Lorcainide

Absorption is complete and bioavailabihty is about 100% at steady state during continuous po dosing. There is extensive hepatic first-pass metabohsm to norlorcainide and hydroxylated metaboUtes. Nodorcainide is equipotent and equieffective to lorcainide in antiarrhythmic activity. 

Therapeutic plasma concentrations are 0.15—0.50 )J.g/mL. The elimination half-life of lorcainide is about 8 h and that of norlorcainide, 26 h (32). Lorcainide has low cardiovascular toxicity (32). 

Schiff s base (j ) derived by reaction of p-chloro-anil ine and borohydride followed by acylation with phenylacetyl chloride produces amide 22,. Selective hydrolysis with HBr followed by alkylation with isopropyl bromide completes the synthesis of lorcainide (20). ... 

I c With only little effect on action potential duration Lorcainide, Flecainide, Propafenone... 

The structural requirements for such activity are not very confining, as can be seen in part by comparing the structure of lorcainide with oxi ramide (21). Anti arrhythmic oxi ramide... 

Lorcainide has been reported to cause hyponatremia, attributed to inappropriate secretion of ADH (707). 

Meinertz T, Kasper W, Kersting F, Just H, Bechtold H, Jahnchen E. Lorcainide. II. Plasma concentration-effect relationship. Clin Pharmacol Ther 1979 26(2) 196-204. 

A B C Blocks Na channels Moderately depresses phase O and lengthens APD, ERP Minimally depresses phase O and shortens APD, ERP Maximally depresses phase O and does not change APD, ERP Quinidine, procainamide Lidocaine, phenytoin Encainde, lorcainide, liecainide... 

Infra-red Spectrum. Principal peaks at wavenumbers 1649, 716, 1094, 1298, 1153, 1016 (lorcainide hydrochloride, KBrdisk). 

Half-life. Plasma half-life, lorcainide 3 to 15 hours (mean 8), increased in subjects with cirrhosis of the liver and during chronic oral dosing norlorcainide 20 to 40 hours (mean 27). 

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