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Lidocaine, also known as lignocaine and sold under the brand name Xylocaine among others, is a local anesthetic of the amino amide type. [10] It is also used to treat ventricular tachycardia and ventricular fibrillation .
Notable drugs that experience a significant first pass effect are buprenorphine, chlorpromazine, cimetidine, diazepam, ethanol (drinking alcohol), imipramine, insulin, lidocaine, midazolam, morphine, pethidine, propranolol, and tetrahydrocannabinol (THC). First-pass metabolism is not to be confused with Phase I metabolism, which is a separate ...
Many local anesthetics fall into two general chemical classes, amino esters (top) and amino amides (bottom). A local anesthetic (LA) is a medication that causes absence of all sensation (including pain) in a specific body part without loss of consciousness, [1] providing local anesthesia, as opposed to a general anesthetic, which eliminates all sensation in the entire body and causes ...
Tocainide is a lidocaine derivative, that undergoes very less first pass metabolism. It occurs as two enantiomers. The R isomer is three times more potent than the S isomer. [5] Tocainide's oral bioavailability is almost 100%. [6] Plasma half-life generally lasts for 11.5-15.5 hours (13.5 ± 2 hours [7]). In the blood, tocainide is 10-20% ...
Structurally, amino esters consist of three molecular components: a lipophilic part (ester); an intermediate aliphatic chain; a hydrophilic part (amine); The chemical linkage between the lipophilic part and the intermediate chain can be of the amide-type or the ester-type, and is the general basis for the current classification of local anesthetics.
Studies comparing lidocaine and articaine found that articaine is more effective than lidocaine in anaesthetising the posterior first molar region. [12] Articaine has been found to be 3.81 times more likely than lidocaine to produce successful anaesthesia when used for infiltration injections.
It is used as a eutectic mixture with lidocaine, 50% w/w, as lidocaine/prilocaine. The mixture is an oil with a melting point of 18 °C (64 °F). A 5% emulsion preparation, containing 2.5% each of lidocaine/prilocaine, is marketed by APP Pharmaceuticals under the trade name EMLA (an abbreviation for eutectic mixture of local anesthetics). [3]
It attempts to analyze chemical metabolism and to discover the fate of a chemical from the moment that it is administered up to the point at which it is completely eliminated from the body. Pharmacokinetics is based on mathematical modeling that places great emphasis on the relationship between drug plasma concentration and the time elapsed ...