 59-62% – kidney, 20-25% – through the intestine.

Testimony

Arterial hypertension (incl. in a combination therapy), stable angina, unstable angina, Prinzmetal angina.

Dosage regimen

For adults, when taken orally, the initial dose is 5 mg 1 time / day. If necessary, the dose may be increased.

The maximum dose: ingestion – 10 mg / day.

Side effect

Cardio-vascular system: peripheral edema, tachycardia, flushing of the skin; when used in high doses – hypotension, Arrhythmia, breathlessness.

From the digestive system: nausea, stomach ache; rarely – giperplaziya right.

From the central and peripheral nervous system: headache, fatigue, drowsiness, dizziness; prolonged use – paresthesia.

Allergic reactions: skin rash, itch.

Other: prolonged use – pain in the limbs.

Contraindications

Severe arterial hypotension, hypersensitivity to dihydropyridine derivatives.

Pregnancy and lactation

Safety of amlodipine during pregnancy and lactation (breast-feeding) not installed. Application is possible only in cases, when the intended benefits to the mother outweighs the potential risk to the fetus or child.

Cautions

Use with caution in violations of the liver and kidneys, with aortic stenosis. Elderly patients do not need dose reduction..

Amlodipine may be used to treat patients with dilated (non-ischemic) kardiomiopatiej, accompanied by a severe form of chronic heart failure.

Clinical data on the use of amlodipine in pediatrics are not available..

Drug Interactions

With the simultaneous use of amlodipine and calcium channel blockers, an increase in the hypotensive effect is possible..

With the simultaneous use of sympathomimetics, estrogen may reduce the antihypertensive effect due to sodium retention in the body.

With the simultaneous use of drugs for inhalation anesthesia, an increase in the hypotensive effect is possible..

With the simultaneous use of amiodarone, an increase in the antihypertensive effect is possible..

With the simultaneous use of lithium carbonate, manifestations of neurotoxicity are possible. (incl. nausea, vomiting, diarrhea, ataxia, trembling and/or tinnitus).

With simultaneous use, orlistat reduces the antihypertensive effect of amlodipine., that can lead to a significant improvement in HELL, development gipertoniceski kriza.

With the simultaneous use of indomethacin and other NSAIDs, it is possible to reduce the antihypertensive effect of amlodipine due to inhibition of prostaglandin synthesis in the kidneys and fluid retention under the influence of NSAIDs..

With the simultaneous use of quinidine, an increase in the antihypertensive effect is possible..