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

Composition:1 ml solution for injection 20 mg / ml contains: active ingredient - lidocaine hydrochloride monohydrate (in terms of lidocaine hydrochloride) 20 mg; auxiliary substances - sodium chloride 6.0 mg; sodium hydroxide to pH 5.0-7.0; water for injection up to 1 ml.

Description:Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:Local anesthetic.

ATX: & nbsp

N.01.B.B Amides

N.01.B.B.02 Lidocaine

C.01.B.B.01 Lidocaine

C.01.B.B Antiarrhythmic drugs Ib class

Pharmacodynamics: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. Suppresses carrying out not only pain impulses, but also impulses of other modality. The anesthetic effect of lidocaine is 2-6 times stronger than procaine (it acts faster and longer - up to 75 minutes, and after the addition of epinephrine - more than 2 hours). With topical application dilates blood vessels, does not have a locally irritating effect.

Pharmacokinetics:Absorption is complete (the rate of absorption depends on the site of administration and the dose). With intramuscular injection, the time to reach the maximum concentration is 30-45 minutes.The connection with plasma proteins is 50-80%. It is distributed quickly (the half-life of the distribution phase is 6-9 minutes), first it enters the well-blood-supplying tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. It penetrates the blood-brain barrier, the placental barrier and into breast milk (40% of the concentration in the mother plasma).

Metabolised in the liver (by 90-95%) with the participation of cytochrome P450 by dealkylation of the amino group and breaking of the amide bond with the formation of active metabolites (monoethylglycine silidine and glycine silidine), the half-life of which is 2 h and 10 h respectively. With liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value.

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

Indications:All kinds of local anesthesia (anesthesia with trauma, surgical interventions, including cesarean section, analgesia of labor, painful diagnostic procedures, for example, arthroscopy): terminal (superficial) anesthesia, local infiltration anesthesia (subconjunctival), conductive anesthesia (incl.in dentistry, intercostal blockade, cervical vagosympathetic, intravenous regional anesthesia), caudal or lumbar epidural block, spinal (subarachnoid) anesthesia, conductive (retrobulbar, parabulbar) anesthesia.

Contraindications:Hypersensitivity; severe bleeding, shock, infection of the site of the proposed injection, arterial hypotension. For subarachnoid anesthesia - complete heart block, bleeding, arterial hypotension, shock, infection of the site of lumbar puncture, septicemia. Syndrome of weakness of the sinus node (especially in elderly patients), marked bradycardia, atrioventricular blockade of II-III degree (except when the probe is inserted for ventricular stimulation), sinoatrial blockade, Wolff-Parkinson-White syndrome, acute and chronic heart failure (II1 -IV functional class), cardiogenic shock, violations of intraventricular conduction, marked decrease in blood pressure, Adams-Stokes syndrome, retrobulbar injection to patients with glaucoma.

Carefully:State, accompanied by a decrease in hepatic blood flow (eg, chronic heart failure, liver disease), progression of cardiovascular disease (usually due to the development of heart block and shock), very sick, debilitated patients, older age (over 65 years), pregnancy, lactation (penetrates into the mother's milk); increased sensitivity to other amide local anesthetics in history.

Pregnancy and lactation:Lidocaine penetrates the placental barrier, excreted in breast milk. The application is possible only on strict indications.

Dosing and Administration:

For conduction anesthesia (anesthesia peripheral nerves, including in the nerve plexus blockade) is usually 5-10 ml of 20 mg / ml; the maximum total dose is up to 400 mg (20 ml of lidocaine solution 20 mg / ml).

Epidural anesthesia - to obtain analgesia 25-30 ml (250-300 mg) of a solution of 10 mg / ml is used; for anesthesia 15-20 ml (225-300 mg) solution 15 mg / ml or 10-15 ml (200-300 mg), 20 mg / ml; for thoracic epidural anesthesia - 20-30 ml (200-300 mg) of a solution of 10 mg / ml. It is not recommended to use continuous administration of anesthetic with a catheter; the maximum dose should not be repeated more than 90 minutes later.

When using caudal anesthesia: in obstetrical practice 200-300 mg (10-15 ml) of a solution of 20 mg / ml; in surgical practice - 15-20 ml (225-300 mg) of a solution of 15 mg / ml. It is not recommended to use continuous administration of anesthetic with a catheter; the maximum dose should not be repeated more than 90 minutes later. For conductive anesthesia of peripheral nerves: humerus - 15-20 ml (225-300 mg) of a solution of 15 mg / ml; in dental practice - 1-5 ml (20-100 mg) of a solution of 20 mg / ml; blockade of intercostal nerves - 3 ml (30 mg) of a solution of 10 mg / ml; paracervical anesthesia - 10 ml (100 mg) of a solution of 10 mg / ml in each direction, if necessary, repeated administration is possible in not less than 1.5 hours; paravertebral anesthesia - from 3 to 5 ml (30-50 mg) of a solution of 10 mg / ml.

Retrobulbaric anesthesia - 3-4 ml of a solution of 20 mg / ml. Parabulbar anesthesia -1-2 ml of a solution of 20 mg / ml.

Local infiltration (subconjunctival) - 0.5-1.0 ml of a solution of 20 mg / ml. Vagosimpathetic blockade: cervical spine (stellate node) - 5 ml (50 mg) of a solution of 10 mg / ml, lumbar - 5-10 ml (50-100 mg) of a solution of 10 mg / ml.

The maximum dose for adults is not more than 4.5 mg / kg or 300 mg; for intravenous regional anesthesia - no more than 4 mg / kg.

The effect of lidocaine can be prolonged by the addition of a 0.1% solution of epinephrine (0.1 ml per 20 ml of lidocaine).In this case, with regional anesthesia, the dose of lidocaine can be increased to 600 mg.

Side effects:

From the central and peripheral nervous system: 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 a vasoconstrictor, peripheral vasodilation, collapse, pain in the chest.

From the digestive system: nausea, vomiting, involuntary defecation.

From the side of the blood: methemoglobinemia.

From the urinary system: involuntary urination.

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

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

Measures to help with overdose

At the first signs of intoxication, the administration is discontinued. 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 ineffective.

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 decreased hepatic blood flow) and increases the risk of toxic effects. Beta-adrenoblockers slow the metabolism of lidocaine, increasing its toxicity (reducing the value of hepatic blood flow), increase the risk of developing bradycardia. Cardiac glycosides weaken the cardiotonic effect. With the simultaneous administration of lidocaine and hypnotics and sedatives, it is possible to intensify their inhibitory effect on the central nervous system. When combined with narcotic analgesics, the additive effect develops, which is used in epicurescent anesthesia, but respiratory depression is increased. Use with monoamine oxidase inhibitors (MAO) - furazolidone, procarbazine, selegiline, increases the risk of lowering blood pressure. Anticoagulants (including ardeparin sodium, dalteparin sodium, sodium danaparoid, sodium enoxaparin, heparin, warfarin and others) increase the risk of bleeding. Lidocaine reduces the effect of antimiasthenic drugs, enhances and lengthens the effect of myorelaxing drugs.

Alcohol enhances the oppressive effect of lidocaine on the center of breathing.

Special instructions:

Particular caution should be exercised when carrying out local anesthesia of vascular-rich organs; Avoid intravascular injection during administration. When administered to a vascularized tissue, an aspirating test is recommended.

It is necessary to abolish MAO inhibitors no less than 10 days before the planning of subarachnoid anesthesia with lidocaine.

Effect on the ability to drive transp. cf. and fur:During the treatment period, due to possible side effects from the cardiovascular and nervous system, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection 20 mg / ml 2 ml in ampoules.

Packaging:

5 ampoules are placed in a contour cell box made of a polyvinylchloride (PVC) film.

1 or 2 contour mesh packages together with the instruction for use and the ampoule ampoule or ampoule scarifier are placed in a pack of cardboard. 5 or 10 ampoules, together with the instruction for use and a scarifier ampoule or a knife ampoule, are placed in a pack of cardboard with a corrugated liner.

When using ampoules with a dot or a ring of fracture, a scarifier or ampoule knife is not inserted.

Storage conditions:In the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001065

Date of registration:27.10.2011/20.05.2014

Date of cancellation:2016-10-27

The owner of the registration certificate:ELLARA, LTD. ELLARA, LTD. Russia

Manufacturer: & nbsp

ELLARA, LTD. Russia

Information update date: & nbsp11.04.2016

Illustrated instructions

Instructions

Lidocaine (Lidocaine)