MECHANISM OF ACTION
- act via benzodiazepine receptor in CNS
- linked and facilitate action of the GABA receptor.
- chloride channel activation -> hyperpolarises membrane.
- also a kappa-opioid agonist -> benzodiazepine induced spinal analgesia.
- anterograde anaesthesia
- muscle relaxation
- clear, colourless solution, glass vial
- IV, PR, Intrathecal, Epidural, PO
- IM – 0.08mg/kg (premed)
- IV – 0.1mg/kg (sedation) – titrated to response, end point = slurred speech, onset 3min, infusion 0.03-0.2mg/kg/hr
- Intrathecal – 0.5 to 2mg
- Epidural – 0.1 to 0.2mg/kg
- induction of anaesthesia
- treatment of chronic pain
- withdrawal effect during prolonged infusion
- Absorption – bioavailability 40%
- Distribution – 96% protein bound, Vd 1L/kg
- Metabolism – hepatic, active metabolites
- Elimination – urinary, t1/2 = 2.5 hrs