Pharmacokinetics and Cardiovascular Effect of Etoricoxib in the Absence or Presence of St. John’s Wort in Rats

M. A. Radwan; N.A. A. Baky; I. Zaghloul; H. Y. Aboul-Enein

doi:10.1055/s-0032-1309043

Arzneimittelforschung, Table of Contents

Arzneimittelforschung 2012; 62(07): 313-318
DOI: 10.1055/s-0032-1309043

Original Article

Pharmacokinetics and Cardiovascular Effect of Etoricoxib in the Absence or Presence of St. John’s Wort in Rats

Authors

M. A. Radwan

¹Department of Pharmacy Practice, College of Pharmacy, Princess Noura Bint Abdelrahman, Riyadh, Saudi Arabia
N.A. A. Baky

²Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
I. Zaghloul

²Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
H. Y. Aboul-Enein

³Pharmaceutical and Medicinal Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Cairo, Egypt

Abstract

Objectives:

The effect of chronic administration of etoricoxib (EXB), in the absence or presence of St. John’s Wort (SJW), on its pharmacokinetic parameters and blood pressure was investigated in rats.

Methods:

Rats were divided into 3 groups, each group received daily different oral treatment for 3 weeks. Rats’ blood pressures were monitored initially, after 1 and 3 weeks of treatment, and after 1 week of discontinuing dosing of both drugs. EXB pharmacokinetic parameters in the absence or presence of SJW were calculated after 3 weeks.

Key findings:

SJW was significantly affected EXB pharmacokinetic parameters. The steady state peak plasma concentration and terminal half-life were reduced by 32% and 91%, respectively, due to a > 3 fold increase in its apparent clearance which is a concentration and time dependent effect. EXB was significantly increased (P<0.001) Rats’ blood pressure while, co-administration of EXB and SJW was not significantly affect (P>0.05) rats’ blood pressure as compared to the control.

Conclusions:

Monitoring blood pressure of patients anticipated taking EXB for extended period should be advised. The co-administration of SJW with EXB should be avoided since SJW would greatly reduce EXB concentrations by inducing its metabolism.

Key words

etoricoxib - St. John’s Wort - pharmacokinetics - blood pressure - rats

Full Text

References

References
1 Katz N. Coxibs: Evolving role in pain management. Seminars in Arthritis and Rheumatism 2002; 32 3 (Suppl. 01) 15-24
2 Matsumoto AK, Cavanaugh PF Jr. Etoricoxib. Drugs of Today 2004; 40: 395-414
3 Hawley C. COX-2 inhibitors. Lancet 1999; 353: 307
4 Simmons DL, Botting RM, Hla T. Cyclooxygenase isozymes: the biology of prostaglandin synthesis and inhibition. Pharmacol Rev 2004; 56: 387-437
5 Prasit P, Wang Z, Brideau C et al. The discovery of rofecoxib, [MK 966, Vioxx, 4-(4′-methylsulfonylphenyl) 3-phenyl-2(5H)-furanone], an orally active cyclooxygenase -2-inhibitor. Bioorg Med Chem Lett 1999; 9: 1773-1778
6 Chan CC, Boyce S, Brideau C et al. Rofecoxib [Vioxx, MK-0966; 4-(4′-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles. Pharmacol Exp Ther 1999; 290: 551-560
7 Penning TD, Talley JJ, Bertenshaw SR et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benze nesulfonamide (SC-58635, celecoxib). J Med Chem 1997; 40: 1347-1365
8 Chauret N, Yergey JA, Brideau C et al. In Vitro Metabolism Considerations, Including Activity Testing of Metabolites, in the Discovery and Selection of the COX-2 Inhibitor Etoricoxib (MK-0663). Bioorg Med Chem Lett 2001; 11: 1059-1062
9 Bombardier C, Laine L, Reicin A et al. Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. N Engl J Med 2000; 343: 1520-1528
10 Bertagnolli MM, Eagle CJ, Zauber AG et al. Celecoxib for the prevention of sporadic colorectal adenomas. N Engl J Med 2006; 355: 873-884
11 Ott E, Nussmeier NA, Duke PC et al. Efficacy and safety of the cyclooxygenase 2 inhibitors parecoxib and valdecoxib in patients undergoing coronary artery bypass surgery. J Thorac Cardiovasc Surg 2003; 125: 1481-1492
12 Solomon SD, McMurray JJ, Pfeffer MA et al. Cardiovascular risk associated with celecoxib in a clinical trial for colorectal adenoma prevention. N Engl J Med 2005; 352: 1071-1080
13 Nussmeier NA, Whelton AA, Brown MT et al. Complications of the COX-2 inhibitors parecoxib and valdecoxib after cardiac surgery. N Engl J Med 2005; 352: 1081-1091
14 Bresalier RS, Sandler RS, Quan H et al. Cardiovascular events associated with rofecoxib in a colorectal adenoma chemoprevention trial. N Engl J Med 2005; 352: 1092-1102
15 Kearney PM, Baigent C, Godwin J et al. Do selective cyclo-oxygenase-2 inhibitors and traditional non-steroidal anti-inflammatory drugs increase the risk of atherothrombosis? Meta-analysis of randomised trials. BMJ 2006; 332: 1302-1308
16 Catella-Lawson F, McAdam B, Morrison BW et al. Effects of specific inhibition of cyclooxygenase-2 on sodium balance, hemodynamics, and vasoactive eicosanoids. J Pharmacol Exp The 1999; 289: 735-741
17 McAdam BF, Catella-Lawson F, Mardini IA et al. Systemic biosynthesis of prostacyclin by cyclooxygenase (COX)-2: The human pharmacology of a selective inhibitor of COX-2. Proc Natl Acad Sc U.S.A 1999; 96: 272-277
18 Brater DC, Anderson SA, Brown-Cartwright D et al. Effects of nonsteroidal anti-inflammatory drugs on renal function: Focus of cyclooxygenase-2- selective inhibition. Am J Med 1999; 107: 565-570
19 Riendeau D, Percival MD, Brideau C et al. Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2. J Pharm Exp Ther 2001; 296: 558-566
20 Dallob A, Hawkey CJ, Greenberg H et al. Characterization of etoricoxib, a novel, selective COX-2 inhibitor. J Clin Pharmacol 2003; 43: 573-585
21 Takemoto JK, Reynolds JK, Remsberg CM et al. Clinical pharmacokinetic and pharmacodynamic profile of etoricoxib. Clin Pharmacokinet 2008; 47: 703-720
22 Cochrane DJ, Jarvis B, Keating GM. Etoricoxib. Drugs 2002; 62: 2637-2651
23 Agrawal NG, Porras AG, Matthews CZ et al. Dose proportionality of oral etoricoxib, a highly selective cyclooxygenase-2 inhibitor, in healthy volunteers. J Clin Pharmacol 2001; 41: 1106-1110
24 Schwartz JI, Thach C, Lasseter KC et al. Effects of Etoricoxib and Comparator Nonsteroidal Anti-Inflammatory Drugs on Urinary Sodium Excretion, Blood Pressure, and Other Renal Function Indicators in Elderly Subjects Consuming a Controlled Sodium Diet. J Clin Pharmacol 2007; 47: 1521-1531
25 Cannon CP, Curtis SP, FitzGerald GA et al. Cardiovascular outcomes with etoricoxib and diclofenac in patients with osteoarthritis and rheumatoid arthritis in the Multinational Etoricoxib and Diclofenac Arthritis Long-term (MEDAL) programme: a randomised comparison. Lancet 2006; 368: 1771-1781
26 Wheaton AG, Blanck HM, Gizlice Z et al. Medicinal herb use in a population-based survey of adults: prevalence and frequency of use, reasons for use, and use among their children. Ann Epidemiol 2005; 15: 678-685
27 McNaughton SA, Mishra GD, Paul AA et al. Supplement use is associated with health status and health related behaviors in the 1946 British birth cohort. J Nutr 2005; 135: 1782-1789
28 Peng CC, Glassman PA, Trilli LE et al. Incidence and severity of potential drug–dietary supplement interactions in primary care patients: an exploratory study of 2 outpatient practices. Arch Intern Med 2004; 164: 630-636
29 Bailey DG, Dresser GK. Natural products and adverse drug interactions. CMAJ 2004; 170: 1531-1532
30 Morrow JD, Edeki TI, El Mouelhi M et al. American Society for Clinical Pharmacology and Therapeutics position statement on dietary supplement safety and regulation. Clin Pharmacol Ther 2005; 77: 113-122
31 Linde K, Ramirez G, Mulrow CD et al. John’s Wort for depression – an overview and meta-analysis of randomized clinical trials. BMJ 1996; 313: 253-258
32 Gaster B, Holroyd J. St John’s Wort for depression. Arch Intern Med 2000; 160: 152-156
33 Morris CA, Avorn J. Internet Marketing Herbal Products. JAMA 2003; 290: 1505-1509
34 Fugh-Berman A, Ernst E. Herb–drug interactions: review and assessment of report reliability. Br J Clin Pharmacol 2001; 52: 587-595
35 Dresser GK, Schwarz UI, Wilkinson GR et al. Coordinate induction of both cytochrome P4503A and MDR1 by St John’s wort in healthy subjects. Clin Pharmacol Ther 2003; 73: 41-50
36 Markowitz JS, Donovan JL, DeVane CL et al. Effect of St John’s Wort on drug metabolism by induction of cytochrome P450 3A4 enzyme. JAMA 2003; 290: 1500-1504
37 Kawaguchi A, Ohmori M, Tsuruoka S et al. Drug interaction between St John’s wort and quazepam. Br J Clin Pharmacol 2004; 58: 403-410
38 Nebel A, Schneider BJ, Baker RK et al. Potential metabolic interaction between St. John’s wort and theophylline. Ann Pharmacother 1999; 33: 502
39 Murakami Y, Tanaka T, Murakami H et al. Pharmacokinetic modelling of the interaction between St John’s wort and ciclosporin A. Br J Clin Pharmacol 2006; 61: 671-676
40 Radwan MA, Zaghloul IY, Abd Elbaky NA. Stability indicating high performance liquid chromatographic assay for the pharmacokinetics of Cyclooxygenase (COX-2) inhibitor etoricoxib in rats. Afr J Pharm Pharmacol 2009; 3: 339-346
41 Gibaldi M, Perrier D. Pharmacokinetics. 2^nd Ed. New York: Marcel Dekker Inc.; 1982
42 Solomon DH, Schneeweiss S, Levin R et al. The relationship between COX-2 specific inhibitors and hypertension. Hypertension 2004; 44: 140-145
43 Dürr D, Stieger B, Kullak-Ublick GA et al. John’s Wort induces intestinal Pglycoprotein/MDR1 and intestinal and hepatic CYP3A4. Clin Pharmacol Ther 2000; 68: 598-604
44 Ruschitzka F, Meier PJ, Turina M et al. Acute heart transplant rejection due to Saint John’s wort. Lancet 2000; 355: 548-549
45 Piscitelli SC, Burstein AH, Chaitt D et al. Indinavir concentrations and St John’s wort. Lancet 2000; 355: 547-548
46 Johne A, Brockmöller J, Bauer S et al. Pharmacokinetic interaction of digoxin with an herbal extract from St John’s wort (Hypericum perforatum). Clin Pharmacol Ther 1999; 66: 338-345
47 Frye RF, Fitzgerald SM, Lagattuta TF et al. Effect of St John’s wort on imatinib mesylate pharmacokinetics. Clin Pharmacol Ther 2004; 76: 323-329
48 Schwarz UI, Büschel B, Kirch W. Unwanted pregnancy on selfmedication with St John’s wort despite hormonal contraception. Br J Clin Pharmacol 2003; 55: 112-113
49 Mai I, Störmer E, Bauer S et al. Impact of St John’s wort treatment on the pharmacokinetics of tacrolimus and mycophenolic acid in renal transplant patients. Nephrol Dial Transplant 2003; 18: 819-822
50 Bennett WM, Henrich WL, Stoff JS. The renal effects of nonsteroidal anti-inflammatory drugs: Summary and recommendations. Am J Kidney Dis 1996; 28 (Suppl. 01) 556-562
51 Whelton A, Hamilton CW. Nonsteroidal anti-inflammatory drugs: Effects on kidney function. J Clin Pharmacol 1991; 31: 588-598
52 Heerdink ER, Leufkens HG, Herings RM et al. NSAIDs associated with increased risk of congestive heart failure in elderly patients taking diuretics. Arch Intern Med 1998; 158: 1108-1112
53 De Leeuw PW. Nonsteroidal anti-inflammatory drugs and hypertension. The risks in perspective. Drugs 1996; 51: 179-187