Naloxone

Category: pharmacological

Aliases: Narcan

Pharmacological Mechanism

Pure µ-opioid receptor antagonist — competitive blockade with no agonist activity. Reverses opioid overdose in seconds (IV) to minutes (IN). OTC nasal spray (Narcan) available in most US states without prescription; precipitates opioid withdrawal in opioid-dependent users.

Half-Life (t½)

IV: 1h, IN: 1h

Dosing Guidelines

• IV: Typical 0.4 mg (Range: 0.4–4 mg)

Target Organ Systems

• nervous

Pathways It Modulates

• Opioid receptor signaling (inhibitor) — MOR + KOR + DOR antagonist (reversal)

Chemical Identifiers

• PubChem CID: 5284596
• Formula: C19H21NO4
• Molecular weight: 327.37 g/mol
• InChIKey: UZHSEJADLWPNLE-GRGSLBFTSA-N
• SMILES: C=CCN1CC[C@]23[C@@H]4C(=O)CC[C@]2([C@H]1CC5=C3C(=C(C=C5)O)O4)O

References

• PMID 31556537
• PMID 3963538
• PMID 9686407