Mild-to-moderate sodium channel blockers

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Chapter: Medicinal Chemistry : Antiarrhythmic Drugs

Antiarrhythmic Drugs : Mild-to-moderate sodium channel blockers : i. Lidocaine ii. Phenytoin (Dilantin, Eptoin) iii. Mexiletine HCl iv. Tocainide HCl (Tonocard) - Synthesis and Drug Profile - Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose


SYNTHESIS AND DRUG PROFILE



Mild-to-moderate sodium channel blockers


i. Lidocaine


Synthesis and drug profile are discussed under sec III, ‘Local Anaesthetics’.


ii. Phenytoin (Dilantin, Eptoin)


Synthesis

Synthesis and drug profile are discussed under sec III, Chapter ‘Anticonvulsants’.

Dose: Orally 15 mg/kg first day; 7.5 mg/kg on the second day, followed by 300 to 400 mg per day.


iii. Mexiletine HCl


Synthesis


Properties and uses: It exists as white crystals, which is soluble in water and alcohol. It resembles lidocaine as it possesses a xylyl moiety, but is otherwise different chemically. Mexiletine is most useful in suppressing symptomatic ventricular arrhythmias.


iv. Tocainide HCl (Tonocard)


Properties and uses: It exists as a white crystalline powder with bitter taste and soluble in water or in alcohol. Tocainide is another lidocaine congener and is similar to mexiletine in its electro-physiologic properties and antiarrhythmic action.

Dose: The usual dose is orally 400–1200 mg in two or three divided doses.

Synthesis 



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