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

Composition:1 ml of the solution contains the active substance: lidocaine hydrochloride (in terms of anhydrous substance) - 20.0 mg or 100.0 mg; auxiliary substances: sodium chloride - 6.0 mg, sodium hydroxide 1 M solution - to a pH of 5.0-7.0, water for injection - up to 1 ml.

Description:Transparent, colorless or slightly colored liquid.

Pharmacotherapeutic group:local anesthetic, antiarrhythmic agent.

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:

Lidocaine in chemical structure refers to acetanilide derivatives. Has a pronounced local anesthetic and antiarrhythmic (lb class) action. The local anesthetic effect is due to the inhibition of nerve conduction by blocking the sodium channels in nerve endings and nerve fibers. By its anesthetic action lidocaine significantly (2-6 times) exceeds procaine; the action of lidocaine develops faster and lasts longer - up to 75 minutes, while with simultaneous application with epinephrine - more than 2 hours. With topical application dilates blood vessels, does not have a locally irritating effect.

Antiarrhythmic properties of lidocaine are due to its ability to stabilize the cell membrane, block sodium channels, increase the permeability of membranes for potassium ions. Virtually without affecting the electrophysiological state of the atria, lidocaine accelerates repolarization in the ventricles, depresses the IV depolarization phase in Purkinje fibers (diastolic depolarization phase), reducing their automatism and duration of action potential, increases the minimal potential difference at which myofibrils react to premature stimulation. The speed of rapid depolarization (phase 0) does not affect or slightly reduces. Has no significant effect on conduction and contractility of the myocardium (inhibits conductivity only in large, close to toxic doses). Intervals PQ, QRS and QT under its influence on the electrocardiogram (ECG) do not change. Negative inotropic effect is also expressed slightly and manifests itself briefly only with the rapid administration of the drug in large doses.

Pharmacokinetics:

Time to reach the maximum concentration in the blood plasma after intramuscular injection - 5-15 minutes,with a slow intravenous infusion of the initial saturating dose - after 5-6 hours (in patients with acute myocardial infarction - up to 10 hours). Proteins of blood plasma bind 50-80% of the drug. Rapidly distributed (half-life of the distribution phase - 6-9 minutes) in organs and tissues with good perfusion, incl. in the heart, lungs, liver, kidneys, then in muscle and adipose tissue.

Penetrates through the blood-brain and placental barriers, is secreted with the mother's milk (up to 40% of the concentration in the mother's plasma). Metabolized mainly in the liver (90-95%) with the participation of microsomal enzymes with the formation of active metabolites - monoethylglycinexylidide and glycinexylidide, having a half-life of 2 hours and 10 hours, respectively. The intensity of metabolism decreases with liver diseases (can be from 50 to 10% of the normal value); if there is a violation of liver perfusion in patients after myocardial infarction and / or with congestive heart failure. Half-life with continuous infusion for 24-48 hours - about 3 hours; if the kidney function is impaired - can increase 2 or more times. It is excreted with bile and urine (up to 10% unchanged).Acidification increases the excretion of lidocaine.

Indications:Infiltration, conductive, spinal and epidural anesthesia. Terminal anesthesia in ophthalmology. Preventing re ventricular fibrillation during acute coronary syndrome and recurrent paroxysmal ventricular tachycardia (usually within 12-24 hours). Ventricular arrhythmias due to glycosidic intoxication.

Contraindications:Syndrome of weakness of the sinus node; severe bradycardia; atrioventricular block II-III level (except in cases where a probe to ventricular pacing): sinoatrial block, Wolff-Parkinson-White syndrome, acute and chronic heart failure (III-IV functional class): cardiogenic shock, marked decrease in blood pressure, Adams-Stokes syndrome: violations of intraventricular conduction, hypersensitivity to any of the components of the drug; retrobulbar injection to patients with glaucoma.

Carefully:Chronic heart failure II-III functional class, severe hepatic and / or renal failure, hypovolemia, degree atrioventricular block III,sinus bradycardia, arterial hypotension, severe myasthenia gravis, epileptiform cramps (including in anamnesis).

Pregnancy and lactation:During pregnancy and lactation, the drug should be used when the benefit exceeds the risk for the pregnant and the mother, for the fetus and the newborn (penetrates the placental barrier, excreted in breast milk).

Dosing and Administration:

For infiltration anesthesia: intradermally, subcutaneously, intramuscularly. Apply lidocaine solution for blockade of peripheral nerves and nerve plexuses: perineurally, 5-10 ml of solution 20 mg / ml, for conductive anesthesia: perineurally apply a solution of 20 mg / ml (not more than 400 mg), for epidural anesthesia: epidural solution of 20 mg / ml (not more than 300 mg), for spinal anesthesia: subarachnoid, 3-4 ml of a solution of 20 mg / ml (60-80 mg), in ophthalmology: a solution of 20 mg / ml is instilled in a conjunctival bag 2 drops 2-3 times with an interval of 30-60 seconds immediately before surgery or research.

To prolong the action of lidocaine, it is possible to add ex tempore 0.1% adrenaline solution (1 drop per 5-10 ml lidocaine solution, but not more than 5 drops for the entire volume of the solution).It is recommended to reduce the dose of lidocaine in elderly patients and patients with liver diseases (cirrhosis, hepatitis) or with reduced hepatic blood flow (chronic heart failure) by 40-50%. With chronic renal failure, dose adjustment is not required.

As an antiarrhythmic drug intravenously, 25 ml of a solution of 100 mg / ml, 100 ml of physiological solution should be diluted to a lidocaine concentration of 20 mg / ml. This diluted solution is used to administer a loading dose. The administration begins with a loading dose of 1 mg / kg (for 2-4 minutes at a rate of 25-50 mg / min) with immediate connection of a constant infusion at a rate of 1-4 mg / min. Due to the rapid distribution (half-life of approximately 8 minutes), 10-20 minutes after the first dose, the concentration of the drug in the blood plasma decreases, which may require repeated bolus administration (against a background of constant infusion) at a dose of 1 / 2-1 / 3 loading dose, with an interval of 8-10 minutes. The maximum dose at 1 hour is 300 mg, per day 2000 mg. Intravenous infusion is usually performed for 12-24 hours with constant ECG monitoring, after which the infusion is discontinued to assess the need for changing antiarrhythmic therapy in the patient.

Side effects:

From the central and peripheral nervous system: headache, dizziness, weakness, motor anxiety, nystagmus, unconsciousness, drowsiness, visual and auditory disorders, tremors, convulsions (the risk of their development rises in the background of hypercapnia and acidosis), the syndrome of "horse tail" (paralysis of legs, paresthesia) - causes more often other local anesthetics, paralysis of the respiratory muscles, respiratory arrest, motor and sensory block, respiratory paralysis (more often with subarachnoid anesthesia), numbness of the tongue (when used in dentistry).

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

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

From the urinary system: involuntary urination.

From the digestive system: 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, decreased libido and / or potency, hypothermia.

Overdose:

Symptoms: the first signs of intoxication - dizziness, nausea, vomiting, euphoria; then - convulsions of mimic muscles of the face with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, asthenia, 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 case of seizures, 10 mg of diazepam is administered intravenously. With bradycardia - m-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is ineffective.

Interaction:Beta-blockers and cimetidine increase the risk of toxic effects. Reduces the cardiotonic effect of digitoxin. It enhances the muscle relaxation of curare-like drugs. Strengthens and prolongs the action of muscle relaxants. Aymalin, amiodarone, verapamil and quinidine increase the negative inotropic effect. Inducers of microsomal liver enzymes (barbiturates, phenytoin, rifampicin) reduce the effectiveness of lidocaine. In addition, when combined with phenytoin may develop cardiodepressant effect. Vasoconstrictors (epinephrine, methoxamine, phenylephrine) lengthen the local anesthetic effect of lidocaine and can cause an increase in blood pressure and tachycardia. Lidocaine reduces the effect of antimiasthenic drugs (proserine, oxazil, etc.). Co-administration with procainamide can cause excitation of the central nervous system, hallucinations. Guanadrel, guanethidine. mecamylamine, trimetaphan increase the risk of a marked decrease in blood pressure and bradycardia. Under the influence of monoamine oxidase inhibitors, local anesthetic action of lidocaine and a decrease in blood pressure are likely. Patients taking monoamine oxidase inhibitors should not be prescribed lidocaine parenterally. With the simultaneous administration of lidocaine and polymyxin-B, it is necessary to monitor the function of the patient's breathing.With the combined use of lidocaine with hypnotics or sedatives, narcotic analgesics, hexenal or thiopental sodium, it is possible to intensify the inhibitory effect on the central nervous system and respiration. When intravenous lidocaine is administered to patients receiving cimetidine, such undesirable effects as stunnedness, drowsiness, bradycardia, paresthesia, etc. are possible. This is due to the increase in lidocaine in the blood plasma, which is explained by the release of lidocaine from the connection with blood proteins, as well as the slowing of its inactivation in the liver. If the need for combined therapy with these drugs should reduce the dose of lidocaine. When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of tenderness and swelling increases.

Special instructions:

Particular caution should be exercised when carrying out local anesthesia of vascular-rich organs; Avoid intravascular injection during administration.

When injected into vascularized tissue, it is recommended that an aspiration test be performed.It is necessary to abolish monoamine oxidase inhibitors at least 10 days before the planning of sub-archnoid anesthesia with lidocaine. During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for injection 20 mg / ml and 100 mg / ml.

Packaging:For 10 ampoules of 2 ml together with the instructions for use and a knife ampoule or scarifier in a box of cardboard.

Storage conditions:In the 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 the product after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003576 / 01

Date of registration:15.05.2009/02.10.2009

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp13.04.2016

Illustrated instructions

Instructions

Lidocaine (Lidocaine)