Lidocain - Lidocaine

Schmidt SH, Anniko M, Hellstrom S. 1990. Electrophysiological effects of the clinically used local anesthetics lidocaine, lidocaine-prilocaine and phenol on the rat s inner ear. Eur Arch Otorhinolaryngol 248 87-94. 

Lidocaine Lidocaine, 2-(diethylamino)-A-(2,6-dimethylphenyl)acetamide (2.2.2), is synthesized from 2,6-dimethylaniline upon reaction with chloroacetic acid chloride, which gives a-chloro-2,6-dimethylacetanilide (2.1.1), and its subsequent reaction with diethy-lamine [11]. 

Lidocaine Lidocaine is 2-diethylamino-2, 6 -dimethylacetanilide (2.2.3). Synthesis of lidocaine is described in Chapter 2. 

LIDOCAINE Lidocaine (xylocaine) is a local anesthetic that also is useful in the acute intravenous therapy of ventricular arrhythmias. 

Patients with hypersensitivity reactions to amide local anesthetics should not receive lidocaine. Lidocaine should be used with caution in patients with severe hepatic dysfunction or congestive heart failure, both of which may impair hepatic metabolism and lead to toxic serum levels of the drug. 

Trialkylammonium salts, such as lidocaine hydrochloride, are titrated in an aqueous solution containing a surfactant. The presence of the surfactant increases the trialkylammonium salt s K , giving a titration curve with a more pronounced break. The effect of adding an immiscible organic solvent, such as methylene chloride or toluene, also is demonstrated. 

Lidocaine hydrochloride [73-78-9] (Xylocaine), is the most versatile local anesthetic agent because of its moderate potency and duration of action, rapid onset, topical activity, and low toxicity. Its main indications are for infiltration, peripheral nerve blocks, extradural anesthesia, and in spinal anesthesia where a duration of 30 to 60 min is desirable. Because of its vasodilator activity, addition of the vasoconstrictor, epinephrine, increases the duration of action of Hdocaine markedly. It is also available in ointment or aerosol preparations for a variety of topical appHcations. 

Lldoc ine. Lidocaine hydrochloride, an anilide, was originally introduced as a local anesthetic in 1943 and found to be a potent antiarrhythmic in 1960. The compound is a reverse amide of procainamide. Lidocaine is generally considered to be the dmg of choice in the treatment of ventricular arrhythmias and those originating from digitalis glycoside toxicity (1,2,15—17). 

Mexilltene. Mexifitene hydrochloride, a phenyl ether, is a po active congener of lidocaine. It is used clinically for suppression of ventricular arrhythmias (1,2). 

Tocainide. Tocainide is a po active primary amine analogue of lidocaine. It consists of the (3)-(—) and the more active (R)-(+) enantiomers. 

Tocainide is rapidly and well absorbed from the GI tract and undergoes very fitde hepatic first-pass metabolism. Unlike lidocaine which is - 30% bioavailable, tocainide s availability approaches 100% of the administered dose. Eood delays absorption and decreases plasma levels but does not affect bio availability. Less than 10% of the dmg is bound to plasma proteins. Therapeutic plasma concentrations are 3—9 jig/mL. Toxic plasma levels are >10 fig/mL. Peak plasma concentrations are achieved in 0.5—2 h. About 30—40% of tocainide is metabolized in the fiver by deamination and glucuronidation to inactive metabolites. The metabolism is stereoselective and the steady-state plasma concentration of the (3)-(—) enantiomer is about four times that of the (R)-(+) enantiomer. About 50% of the tocainide dose is efirninated by the kidneys unchanged, and the rest is efirninated as metabolites. The elimination half-life of tocainide is about 15 h, and is prolonged in patients with renal disease (1,2,23). 

E. H. M. Koster, C. Wemes, J. B. Morsink and G. J. de Jong, Determination of lidocaine in plasma by direct solid-phase microexti action combined with gas chromatography , J. Chromatogr. B 739 175-182 (2000). 

Chloroacetyl chloride Chlordiazepoxide HCI Clemizole Diazepam LIdocaine Lorazepam Mianserin Tromantidine HCI... 

Hydrocortamate HCI Lidocaine Oxeladin Proxazole citrate Rociverine Tilidine HCI T rapidil... 

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