Lidocaine

Chemical name

(2-Диэтиламино)-N-(2,6-дим етилфенил)ацетамид (and as hydrochloride)

Gross

C14-H22-N2-O

Characteristics

White or almost white crystalline powder, poorly soluble in water. Used in the form of muriate of salt, easily soluble in water.

Of drugs

The drugs-mestnoanestezirutee, antiaritmicescoe. Antiaritmical activity from oppression phase 4 (diastolicescoy depolarization) in the Purkinje fibres, the lower automaticity, down ectopiceskih pockets institute. The speed rapid depolarization (phase 0) does not affect or slightly lower. Increases permeability membrane potassium ions, accelerating the repolarization and shorter potential actions. Do not alter anxiety sinusno-predserdnyi unit have little impact on the conductivity and airway diseases. When in / with the introduction of the fast and short (10-20 minutes). Mechanism местноанестезирующег о effect is to stabilize neironalna membrane, reducing its permeability to sodium ions, which prevent the emergence of potential actions and impulses. Chance of antagonism with calcium ions. Rapidly hydrolyses in alkalescent environment tissues and after a short latent period is valid for 60-90 min. When sprouts (tissue disorders) anestezirutaya activity declining. Effective in all types of local anaesthetics. Increase receptacles. There is irritating to the Tkani.pri in / in a C_max is created on the fabric (a 45-90 s) at the m-by 5-15 min. It is rapidly absorbed by the mucous membrane upper respiratory tract or of the oral cavity (C_max is 10 to 20 minutes). After intake of material is 15-35%, as 70% vsosavchegosa drug biotransformation is the "first pass" through the liver. The plasma to 50-80% is associated with malnutrition. Stable concentration in the blood in 3-4 hour with continuous on / in the introduction (in patients with acute myocardial infarction, through the 8-10 h). Therapeutic effect dispensed with the concentration of 1.5-5 µ g / J Easily passes through gistogematicalkie barriers, including GEB. First is a well krovosnabjatesa tissue (heart, lungs, brain, liver, spleen), then at jirovu and muscle tissue. Penetrates through the placenta, in the body of a newborn found 55% of mothers. T_1/2 after in / in bolusni a-half hours (from newborns to three hours), with the long / in infuziah to three hours or more. If any liver T_1/2 may be extended twice or more. Quickly and almost completely metabolized in the liver (unchanged to the urine output of less than 10%). The main way of oxidative - N-desalkilirovnie, with the formation of active metabolites (моноэтилглицинксили��ин and glitzinksilidin) with T_1/2 2 h and 10 h respectively. The duration of 10 to 20 minutes in the on / in the introduction and 60-90 min, with the on / m.

Indications

Jeludockove ekstrasistolia and tahiaritmii, incl. Acute myocardial infarct, in aftercare period fibrillace testing; Local anaesthesia : superficial, infiltrazionnaya, provodnikova, epiduralnaya, spinalnaya, intraligamentarnaya with operational intervention painful manipulation, endoscopic and instrumental studies.

Restrictions on the use of

Pregnancy, breast-feeding (at the time of treatment should stop breastfeeding).

Contraindications

Hypersensitivity, in the history epileptiformnah convulsing on the lidocaine, Wpw-sindrom, cardiogenny shock weakness sinusnogo unit blockade hearts (AV, vnutrijeludockova, sinusno-predserdnaya), severe liver disease, male.

Side-Effects

Oppression or initiation CNS, nervousness, euphoria, drowsiness, headache, dizziness, nausea, noise in the ears, a sense of heat, cold or numb limbs, the consciousness, stops breathing, muscle apnoea, tremor, disorientation, convulsions, sinusova aetiology, the conductivity, transverse blockade heart, hypotension, collapse, malignant hyperthermia, oppression immune system, allergic reaction (rash, generalizovanny exfoliativei dermatitis, anaphylactic shock); brief stinging sensation in the area of the spray.

Specific guidance

Extension of anestetika possible to add one drop of 0.1% solution of adrenalin by 5-10 ml lidocaine (with a maximum permissible dose is increased to 500 mg).

Patient interaction

Beta-adrenoblokatora more likely bradikardii and hypotonia. Noradrenalin and beta-adrenoblokatora reducing liver blood reduces (increases toxicity), and izadrin glukagon - Cl increase lidocaine. Zimetidin increases concentration in plasma (excluding from the protein and inachtiwatia down in the liver). Barbiturates, causing induction mikrosomaionah enzymes stimulate degradation of lidocaine and less active. Anti funds (gidantoina derivatives) also biotransformatia up in the liver (decreasing concentration in the blood), potenziruut as antiaritmiki (amiodaron, verapamil, quinidine, aymalin) cardiodepressiu. Combining with novokainamidom may cause the initiation of CNS and hallucinations. Do dampening effect anaesthesia (gexenal, thiopental), and sleeping sedative drugs at the centre of breathing weakens cardiotonicescoe influence digitoksina, deepens miorelaksaciu caused kurarepodobnami drugs (possible paralysis of the respiratory muscles). MAO inhibitors prolong local anaesthesia.

Overdosing

Symptoms : agitation, dizziness, general weakness, the decline AD tremor, tonico-clauniceskie convulsions, coma, collapse possible AV blockade oppression of the central nervous system and it stops Dahania.lechenie : Halt reception pneumonic ventilated rooms, anti-convulsants, vazokonstrictora (noradrenalin, mezaton), and bradikardii - holinolitiki (atropine). Perhaps the intubations, IVL, coming events. Dialysis ineffective.

Precautions

Caution must be exercised liver and kidney diseases, gipovolemii, severe heart failure in violation sokratimosti, genetic predisposition to malignant gipertermii. The children, handicapped and elderly patients require dose adjustment in accordance with the age and physical status. With the vascularizirovanne tissue recommended aspiratinuyu sample.

Dosing and Administration

Adults : in / in struino (within 3-4 minutes) 50-100 mg / kg body weight) with a speed of 25 to 50 mg / min, and then drip Quick 1-4 mg / min. V / m at the rate of 4.3 mg / kg body weight, if necessary again in 60-90 min. The maximum dose for adults with the in / in and / m introduction to 300-400 mg for 1 h. The maximum daily dose is 2,000 mg. Children entering struino 1 mg / kg at a speed of 25 to 50 mg / min, 5 min possible reintroduction of the (total dose should not exceed 3 mg / kg). Infuziruut Then at the speed of 30 µ g / kg / min. The maximum daily dose for children - 4 mg / Cg.dla surface anaesthesia-10% solution (200 mg-2 ml). The adults for branches anaesthesia used 0.5% solution for the conductive 1-2% solution. The maximum total dose-400 Mg.detam up to two years to appoint surface anaesthesia previously causing at 28C Tampon, 1-2 aerosol dose (4,8-9,6 mg). In ophthalmology-2 drops 2-4% solution in kongungualny bag for 30-60 min before the operation.

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