TB Phenihydinum. 0,01 No. 50

General characteristics. Structure:

Active ingredient: nifedipine.

Chemical: 1,4-Digidro-2,6-dimetil-4-(2 nitrophenyl) - 3,5-pyridine dicarboxylic acid dimethyl ether.

Pharmacological properties:

The selection blocker of calcium channels of the II class, derivative dihydropyridine. Slows down intake of calcium in cardiomyocytes and cells of smooth muscles of vessels. Has anti-anginal and hypotensive effect. Reduces a tone of smooth muscles of vessels. Expands coronary and peripheral arteries, reduces OPSS, the ABP and it is insignificant - contractility of a myocardium, reduces an afterload and the need of a myocardium for oxygen. Improves a coronary blood stream. Practically has no antiarrhytmic activity. Conductivity of a myocardium does not oppress.

Pharmacokinetics. At intake it is quickly soaked up from a GIT. Is exposed to metabolism at "the first passing" through a liver. Linkng with proteins makes 92-98%. It is metabolized in a liver with formation of inactive metabolites. T1/2 is about 2 h. It is removed preferential by kidneys in the form of metabolites and in trace quantities in not changed look; 20% are removed through intestines in the form of metabolites.

Indications to use:

Prevention of attacks of stenocardia (including vasospastic stenocardia), in some cases - stopping of attacks of stenocardia; arterial hypertension, hypertensive crises; Raynaud's disease.

Route of administration and doses:

Individual. For intake an initial dose - on 10 mg of 3-4 times/days. If necessary the dose is gradually increased to 20 mg of 3-4 times/days. In special cases (alternative stenocardia, heavy arterial hypertension) for a short time it is possible to increase a dose to 30 mg of 3-4 times/days. It is possible to apply to stopping of hypertensive crisis, and also an attack of stenocardia sublingual on 10-20 mg (seldom 30 mg). In/in for stopping of an attack of stenocardia or hypertensive crisis - on 5 mg during 4-8 h Vnutrikoronarno for stopping of acute spasms of coronary arteries enter a bolus 100-200 mkg. At stenoses of large coronary vessels the initial dose makes 50-100 mkg. Maximum doses: at intake - 120 mg/days, at in introduction - 30 mg/days.

Features of use:

Nifedipine should be applied only in the conditions of clinic under strict control of the doctor at an acute myocardial infarction, heavy disturbances of cerebral circulation, a diabetes mellitus, abnormal liver functions and kidneys, at malignant arterial hypertension and a hypovolemia, and also at the patients who are on a hemodialysis. At patients with abnormal liver functions and/or kidneys it is necessary to avoid use of nifedipine in high doses. At patients of advanced age reduction of a cerebral blood-groove because of a sharp peripheral vazodilatation is more probable. At intake for acceleration of effect nifedipine can be chewed. At emergence against the background of treatment of pains behind a breast nifedipine should be cancelled. It is necessary to cancel nifedipine gradually as at the sudden termination of reception (especially after prolonged treatment) development of a withdrawal is possible. At intra coronary introduction in the presence of a stenosis of two vessels it is impossible to enter nifedipine into the third open vessel because of danger of the expressed negative inotropic effect. During course treatment not to allow alcohol intake owing to risk of excessive decrease in the ABP. Influence on ability to driving of motor transport and to control of mechanisms In an initiation of treatment it is necessary to avoid driving of the vehicles and other potentially dangerous types of activity demanding speed of psychomotor reactions. In the course of further treatment extent of restrictions is defined depending on individual portability of nifedipine.

Side effects:

From cardiovascular system: hyperemia of integuments, caumesthesia, tachycardia, arterial hypotension, peripheral hypostases; seldom - bradycardia, ventricular tachycardia, an asystolia, strengthening of attacks of stenocardia. From the alimentary system: nausea, heartburn, diarrhea; seldom - deterioration in function of a liver; in isolated cases - a hyperplasia of gums. At long reception in high doses dispeptic symptoms, increase in activity of hepatic transaminases, an intra hepatic cholestasia are possible. From TsNS and a peripheral nervous system: headache. At long reception in high doses paresthesias, muscle pains, a tremor, easy visual disturbances, sleep disorders are possible. From system of a hemopoiesis: in isolated cases - a leukopenia, thrombocytopenia. From an urinary system: increase in a daily urine. At long reception in high doses renal failures are possible. From endocrine system: in isolated cases - a gynecomastia. Allergic reactions: skin rash. Local reactions: at in introduction burning in the place of an injection is possible. Within 1 min. after intra coronary introduction manifestation of negative inotropic effect of nifedipine, increase in ChSS, arterial hypotension is possible; these symptoms gradually disappear in 5-15 min.

Interaction with other medicines:

At simultaneous use with the anti-hypertensive drugs, diuretics derivative of a fenotiazin anti-hypertensive effect of nifedipine amplifies. At simultaneous use with anticholinergics disturbances of memory and attention at patients of advanced age are possible. At simultaneous use with beta adrenoblockers development of the expressed arterial hypotension is possible; in some cases - development of heart failure. At simultaneous use with nitrates the anti-anginal effect of nifedipine amplifies. At simultaneous use with drugs of calcium efficiency of nifedipine in connection with the antagonistic interaction caused by increase in concentration of calcium ions in extracellular liquid decreases. Cases of development of muscular weakness at simultaneous use with magnesium salts are described. At simultaneous use with digoxin delay of removal of digoxin from an organism and, therefore, increase in its concentration in a blood plasma is possible. At simultaneous use with diltiazem anti-hypertensive action amplifies. At simultaneous use with theophylline changes of concentration of theophylline in a blood plasma are possible. Rifampicin induces activity of enzymes of a liver, accelerating nifedipine metabolism that leads to reduction of its efficiency. At simultaneous use with phenobarbital, Phenytoinum, carbamazepine concentration of nifedipine in a blood plasma decreases. There are messages on increase in concentration of nifedipine in a blood plasma and increase in its AUC at simultaneous use with flukonazoly, itrakonazoly. At simultaneous use with fluoxetine strengthening of side effect of nifedipine is possible. In some cases at simultaneous use with quinidine decrease in concentration of quinidine in a blood plasma is possible, and at nifedipine cancellation perhaps substantial increase of concentration of quinidine that is followed by lengthening of an interval of QT on an ECG. Concentration of nifedipine in a blood plasma can moderately increase. Cimetidinum and, to a lesser extent ranitidine, increase concentration of nifedipine in a blood plasma and, thus, strengthen its anti-hypertensive action. Ethanol can strengthen effect of nifedipine (excessive arterial hypotension) that causes dizziness and other undesirable reactions.

Contraindications:

Arterial hypotension (systolic the ABP is lower than 90 mm hg), collapse, cardiogenic shock, heavy heart failure, heavy aortal stenosis; hypersensitivity to nifedipine.

Issue conditions:

According to the recipe

Packaging:

In packaging on 50 tablets.