Lidocaine
Producer: JSC Himfarm Republic of Kazakhstan
Code of automatic telephone exchange: N01BB02
Release form: Liquid dosage forms. Solution for injections.
General characteristics. Structure:
Active agent - lidocaine a hydrochloride (in terms of 100% substance) 40 mg.
Excipients: sodium chloride, sodium hydroxide, water for injections.
Pharmacological properties:
Pharmacokinetics. After intramuscular introduction absorption almost full. Distribution is bystry, the volume of distribution makes about 1 l/kg (at patients with heart failure lower). Linkng with proteins depends on concentration of active agent in plasma and makes 60-80%. It is metabolized, mainly, in a liver with formation of active metabolites which can promote manifestation of therapeutic and toxic action, especially after infusion during 24 h and more.
The elimination half-life of drug tends to two-staging with a phase of distribution of 7-9 min. In general, the elimination half-life of drug depends on a dose, makes 1-2 h and can increase to 3 h and more during long intravenous infusions (more than 24 h). 10% in not changed look are removed by kidneys in the form of metabolites.
Pharmacodynamics. Derivative acetanilide. Antiarrhytmic, mestnoanesteziruyushchy means. Causes all types of local anesthesia: terminal, infiltration, conduction. Stabilizes cellular membranes, blocks natrium channels. In a myocardium suppresses automatism of the ectopic centers, mainly in ventricles; practically conductivity and contractility of a myocardium does not oppress. Promotes an exit of potassium ions from cells of a myocardium and accelerates process of repolarization of cellular membranes, shortens duration of action potential and the effective refractory period.
Indications to use:
- treatment and prevention of ventricular arrhythmias (premature ventricular contraction, tachycardia, trembling, fibrillation), including in the acute period of a myocardial infarction, at implantation of an artificial pacemaker, at glikozidny intoxication, an anesthesia
- anesthesia: terminal, infiltration, conduction, spinal (epidural) at operative measures in surgery, ophthalmology, stomatology, otorhinolaryngology, obstetrics, gynecology, dermatology
- blockade of peripheral nerves and nerve knots.
To apply strictly on doctor's orders in order to avoid complications.
Route of administration and doses:
Intramusculary, intravenously. As antiarrhytmic means the drug is administered intravenously or intramusculary. At intravenous administration for achievement of effective therapeutic concentration in blood begin with bolyusny administration of drug. The shock dose of solution of 80-120 mg (8-12 ml of 1% or 4-6 ml of 2% of solution) is entered within 3-4 minutes. After this continue drop introduction with a speed of 2 mg/min. (only 250-500 mg of lidocaine of a hydrochloride on isotonic solution of sodium of chloride). For infusion part 2% lidocaine solution in isotonic solution of sodium of chloride (for receiving the solution containing 2 mg in 1 ml part 6 ml of 2% of solution of Lidocaine in 60 ml of isotonic solution of sodium of chloride).
Intramusculary enter 2-4 mg/kg, if necessary repeated introduction is possible in 60-90 min.
To children at intravenous administration of a load dose – 2 mg/kg, then pass to intravenous drop injection in a dose 4-6 mg / кг.ч within 24-36 hours For continuous intravenous infusion (usually after introduction of a load dose) – 20-30 mkg/kg/min.
For use in obstetrics, gynecology, stomatology, the ENT SPECIALIST - to practice the mode of dosing is established individually, depending on indications, a clinical situation.
Maximum doses:
- the adult at intravenous administration a load dose – 100 mg, at the subsequent drop infusion – 2 mg/min.; at intramuscular introduction (the maximum single dose) of 200 mg during 1 h;
- to children in case of repeated introduction of a load dose with an interval of 5 min. the total dose makes 2 mg/kg; at continuous intravenous infusion (usually after introduction of a load dose) – 50 mkg/kg/min.
Features of use:
With care apply at patients with heart failure, arterial hypotension, a sinus bradycardia, an incomplete atrioventricular block, disturbances of intra ventricular conductivity, renal failures and a liver, at a hypovolemia. Administration of drug has to be carried out only by experienced medical personnel. At administration of lidocaine the equipment for resuscitation and maintenance of the vital functions has to be available. Administration of lidocaine in the preventive purposes is not recommended to all patients with an acute myocardial infarction.
At pregnancy and in the period of a lactation use of lidocaine is possible only according to vital indications.
Use of lidocaine influences ability to manage the vehicle or potentially dangerous mechanisms.
Side effects:
- headache, dizziness, sleep disorder, concern
- at bystry intravenous administration spasms, a tremor, paresthesias, a disorientation, euphoria, a sonitus, a bradyarthria are possible
- at use in high doses bradycardia, conductivity delay, arterial hypotension are possible.
Extremely seldom:
- skin rash, itch
- Quincke's disease.
Interaction with other medicines:
At simultaneous use with barbiturates (including with phenobarbital) increase in metabolism of lidocaine in a liver, decrease in concentration in a blood plasma and thereof, reduction of its therapeutic effectiveness is possible. At simultaneous use with beta adrenoblockers (including propranolol, Nadololum) strengthening of effects of lidocaine (including toxic), apparently, owing to delay of his metabolism in a liver is possible. At simultaneous use with inhibitors of a monoaminooxidase strengthening of mestnoanesteziruyushchy effect of lidocaine is possible.
At simultaneous use with the drugs causing neuromuscular transmission blockade (including from succinylcholine chloride) strengthening of effect of the drugs causing neuromuscular transmission blockade is possible.
At simultaneous use with hypnotic drugs and sedatives strengthening of the oppressing action on the central nervous system is possible; with Ajmalinum, quinidine – strengthening of cardio-depressive action is possible; with Amiodaronum – cases of development of spasms and a sick sinus syndrome are described.
At simultaneous use with hexenal, thiopental of sodium respiratory depression is (intravenously) possible.
At simultaneous use with meksiletiny toxicity of lidocaine increases; with amidazoly – moderate reduction of concentration of lidocaine in a blood plasma; with morphine – strengthening of analgeziruyushchy effect of morphine.
At simultaneous use with Prenylaminum the risk of development of ventricular arrhythmia "pirouette" develops.
Cases of excitement, hallucination at simultaneous use with procaineamide are described.
At simultaneous use with propafenony increase in duration and increase in severity of side effects from the central nervous system is possible.
Believe that under the influence of rifampicin reduction of concentration of lidocaine in a blood plasma is possible.
At simultaneous intravenous infusion of lidocaine and Phenytoinum strengthening of side effects of the central genesis is possible; the case of sinuatrial blockade owing to the additive cardiodepressive effect of lidocaine and Phenytoinum is described.
At the patients receiving Phenytoinum as an anticonvulsant reduction of concentration of lidocaine in a blood plasma is possible that is caused by induction of microsomal enzymes of a liver under the influence of Phenytoinum.
At simultaneous use with Cimetidinum the clearance of lidocaine moderately decreases and its concentration in a blood plasma increases, there is a risk of strengthening of side effect of lidocaine.
Contraindications:
- the expressed bradycardia
- the expressed arterial hypotension
- severe forms of chronic heart failure
- a sick sinus syndrome at patients of advanced age
- atrioventricular block of II and III degrees
- heavy abnormal liver functions
- hypersensitivity to lidocaine.
Overdose:
Symptoms: spasms of mimic muscles with transition to toniko-clonic spasms of skeletal muscles, диспноэ, bradycardia, up to a cardiac standstill, the expressed lowering of arterial pressure, up to a collapse, dizziness, nausea, vomiting.
Treatment: the patient has to be in horizontal position with careful monitoring of the vital indicators, control of passability of respiratory tracts and administration of oxygen, at disturbance from the central nervous system - administration of benzodiazepines (for example, diazepam) or barbiturates supershort (for example, thiopental) or short action (for example, phenobarbital), from cardiovascular system - administration of atropine. The hemodialysis is inefficient. At a cardiac standstill - an immediate cardiac massage.
Storage conditions:
To store in the dry, protected from light place, at a temperature not above 30 °C.
To store in the place, unavailable to children!
Issue conditions:
According to the recipe
Packaging:
2% solution for injections in ampoules on 2 ml, a cardboard box on 10 pieces, in a blister strip packaging on 5 and 10 pieces.
