Histamine receptor antagonists pharmacokinetics

Simons PE, Simons KJ. Clinical pharmacology of new histamine HI receptor antagonists. Clin Pharmacokinet... 

The available data on a possible interaction between histamine H2 receptor antagonists and ciclosporin are inconclusive. Whereas neither cimetidine nor ranitidine significantly altered ciclosporin pharmacokinetics, there was an increase in serum creatinine concentration in patients taking both ciclosporin and cimetidine, but not ranitidine. The clinical significance of this interaction is probably limited, and it has been attributed to competition of cimetidine with creatinine for tubular secretion (251). 

North DS, Mattern AL, Kapil RP, Lalonde RL. The effect of histamine-2 receptor antagonists on tocainide pharmacokinetics. J Clin Pharmacol 1988 28(7) 640-3. 

Nathan PJ, Boardley R, Scott N, Berges A, Maruff P, Sivananthan T et al (2013) The safety, tolerability, pharmacokinetics and cognitive effects of GSK239512, a selective histamine H3 receptor antagonist in patients with mild to moderate Alzheimer s disease A preliminary investigation. Curr Alzheimer Res 10 240-251... 

Single-dose interaction studies have demonstrated that concurrent administration of tolterodine LA with antacid leads to a rapid release of drug (70% within 4 hours) and results in a 1.5-fold elevation in tolterodine peak plasma concentration compared with placebo. The clinical implications of this interaction and whether a similar interaction exists with gastric acid suppressants such as the histamine H2 -receptor antagonists and proton pump inhibitors are unclear. In the same study, the pharmacokinetics of oxybutynin XL were unaltered by antacid administration. ... 

The H2-receptor antagonists inhibit acid production by reversibly competing with histamine for binding to H2 receptors on the basolateral membrane of parietal cells. Four different H2-receptor antagonists, which differ mainly in their pharmacokinetics and propensity to cause drug interactions, are available in the United States cimetidine (Tagamet), ranitidine (Zantac), famotidine (Pepcid), and nizatidine (Axid). These drugs are less potent than proton-pump... 

Purkins L, Wood N, Kleinermans D, Nichols D. Histamine H2-receptor antagonists have no clinicalty significant effect on the steady-state pharmacokinetics of voriconazole. BrJ Clin Pharmacol (2003) 56, 51-5. 

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