Naloxone

Indications
Oral
Opioid dependence
Adult: As hydrochloride: 200 mg to 3 g daily.
Intravenous
Opioid overdosage
Adult: As hydrochloride: 0.4-2 mg repeated if necessary at 2-3 min intervals. If there is no response after a total of 10 mg has been given, consider the possibility of overdosage with other drugs. Reduce dose for opioid-dependent patients: 0.1-0.2 mg. IM/SC routes may be used (at IV doses) if IV admin is not feasible.
Child: As hydrochloride: Initially 10 mcg/kg IV followed by 100 mcg/kg IV if necessary. Alternatively, 0.4-0.8 mg IM or SC, repeated as necessary, if IV admin is not feasible.
Parenteral
Opioid-induced depression in neonates due to obstetric analgesia
Child: As hydrochloride: 10 mcg/kg IV, IM or SC repeated at 2-3 min intervals if necessary or 60 mcg/kg as a single IM dose.
Intravenous
Reversal of central depression from opioid use during surgery
Adult: As hydrochloride: 100-200 mcg at intervals of 2-3 minute, titrate dose according to response while maintaining analgesia.
Child: As hydrochloride: 5-10 mcg IV at 2-3 min intervals.

Reconstitution: Stable in 0.9% sodium chloride and 5% dextrose inj at 4 mcg/ml for 24 hr.
Incompatibility: Preparations containing bisulfite, metabisulfite, long-chain or high-molecular wt anions, or solutions with an alkaline pH.
Warnings / Precautions
Patients physically dependent on opioids, or who have received large doses of opioids (acute withdrawal syndrome may be precipitated). Pregnancy and lactation.
Adverse Reactions
Occur secondarily to reversal (withdrawal) of narcotic analgesia and sedation. Mental depression, apathy, inability to concentrate, sleepiness, irritability, anorexia, nausea, and vomiting in high oral doses during initial treatment of opiate addiction.
Potentially Fatal: Severe cardiopulmonary effects (e.g. hypotension, hypertension, ventricular tachycardia and fibrillation, dyspnoea, pulmonary oedema, cardiac arrest) in postoperative patients, most frequently in those with preexisting CV disease. Recurrence of respiratory depression in long-acting opioids.
Drug Interactions
Decreased effect of opioid analgesics.
Potentially Fatal: Acute withdrawal reaction in physically dependent patients may occur with opioid analgesics. Severe cardiopulmonary effects may occur with cardiotoxic drugs.
See Below for More naloxone Drug Interactions
Mechanism of Actions
Naloxone is a pure opioid antagonist that acts competitively at opioid receptors.
Onset: 2 min (IV); 2-5 min (endotracheal, IM, SC).
Duration: 30-120 min depending on route; IV has a shorter duration than IM.
Distribution: Crosses placenta.
Metabolism: Extensively hepatic via glucuronidation.
Excretion: Urine (as metabolites); elimination half-life: 0.5-1.5 hr (adult); 3-4 hr (neonates).
Storage Conditions
Intravenous: Store at 25°C. Protect from light. Oral: Store at 25°C. Protect from light. Parenteral: Store at 25°C. Protect from light.
ATC Classification
V03AB15 - naloxone ; Belongs to the class of antidotes. Used in the management of opioid analgesic overdose.
Storage
Intravenous: Store at 25°C. Protect from light. Oral: Store at 25°C. Protect from light. Parenteral: Store at 25°C. Protect from light.
Available As
  • Naloxone 20 mcg
  • Naloxone 400 mcg
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