Lidocaine hydrochloride

Lidocaine hydrochloride, an organic compound with the chemical formula C14H23ClN2O, is used primarily as a local anesthetic and antiarrhythmic agent.

Pharmacology and toxicology

When the concentration of blood drug exceeds 5μg·mL-1, convulsion can occur, and at low doses, it can promote the outflow of k+ in cardiomyocytes, reduce the myocardial automatism, and has the effect of anti-ventricular arrhythmia. At the treatment dose, the electrical activity of cardiomyocytes, atrioventricular conduction and myocardial contraction had no significant effect. The further increase of blood concentration can cause the heart conduction speed to slow down, atrioventricular block, inhibit myocardial contractility and reduce cardiac output.

It is a local anesthetic and antiarrhythmic drug. It is mainly used in infiltration anesthesia, epidural anesthesia, surface anesthesia (including mucosal anesthesia during thoracoscopy or abdominal surgery) and nerve block. It can be used for premature ventricular beats and ventricular tachycardia after acute myocardial infarction. It can also be used for digitalis poisoning, cardiac surgery, and ventricular arrhythmias caused by cardiac catheterization. It is usually ineffective against supraventricular arrhythmias.

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pharmacokinetics

After injection, tissue distribution is rapid and wide, and it can penetrate the blood-brain barrier and the placenta. The drug has high anesthetic intensity, rapid effect and strong dispersion. It takes about 2 hours for the drug to be eliminated locally. The addition of epinephrine can prolong its action time. Most of them were first degraded by liver microenzyme to the deethylated intermediate metabolite monoethyl glycinamide xylene, which still had local anesthetic effect, with increased toxicity, and then hydrolyzed by amidase, and excreted in urine, about 10% of the dosage was excreted in its original form, and a small amount appeared in bile.