Pharmacokinetic interactions of valsartan and hydrochlorothiazide: An open-label, randomized, 4-period crossover study in healthy egyptian male volunteers

Clinical Therapeutics

Volumn 35, Issue 6, 2013, Pages 846-861

  Hedaya, Mohsen A ^a   Helmy, Sally A ^b  

^a KUWAIT UNIVERSITY   (Kuwait)

^b Damanhour University   (Egypt)

Author keywords

Fixed dose combination; Hydrochlorothiazide; Pharmacokinetics; Valsartan

Indexed keywords

HYDROCHLOROTHIAZIDE; HYDROCHLOROTHIAZIDE PLUS VALSARTAN; VALSARTAN; ANTIHYPERTENSIVE AGENT; TETRAZOLE DERIVATIVE; VALINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; BLOOD SAMPLING; CLINICAL ARTICLE; CONCENTRATION RESPONSE; CROSSOVER PROCEDURE; DIASTOLIC BLOOD PRESSURE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG EXPOSURE; DRUG SAFETY; DRUG TOLERABILITY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HYPERTENSION; IN VIVO STUDY; MALE; NORMAL HUMAN; OPEN STUDY; PHYSICAL EXAMINATION; SINGLE DRUG DOSE; SYSTOLIC BLOOD PRESSURE; TABLET; UNSPECIFIED SIDE EFFECT; WELLBEING; ANALOGS AND DERIVATIVES; CLINICAL TRIAL; DRUG COMBINATION; EGYPT; ORAL DRUG ADMINISTRATION; PATIENT COMPLIANCE;

ADMINISTRATION, ORAL; ANTIHYPERTENSIVE AGENTS; CROSS-OVER STUDIES; DRUG THERAPY, COMBINATION; EGYPT; HEALTHY VOLUNTEERS; HUMANS; HYDROCHLOROTHIAZIDE; MALE; PATIENT COMPLIANCE; TETRAZOLES; VALINE;

EID: 84879458971     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2013.04.014     Document Type: Article

References (72)

1. Mancia G., Laurent S., Agabiti-Rosei E., et al. European Society of Hypertension. Reappraisal of European guidelines on hypertension management: a European Society of Hypertension Task Force document. J Hypertens 2009, 27:2121-2158.
2. Chobanian A.V., Bakris G.L., Black H.R., et al. Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure. National Heart, Lung, and Blood Institute; National High Blood Pressure Education Program Coordinating Committee. Seventh report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure. Hypertension 2003, 42:1206-1252.
3. Jamerson K., Bakris G.L., Dahlöf B., et al. ACCOMPLISH Investigators. Exceptional early blood pressure control rates: the ACCOMPLISH trial. Blood Press 2007, 16:80-86.
4. Jamerson K., Weber M.A., Bakris G.L., et al. ACCOMPLISH Trial Investigators. Benazepril plus amlodipine or hydrochlorothiazide for hypertension in high-risk patients. N Engl J Med 2008, 359:2417-2428.
5. Timmermans P.B., Wong P.C., Chiu A.T., et al. Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol Rev 1993, 45:205-251.
6. Bauer J.H., Reams G.P. The angiotensin II type 1 receptor antagonists. A new class of antihypertensive drugs. Arch Intern Med 1995, 155:1361-1368.
7. Mycek M.J. Illustrated Reviews Pharmacology 2000, 179-187. Lippincott's Williams & Wilkins, Philadelphia, Pa. 2nd ed.
8. Benz J., Oshrain C., Henry D., et al. Valsartan, a new angiotensin II receptor antagonist: a double-blind study comparing the incidence of cough with lisinopril and hydrochlorothiazide. J Clin Pharmacol 1997, 37:101-107.
9. Diovan prescribing information: Novartis. Accessed December 7, 2011. http://www.pharma.us.novartis.com/product/pi/pdf/diovan.pdf.
10. Wang J., Ho L., Chen L., et al. Valsartan lowers brain β-amyloid protein levels and improves spatial learning in a mouse model of Alzheimer disease. J Clin Invest 2007, 117:3393-3402.
11. Flesch G., Muller P., Lloyd P. Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist, in man. Eur J Clin Pharmacol 1997, 52:115-120.
12. Zaid A.N., Cortesi R., Qaddomi A., et al. Formulation and bioequivalence of two valsartan tablets after a single oral administration. Sci Pharm 2011, 79:123-135.
13. Thurmann P. Valsartan: a novel angiotensin type I receptor antagonist. Expert Opin Pharmacother 2000, 1:337-350.
14. Waldmeier F., Flesch G., Müller P., et al. Pharmacokinetics, disposition and biotransformation of [14C]-radiolabelled valsartan in healthy male volunteers after a single oral dose. Xenobiotica 1997, 27:59-71.
15. Nakashima A., Kawashita H., Masuda N., et al. Identification of cytochrome P450 forms involved in the 4-hydroxylation of valsartan, a potent and specific angiotensin II receptor antagonist, in human liver microsomes. Xenobiotica 2005, 35:589-602.
16. Shah S., Khatri I., Freis E.D. Mechanism of antihypertensive effect of thiazide diuretics. Am Heart J 1978, 5:611-618.
17. Hardman JG, Limbird LE, Gilman AG. In: Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th Edition. New York, NY: McGraw-Hill; 1996.
18. Beermann B., Groschinsky-Grind M. Pharmacokinetics of hydrochlorothiazide in man. Eur J Clin Pharmacol 1977, 12:297-303.
19. Flockhart D., Tanus-Santos J. Implications of cytochrome P450 interactions when prescribing medication for hypertension. Arch Intern Med 2002, 162:405-412.
20. Yan J.H., Jarugula V., Sabo R., et al. Pharmacokinetics and pharmacodynamics of aliskiren/hydrochlorothiazide single-pill combination tablets and free combination of aliskiren and hydrochlorothiazide. J Clin Pharmacol 2012, 52:645-655.
21. Tutunji L.F., Tutunji M.F., Alzoubi M.I., et al. Simultaneous determination of irbesartan and hydrochlorothiazide in human plasma using HPLC coupled with tandem mass spectrometry: application to bioequivalence studies. J Pharm Biomed Anal 2010, 51:985-990.
22. Skolnik M.S., Beck J.D., Clark M. Combination antihypertensive drugs: recommendations for use. Am Fam Physician 2000, 61:3049-3056.
23. Waeber B. Combination therapy with ACE inhibitors/angiotensin II receptor antagonists and diuretics in hypertension. Expert Rev Cardiovasc Ther 2003, 1:43-50.
24. Co Diovan prescribing information: Novartis. Accessed December 7, 2011. http://www.novartis.com.au/pi_pdf/cod.pdf.
25. Lijnen P., Fagard R., Staessen J., et al. Effect of chronic diuretic treatment on the plasma renin-angiotensin-aldosterone system in essential hypertension. Br J Clin Pharmacol 1981, 12:387-392.
26. Brenner B.M., Cooper M.E., de Zeeuw D., et al. RENAAL Study Investigators. Effects of losartan on renal and cardiovascular outcomes in patients with type 2 diabetes and nephropathy. N Engl J Med 2001, 345:861-869.
27. Lewis E.J., Hunsicker L.G., Clarke W.R., et al. Collaborative Study Group. Renoprotective effect of the angiotensin-receptor antagonist irbesartan in patients with nephropathy due to type 2 diabetes. N Engl J Med 2001, 345:851-860.
28. Parving H.H., Lehnert H., Bröchner-Mortensen J., et al. Irbesartan in Patients with Type 2 Diabetes and Microalbuminuria Study Group. The effect of irbesartan on the development of diabetic nephropathy in patients with type 2 diabetes. N Engl J Med 2001, 345:870-878.
29. Schmidt A., Adam S.A., Kolloch R., et al. Antihypertensive effects of valsartan/hydrochlorothiazide combination in essential hypertension. Blood Press 2001, 10:230-237.
30. Ruilope L.M., Malacco E., Khder Y., et al. Efficacy and tolerability of combination therapy with valsartan plus hydrochlorothiazide compared with amlodipine monotherapy in hypertensive patients with other cardiovascular risk factors: the VAST study. Clin Ther 2005, 27:578-587.
31. Langtry H.D., McClellan K.J. Valsartan/hydrochlorothiazide. Drugs 1999, 57:751-755. discussion 756-758.
32. Wellington K., Faulds D.M. Valsartan/hydrochlorothiazide: a review of its pharmacology, therapeutic efficacy and place in the management of hypertension. Drugs 2002, 62:1983-2005.
33. Calhoun D.A., Glazer R.D., Pettyjohn F.S., et al. Efficacy and tolerability of combination therapy with valsartan/hydrochlorothiazide in the initial treatment of severe hypertension. Curr Med Res Opin 2008, 24:2303-2311.
34. US Food and Drug Administration Centre for Drug Evaluation and Research (FDA). Guidance for Industry: Bioavailability and Bioequivalence Studies for Orally Administered Drug Products-General Considerations, Office of Training and Communications, Division of Communications Management, Drug Information Branch, HFD-210, Rockville MD 20857, March 2003. Accessed January 3, 2013. http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm070124.pdf.
35. European Medicines Agency (EMA). CHMP Guideline on the Investigation of Bioequivalence. Accessed December 21, 2010. http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/01/WC500070039.pdf.
36. Zhang L., Zhao Y., Wang T., et al. Bioequivalence of compound valsartan dispersible tablets in healthy volunteers. Chin J of New Drugs and Clin Rems 2009, 08.
37. Ogu C.C., Maxa J.L. Drug interactions due to cytochrome P450. Proc (Bayl Univ Med Cent) 2000, 13:421-423.
38. Ho R.H., Kim R.B. Review transporters and drug therapy: implications for drug disposition and disease. Clin Pharmacol Ther 2005, 78:260-277.
39. Jiang J., Tian L., Huang Y., et al. Pharmacokinetic profiles of hydrochlorothiazide alone and in combination with benazepril or valsartan in healthy Chinese volunteers: evaluation of the potential interaction. Int J Clin Pharmacol Ther 2011, 49:756-764.
40. International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use. ICH Harmonised Tripartite Guideline: Guideline for Good Clinical Practice: . Accessed August 23, 2010. http://www.ikev.org/haber/stabilite/cd/14%201.13%20ICH%20M4%20CTD%20%20for%20CD.pdf.
41. US Dept of Health and Human Services (HHS), Food and Drug Administration (FDA), Center for Drug Evaluation and Research (CDER), Center for Veterinary Medicine (CVM). Guidance for Industry. Bioanalytical method validation. Accessed November 13, 2008. http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM070107.pdf.
42. Gibaldi M, Perrier D. "Pharmacokinetics" Swarbrick J Ed. (1982) Informa Healthcare USA, Inc, New York, USA.
43. Hedaya MA. "Basic pharmacokinetics" 1st Ed. (2007) Taylor and Francis group, Boca Raton, FL, USA.
44. Diletti E., Hauschke D., Steinijans V.W. Sample size determination for bioequivalence assessment by means of confidence intervals. Int J Clin Pharmacol Ther Toxicol 1992, 30(Suppl 1):S51-S58.
45. SAS Institute Inc, SAS/STAT User's guide, Version 6, 4th Edition,Vol. 2, SAS Institute, Cary, NC. 1990.
46. Westlake W.F. Use of confidence interval in analysis of comparative bioavailability trials. J Pharm Sci 1972, 61:1340-1341.
47. Locke S. An exact confidence interval from untransformed data for the ratio of two formulations means. J Pharmacokinet Biopharm 1984, 12:649-655.
48. Bangalore S., Ley L. Improving treatment adherence to antihypertensive therapy: the role of single-pill combinations. Expert Opin Pharmacother 2012, 13:345-355.
49. Valsartan/hydrochlorothiazid Film-coated tablets Public Assessment Report and scientific discussion: Teva.http://www.hma.eu/fileadmin/dateien/pipar/dk1105/parmod5_dk1105valsartanhydrochlorothiazidteva.pdf. Accessed January 14, 2013.
50. Beermann B., Groschinsky-Grind M. Pharmacokinetics of hydrochlorothiazide in man. Eur J Clin Pharmacol 1977, 12:297-303.
51. Iqbal M., Khuroo A., Batolar L., et al. Pharmacokinetics and bioequivalence study of three oral formulations of valsartan 160 mg: a single-dose, randomized, open-label, three-period crossover comparison in healthy Indian male volunteers. Clin Ther 2010, 32:588-596.
52. Sṕnola A., Almeida S., Filipe A., et al. Results of a single-center, single-dose, randomized- sequence, open-label, two-way crossover bioequivalence study of two formulations of valsartan 160-mg tablets in healthy volunteers under fasting conditions. Clin Ther 2009, 31:1993-2001.
53. Pèrez M., Càrdenas W., Ramirez G., et al. A comparative, cross-over, double blind, randomized study for bioequivalence assessment between two formulations of valsartan capsules vs. tablets. Colomb Med 2006, 37:114-120.
54. Patel R.B., Patel U.R., Rogge M.C., et al. Bioavailability of hydrochlorothiazide from tablets and suspensions. J Pharm Sci 1984, 73:359-361.
55. Schmidt E.K., Antonin K.H., Flesch G., Racine-Poon A. An interaction study with cimetidine and the new angiotensin II antagonist valsartan. Eur J Clin Pharmacol 1998, 53:451-458.
56. Prasad P.P., Yeh C.M., Gurrieri P., et al. Pharmacokinetics of multiple doses of valsartan in patients with heart failure. J Cardiovasc Pharmacol 2000, 40:801-807.
57. Kalliokoski A., Niemi M. Impact of OATP transporters on pharmacokinetics. Br J Pharmacol 2009, 158:693-705.
58. Waldmeier F., Flesch G., Muller P., et al. Pharmacokinetics, disposition and biotransformation of [14C]-radiolabelled valsartan in healthy male volunteers after a single oral dose. Xenobiotica 1997, 27:59-71.
59. McElnay J.C., D'Arcy P.F. Protein binding displacement interactions and their clinical importance. Drugs 1983, 25:495-513.
60. MacKichan J.J. Pharmacokinetic consequences of drug displacement from blood and tissue proteins. Clin Pharmacokinet 1984, 9(Suppl 1):32-41.
61. Colussi D.M., Parisot C., Rossolino M.L., et al. Protein binding in plasma of valsartan, a new angiotensin II receptor antagonist. J Clin Pharmacol 1997, 37:214-221.
62. Saydam M., Takka S. Bioavailability file: valsartan. FABAD J Pharm Sci 2007, 32:185-196.
63. Yu L.X., Straughn A.B., Faustino P.J., et al. The effect of food on the relative bioavailability of rapidly dissolving immediate-release solid oral products containing highly soluble drugs. Mol Pharm 2004, 1:357-362.
64. Roth M., Obaidat A., Hagenbuch B.OATPs OATs and OCTs: the organic anion and cation transporters of the SLCO and SLC22A gene superfamilies. Br J Pharmacol 2012, 165:1260-1287.
65. Yamashiro W., Maeda K., Hirouchi M., et al. Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans. Drug Metab Dispos 2006, 34:1247-1254.
66. Kim G.H., Na K.Y., Kim S.Y., et al. Up-regulation of organic anion transporter 1 protein is induced by chronic furosemide or hydrochlorothiazide infusion in rat kidney. Nephrol Dial Transplant 2003, 18:1505-1511.
67. Yun-Feng Han, Xiao-Han Fan, Xiao-Jian Wang, et al. Association of intergenic polymorphism of organic anion transporter 1 and 3 genes with hypertension and blood pressure response to hydrochlorothiazide. Am J Hypertens 2011, 24:340-346.
68. Hasannejad H., Takeda M., Taki K., et al. Interactions of human organic anion transporters with diuretics. JPET 2004, 308:1021-1029.
69. Fromm M.F. P-glycoprotein: a defense mechanism limiting oral bioavailability and CNS accumulation of drugs. Int J Clin Pharmacol Ther 2000, 38:69-74.
70. Challa V.R., Ravindra Babu P., Challa S.R., et al. Pharmacokinetic interaction study between quercetin and valsartan in rats and in vitro models. Drug Dev Ind Pharm 2013, 39:865-872.
71. Liao X.H., Wang J.J., Gao M.Y., et al. Effect of major components of maijunan tablets on the transport of hydrochlorothiazide in Caco-2 cell monolayer model [article in Chinese]. Yao Xue Xue Bao 2010, 45:104-108.
72. Smith N.F., Figg W.D., Sparreboom A. Review role of the liver-specific transporters OATP1B1 and OATP1B3 in governing drug elimination. Expert Opin Drug Metab Toxicol 2005, 1:429-445.