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Active ingredients

Nifedipine

Release form

Pills

Composition

Nifedipine 20 mgvspomogatelnye substances: microcrystalline cellulose, glyceryl palmitostearate, talc, colloidal anhydrous silica, sodium lauryl sulphate, magnesium stearate, povidon.sostav shell: copolymer of methacrylic acid, talc, titanium dioxide, macrogol, quinoline yellow dye (E104).

Pharmacological effect

A selective class II calcium channel blocker derived from dihydropyridine. Inhibits calcium intake in cardiomyocytes and vascular smooth muscle cells. It has antianginal and hypotensive effects. Reduces the tone of the smooth muscles of blood vessels. It expands the coronary and peripheral arteries, decreases the round focal system, the arterial pressure and, slightly, the contractility of the myocardium, decreases the afterload and myocardial oxygen demand. Improves coronary blood flow. Practically does not possess antiarrhythmic activity. Does not inhibit myocardial conductivity.

Pharmacokinetics

When ingestion is rapidly absorbed from the digestive tract. Metabolized by first passing through the liver. Binding to proteins is 92-98%. Metabolized in the liver to form inactive metabolites. T1 / 2 - about 2 hours. It is mainly excreted by the kidneys as metabolites and in trace amounts in unchanged form; 20% is excreted through the intestines as metabolites.

Indications

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

Contraindications

Hypotension (systolic blood pressure below 90 mm Hg), collapse, cardiogenic shock, severe heart failure, severe aortic stenosis; Hypersensitivity to nifedipine.

Precautionary measures

During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects.The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.

Use during pregnancy and lactation

Adequate and strictly controlled studies of the safety of nifedipine during pregnancy have not been conducted. The use of nifedipine during pregnancy is not recommended. Since nifedipine is excreted in breast milk, its use should be avoided during lactation or breastfeeding should be stopped during treatment. Embryotoxic, fetotoxic and teratogenic effects of nifedipine have been identified in experimental studies.

Dosage and administration

Individual. For oral administration, the initial dose is 10 mg 3-4 times / day. If necessary, gradually increase the dose to 20 mg 3-4 times / day. In special cases (variant angina, severe arterial hypertension) for a short time the dose can be increased to 30 mg 3-4 times / day. For the relief of hypertensive crisis, as well as an attack of angina pectoris, it is possible to apply sublingually 10-20 mg (rarely 30 mg). V / B for the relief of an attack of angina pectoris or hypertensive crisis - 5 mg for 4-8 h. arteries injected with a bolus of 100–200 mcg. With stenoses of large coronary vessels, the initial dose is 50-100 mcg. Maximum daily doses: when administered orally - 120 mg, with a / in the introduction - 30 mg.

Side effects

Since the cardiovascular system: skin hyperemia, a feeling of warmth, tachycardia, arterial hypotension, peripheral edema; rarely - bradycardia, ventricular tachycardia, asystole, increased angina attacks. On the digestive system: nausea, heartburn, diarrhea; rarely, impaired liver function; in rare cases - gingival hyperplasia. With long-term administration in high doses, dyspeptic symptoms, increased activity of hepatic transaminases, intrahepatic cholestasis are possible. On the CNS and peripheral nervous system: headache. With long-term administration in high doses, paresthesia, muscle pain, tremor, mild visual disturbances, sleep disturbances are possible. From the hematopoietic system: in isolated cases - leukopenia, thrombocytopenia. From the urinary system: an increase in daily urine output.With long-term intake in high doses, renal dysfunction is possible. From the endocrine system: in isolated cases - gynecomastia. Allergic reactions: skin rash. Local reactions: intravenous injection may cause a burning sensation at the injection site. manifestation of a negative inotropic effect of nifedipine, an increase in heart rate, arterial hypotension; these symptoms gradually disappear after 5-15 minutes.

Interaction with other drugs

With simultaneous use with antihypertensive drugs, diuretics, phenothiazine derivatives, the antihypertensive effect of nifedipine is enhanced. If used concurrently with anticholinergics, impaired memory and attention are possible in elderly patients. If used simultaneously with beta-adrenergic blockers, severe arterial hypotension may develop; in some cases - the development of heart failure. When used simultaneously with nitrates, the antianginal effect of nifedipine is enhanced. When used with calcium preparations, the effectiveness of nifedipine is reduced due to antagonistic interaction caused by an increase in the concentration of calcium ions in the extracellular fluid. Cases of muscular weakness with simultaneous use are described with magnesium salts. When used simultaneously with digoxin, it is possible to slow the elimination of digoxin from It also increases antihypertensive effects. When used simultaneously with theophylline, theophylline concentration in plasma can be changed. Rifampicin induces the activity of liver enzymes, accelerating nifedipine metabolism, which leads to a decrease in its effectiveness .In simultaneous use with phenobarbital, phenytoin, carbamazepine, the concentration of nifedipine in the blood plasma decreases. There are reports of an increase and concentration of nifedipine in the blood plasma and an increase in its AUC with simultaneous use with fluconazole, itraconazole. With simultaneous use with fluoxetine, the side effect of nifedipine may be increased. a significant increase in the concentration of quinidine, which is accompanied by a prolongation of the QT interval on the ECG. Cimetidine and, to a lesser extent, ranitidine,increase the concentration of nifedipine in the blood plasma and, thus, increase its antihypertensive effect. Ethanol may enhance the effect of nifedipine (excessive arterial hypotension), which causes dizziness and other undesirable reactions.

special instructions

Nifedipine should be used only in the clinic under the strict supervision of a physician in acute myocardial infarction, severe cerebral circulation disorders, diabetes mellitus, abnormal liver function and kidney function, in case of malignant hypertension and hypovolemia, as well as in patients undergoing hemodialysis. In patients with impaired liver and / or kidney function, the use of high doses of nifedipine should be avoided. Elderly patients are more likely to decrease cerebral blood flow due to abrupt peripheral vasodilation. When ingested to accelerate the effect, nifedipine can be chewed. When niphedipine appears in the background of chest pain treatment, it should be canceled. Nifedipine should be canceled gradually, since abrupt discontinuation (especially after long-term treatment) may lead to the development of withdrawal syndrome. When intracoronary administration is present in the presence of stenosis of two vessels, nifedipine cannot be administered to the third open vessel due to the danger of pronounced negative inotropic effect. allow alcohol consumption due to the risk of an excessive decrease in blood pressure. Impact on the ability to drive vehicles and control mechanisms. At the beginning of treatment should be causeway driving vehicles and other potentially hazardous activities requiring psychomotor speed reactions. In the course of further treatment, the degree of restriction is determined depending on the individual tolerance of nifedipine.

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