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Lidocaine hydrochloride is an amide-type local anaesthetic. After blood absorption or intravenous administration, it has obvious excitatory and inhibitory biphasic effects on the central nervous system, and can be excitatory without precursor, when the blood concentration is low, there is analgesia and drowsiness, and the pain threshold is increased; with the increase of the dose, the effect or toxicity is enhanced, and there is an anticonvulsant effect at subintoxicating blood concentrations; when the blood concentration exceeds 5 μg - ml-1 there can be convulsions.
Lidocaine hydrochloride in low doses, can promote the cardiomyocyte K + outflow, reduce myocardial autoregulation, and anti-ventricular arrhythmia effect; in therapeutic doses, the electrical activity of cardiomyocytes, atrial conduction and myocardial contraction has no significant effect; blood concentration further increase, can cause cardiac conduction slowing down, atrioventricular conduction block, inhibition of myocardial contraction and so that the volume of cardiac blood discharge decreased.
Uses and functions of Lidocaine Hcl.
Lidocaine hydrochloride is a medium-acting amide local anaesthetic. It is used as local anaesthetic and antiarrhythmic drug.
It is mainly used for:
(1) Infiltration anaesthesia, epidural anaesthesia, surface anaesthesia (including for mucosal anaesthesia during thoracoscopy or laparotomy) and nerve conduction block.
(2) Treatment of ventricular premature beats and ventricular tachycardia after acute myocardial infarction (AMI) and ventricular arrhythmia caused by digitalis intoxication, cardiac surgery, cardiac catheterisation, but usually ineffective for supraventricular arrhythmia.
Local anaesthetics, antiarrhythmics for various anaesthesia and tachy ventricular arrhythmias.
Drug interactions of Lidocaine Hcl.
(1) Cimetidine, β-blockers can inhibit the metabolism of lidocaine through the liver, so that its blood concentration increases, cardiac and neurological adverse reactions can occur, the dose of lidocaine hydrochloride should be adjusted. (2) Barbiturates can promote the metabolism of lidocaine hydrochloride, and the combination of the two drugs can cause bradycardia and sinus arrest.
(3)Combination with procainamide can produce transient delirium and hallucinations, but does not affect the blood concentration of this product.
(4) Isopropyl adrenaline can increase the total clearance of this product due to increased hepatic blood flow; norepinephrine can decrease the total clearance of lidocaine hydrochloride due to decreased hepatic blood flow.
(5) Contraindicated with the following drugs: phenobarbital, sodium thiopental, sodium nitroprusside, mannitol, amphotericin B, ampicillin, sulfasalazine.
Adverse reactions of Bulk Lidocaine Hcl Powder.
The incidence of adverse reactions to lidocaine hydrochloride is approximately 6.3%. Most adverse reactions are dose-related.
Adverse reactions include drowsiness, dizziness, vertigo, nausea, vomiting, lethargy, euphoria, confusion, muscle twitching, convulsions, blurred vision, confusion and dyspnoea, etc. High doses may produce severe sinus bradycardia, cardiac arrest, severe atrioventricular block and diminished myocardial contraction, and decreased blood pressure.
Excessive concentration of lidocaine hydrochloride in the blood can cause slowing of atrial conduction velocity, atrioventricular block (A-V-B) as well as inhibition of myocardial contractility and decreased cardiac output.
Few have allergic reactions such as erythematous rash and angioneurotic oedema.
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