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CAS No: 137-58-6
Appearance: White crystalline powder
Melting point: 66-69º C
Solubility: Soluble in water
Water solubility: Practically insoluble
Storage: Store in a well-closed container away from moisture and strong light
Application: It is a common local anesthetic and antiarrhythmic drug.
Lidocaine is a common local anesthetic and class-1b antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning, and pain from skin inflammations, injected as a dental anesthetic, or used as a local anesthetic for minor surgery. It replaces procaine,being widely used in plastic and cosmetic operation in local infiltration anesthesia, the sodium channel inhibition of the nerve cell membrane to block nerve excitability and conduction.
It is on the World Health Organization's List of Essential Medicines, a list of the most important medications needed in a basic healthcare system
The efficacy profile of lidocaine as a local anesthetic is characterized by a rapid onset of action and intermediate duration of efficacy. Therefore, lidocaine is suitable for infiltration, block, and surface anesthesia. Longer-acting substances such as bupivacaine are sometimes given preference for subdural and epidural anesthesias; Lidocaine, though, has the advantage of a rapid onset of action. Epinephrine vasoconstricts arteries, reducing bleeding and also delays the resorption of lidocaine, almost doubling the duration of anaesthesia. For surface anesthesia, several available formulations can be used e. G. For endoscopies, before intubations, etc. Buffering the pH of lidocaine makes local freezing less painful. Lidocaine drops can be used on the eyes for short ophthalmic procedures.
Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.
Lidocaine is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide. The pharmacological/toxicological actions of these metabolites are similar to, but less potent than, those of Lidocaine. Approximately 90% of Lidocaine administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged. The primary metabolite in urine is a conjugate of 4-hydroxy-2, 6-dimethylaniline.
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