2005B03 Write brief short notes on the physicochemical properties of lignocaine.

 

Structure

·  Lipophilic modified benzene ring, amide chain, terminal amine N(C2H5)2

·  Achiral

·  Molecular weight 234g/mols

Behaviour

·  Weak base

o pKa 7.9

o ECF pH: 25% unionised

o ICF pH: <10% unionised

·  Lipid solubility 150x procaine

Additives

·  HCl: ↓pH -> ↑ionisation -> ↑solubility

·  Sodium metabisulfite: antioxidant/antibacterial (can cause hypersensitivity)

Formulation

·  Aqueous solution for injection

·  Solution for spray onto upper airway

·  Topical gel

·  With prilocaine as EMLA

 

 

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