KORDIPIN RETARD

Active material: Nifedipine
When ATH: C08CA05
CCF: Kalьcievыh channel blocker. Antianginal and antihypertensive drug.
When CSF: 01.03.02
Manufacturer: KRKA d.d. (Slovenia)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Excipients: microcrystalline cellulose, glyceryl palmitostearate, talc, Colloidal anhydrous silica, sodium lauryl, magnesium stearate, povidone.

The composition of the shell: methacrylic acid, talc, Titanium dioxide, macrogol, quinoline yellow dye (E104).

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

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Selective calcium channel blocker class II, dihydropyridine derivative. It stops the flow of calcium into cardiomyocytes and vascular smooth muscle cells. It has antianginal and hypotensive action. It reduces the tone of smooth muscles of blood vessels. Extends the coronary and peripheral arteries, reduces peripheral vascular resistance, Blood pressure slightly – myocardial contractility, reduces afterload and myocardial oxygen demand. Improves coronary blood flow. Almost does not possess antiarrhythmic activity. Do not oppress the conductivity of the myocardium.

Pharmacokinetics

If ingestion is rapidly absorbed from the gastrointestinal tract. Metabolized in the “first pass” through the liver. Protein binding is 92-98%. It is metabolized in the liver with the formation of active metabolites. T_1/2 – about 2 no. Write mainly by the kidneys as metabolites in trace amounts in unchanged form; 20% is output through the intestine as metabolites.

Testimony

Prevention of angina attacks (incl. vasospastic angina), in some cases – relief of angina attacks; arterial hypertension, hypertensive crises; Raynaud's disease.

Dosage regimen

Individual. To be accepted into the initial dose – by 10 mg 3-4 times / day. If necessary, the dose is gradually increased until 20 mg 3-4 times / day. In special cases (variant angina, severe hypertension) a short time the dose can be increased to 30 mg 3-4 times / day. For relief of hypertensive crisis, and angina attack can be used for sublingual 10-20 mg (rarely 30 mg).

B / for relief of angina attack or hypertensive crisis – by 5 mg for 4-8 no.

Intracoronary for the relief of acute coronary artery spasm is administered bolus 100-200 g. Stenosis of major coronary arteries starting dose is 50-100 g.

The maximum dose: ingestion – 120 mg / day, at / in the introduction – 30 mg / day.

Side effect

Cardio-vascular system: flushing of the skin, feeling the heat, tachycardia, hypotension, peripheral edema; rarely – bradycardia, ventricular tachycardia, asistolija, increasing angina attacks.

From the digestive system: nausea, heartburn, diarrhea; rarely – deterioration in liver function; in a few cases – giperplaziya right. Chronic administration of high doses may dyspeptic symptoms, increase in liver transaminases, intrahepatic cholestasis.

From the central and peripheral nervous system: headache. Chronic administration of high doses may be paresthesia, muscle aches, tremor, disorders of the lungs, sleep disorders.

From the hematopoietic system: in a few cases – leukopenia, thrombocytopenia.

From the urinary system: increase in daily diuresis. Chronic administration of high doses may be impaired renal function.

On the part of the endocrine system: in a few cases – gynecomastia.

Allergic reactions: skin rash.

Local reactions: at / in a possible burning at the injection site.

During 1 minutes after intracoronary administration may be a manifestation of the negative inotropic effects of nifedipine, increase in heart rate, hypotension; These symptoms gradually disappear after 5-15 m.

Contraindications

Hypotension (systolic BP below 90 mmHg.), collapse, cardiogenic shock, severe heart failure, Heavy aortalnыy stenosis; Hypersensitivity to nifedipine.

Pregnancy and lactation

Adequate and well-controlled studies of the safety of nifedipine during pregnancy has not been. The use of nifedipine in pregnancy is not recommended.

Since nifedipine is excreted in breast milk, Avoid its use during lactation or to stop breastfeeding during treatment.

IN experimental studies It was found fetotoxic, fetotoksicheskoe and teratogenic action nifedipine.

Cautions

Nifedipine should be used only in a hospital under strict medical supervision in acute myocardial infarction, severe violations of cerebral circulation, diabetes, human liver and kidneys, malignant hypertension and hypovolemia, as well as in patients, hemodialysis. In patients with impaired liver and / or kidney disease should avoid the use of high doses of nifedipine. Elderly patients are more likely to decrease in cerebral blood flow due to the sharp peripheral vasodilatation.

When administered to accelerate the effect of nifedipine can chew.

When during the treatment of pain behind the breastbone nifedipine should be abolished. Cancelling nifedipine should be gradually, because the sudden discontinuation (especially after prolonged treatment) may develop withdrawal.

When intracoronary administration in the presence of stenosis of the two vessels can not enter the third nifedipine open vessel at risk of pronounced negative inotropic effects.

During the course of treatment to avoid alcohol because of the risk of excessive blood pressure lowering.

Effects on ability to drive vehicles and management mechanisms

At the beginning of treatment should avoid driving and other potentially dangerous activities, requiring quickness of psychomotor reactions. In the course of further treatment the degree of limitation is determined depending on individual tolerability of nifedipine.

Drug Interactions

While the use of antihypertensive drugs, Diuretics, phenothiazine derivatives increased antihypertensive effect of nifedipine.

While the use of anticholinergics may be impaired memory and attention in elderly patients.

While the use of beta-blockers may develop severe hypotension; in some cases – development of heart failure.

In an application with nitrates increase antianginal effect of nifedipine.

While the use of calcium supplementation decreases the effectiveness of nifedipine due to an antagonistic interaction, due to an increase in the concentration of calcium ions in the extracellular fluid.

There are cases of muscle weakness while the use of magnesium salts.

In an application with digoxin may slow excretion from the body and digoxin, Consequently, increase its concentration in blood plasma.

While the use of diltiazem increased antihypertensive effect.

While the use of theophylline may be changes in the concentration of theophylline in the blood plasma.

Rifampicin induces liver enzymes, speeding up the metabolism of nifedipine, which reduces its effectiveness.

In an application with phenobarbital, phenytoin, carbamazepine decreasing nifedipine concentration in blood plasma.

There are reports of increasing the concentration of nifedipine in blood plasma and increase of its AUC while the use of fluconazole, itraconazole.

In an application with fluoxetine may increase the side effects of nifedipine.

In some cases, while the use of quinidine is possible to reduce the concentration of quinidine plasma, and the abolition of nifedipine may be a significant increase in the concentration of quinidine, which is accompanied by elongation of the QT interval on an electrocardiogram.

Nifedipine concentration in blood plasma can rise moderately.

And cimetidine, less ranitidine, increase the concentration of nifedipine in the blood plasma, and, thus, enhance its antihypertensive effect.

Ethanol may increase the effects of nifedipine (Excessive hypotension), which causes dizziness and other adverse reactions.