anaesthetics Flashcards
structure of a local anaesthetic
aromatic region + ester/amide bond: amide bonds have longer half lives and are more widely distributed
MOA of local anaesthetics
are weak bases, ionised form blocks Na+ channels, act on inner part, block nerve conduction in order of C fibre, A delta, A beta, A alpha
what rapidly hydrolyses ester type local anaesthetics?
pseudo-cholinesterase
what hydrolyses amide type local anaesthetics?
liver microsomal P450 enzyme
Why are adrenaline and felypressin (non catecholamine) used with local anaesthetics?
vasoconstrictors, temporarily limit the spread of the local anaesthetic into systemic circulation
ADRs of local anaesthetics?
CNS - dose-dependent: depression, excitation
- restlessness, shivering, tongue numbness/metallic taste
- CNS depression/convulsions (depression of cortical inhibitory pathways)
- respiratory depression
CV: - myocardial depression/conduction block
- vasodilation
- pronounced fall in BP and death