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  • Title: Lack of effect of certain histamine H2-receptor blockers on the glucuronidation of 7-hydroxy-4-methylcoumarin by human liver microsomes.
    Author: Irshaid Y, Abu-Khalaf M.
    Journal: Pharmacol Toxicol; 1992 Oct; 71(4):294-6. PubMed ID: 1360658.
    Abstract:
    Contrary to the general belief that cimetidine and ranitidine spare glucuronidation of drugs, some authors have indicated that both cimetidine and ranitidine could inhibit the glucuronidation of paracetamol (acetaminophen) by cultured rat hepatocytes. Thus, we tested the effect of three histamine H2-receptor blockers (cimetidine, ranitidine and famotidine) on the glucuronidation of 7-hydroxy-4-methylcoumarin (7-OH-4-MC) by human liver microsomes. None of the drugs studied produced significant inhibition of the glucuronidation of 7-OH-4-MC when used at concentrations up to 1.5 mM. Thus, even the new H2-receptor blocker, famotidine, spares glucuronidation. These findings further support the previous reports which suggest that glucuronide conjugation in humans is spared by H2-receptor blockers.
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