NIFEDIPINE (Nifedipine) *. 2, 6-Dimetil-4-(2 '-nitrophenyl) - 1, 4-dihydropyridine '-Z, the 5th dicarboxylic acid dimethyl ether.
Synonyms: Adalatum, Kordafen, Kordipin, Corinfarum, Nifangin, Nifekard, Adalat, Adarat, Calcigard, Cordafen, Cordipin, Corinfar, Nifangin, Nifacard, Nifelat, Procardia, etc.
The corresponding domestic drug - Phenihydinum (Phenyhydinum; Phenigidin, Phenihidin). Yellow crystal powder. It is almost insoluble in water, is difficult alcohol-soluble.
Nifedipine (Phenihydinum) is the main representative of antagonists of calcium ions - derivatives 1, 4 dihydropyridines.
Like verapamil and other antagonists of calcium ions nifedipine expands coronary and peripheral (mainly arterial) vessels, has negative inotropic effect, reduces the need of a myocardium for oxygen. Unlike verapamil has no oppressing impact on the carrying-out system of heart and has weak antiarrhytmic activity. In comparison with verapamil reduces peripheric vascular resistance stronger and more significantly lowers the arterial blood pressure.
Drug is quickly soaked up at intake. The maximum concentration in blood plasma is observed through 1/2 - 1 h after reception. Has short elimination half-life - 2 - 4 h. About 80% are removed by kidneys in the form of inactive metabolites, about 15% - with a stake. It is established that at long reception (2 - 3 months) the tolerance (unlike verapamil) to effect of drug develops.
Apply nifedipine (Phenihydinum) as anti-anginal means at an ischemic heart disease with stenocardia attacks, to decrease in the ABP at different types of hypertensia, including renal hypertensia. There are instructions that nifedipine (and verapamil) in nephrogenic hypertensia slows down progressing of a renal failure.
Apply also in complex therapy of chronic heart failure. Earlier considered that nifedipine and other antagonists of calcium ions are not shown in heart failure because of negative inotropic effect. Recently it is established that all these drugs thanks to peripheral vazodilatatorny action improve function of heart and promote reduction of its sizes in chronic heart failure. Also pressure decrease in a pulmonary artery is observed. However it is not necessary to exclude a possibility of negative inotropic effect of nifedipine, it is necessary to show care in the profound heart failure. In the latest time there were messages about inexpediency of use of nifedipine in arterial hypertension, in connection with increase in risk of developing a myocardial infarction and also with a possibility of increase in risk of lethal outcomes at patients with coronary heart disease at prolonged use of the idenfat.
It generally concerns use of 'usual' nifedipine (short action), but not its prolonged dosage forms and dihydropyridines of long action (for example, an amlodipina). This question, however, remains debatable.
There are data on positive influence of nifedipine on a cerebral hemodynamics, its efficiency in a Raynaud's disease. At patients with bronchial asthma of considerable bronchodilatory action it is noted, but drug can be used in combination with other bronchodilatory means (sympathomimetics) for maintenance therapy.
Accept nifedipine (Phenihydinum) inside (irrespective of meal time) on 0, 01 - 0, 03 g (10 - mg Z0) 3 - 4 times a day (up to 120 mg a day). Duration of treatment is 1 - 2 month and more.
For stopping of gipertonichssky crisis (and sometimes at stenocardia attacks) use drug sublingual. The tablet (1O of mg) is placed under language. For acceleration of effect the tablet of Phenihydinum is chewed and held, without swallowing, under language. At this way, patients within 30 - 60 min. have to be in a prone position. If necessary in 20 - 30 min. repeat administration of drug; sometimes increase a dose to 20 - 30 mg. After stopping of attacks pass to oral administration.
The latest results allow to consider sublingual use of nifedipine inexpedient, in connection with increase in risk of manifestations of side effects of action, at fast increase in 'peak' of concentration of drug in blood.
Phenihydinum (nifedipine) is usually well transferred. However face reddening and skins of an upper part of a trunk, a headache probably connected with decrease in a tone of cerebral vessels of a brain (mainly capacity) and their stretching owing to increase in inflow of blood on an arteriovenous anastomosis are rather often observed. In these cases, the dose is reduced or the drug is taken after a meal.
Also heartbeat, nausea, dizziness, hypostasis of the lower extremities, hypotension, drowsiness are possible.
Contraindications: severe forms of heart failure, syndrome of weakness of a sinus node, profound arterial hypotension. In moderate hypotension appoint drug in the reduced doses (0, 01 g 3 times a day) under obligatory control of the ABP.
Nifedipine (Phenihydinum) is contraindicated at pregnancy and feeding by a breast.
The care is necessary when prescribing drug to drivers of transport and persons of other professions demanding fast mental and physical reaction.
Packaging: tablets, coated yellow color, containing 0, 01 g (10 mg) of drug, in packing on 40 pieces; Corinfarum, kordafen, nifekard - on 50 pieces.
Storage: B list. In the place protected from light.
Nifekard retard (Nifecard retard) contains 20 mg of nifedipine in 1 tablet.
Packaging: tablets in packing on ZO of pieces.
Recently the injection form of nifedipine is released abroad (adalit) in ampoules 50 ml (5 mg of drug in 18% alcohol solution). Enter into a vein at first 1 mg (bolus), then at the rate of 1 mg an hour or 17 mkg/min.