Lidocaine - instructions for use, dose, side effects, contraindications

It has a local anesthetic effect, blocks potential-dependent sodium channels, which prevents generation of pulses in the endings of the sensory nerves and impulses along nerve fibers. It suppresses not only pain impulses, but also impulses of another modality.

The anesthetic effect of lidocaine is 2-6 times stronger than procaine (it acts faster and longer - up to 75 min, and after the addition of epinephrine - more than 2 hours). With topical application dilates blood vessels, does not have a locally irritating effect.

Pharmacokinetics:With parenteral absorption, absorption is complete.The rate of absorption depends on the site of administration and the dose. At a concentration of 20 mg / ml is not administered intravenously. The period of reaching the maximum concentration (TCam) with epidural administration is less than 30 minutes. The connection with plasma proteins is 50-80%. It is distributed quickly (the half-distribution period is 6-9 min), first it enters the well-blood-supplying tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. Penetrates through the hematogen-cephalic barrier and the placental barrier, penetrates into breast milk (40% of the concentration in the mother's plasma).

Metabolised in the liver (by 90-95%) with participation of microsomal enzymes by dealkylation of the amino group and breaking of the amide bond with the formation of active metabolites (monoethylglycinexylidine and glycinexylidine) having a half-life (T1 / 2) - 2 hours and 10 hours, respectively. With liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value.

It is excreted with bile (part of the dose is reabsorbed in the digestive tract) and kidneys (up to 10% unchanged). With chronic renal failure, cumulation of metabolites is possible. Acidification increases the excretion of lidocaine.

Indications:Infiltration, conduction (including retrobulbar, parabulbarno anesthesia), spinal (subarachnoid) and epidural anesthesia.

Contraindications:

Hypersensitivity (including other amide local anesthetic drugs); infection of the site of the proposed injection; syndrome of weakness of the sinus node; atrioventricular blockade of II-III degree (except when an artificial pacemaker is installed); sinoauric blockade; Wolff-Parkinson-White syndrome (WPW syndrome); cardiogenic shock; violations of intraventricular conduction; closed angle glaucoma (with retrobulbar injection); pregnancy, breastfeeding (crosses the placental barrier, excreted in breast milk).

It is also necessary to take into account the general contraindications to the conduct of a particular type of anesthesia.

Carefully:

Chronic heart failure, severe renal insufficiency, hypovolemia, bradycardia, hypotension, myasthenia gravis, epileptiform convulsions (including history), acute disease, weakened patients,children's age (due to delayed metabolism, possible accumulation of the drug), elderly age (over 65 years), local anesthesia of the blood-rich areas.

For spinal (subarachnoid) and epidural anesthesia - chronic back pain, diseases of the central nervous system (including infection, tumors), peripheral neuropathy, headache (including migraine in the anamnesis), the presence of blood impurities in the cerebrospinal fluid, paresthesia, psychosis, dementia, hysteria, spinal deformity, aortic stenosis, idiopathic hypertrophic subaortic stenosis, treatment with acetylsalicylic acid or other antiplatelet agents.

Pregnancy and lactation:Data on the safety of lidocaine when it is used by pregnant women are not available. The use of the drug during pregnancy and during breastfeeding is possible only if the intended benefit to the mother exceeds the potential risk to the fetus and the baby. If it is necessary to prescribe the drug during breastfeeding, breastfeeding should be stopped.

Dosing and Administration:

The amount of solution and the total dose of lidocaine depends on the type of anesthesia, the nature and duration of the surgery.

For infiltration anesthesia: intradermally, subcutaneously. Apply a solution of lidocaine 5 mg / ml (maximum dose of 300 mg).

Conductive anesthesia: in dentistry - perineural, from 1 to 5 ml of a solution of lidocaine 20 mg / ml, total dose to 100 mg; when blocking the nerve plexuses - perineurally, from 5 to 10 ml of a solution of lidocaine 20 mg / ml (total dose up to 200 mg).

Parabulbar anesthesia: parabulbar, from 1 to 2 ml of a solution of lidocaine 20 mg / ml (total dose 20-40 mg).

Retrobulbaric anesthesia: retrobulbarno, 3 to 4 ml lidocaine 20 mg / ml (total dose 60-80 mg).

Spinal anesthesia: subarachnoid, 3 to 4 ml lidocaine 20 mg / ml (total dose 60-80 mg).

Epidural anesthesia: epidural, 10 to 15 ml of lidocaine 20 mg / ml (maximum total dose to 300 mg) or 1 to 2 ml of an anesthetic solution for each segment of the spinal cord to be blocked.

To prolong the action of lidocaine, it is possible to add ex tempore 0.1% (1 mg / ml) solution of adrenaline (epinephrine) (1 drop per 5-10 ml lidocaine solution, but not more than 5 drops for the entire volume of solution).

The maximum dose for adults is 4.5 mg / kg, but not more than 400 mg.

Recommended dosages for children with neuromuscular blockade are up to 5 mg / kg 0.25-1% (2.5-10 mg / ml) solution. The maximum dose for children is 5 mg / kg.

Side effects:

From the nervous system and sensory organs: dizziness, headache, weakness, motor anxiety, nystagmus, unconsciousness, drowsiness, visual and auditory disorders, tremor, trismus, convulsions (the risk of their development rises in the background of hypercapnia and acidosis), respiratory muscle paralysis, respiratory arrest, motor block and sensitive , respiratory paralysis (often develops with subarachnoid anesthesia).

From the cardiovascular system: increase or decrease in blood pressure, bradycardia, arrhythmia, tachycardia - when administered with vasoconstrictor, peripheral vasodilation, collapse, pain in the chest.

Allergic reactions: skin rash, hives (on the skin and mucous membranes), skin itching, angioedema, anaphylactic shock.

On the part of the organs of the gastrointestinal tract: nausea, vomiting, involuntary defecation.

From the side of the blood: methemoglobinemia.

Local Reactions: with spinal anesthesia - pain in the back, with epidural anesthesia - accidental entry into the subarachnoid space.

Other: persistent anesthesia, respiratory depression, up to a stop, hypothermia.

Overdose:

Symptoms: the first signs of intoxication - dizziness, nausea, vomiting, euphoria; then - convulsions of facial muscles of the face with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, general weakness, apnea, bradycardia, lowering of arterial pressure, collapse, methemoglobinemia; when used at birth in a newborn - bradycardia, oppression of the respiratory center, apnea.

Treatment: the patient should be in a horizontal position; prescribe oxygen inhalation. In cases of seizures, 10 mg of diazepam is administered intravenously. With bradycardia - M-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is not effective.

Interaction:

Vasoconstrictors (epinephrine, methoxamine, phenylephrine) extend the local anesthetic effect.

Cimetidine reduces hepatic clearance of lidocaine (decreased metabolism due to inhibition of microsomal oxidation) and increases the risk of toxic effects.

Reduces the effect of angiasthenic drugs.

When treating the site of injection of a local anesthetic with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of tenderness and swelling increases.

With the use of local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimetaphan camsyl-tom, the risk of a marked decrease in blood pressure and bradycardia increases. Beta-adrenoblockers slow the metabolism of lidocaine, increasing its toxicity (lowering the value of hepatic blood flow).

Lidocaine weakens the cardiotonic effect of cardiac glycosides. Strengthens and lengthens the effect of myorelaxing drugs. With the simultaneous use of lidocaine and hypnotics and sedatives, it is possible to intensify their inhibitory effect on the central nervous system. When combined with narcotic analgesics, an additive effect develops, which is used in epidural anesthesia, but respiratory depression is increased.

Use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of lowering blood pressure.

Anticoagulants (including ardeparin sodium, dalteparin sodium, sodium danarolide, sodium enoxaparin, heparin sodium, warfarin and others) increase the risk of bleeding.

Special instructions:

Avoid intravascular injection during administration. When diluted, the toxicity decreases. The use of epinephrine (epinephrine) is contraindicated in diabetes mellitus; glaucoma (narrow-angle form); thyrotoxicosis; decompensated form of cardiovascular diseases.

During the treatment period it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection 20 mg / ml.

Packaging:

Solution for injection 20 mg / ml in ampoules of 2 ml. For 10 ampoules with instructions for use, with an ampoule or ampoule ampoule knife in a pack or box of cardboard.

When packaging ampoules that have a break ring or an opening point, the ampoule knife or the ampoule scapegrator is not put in.

5 ampoules in a cassette outline package. 2 cassette contour packs with instructions for use in a pack of cardboard.

Storage conditions:Store in a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001555

Date of registration:11.02.2012/03.06.2013

The owner of the registration certificate:MICROGEN FGUP Scientific and Production Association MICROGEN FGUP Scientific and Production Association Russia

Manufacturer: & nbsp

MICROGEN FGUP NGO Russia

Information update date: & nbsp09.04.2016

Illustrated instructions

Instructions

Lidocaine (Lidocaine)