Project Description

Novocainamid

(solution for injection) 10%-5ml N°5 Solution Novocainamidi 10% pro injectionibus

international nonproprietary name

Procainamide.

Ref

BP-0090

Pharmacotherapeutic group

Antiarhythmics.

Composition of the preparation

1 ml of solution contains 100 mg of Novocainamide.

Pharmacological action

Pharmacodynamics

Novocainamide is an antiarrhythmic drug of class 1A, it is a membrane stabilizer. It suppresses conduction of impulses through atriums, atrioventicular node and ventricles. It stretches effective refractory period of atriums. It suppresses automatism of sinus node and ectopic pacemakers so enlarging the threshold of ventricular fibrillation.

Novocainamide has a local anaesthetic action. It possesses weak inotropic effect. It has vagolytic and vasodilating properties that mediate tachycardia and reduction of blood pressure.

Time of reaching maximum effect after intravenous introduction is immediate, after intramuscular introduction – within 15-60 minutes.

Pharmacokinetics

At parenteral introduction it is bound with plasma proteins by 15-25%. It is biotransformed followed with formation of active metabolite – N-acetylprocainamide. The period of semi-coagulation is 2.5-4.5 hours. It is excreted by kidneys, 50-60% of introduced dose is exctreted unchanged. It passes through placenta and penetrates to breast milk.

Indications 

It is used at different disorders of cardiac rate, such as paroxysmal ciliary arrhythmia, paroxysmal tachycardia, extrasystoles and other disorders of cardiac rate. During heart surgery, surgery of large vesserls and lungs the drug is applied for prophylactics to prevent and to cure  disorders of cardiac rate appearing in the process of surgery.

special indication

Care should be taken when driving vehicles and /or when performing works requiring heightened concentration of attention.

special warning

Be particularly  careful in using the drug  at  myocardial infarction due to possible suppression of contractive myocardium ability and hypotension. It is not recommended to use the drug at severe atherosclerosis. When using novocainamide during pregnancxy there exists potential risk of cumulation and development of hypotension of mother, that may cause uteroplacental insufficiency.

Dosage and method of administration

10% solution of novocainamide is injected by intravenous and intramuscular introduction.

For rapid relief of symptoms of ventricular tachycardia the drug if injected intravenously being previously diluted in 5% solution of glucose or isotonic solution of sodium chloride. Dose of introduction is 200-500 mg , the rate of introduction is 25-50 mg/min. The drug may be prescribed for intramuscular introduction in a dose of  0.5-1 g (5-10 ml of 10% solution), and then with the intervals of 6 hours it is injected intravenously ( by slow introduction) in a dose of 0.2-0.5 g or on the basis of 10-20 mg/kg during 40 minutes followed by subsequent infusion  with the rate of 2-3 mg/min.

Intravenous introduction is made slowly with the rate of not exceeding 1 ml per a minute taking systematic measurements of blood pressure till restoration of normal cardiac rate. At fast introduction of drug there may occur unwanted hypotension, thereat injection should be immediately terminated. It is recommended to perform introduction of drug under the control of electrocardiogram. In case of drop of blood  tension mesaton should be applied (0.3-0.3 ml of 1% solution).

overdosage

Symptoms: mental confusion, weak urine passage, strong giddiness or syncope, palpitation or arythmic palpitation, nausea or vomiting.

Treatment: hemodialysis, introduction of vasoconstrictive agents, maintaining of patency of airways.

safety measures

Not established

Side effects

At using novocainamide there may be observed general weakness, headache, nausea, vomiting,  bitter taste, loss of appetite, diarrhea, excitation,  sleeplessness, hallucinations, bradycardia, disorder of myocardium conduction, hypotension, seldom ventricular asystolia, eosinophilia, agranulocytosis, allergic reaction. In such cases the drug should be withdrawn.

Contraindications

Novocainamide is contraindicted at individual intolerance, ventricular arrhythmia caused by intozication with cardiac glycosides, atrioventricular block, cardiac decompensation, severe forms of renal insufficiency.

Interactions with other medicinal preparations

It amplifies the effect of antiarrhythmic, anticholinergic and cytostatic agents, muscle  relaxants, adverse effects of  bretylium. The drug reduces the activity of antimyasthenic agents.

The form of release

10% solution for injections in ampulas, 5 ml each. 5-10 ampulas in packages or contour cellular packs. 1 or 2 contour cellular packs in a package.