Effect of coadministered ketoconazole, a strong cytochrome P450 3A4 enzyme inhibitor, on the pharmacokinetics of ciclesonide and its active metabolite desisobutyryl-ciclesonide

Clinical Pharmacokinetics

Volumn 47, Issue 5, 2008, Pages 343-349

  Böhmer, Gabriele M ^a   Drollmann, Anton ^b   Gleiter, Christoph H ^a   Nave, Rüdiger ^c  

^a UNIVERSITY HOSPITAL TÜBINGEN   (Germany)

^b ALTANA PHARMA AG   (Germany)

^c Nycomed GmbH   (Germany)

Author keywords

Antiasthmatics, drug interactions; Ciclesonide, drug interactions; Ciclesonide, pharmacokinetics; Cytochrome P450 inhibitors, drug interactions; Drug interactions; Ketoconazole, drug interactions

Indexed keywords

CICLESONIDE; CYTOCHROME P450 3A4; DESISOBUTYRYL CICLESONIDE; DRUG METABOLITE; KETOCONAZOLE; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CLINICAL TRIAL; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; DYSGEUSIA; FATIGUE; FEMALE; HEADACHE; HEMATOMA; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; OPEN STUDY; PRIORITY JOURNAL; REPEATED DRUG DOSE; STATISTICAL ANALYSIS; VOLUNTEER;

EID: 41949128962     PISSN: 03125963     EISSN: 03125963     Source Type: Journal    
DOI: 10.2165/00003088-200847050-00005     Document Type: Article

References (29)

1. Busse WW, Lemanske Jr RF. Asthma. N Engl J Med 2001; 344 (5): 350-62
2. Canonica GW. Treating asthma as an inflammatory disease. Chest 2006; 130 (1 Suppl.): 21S-8S
3. Holgate ST, Polosa R. The mechanisms, diagnosis, and management of severe asthma in adults. Lancet 2006; 368 (9537): 780-93
4. Wenzel SE. Inflammation, leukotrienes and the pathogenesis of the late asthmatic response. Clin Exp Allergy 1999; 29 (1): 1-3
5. Tattersfield AE, Knox AJ, Britton JR, et al. Asthma. Lancet 2002; 360 (9342): 1313-22
6. Braman SS. The global burden of asthma. Chest 2006; 130 (1 Suppl.): 4S-12S
7. Hubner M, Hochhaus G, Derendorf H. Comparative pharmacology, bioavailability, pharmacokinetics, and pharmacodynamics of inhaled glucocorticosteroids. Immunol Allergy Clin North Am 2005; 25 (3): 469-88
8. Barnes PJ. How corticosteroids control inflammation: Quintiles Prize Lecture 2005. Br J Pharmacol 2006; 148 (3): 245-54
9. Barnes PJ. Molecular mechanisms of corticosteroids in allergic diseases. Allergy 2001; 56 (10): 928-36
10. Meltzer EO, Derendorf H. The systemic safety of inhaled corticosteroid therapy: a focus on ciclesonide. Ann Allergy Asthma Immunol 2006; 97 (2): 149-57
11. Stoeck M, Riedel R, Hochhaus G, et al. In vitro and in vivo anti-inflammatory activity of the new glucocorticoid ciclesonide. J Pharmacol Exp Ther 2004; 309 (1): 249-58
12. Nave R, Zech K, Bethke TD. Lower oropharyngeal deposition of inhaled ciclesonide via hydrofluoroalkane metered-dose inhaler compared with budesonide via chlorofluorocarbon metered-dose inhaler in healthy subjects. Eur J Clin Pharmacol 2005; 61 (3): 203-8
13. Langdon CG, Adler M, Mehra S, et al. Once-daily ciclesonide 80 or 320 microg for 12 weeks is safe and effective in patients with persistent asthma. Respir Med 2005; 99 (10): 1275-85
14. Nave R, Bethke TD, van Marle SP, et al. Pharmacokinetics of [14C]ciclesonide after oral and intravenous administration to healthy subjects. Clin Pharma-cokinet 2004; 43 (7): 479-86
15. Bethke TD, Boudreau RJ, Hasselquist BE, et al. High lung deposition of ciclesonide in 2D- and 3D-imaging [abstract]. E Respir J 2002; 20 (38 Suppl.): 109s
16. Newman S, Salmon A, Nave R, et al. High lung deposition of (99m)Tc-labeled ciclesonide administered via HFA-MDI to patients with asthma. Respir Med 2006; 100 (3): 375-84
17. Rohatagi S, Luo Y, Shen L, et al. Protein binding and its potential for eliciting minimal systemic side effects with a novel inhaled corticosteroid, ciclesonide. Am J Ther 2005; 12 (3): 201-9
18. Rohatagi S, Arya V, Zech K, et al. Population pharmacokinetics and pharmaco-dynamics of ciclesonide. J Clin Pharmacol 2003; 43 (4): 365-78
19. Derendorf H, Nave R, Drollmann A, et al. Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma. Eur Respir J 2006; 28 (5): 1042-50
20. Peet CF, Enos T, Nave R, et al. Identification of enzymes involved in phase I metabolism of ciclesonide by human liver microsomes. Eur J Drug Metab Pharmacokinet 2005; 30 (4): 275-86
21. GlaxoSmithKline. Flonase® nasal spray [prescribing information]. Research Tri-angle Park (NC): GlaxoSmithKline, 2004
22. Raaska K, Niemi M, Neuvonen M, et al. Plasma concentrations of inhaled budesonide and its effects on plasma cortisol are increased by the cytochrome P4503A4 inhibitor itraconazole. Clin Pharmacol Ther 2002; 72 (4): 362-9
23. US FDA Center for Drug Evaluation and Research. Drug development and drug interactions: table of substrates, inhibitors and inducers [online]. Available from URL: http://www.fda.gov/cder/drug/drugInteractions/tableSubstrates.htm [Accessed 2008 Feb 27]
24. Grimm SW, Richtand NM, Winter HR, et al. Effects of cytochrome P450 3A modulators ketoconazole and carbamazepine on quetiapine pharmacokinetics. Br J Clin Pharmacol 2006; 61 (1): 58-69
25. Venkatakrishnan K, von Moltke LL, Greenblatt DJ. Effects of the antifungal agents on oxidative drug metabolism: clinical relevance. Clin Pharmacokinet 2000; 38 (2): 111-80
26. Kohle C, Mohrle B, Munzel PA, et al. Frequent co-occurrence of the TATA box mutation associated with Gilbert's syndrome (UGT1A1*28) with other polymorphisms of the UDP-glucuronosyltransferase-1 locus (UGT1A6*2 and UGT1A7*3) in Caucasians and Egyptians. Biochem Pharmacol 2003; 65 (9): 1521-7
27. Mutch E, Nave R, McCracken N, et al. The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissue. Biochem Pharmacol 2007; 73 (10): 1657-64
28. Nave R, Drollmann A, Steinijans VW, et al. Lack of pharmacokinetic drug-drug interaction between ciclesonide and erythromycin. Int J Clin Pharmacol Ther 2005; 43 (6): 264-70
29. Derom E, Van De Velde, V, et al. Effects of inhaled ciclesonide and fluticasone propionate on cortisol secretion and airway responsiveness to adenosine 5′monophosphate in asthmatic patients. Pulm Pharmacol Ther 2005; 18 (5): 328-36