- Selective agonist at presynaptic alpha-2 adrenoceptors:
- Less selective than dexmedetomidine with ratio of alpha-1:alpha-2 1:200
- Acts particularly on the locus coeruleus in the floor of the fourth ventricle, producing depression of thalamic transmission to the cerebral cortex
- Primarily responsible for sedation, anxiolysis and analgesia
- Reduce sympathetic outflow resulting in hypotension and bradycardia
- Some activity at alpha-1 receptors:
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- Produces vasoconstriction at higher doses
- Some activity at imidazole receptors:
- Produces centrally mediated hypotension
One moment...