Nifedipine 10m coated pills N50
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Active ingredients
Nifedipine
Release form
Pills
Composition
Nifedipine 10 mg
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 gastrointestinal 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 administration 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. Within 1 min after intracoronary administration, it is possible manifestation of the negative inotropic action of nifedipine,increase in heart rate, hypotension; these symptoms gradually disappear after 5-15 minutes.
Overdose
Symptoms: headache, flushing of the skin of the face, lowering blood pressure, depression of the sinus node, bradycardia, arrhythmia. Treatment: gastric lavage with the appointment of activated carbon, symptomatic therapy aimed at stabilizing the activity of the cardiovascular system. Calcium is the antidote; slow intravenous administration of 10% calcium chloride or calcium gluconate is indicated, followed by a switch to a long-term infusion. With a pronounced decrease in blood pressure - intravenous dopamine or dobutamine. At disturbances of conductivity, administration of atropine, isoprenaline or the establishment of an artificial pacemaker is indicated. With the development of heart failure, intravenous administration of strophanthin. Catecholamines should be used only when life-threatening blood circulation is insufficient (due to their reduced efficiency, a high dosage is required, and as a result, the risk of an increased tendency to arrhythmia due to intoxication increases.) Controlling blood glucose and electrolytes (potassium ions, calcium) is recommended, since insulin release is disturbed. Hemodialysis is ineffective.
Interaction with other drugs
With simultaneous use with antihypertensive drugs, diuretics, phenothiazine derivatives, the antihypertensive effect of nifedipine is enhanced. If used simultaneously 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 rganizma and thereforeincreasing its concentration in blood plasma. When used simultaneously with diltiazem, the antihypertensive effect is enhanced. If used simultaneously with theophylline, changes in theophylline concentration in the blood plasma are possible. Phenobarbital, phenytoin, carbamazepine decreases the concentration of nifedipine in the blood plasma. There are reports of an increase in the concentration of nifedipine 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 enhanced. In some cases, while using quinidine, the concentration of quinidine in the blood plasma may decrease, that is accompanied by prolongation of the QT interval on the ECG. Tsimetidin and, to a lesser extent, ranitidine, increase the concentration of nifedipine in the blood plasma and, thus, they enhance 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 for acute myocardial infarction, severe cerebral circulation disorders, diabetes mellitus, abnormal liver and kidney function, for 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 discontinued 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 injected into the third open vessel due tothe danger of a pronounced negative inotropic effect. During the course of a course of treatment, avoid alcohol consumption due to the risk of an excessive decrease in BP. In the course of further treatment, the degree of restriction is determined depending on the individual tolerance of nifedipine.