Lignocaine

Chemical

Tertiary amine amide

Class IB antiarrhythmic

Tx of ventricular arrhythmias, esp. assoc with AMI

Loading: 1.5mg/kg

Infusion: 1.5mg/kg/hr

To achieve therapeutic plasma level 2 – 6mcg/mL

IV only → extensive 1^st pass hepatic metabolism, only 3% oral dose reaches plasma

15 mins

→ More effect on cells with long AP (Purkinje, ventricular)

→ Doesn’t really affect atrial cells

→ ∴not used for SVTs

→ ↓refractory period → shortens AP

ECG effects: no ECG ∆ at therapeutic levels

* One of the least cardiotoxic Na channel blockers *

Neuro: reversible neural blockade

Biphasic → CNS excitement → CNS depression

–

65% PPB

α₁glycoprotein

0.7 – 1.5L/kg

Liver, N-dealkylation

Metabolites excreted in urine

<10% unchanged

t ½ B = 90 mins