Novokainamid

General characteristics. Structure:

Active ingredient: 250 mg of a novokainamid.

Excipients: potato starch; sugar milk (lactose); calcium stearate.

The medicine reducing excitability of a cardiac muscle, suppressing the displaced sources of a cordial rhythm, having mestnoanesteziruyushchy effect.

Pharmacological properties:

Pharmacodynamics. Antiarrhytmic means of the class IA, has membrane stabilizing activity. Brakes the entering bystry current of ions of sodium, reduces depolarization speed in a phase 0. Conductivity oppresses, slows down repolarization. Reduces excitability of a myocardium of auricles and ventricles. Increases duration of the effective refractory period of action potential (in the affected myocardium - more). Conductivity delay which is observed irrespective of rest potential size is more expressed in auricles and ventricles, it is less - in an AV node. The indirect m-holinoblokiruyushchy effect, in comparison with quinidine and Disopyramidum, is expressed less therefore paradoxical improvement of AV conductivity usually is not noted. 4 depolarizations influence a phase, reduces automatism of the intact and affected myocardium, oppresses function of a sinus node and ectopic pacemakers at some patients. The active metabolite - N-atsetilprokainamid has the expressed activity of antiarrhytmic means of the III class, extends action potential duration. Possesses a weak negative inotropic effect (without significant effect on minute volume), vagolytic and vazodilatiruyushchy properties that causes tachycardia and decrease in the ABP, OPSS. Electrophysiologic effects are shown in broadening of the QRS complex and lengthening of intervals of PQ and QT. Time of achievement of the maximum effect at intake of 60-90 min., at in introduction - immediately, at in oil - 15-60 min.

Indications to use:

Ventricular arrhythmias: premature ventricular contraction, Bouveret's ventricular disease. Supraventricular arrhythmias. Paroxysm of a ciliary arrhythmia or atrial flutter. Supraventricular tachycardia (including WPW syndrome).

Route of administration and doses:

Individual. At intake the initial dose makes from 250 mg to 1 g, further in need of and taking into account portability - 250-500 mg each 3-6 h.

At introduction in oil - on 50 mg/kg/days in the divided doses each 3-6 h.

At in jet introduction a single dose - 100 mg, if necessary are possible repeated introductions before the termination of arrhythmia. At in/in infusion the dose makes 500-600 mg.

Maximum doses: the adult at intake - 4 g/days; in/in struyno at repeated introductions a total dose - 1 g.

Features of use:

Aritmogenny effect of procaineamide was noted in 5-9% of cases. Due to the possible oppression of sokratitelny ability of a myocardium and decrease in the ABP it is necessary to apply carefully at a myocardial infarction. At the expressed atherosclerosis procaineamide is not recommended to be applied.

With care to apply at blockade of legs of a ventriculonector, arrhythmia against the background of intoxication cardiac glycosides, myasthenias, a liver and/or renal failure, hard currency (including in the anamnesis), bronchial asthma, chronic heart failure in a stage of a decompensation, ventricular tachycardia at occlusion of a coronary artery, surgical interventions (including in surgical stomatology), when lengthening an interval of QT, arterial hypotension, atherosclerosis, at a myasthenia, at patients of advanced age.

In need of use of procaineamide at pregnancy and in the period of a lactation (breastfeeding) it is necessary to consider that active agent gets through a placental barrier and is allocated with breast milk. Therefore use of procaineamide is possible only in that case when the potential advantage for mother surpasses possible risk for a fruit or the baby.

Side effects:

From cardiovascular system: arterial hypotension (up to development of a collapse), intra ventricular blockade, ventricular tachycardia, a tachyarrhythmia; at bystry in introduction - a collapse, intra ventricular blockade, an asystolia.

From TsNS: hallucinations, a depression, a myasthenia, dizziness, a headache, spasms, psychotic reactions with productive symptoms, an ataxy.

From system of a hemopoiesis: at prolonged use - oppression of a marrowy hemopoiesis (a leukopenia, thrombocytopenia, a neutropenia, an agranulocytosis, hypoplastic anemia), hemolitic anemia with positive test of Koombs.

Allergic reactions: skin rash, itch.

Others: bitterness in a mouth, at prolonged use - a medicinal lupus erythematosus (at 30% of patients lasting therapy more than 6 months); microbic infections, delay of processes of healing and bleeding of gums in connection with risk of a leukopenia and thrombocytopenia are possible.

Interaction with other medicines:

At simultaneous use with antiarrhytmic means the perhaps additive cardiodepressive action; with anti-hypertensive means - anti-hypertensive action amplifies; with antikholinesterazny means - efficiency of antikholinesterazny means decreases.

At simultaneous use with m-holinoblokatorami, antihistaminic drugs their cholinolytic action amplifies.

At simultaneous use action of the means blocking neuromuscular transmission amplifies; at simultaneous use of the means causing oppression of a marrowy hemopoiesis strengthening of a leukopenia and thrombocytopenia is possible.

At simultaneous use with Amiodaronum QT interval owing to the additive action increases by its duration and risk of development of ventricular arrhythmia like "pirouette". Concentration in a blood plasma of procaineamide and its metabolite of N-atsetilprokainamida increases, strengthening of side effects is possible.

At simultaneous use with captopril increase in risk of development of a leukopenia is possible.

At simultaneous use with ofloksatsiny increase in concentration of procaineamide in a blood plasma is possible; with Prenylaminum - negative inotropic effect and risk of development of ventricular arrhythmia like "pirouette" amplifies.

At simultaneous use with sotaloly, quinidine the perhaps additive increase in an interval of QT.

At simultaneous use with Trimethoprimum concentration in a blood plasma of Procainum and its active metabolite of N-atsetilprokainamida increases, there is a risk of development of toxic reactions.

At simultaneous use with tsizapridy QT interval duration owing to the additive action considerably increases, there is a risk of development of ventricular arrhythmia (including the pirouette type).

At simultaneous use with Cimetidinum concentration of procaineamide in a blood plasma and risk of strengthening of side effect, especially at patients of advanced age increases and at renal failures that is caused by reduction of excretion of procaineamide kidneys under the influence of Cimetidinum almost on 1/3 and more.

Contraindications:

AV blockade of II and III degrees (except for cases of use of an electrocardiostimulator), trembling or ventricular fibrillation, arrhythmias against the background of intoxication cardiac glycosides, a leukopenia, hypersensitivity to procaineamide.

Overdose:

At overdose of drug the oliguria, a syncope, confusion of consciousness, dizziness, drowsiness, tachycardia, vomiting, deterioration in appetite, nausea, diarrhea, a collapse, an asystolia, ventricular tachycardia are observed.

For overdose treatment to the patient wash out a stomach, appoint administration of drugs, acidifying urine, carry out a hemodialysis. If the expressed pressure decrease is noted, enter Phenylephrinum, Norepinephrinum.

Storage conditions:

List B. To store in the unavailable to children, protected from light place at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

On 20 pieces of tablets in banks from dark glass (1) in packs cardboard.