Naloxone Data - Uses, Dosage, Drug class, Brand name, Warnings, etc

Pharmacology	Naloxone, an N-allyl derivative of oxymorphone, is a narcotic antagonist that competitively binds at opiate receptors. It is essentially free of narcotic agonist properties and is used to reverse the effects of narcotic agonists and drugs with partial agonist properties.
Administration and Adult Dosage	- IV (preferred) or SC for known/suspected narcotic overdose: 0.1–0.2 mg initial dose, then double dose every 2–3 min or 0.4 mg diluted in 9 mL saline, injected in 1-mL increments every 30–60 sec, until respiration and consciousness normalize or 10 mg total given. If response occurs, use IV infusion at hourly rate equal to initial effective dose, with possible 50% repeat bolus 20–30 min after infusion start to prevent recurrent toxicity - IV for postoperative narcotic depression: 0.1–0.2 mg initially, repeat every 2–3 min until desired reversal level reached; additional doses may be needed if narcotic effect outlasts naloxone - IV for epidural opioid-induced pruritus: 0.005–0.01 mg/kg as incremental doses or hourly infusion - PO for opioid-induced constipation: 4–12 mg not more than every 6 hr, ~20% of 24-hr morphine dose; initial doses ≤5 mg to avoid withdrawal
Special Populations - Pediatric Dosage	- IV for known/suspected narcotic overdose: 0.01 mg/kg, repeat as needed - IV for postoperative narcotic depression: 0.005–0.01 mg initially, repeat every 2–3 min until desired reversal - IV (preferred) or SC for narcotic depression (neonates): 0.01 mg/kg initially, repeat every 2–3 min until desired reversal
Special Populations - Geriatric Dosage	Same as adult dosage.
Dosage Forms	- Injection: 0.02, 0.4, 1 mg/mL
Patient Instructions	- Administered by a healthcare professional - Report symptoms such as rapid heartbeat, difficulty breathing, or agitation immediately after administration
Missed Doses	- Not applicable; administered as needed by healthcare professionals
Pharmacokinetics - Onset and Duration	- Onset: IV within 2–3 min; IM or SC up to 15 min - Duration: Usually 1 hr or less
Pharmacokinetics - Fate	- Metabolism: 59–67% by hepatic conjugation - Excretion: Renal elimination of conjugated compound - Distribution: Vd = 2–3 L/kg - Clearance: Cl = ~1.3 L/hr/kg
Pharmacokinetics - t¹⁄₂	- Elimination half-life: 64 ± 12 min (adults); 71 ± 36 min (neonates)
Adverse Reactions & Side Effects	- Occasional: Life-threatening complications within 10 min of parenteral administration, including pulmonary edema, seizures, hypertension, arrhythmias, violent behavior
Contraindications	- None known
Precautions & Warnings	- May precipitate acute withdrawal symptoms in narcotic-dependent individuals, including neonates of dependent mothers
Drug Interactions	- None known, except for opioid antagonism
Parameters to Monitor	- Respiratory rate, pupil size (may not be useful in mixed-drug or partial agonist overdoses), heart rate, blood pressure, symptoms of acute narcotic withdrawal
Class and Drug Brand Name	- Class: Opioid Antagonist - Brand Names: Narcan, Various
Notes	- Effective via endotracheal administration in patients with difficult venous access - Routinely used for coma of unknown origin - Mixed results in clonidine overdose; ineffective in septic or hemorrhagic shock - If no response after 10 mg, reconsider narcotic overdose diagnosis

References

Hand of Clinical Drug Data