The reversal of respiratory depression due to opiods and the diagnosis of suspected opiod overdose.
Substitued oxymorphne derivative
Solution containing 0.4mg/ml naloxone HCl
Reversal of mu-opiod receptor effects
Competive antagonist at mu, delta, kappa and sigma opiod receptors.
For reversla of respiratory depression 100-200µg i.v. In treatment of known or suspected opiod overdose 0.4 - 2.0mg may be required and this may be given iv, im or sc.
Acute withdrawal in opiate addicts
91% absorbed orally but has only 2% bioavailabiliy because of an extensive first-pass metabolism.
46% protein-bound with a VD of 2l/kg
Hepatic conjugation to form a glucuronide.
Clearance of 25ml/min/kg and a plasma T½ of 1.2hrs
Duration of action is only about 20 minutes and as a result, care must be exercised that the patient does not become obtunded as the effects of the naloxone wear off.