Pharmacokinetics of barbiturates

PHARMACOKINETICS OF BARBITURATES

  • Absorption—readily absorbed from GI tract when given orally
  • Distribution – Cross BBB. High levels reached in brain, liver and kidney. Lipid soluble and redistribute to muscle leading to decrease  in plasma level of barbiturate.
  • Large store in adipose tissue.
  • Animal seems to recover once the plasma level goes down
  • Then sedate and drowsy as the drug keeps coming back to circulation from storage resulting in  long periods of CNS depression
  • Repeated doses end up in  cumulation.
  • Once stores are saturated can cause severe depression of CVS and respiration
  • Excretion – renal, after oxidation in hepatic and extra-hepatic sites
  • Barbiturates – known inducers of microsomal enzymes. Induces its own metabolism resulting in tolerance to the effects. Tolerance disappears after withdrawal of the drug.
  • Cats are sensitive to the respiratory depression and dogs to the CVS depression of barbiturates
  • Antidote – Bemegride. a CNS stimulant
Last modified: Tuesday, 15 May 2012, 12:10 PM