- 0.5% or 1% drops for topical use (may initially produce a burning sensation)
- 4% cream for topical anaesthesia to the skin
- Onset 30mins
- Causes local histamine release and vasodilation
- Effects last 4-6hrs
Amethocaine
Amethocaine
- Amethocaine is an ester-linked local anaesthetic used primarily for topical anaesthesia
Absorption
- pKa 8.5
- 7% unionised at physiological pH, giving it a slow onset time
Distribution
- 75% protein bound
- Relative lipid solubility vs. cocaine: 200x
Metabolism
- Ester hydrolysis
Excretion
- Elimination half-life 80mins