Has locally anesthetic effect, blocking the voltage-dependent sodium channels, which prevents the generation of pulses in the endings of the sensory nerves and the conduction of impulses along nerve fibers. It suppresses the conduct not only of pain impulses, but impulses another modality. It is used in all kinds anadrol pills of local anesthesia: infiltration, conduction and surface.
Lidocaine anesthetic effect lasts for up to 75 min, and after addition of epinephrine -. 2 hours, When applied topically, dilates blood vessels, has no irritant action. It has antiarrhythmic (Ib class) properties.Stabilizes cell membranes, inhibit sodium channels, increases the permeability of membranes for potassium ions. Almost no effect on atrial electrophysiological state, accelerates repolarization in the ventricles, inhibits the depolarization phase IV in Purkinje fibers (especially ischemic myocardium), reducing their automaticity and the length of the building.
At therapeutic doses, it improves conductivity in Purkinje fibers in place of their connection with ventricular myocardial contractility, thereby contributing to the elimination of conditions for the formation of the phenomenon of “re-entry” (re-entry), especially in the conditions of ischemic damage to the heart muscle, such as myocardial infarction. It shortens the duration of the action potential and the effective refractory period. Virtually no effect on myocardial contractility and conductivity (conductivity inhibition observed when assigning only in large, close to the toxic dose) – the duration of PQ interval, QT and QRS complex width electrocardiographic changes. The negative inotropic effect is also expressed slightly and appears only briefly with the rapid introduction of the drug in high doses.
For parenteral administration, total absorption (absorption rate depends on the site of administration and dose). The period to reach maximum concentration (Tmax) when administered intravenously – 3-5 minutes after intramuscular injection – 30-45 minutes. Connection with the plasma protein -50-80%. Rapidly distributed (distribution half-life phase – 6-9 minutes), first enters the well-perfused tissues (heart, lungs, brain, liver, spleen), followed by fat and muscle tissue. It penetrates through the blood-brain barrier and the placental barrier, is secreted in human milk (40% of maternal plasma concentrations). The half-life (T1 / 2) (after intravenous bolus) – 1.5-2 hours; neonatal -. 3 h after prolonged infusion over 24-48 hr significantly increased (up to 3 hours). If any of the T1 / 2 of the liver is increased by 2-fold or more. At a constant infusion (administration without an initial loading dose) a therapeutically effective concentration (2.6 .mu.g / ml) is achieved in 5-9 hours.
It is metabolized in the liver (90-95%) with microsomal enzymes by dealkylation amino group and an amide bond rupture to form active metabolites (monoetilglitsinksilidin and glitsinksilidin) having a T1 / 2 – 2 hours and 10 hours, respectively. Liver diseases and metabolic rate is reduced from 50% to 10% of the normal value.
Excreted in the bile (the dose undergoes reabsorption in the gastrointestinal tract and kidneys (up to 10% unchanged). In chronic renal failure possible accumulation of metabolites. Acidification of the urine increases the release of lidocaine.
Indications for use:
infiltration, conduction, epidural, spinal anesthesia and the terminal; treatment and prevention of mono- and politopnye tachycardia and ventricular arrhythmias of various origins, especially in the acute phase of myocardial infarction;
- sick sinus syndrome;
- atrioventricular block grade 2 and 3 (with the exception of cases where a probe to stimulate the ventricles);
- severe chronic heart failure;
- cardiogenic shock;
- severe hypotension, collaptoid state;
- liver failure;
- a history of epileptiform seizures caused by lidocaine;
- for paracervical destination in obstetric practice – fetoplacental insufficiency, prematurity, postmaturity, toxemia of pregnancy;
- for epidural anesthesia – neurological diseases, spinal deformity;
- for subarachnoid anesthesia – back pain, central nervous system diseases (including infections, tumors), coagulopathy (caused by anticoagulant or impaired clotting), headache (including migraine history), the presence of blood in cerebrospinal fluid, hypertension, hypotension, paresthesia, psychosis, hysteria, non-contact patient, spinal deformity.
With care – heart failure II-III degree, cardiovascular failure, liver and / or kidney failure, hypovolemia, atrioventricular block I degree, sinus bradycardia, Wolff-Parkinson-White syndrome, hypotension, myasthenia gravis, pregnancy, lactation, children under 6 years old age.
From the anadrol pills nervous system and sensory organs: dizziness, headache, depressed mood, euphoria, neurotic reactions, confusion, drowsiness, tinnitus, paresthesia, diplopia, tremor, trismus facial muscles, seizures, loss of consciousness. Cardio-vascular system: decrease in blood pressure, bradycardia, vasodilation, arrhythmia, collapse, chest pain, cardiac arrest.
Allergic reactions: skin rash, urticaria, pruritus, angioedema, anaphylactic shock.
Local reactions: when spinal anesthesia – the pain in the back, with epidural anesthesia – accidentally getting into the subarachnoid space.
Other: nausea, involuntary urination and defecation, decreased libido, impotence, respiratory depression up to the stop.
Symptoms: The first symptoms of poisoning – dizziness, nausea, vomiting, euphoria; then – spasms of mimic muscles of the face with the transition to tonic-clonic spasms of skeletal muscles, agitation, weakness, apnea, bradycardia, decreased blood pressure, collapse, methaemoglobinaemia; when used in childbirth newborn – bradycardia, respiratory center depression, apnea.
Treatment: The patient must be in a horizontal position; administered oxygen inhaled and intravenously administered 10 mg of diazepam. In cases of manifestations of skeletal muscle cramps, last cropped slow intravenous administration of a 1% solution of sodium thiopental or hexobarbital. If bradycardia – M-anticholinergics (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is not effective.
Interaction with other drugs:
In an application Likaina ® and beta-blockers may increase the toxic effects of lidocaine.
Irrationally appoint Likain ® with aymalinu, amiodarone, quinidine or verapamil due to increased cardiodepressive action.
The combined use of Likaina ® and procainamide can cause central nervous system excitation, hallucinations.
When administered intravenously, hexenal or thiopental sodium on the background of Likaina possible respiratory depression.
Combined use Likaina definina and 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 inhibitors of monoamine oxidase probably strengthen local anesthetic action of lidocaine. Patients receiving monoamine oxidase inhibitors should not be administered parenterally Likain.
When concomitant administration Likaina and polimikisina in under the influence of the latter may increase inhibitory effect on neuromuscular transmission, used as an antiarrhythmic, however in this case it is necessary to monitor the patient’s respiratory function.
The combined application Likaina ® with drugs or sedatives may increase depressant effects on the central nervous system. Under the influence of intravenous cimetidine Likaina ® cause unwanted effects (torpor, lethargy, bradycardia, etc.). If necessary, the combination therapy should decrease a dose Likaina ® .
Barbiturates, phenytoin, rifampin (inducers of microsomal liver enzymes) reduce efficiency (increasing the dose may be required).
It reduces the effect of antimiastenicheskih drugs. In the appointment of aymalinu, phenytoin, quinidine, amiodarone may increase the negative ionotropic effect. Curariform medications increase muscle relaxation. Procainamide increases the risk of central nervous system excitation, hallucinations.
When administered intravenously hexobarbital or thiopental sodium on the background of lidocaine possible respiratory depression. Anticoagulants (including heparin, warfarin, etc.) Increase the risk of bleeding. It does not reduce the antimicrobial activity of sulfonamides (when the metabolism is no formation of para-aminobenzoic acid).
10% solution used only intramuscularly.
Prophylactic all, without exception, patients with acute myocardial infarction is not recommended (routine prophylactic Likaina ® may increase the risk of death due to an increase in the incidence of asystole).
With the ineffectiveness as an antiarrhythmic must first eliminate hypokalemia. In urgent situations possible: a cautious increase in the dose until the side effects of the central nervous system (confusion, slurred speech); or appointment, sometimes joint, IA class of drugs (procainamide), the transition to Class III drugs (amiodarone, bretylium tosylate). The caution should be used when local anesthesia is rich in blood vessels of organs; intravascular injection should be avoided during administration. When breeding toxicity decreases.
In the period of treatment should refrain from activities potentially hazardous activities that require high concentration and psychomotor speed reactions.
With rapid intravenous administration can occur a sharp fall in blood pressure and develop collapse.
In these cases, use phenylephrine, ephedrine, and other decongestants.
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