The pharmacology and toxicology of meta-substituted acetanilide I: acute toxicity of 3-hydroxyacetanilide in mice.

Abstract

Toxicity of meta or 3-hydroxyacetanilide was evaluated in mice. The LD50 was 1025 mg/kg when given intraperitoneally (i.p.). The drug in doses greater than 400 mg/kg i.p. caused significant sedation. 3-Hydroxyacetanilide, 900 mg/kg i.p., did not cause hepatic necrosis evaluated by either histology or changes in plasma glutamate pyruvate transaminase activity. Acetaminophen (4-hydroxyacetanilide, paracetamol) caused significant liver glutathione depletion two hours after dosing. In contrast, liver glutathione was only slightly decreased by 600 mg/kg i.p. of 3-hydroxyacetanilide at 2 or 4 hours after the dose. It is suggested that the meta-substituted acetanilide derivatives might be safer analgesics and antipyretics than acetaminophen.

• Authors: E B Nelson
• Journal: Research communications in chemical pathology and pharmacology (Res Commun Chem Pathol Pharmacol) Vol. 28 Issue 3 Pg. 447-56 (Jun 1980) ISSN: 0034-5164 [Print] United States
• PMID: 7403659 (Publication Type: Journal Article)

Chemical References

• Acetanilides
• Acetaminophen
• 3-hydroxyacetanilide
• Transaminases
• Glutathione

Topics

• Acetaminophen (toxicity)
• Acetanilides (metabolism, pharmacology, toxicity)
• Animals
• Glutathione (analysis)
• Lethal Dose 50
• Liver (drug effects, pathology)
• Male
• Mice
• Transaminases (blood)