Canis ISSN: 2398-2942

Ketoconazole

Contributor(s): Stephen Barr, Rosanna Marsella

Introduction

Name

  • Ketoconazole.

Class of drug

  • Imidazole antifungal agent.

Description

Chemical name

  • Cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxyl]phenyl]piperazine.

Molecular formula

  • C26H28Cl2N4O4.

Uses

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Indications

Administration

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Precautions

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Interactions

with other drugs

Drugs increasing pH of gastric contents, eg antacids, antimuscarinics and H2 blockers

  • The absorption of ketoconazole may be impaired; stagger dosing of these drugs around ketoconazole dose.

Methylprednisolone

Phenytoin

  • Plasma ketoconazole levels are reduced by phenytoin Phenytoin.

Antihistamines, oral hypoglycemics, antiepileptics, cisapride and cyclosporineby suppression of the cytochrome P450 enzymes

  • Antifungal imidazoles and triazoles inhibit metabolism of these drugs leading to increasing levels of the other drugs. More specifically the interactions between ketoconazole and cyclosporine has been recently evaluated. Ketoconazole at the daily dose of 13.6 mg/kg decreased required dose of cyclosporine by 50-75%.

Adverse Reactions

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Further Reading

Publications

Refereed papers

  • Mouatt J G (2002) Cyclosporin and ketoconazole interaction for treatment of perianal fistulas in the dog. Aust Vet J 80(4), 207-211 PubMed.
  • Patricelli A J, Hardie R J & McAnulty J E (2002) Cyclosporine and ketoconazole for the treatment of perianal fistulas in dogs. JAVMA 220(7), 1009-1016 PubMed.
  • Kuroha M, Azumano A, Kuze Y, Shimoda M & Kokue E (2002) Effect of multiple dosing of ketoconazole on pharmacokinetics of midazolam, a cytochrome P-450 3A substrate in beagle dogs. Drug Metab Dispos 30(1), 63-68 PubMed.
  • Peterson M E (2001) Medical treatment of canine pituitary-dependent hyperadrenocorticism (Cushing's disease). Vet Clin North Am Small Anim Pract 31( 5), 1005-1014, viii PubMed.
  • D'mello A, Venkataramanan R, Satake M, Todo S, Takaya S, Ptachcinski R J, Burckart G J & Starzl T E (1989) Pharmacokinetics of the cyclosporine-ketoconazole interaction in dogs.Res Commun Chem Pathol Pharmaco64(3), 441-454 PubMed.

Other sources of information

  • BSAVA Small Animal Formulary. Ramsey I (2017) 9th edn. Cheltenham: BSAVA.

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