Structure
active ingredient - lidocaine hydrochloride (based on anhydrous substance) 20.0 g;
Excipients: sodium chloride 6 0 g, 1 M solution of sodium hydroxide to pH 5.0-7.0, water for injection, to 1 liter.
Pharmacological properties
Pharmacodynamics
It has a local anesthetic action, blocks voltage-dependent sodium channels, preventing the generation of impulses in the sensory nerves and the conduction of impulses along nerve fibers. Conduct not only suppresses pain impulses, but the momentum of the other modality. It is used in all kinds of local anesthesia infiltration, conduction and surface.
Anesthetic effect of lidocaine 2 - 6 times greater than procaine (faster acting and longer - to 75 min, and after addition of epinephrine - over 2 hours). When applied topically, dilates blood vessels, has no irritant action.
Has anti-arrhythmic (Ib class) properties. Stabilizes cell membranes, a sodium channel blocker, increases the permeability of the membrane to K +. Almost no effect on the electrophysiological state of the atrium, accelerates repolarization in the ventricles, inhibits phase IV depolarization in Purkinje fibers (especially ischemic myocardium), reducing their automatic nature and duration of the action potential, increases the minimum potential difference at which cardiomyocytes respond to premature stimulation.
At therapeutic doses improves conductivity in Purkinje fibers in connection with their contractile ventricular myocardium, thereby forming conditions eliminate the phenomenon of "re-entry» (re-entry), especially in ischemic conditions of the heart muscle, such as myocardial infarction. Shortens the duration of the action potential and effective refractory period.
Virtually no effect on the conductivity and contractility (depression of conductivity observed in the appointment only in large, close to the toxic dose) - the duration of the intervals PQ, QT and the width of the QRS complex on the electrocardiogram does not change. The negative inotropic effect was also expressed slightly and appears only briefly with the rapid introduction of the drug in high doses.
Indications for use
- Infiltration, terminal, and a spinal block anesthesia
- Treatment and prevention of mono-and polytopic ventricular tachycardia and of various origins, especially in the acute phase of myocardial infarction
- Relief of ventricular fibrillation
- Aid in the defibrillation of the heart.
Dosage and administration
To block anesthesia using 2% solution. The maximum total dose up to 400 mg (20 ml of 2% lidocaine hydrochloride).
Plexus blockade for 5 - 10 ml of a 2% solution.
For epidural 2% solution (300 mg of lidocaine hydrochloride).
To lengthen the action of lidocaine can be added ex tempore 0,1% solution of epinephrine (1 drop per 5 - 10 ml lidocaine, but not more than 5 drops of the entire volume of solution).
For anesthesia of mucous membranes (for intubation of the trachea, bronhoezo-fagoskopii, removal of polyps, maxillary sinus punctures, etc.) using a 2% solution of no more than 20 ml.
In ophthalmology: 2% solution is instilled into the conjunctival sac of 2 drops 2 - 3 times at intervals of 30 - 60 seconds immediately prior to surgery or examination.
As antiarrhythmic lidocaine injected first bolus (over 3 - 4 min), the average dose of 80 mg (50 - 100 mg), and then continue to enter the drip average from 2 mg per minute. The infusion is diluted 6 mL of 2% lidocaine solution ampoule in 60 ml of isotonic sodium chloride solution. The duration of infusion depends on the patient's condition and the results of the drug. Total amount of solution administered per day is about 1200 ml.
Children intravenously 1 mg / kg (and usually 50-100 mg) as a loading dose infusion rate of 25-50 mg / min (i.e., within 3-4 minutes), if necessary, repeated dosing at 5 min after the Why appoint a continuous intravenous infusion. Intravenously as a continuous infusion (usually after loading dose): The maximum dose for children - 30 ug / kg / min 920-50 ug / kg / min).
Attention!
With the rapid intravenous administration may be a sharp drop in blood pressure and develop collapse.
In these cases apply phenylephrine, ephedrine, and other decongestants.
Side effects
- Dizziness, headache, depressed mood, euphoria, neurotic reactions, confusion, drowsiness, tinnitus, paresthesia, diplopia, tremor, trismus facial muscles, seizures, loss of consciousness
- Reduction arterialnogo pressure, bradycardia, vasodilatation, arrhythmia, collapse, chest pain, cardiac arrest
- Skin rash, urticaria, pruritus, angioedema, anaphylactic shock
- Spinal anesthesia - a pain in the back, with an epidural anesthesia - a random hit in the subarachnoid space
- Nausea, involuntary urination and defecation, decreased libido, impotence, respiratory depression up to the stop.
Contraindications
- Hypersensitivity to the drug
- Sick sinus syndrome
- Bradycardia
- AV block grade 2 and 3 (except for the cases when the probe is introduced to stimulate the ventricles)
- Severe chronic heart failure
- Cardiogenic shock
- Severe hypotension
- Expressed human liver
- Hypersensitivity
- A history of epileptiform convulsions induced by lidocaine
Paracervical-for-purpose in obstetric practice - fetoplacental insufficiency, prematurity, postmaturity, toxemia of pregnancy
- For epidural anesthesia - neurological disease, spinal deformity
- For subarachnoid anesthesia - a pain in the back, central nervous system diseases (including infections, tumors), coagulopathy (due to anticoagulants or blood clotting disorders), headache (including migraine history), the presence of impurities of blood in the cerebro-spinal fluid, hypertension, hypotension, paresthesia, psychosis, hysteria, non-contact patient, spinal deformity.
Drug interactions
With the simultaneous use of lidocaine and beta-blockers may increase the toxic effects of lidocaine.
Irrationally prescribe lidocaine with ajmaline, amiodarone, quinidine or verapamil because of increased cardiodepressive action.
The combined use of lidocaine and procainamide may cause central nervous system excitation, hallucinations.
When administered intravenously geksenala or thiopental sodium on the background of lidocaine possible respiratory depression.
The combined use of lidocaine and definina should be used with caution as possible to reduce the resorptive action of lidocaine, as well as the development of an undesirable effect cardiodepressive.
Under the influence of monoamine oxidase inhibitors probably increased local anesthetic action of lidocaine. Patients receiving monoamine oxidase inhibitors should not be administered parenterally lidocaine.
When concomitant administration of lidocaine and polimikisina In the latter possibly under the influence of increased inhibitory effect on neuromuscular transmission, is used as an antiarrhythmic, so in this case it is necessary to monitor the patient's respiratory function.
The concomitant use of lidocaine with drugs or sedatives may increase depressant effect on the central nervous sitemu.
Under the influence of cimetidine intravenous lidocaine causes undesirable effects (stunning, drowsiness, bradycardia, etc.). If necessary, the combination therapy should decrease a dose of lidocaine.
Cautions
Use with caution. Used with caution in heart failure II-III century, severe liver and / or kidney failure, hypovolemia, AV block I-II degree, sinus bradycardia syndrome WPW, hypotension, myasthenia gravis, epileptiform convulsions (including history ), genetic susceptibility to malignant hyperthermia, acute illness, debilitated patients, in early childhood, in old age.
It should be cautiously administered lidocaine in highly vascularized tissue intravazalnogo to avoid contact with the drug, in this case shows a smaller dose of lidocaine.
Precautions should be administered under local anesthesia is rich in blood vessels of organs, should avoid intravascular injection during administration. When breeding toxicity decreases.
With the introduction of vascularized tissue is recommended to aspirate.
Prophylactic administration of any and all patients with acute myocardial infarction is not recommended (routine prophylactic administration of lidocaine may increase the risk of death due to an increase in the incidence of asystole).
With the ineffectiveness of lidocaine, you must first delete hypokalemia, in an emergency, there are several options for further action: a cautious increase in dose to the occurrence of side effects in the central nervous system (confusion, slurred speech), the appointment, sometimes sharing, drug class IA (procainamide) transition to the drugs class III (amiodarone, bretylium tosylate).
Forbidden to enter lidocaine retrobulbarno glaucoma patients.
Pregnancy and lactation.
Pregnant and lactating women drug should be used under strict indications.
Effects on ability to drive vehicles and management mechanisms.
During the period of treatment should refrain from activities potentially hazardous activities that require high concentration and speed of psychomotor reactions.
Overdose
Symptoms: The first signs of intoxication - dizziness, nausea, vomiting, euphoria, and then - seizures facial muscles with the transition to tonic-clonic spasms of skeletal muscles, agitation, weakness, apnea, bradycardia, decreased blood pressure, collapse, methemoglobinemia, when used in childbirth in newborn - bradycardia, respiratory center depression, apnea.
Treatment: The patient is intubated if necessary, carry out artificial respiration, in convulsions - diazepam 10 mg intravenously. Bradycardia - m-anticholinergics (atropine), vasoconstrictors (norepinephrine, phenylephrine. Dialysis is ineffective.
The above information is the study and can not be used for decision-making on the use of specific drug Any information presented on this site does not replace the advice of a doctor and can not guarantee any positive effect of the drug.
10 ampules 2 ml
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