Nifedipine pills 10 mg 50 pcs
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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 pass" 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.
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 during lactation should be avoided or breastfeeding should be discontinued during treatment. Experimental studies have identified embryotoxic, fetotoxic and teratogenic effects of nifedipine.
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, you can apply sublingually 10-20 mg (rarely 30 mg). In / in for relief of angina pectoris or hypertensive crisis - 5 mg for 4-8 hours.Intracoronary for relief of acute spasms of the coronary arteries, a bolus of 100-200 mcg is administered With stenoses of large coronary vessels, the initial dose is 50-100 mcg. The maximum daily dose: 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 part of 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. From the side of the central nervous system and peripheral nervous system: headache. With long-term administration in high doses, paresthesias, muscle pain, tremor, mild visual disturbances, and sleep disorders are possible. From the hemopoietic system: in isolated cases - leukopenia, thrombocytopenia. From the urinary system: an increase in daily diuresis. With long-term administration in high doses, renal dysfunction is possible. On the part of the endocrine system: in isolated cases - gynecomastia. Allergic reactions: skin rash. Local reactions: with a / in the introduction of a possible burning sensation at the injection site. Within 1 min after intracoronary administration, a manifestation of the negative inotropic effect of nifedipine, an increase in heart rate, arterial hypotension is possible; 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. With simultaneous use with anticholinergic agents, memory and attention disorders in elderly patients are possible. With the simultaneous use of beta-blockers may develop severe hypotension; in some cases - the development of heart failure. With simultaneous use with nitrates, the antianginal effect of nifedipine is enhanced. With simultaneous use with calcium preparations, the effectiveness of nifedipine is reduced due to the antagonistic interaction caused by an increase in the concentration of calcium ions in the extracellular fluid. Cases of the development of muscle weakness with simultaneous use with magnesium salts are described. With simultaneous use with digoxin, it is possible to slow the elimination of digoxin from the body and, consequently, increase its concentration in the blood plasma. With simultaneous use with diltiazem increases antihypertensive effect. With simultaneous use with theophylline, changes in theophylline concentration in the blood plasma are possible. Rifampicin induces the activity of liver enzymes, accelerating the metabolism of nifedipine, which leads to a decrease in its effectiveness. With simultaneous use with phenobarbital, phenytoin, carbamazepine decreases the concentration of nifedipine in the blood plasma. There are reports of an increase in the concentration of nifedipine in the blood plasma and an increase in its AUC with simultaneous use with fluconazole, itraconazole. With simultaneous use with fluoxetine may increase the side effects of nifedipine.In some cases, the simultaneous use of quinidine may decrease the concentration of quinidine in the blood plasma, and with the abolition of nifedipine, a significant increase in the concentration of quinidine is possible, which is accompanied by 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, enhance its antihypertensive effect. Ethanol may increase the effect of nifedipine (excessive 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 severe peripheral vasodilation. When ingested to accelerate the effect nifedipine can be chewed. If you appear on the background of the treatment of pain in the sternum nifedipine should be abolished. Cancel nifedipine should be gradual, because with a sudden cessation of the reception (especially after long-term treatment) may develop withdrawal syndrome. When intracoronary administration in the presence of stenosis of two vessels can not enter nifedipine in the third open vessel because of the danger of pronounced negative inotropic action. During the course of treatment, avoid 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, you should avoid driving vehicles and other potentially hazardous activities that require the speed of psychomotor reactions. In the course of further treatment, the degree of restriction is determined depending on the individual tolerance of nifedipine.