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Naloxone (Narcan)

Pharmacology
Naloxone is a pure opioid antagonist that competitively blocks opiate receptors within the central nervous system (CNS). Sodium Hydrochloride has no opioid agonise properties and can be given safely in large doses without producing respiratory or CNS depression. Naloxone is not effective orally but maybe given subcutaneously, intra muscular or intravenously. After IV administration, opioid antagonise occurs within 1-2 minutes and persist for approximately 1-4 hours. The plasma half life is about 60 minutes.

Indicators :

  1. Use naloxone for reversal of acute opioid intoxication manifested by CNS and respiratory depression.
  2. Use as empirical therapy for stupor or coma suspected to be caused by drug overdose.
Contra indication :
Do not use in patients with a known hypersensitive of naloxone.

Adverse effects :
  1. Use in opiate-dependent patient may precipitate acute withdrawal syndrome.
  2. Pulmonary oedema or Ventricles Fibrillation has occurred shortly after naloxone administration in opioid intoxicated patient.
  3. Agitation, hypertension and ventricular irritability may occur following opiod antagonism when other stimulants are present. Such reaction have been associated with post anaesthetic use of naloxone when cathecolamine and large volumes of fluid have been administered.

Dosage and administration :
IM route: absorption is erratic and incomplete suspected opioid induce coma.
Adult and children:
  1. Administer 0,4-2,0 mg IV bolus injected, repeat doses of 0,4-2,0mg can be given to achieve a clinical effect. If not response has been observed after 10 mg has been administered, the diagnosis of opioid induced toxicity should be questioned.
  2. Repeated doses of naloxone may be required with 20-60minutes to maintain reversal of the effect of opioid with prolonged elimination half lives. (e.g. methadone and propoxyphene).
  3. Singe doses up to 24mg have been given without adverse effect.
  4. Pediatric dose: The American Academy of Pediatrics recommendens a dose of 0,1mg/kg IV for children aged neonates to five years. In order children a minimum of 2mg is recommended.
  5. Manufacturer recommendens an initial pediatric dose of 0,01mg/kg followed 0,1mg/kg if clinical improvement is not optimum.
  6. Continuous infusion may be employed in circumstances of opioid overdose with log acting opioid. The patient is given an initial bolus dose of IV naloxone to achieve reversal of opioid effects and is then started on continuous infusion to maintain this state of antagonism. Utilize two third of the initial dose on an hourly basis. Add ten times this dose to each litre of dextrose 5% and infuse at rate 100ml/hour. One half of the initial bolus should be re administered 15 minute after the star of continuous infusion to prevent a droop in naloxone levels increase infusion rate as needed to assure adequate ventilation. Naloxone requirements may vary during the infusion period necessitating close monitoring of vital signs and increasing or decreasing the dose as needed.

Formulation :

Naloxone (Narcan) 400mg per ml in 1 ml ampules.
Nalaxone Nonatal (Narcan Neonatal) 20mcg per ml in 2 ml ampules.

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