Imidazole-substituted drugs and tendency for inhibition of Cytochrome P450 Isoenzymes: A review

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21 Citations (Scopus)


Nowadays, multi-medicament use is increasing in clinical practice, especially, in the treatment of elder patients. Therefore, the pharmacokinetic drug-drug interaction of medicaments, which are expected to be co administrated in clinical practice, seems to be significant. The present review provides an update for the relationship between type of chemical substitution (aliphatic or aromatic) of imdazole-containig drugs and their tendency to affect hepatic metabolizing enzyme cytochrome P450 (CYP). In the present review, examples of different therapeutically used imidazole-containing drugs are highlighted to support the first evidence regarding the relationship between CYP-inhibition and chemistry of imidazole ring system. The informations provided throughout this article are intended to improve the medicinal chemist's knowledge of imidazole-containig drugs that are therapeutically widely applied as agents including histamine H1 receptor antagonists (antiallergics), histamine H2 receptor antagonists (antiulcers), histamine H3 receptor antagonists (management of cognitive disorders and attention-deficithyperactivity-disorder), antivirals, antiHIV, antibacterials, antifungals, anethelmintics, antiemetics, and antihypertensives.

Original languageEnglish
Pages (from-to)410-419
Number of pages10
JournalDer Pharma Chemica
Issue number1
Publication statusPublished - 2011
Externally publishedYes


  • Cytochrome P450s (CYP450s)
  • Drug-drug interaction
  • Histamine H1-H3 receptor antagonists
  • Imidazole-containing drugs

ASJC Scopus subject areas

  • General Chemistry


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