LIDOKAIN (Solution for injection)

Active material: Lidokain
When ATH: N01BB02
CCF: Mestnый anesthetic. Antiarrhythmic drugs. Class I B.
When CSF: 21.02
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)

DOSAGE FORM, STRUCTURE AND PACKAGING

Solution for injection clear, colorless or near colorless, without smell.

Excipients: sodium chloride (parenteral dosage forms), water d / and.

2 ml – ampoule (5) – packings Valium planimetric (20) – cardboard boxes.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

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, duration – 10-20 m; when i / m administration the onset of action through 5-15 m, duration – 60-90 m.

It causes all kinds of local anesthesia: terminal, infiltration, provodnikovuju.

Pharmacokinetics

After the / m of absorption is almost complete. Distribution of quick, V_d 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.

T_1/2 It tends to be biphasic with a phase distribution 7-9 m. In general, T_1/2 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.

Testimony

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.

Dosage regimen

In an antiarrhythmic adults when administered in a loading dose of / in – 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.

Children with on / in a loading dose – 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: adults with / in a loading dose – 100 mg, on subsequent drip infusion – 2 mg / min; when i / m administration – 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.

Side effect

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), syndrome “cauda equina” (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, tachycardia – when administered vasoconstrictor, 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: spinal anesthesia – backache, with epidural anesthesia – accidentally getting into the subarachnoid space; topically in Urology – uretrit.

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.

Contraindications

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.

For subarachnoid anesthesia – complete heart block, bleeding, hypotension, shock, infection venue lumbar puncture, septicemia.

Increased sensitivity to lidocaine and other local anesthetics of the amide type.

Pregnancy and lactation

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.

Cautions

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); for epidural anesthesia – neurological diseases, Septicemia, impossibility of puncture due to spinal deformity; for subarachnoid anesthesia – when back pain, 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; polymyxin B – should monitor respiratory function.

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.

Drug Interactions

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, xinidinom – may increase cardiodepressive action; with amiodaronom – described cases of seizures and SSS.

In an application with geksenalom, thiopental sodium (I /) possible respiratory depression.

At simultaneous application with Valium increased toxicity of lidocaine; with midazolamom – moderate decrease in the concentration of lidocaine in plasma; with morphine – strengthening the analgesic effect of morphine.

In an application with prenylamine growing risk of ventricular arrhythmia types “pirouette”.

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.