Active material: Lidokain
When ATH: C01BB01
CCF: Antiarrhythmic drugs. Class I B
When CSF: 01.11.01.01.02
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)
Solution for / in the clear, colorless or near colorless, without smell.
| 1 ml | 1 amp. | |
| Lidocaine hydrochloride (monohydrate) | 100 mg | 200 mg |
Excipients: water d / and.
2 мл – ампулы бесцветного стекла (5) – упаковки ячейковые контурные (2) – пачки картонные.
Class IB antiarrhythmic agents, mestnый anesthetic, derivative of acetanilide. It has a membrane stabilizing activity. It causes blockade of sodium channels in excitable neuronal membranes and membranes of cardiomyocytes.
Reduces the duration of the action potential and the effective refractory period of Purkinje fibers, suppresses their automatism. This inhibits the electrical activity of lidocaine depolarized, arrhythmogenic sites, but a minimum effect on the electrical activity of normal tissues. When used in high therapeutic doses hardly changes myocardial contractility and slows AV conduction-. When used as an anti-arrhythmic agent in / in the introduction onset of action through 45-90 sec, длительность – 10-20 m; when i / m administration the onset of action through 5-15 m, длительность – 60-90 m.
It causes all kinds of local anesthesia: terminal, infiltration, provodnikovuju.
After the / m of absorption is almost complete. Distribution of quick, Vd is about 1 l / kg (in patients with heart failure following). Protein binding is dependent on the concentration of active substance in plasma and of 60-80%. Metabolized primarily in the liver with the formation of active metabolites, which may contribute to the manifestation of therapeutic and toxic effects, especially after infusion for 24 h or more.
T1/2 It tends to be biphasic with a phase distribution 7-9 m. In general, T1/2 dose dependent, is 1-2 and h can be increased to 3 hours or more during a long / infusion (more 24 no). Excreted by the kidneys as metabolites, 10% in unchanged form.
In cardiology practice: treatment and prevention of ventricular arrhythmias (arrythmia, tachycardia, flutter, fibrillation), incl. in acute myocardial infarction, when implanted pacemaker, when glycoside intoxication, anesthesia.
For anesthesia: terminal, infiltration, wires, cerebrospinal (Epidural) anesthesia in surgery, obstetrics and gynecology, Urology, Ophthalmology, Dentistry, otorynolarynholohyy; blockade of peripheral nerves and ganglia.
В качестве антиаритмического средства взрослым при введении нагрузочной дозы в/в – 1-2 mg / kg for 3-4 m; The average single dose 80 mg. Then go straight on drip infusion at a rate of 20-55 ug / kg / min. Drip infusion can be carried out during 24-36 no. If necessary background drip infusion can be repeated to / from lidocaine bolus dose 40 mg after 10 minutes after the first loading dose.
V / m are introduced by 2-4 mg / kg, if necessary, re-introduction is possible through 60-90 m.
Детям при в/в введении нагрузочной дозы – 1 mg / kg, if necessary, may re-introduction of 5 m. For continuous / v infusion (usually following administration of the loading dose) – 20-30 ug / kg / min.
For use in surgical and obstetric practice, Dentistry, ENT practice mode set individually, depending on the evidence, clinical situation and the dosage form.
The maximum dose: взрослым при в/в введении нагрузочная доза – 100 mg, при последующей капельной инфузии – 2 mg / min; при в/м введении – 300 mg (about 4.5 mg / kg) during 1 no.
Kids in the case of re-loading dose at intervals 5 min total dose is 3 mg / kg; with continuous I / Infusion (usually following administration of the loading dose) – 50 ug / kg / min.
From the central and peripheral nervous system: dizziness, headache, weakness, restlessness, nistagmo, loss of consciousness, drowsiness, visual and auditory disorders, tremor, Trizm, convulsions (It increases the risk of development against the backdrop of hypercapnia and acidosis), синдром “конского хвоста” (paralysis of the legs, paresthesia), stethoparalysis, respiratory arrest, Engine block and sensitive, Respiratory paralysis (more likely to develop when subarachnoid anesthesia), numbness of the tongue (when used in dentistry).
Cardio-vascular system: increased or decreased blood pressure, тахикардия – при введении с вазоконстриктором, perifericheskaya vasodilation, collapse, chest pain.
From the digestive system: nausea, vomiting, involuntary defecation.
Allergic reactions: skin rash, hives (on the skin and mucous membranes), itchy skin, angioedema, anaphylactic shock.
Local reactions: при спинальной анестезии – боль в спине, при эпидуральной анестезии – случайное попадание в субарахноидальное пространство; при местном применении в урологии – уретрит.
Other: involuntary urination, metgemoglobinemiâ, persistent anesthesia, decreased libido and / or potency, respiratory depression, up to the stop, gipotermiя; under anesthesia in dentistry: nechuvstvitelynosty and paresthesia gub and jazika, extension of anesthesia.
Heavy bleeding, shock, hypotension, the proposed injection site infection, vыrazhennaya bradycardia, cardiogenic shock, severe chronic heart failure, SSS elderly patients, AV-blockade II and III degrees (except, when a probe to stimulate the ventricles), severe liver.
Для субарахноидальной анестезии – полная блокада сердца, bleeding, hypotension, shock, infection venue lumbar puncture, septicemia.
Increased sensitivity to lidocaine and other local anesthetics of the amide type.
During pregnancy and lactation used only for health. Lidocaine is excreted in breast milk.
In obstetric practice used with caution paracervical for violations of fetal development, placental insufficiency, prematurity, perenoshennosti, gestosis.
C care should be used when conditions, accompanied by a decrease in hepatic blood flow (incl. in chronic heart failure, liver diseases), progressive circulatory insufficiency (usually as a result of heart block and shock), in heavy and debilitated patients, in elderly patients (senior 65 years); для эпидуральной анестезии – при неврологических заболеваниях, Septicemia, impossibility of puncture due to spinal deformity; для субарахноидальной анестезии – при боли в спине, brain infections, benign and malignant tumors of the brain, coagulopathies at various origins, migraine, subarachnoid hemorrhage, hypertension, hypotension, paresthesia, psychosis, Hysteria, in uncooperative patients, impossibility of puncture due to spinal deformity.
Caution is administered lidocaine in the tissue with abundant vascularization (eg, in the neck with the thyroid surgery), in such cases, lidocaine applied in lower doses.
While the use of beta-blockers, cimetidine requires a reduction in dose of lidocaine; с полимиксином В – следует контролировать функцию дыхания.
During treatment MAO inhibitors should not be used lidocaine parenteral.
Solutions for injections, composed of epinephrine and norepinephrine, not designed for on / in the.
Lidocaine can not be added to blood transfusions.
Effects on ability to drive vehicles and management mechanisms
After application of lidocaine is not recommended to engage in activities, It requires high concentration of attention and fast psychomotor reactions.
In an application with barbiturates (incl. phenobarbital) may increase the metabolism of lidocaine in the liver, lowering plasma concentrations and, thereby, reduction of its therapeutic effectiveness.
While the use of beta-blockers (incl. with propranolol, nadololom) may increase the effects of lidocaine (incl. toxic), apparently, due to slow its metabolism in the liver.
At simultaneous application with MAO inhibitors may increase the local anesthetic lidocaine action.
In an application with drugs, causing a blockade of neuromuscular transmission (incl. with suxamethonium chloride) may increase the effects of drugs, causing a blockade of neuromuscular transmission.
In an application with drugs and sedatives may increase inhibitory action on the central nervous system; with aymalinu, хинидином – возможно усиление кардиодепрессивного действия; с амиодароном – описаны случаи развития судорог и СССУ.
In an application with geksenalom, thiopental sodium (I /) possible respiratory depression.
At simultaneous application with Valium increased toxicity of lidocaine; с мидазоламом – умеренное уменьшение концентрации лидокаина в плазме крови; с морфином – усиление анальгезирующего эффекта морфина.
При одновременном применении с прениламином развивается риск развития желудочковой аритмии типа “пируэт”.
Cases of excitation, hallucinations while the use of procainamide.
While the use of propafenone may increase the duration and increase the severity of side effects from the CNS.
It is believed, that under the effect of rifampicin may decrease lidocaine concentration in plasma.
When both / v infusion of lidocaine and phenytoin may increase the side effects of central origin; described the case sinoatrial blockade due to the additive action cardiodepressive lidocaine and phenytoin.
Patients, receiving phenytoin as anticonvulsant, possible to reduce the concentration of lidocaine in plasma, due to the induction of hepatic microsomal enzymes under the influence of phenytoin.
In an application with cimetidine moderately reduced clearance of lidocaine and increases its concentration in the blood plasma, there is a risk of increased side effects of lidocaine.
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