Naloxone

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Naloxon, Nexodal; Belgium: Naloxon; Bulgaria: Naloxon; Cyprus: Naloxone; Czech Republic: Intrenon Spofa, Naloxone, Nexodal; Denmark: Naloxon; Estonia: Nexodal; Finland: Naloxon, Nexodal; France: Naloxone, Narcan; Germany: Naloxon, Nexodal; Greece: Narcan; Hungary: Naloxon, Nexodal; Ireland: Naloxone, Nexodal; Italy: Naloxone, Narcan; Latvia: Naloxon, Nexodal; Lithuania: Naloxoni, Nexodal; Luxembourg: Narcan; Malta: Naloxone; Netherlands: Naloxon, Nexodal; Poland: Naloxonum; Portugal: Naloxona, Naxan, Naxolan, Nexodal; Romania: Narcan, Nexodal; Slovakia: Intrenon Spofa, Naloxone, Nexodal; Slovenia: Nexodal; Spain: Naloxona; Sweden: Naloxon; UK: Naloxone.

North America

Canada: Naloxone.

Latin America

Argentina: Grayxona, Naloxona, Narxona; Brazil: Narcan.

Asia

Japan: Naloxone.

Drug combinations

Naloxone and Buprenorphine

Naloxone and Oxycodone

Naloxone and Pentazocine

Naloxone and Tilidine

Chemistry

Naloxone Hydrochloride: C~19~H~21~NO~4~ HCl. Mw: 363.84. (1) Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, hydrochloride, (5α)-; (2) 17-Allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride; (3)(-)-N-Allyl-14-hydroxynordihydromorphinone hydrochloride. CAS-357-08-4; CAS-51481-60-8 (dihydrate); CAS-465-65-6 (naloxone)(1963).

Pharmacologic Category

Opiate Antagonists. Antidotes. (ATC-Code: V03AB15).

Mechanism of action

Pure opioid antagonist which competes and displaces narcotics at opioid receptor sites.

Therapeutic use

Complete or partial reversal of opioid depression, including respiratory depression, induced by natural and synthetic opioids. Diagnosis of suspected opioid tolerance or acute opioid overdose. Adjunctive agent to increase blood pressure in management of septic shock.

Pregnancy and lactiation implications

Benefit to mother and risk to fetus should be considered before administering to a pregnant woman known or suspected to be opioid-dependent. May precipitate withdrawal in both mother and fetus. Not recommended in nursing women.

Unlabeled use

Contraindications

Hypersensitivity to naloxone or any component of the formulation.

Warnings and precautions

May precipitate symptoms of acute withdrawal in opioid-dependent patients, including pain, hypertension, sweating, agitation, irritability; shrill cry, failure to feed in neonates. Use with caution in cardiovascular disease or in patients receiving medications with potential adverse cardiovascular effects (e.g. hypotension, pulmonary edema or arrhythmias), pulmonary edema and cardiovascular instability. Use caution in history of seizures; avoid use in treatment of meperidine-induced seizures. Recurrence of respiratory depression possible if opioid involved is long-acting. Excessive dosages should be avoided after use of opiates in surgery. Abrupt postoperative reversal may result in nausea, vomiting, sweating, tachycardia, hypertension, seizures, and other cardiovascular events.

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