Effect of aliskiren, an oral direct renin inhibitor, on the pharmacokinetics and pharmacodynamics of a single dose of acenocoumarol in healthy volunteers

Current Medical Research and Opinion

Volumn 24, Issue 9, 2008, Pages 2449-2456

  Huang, H L A ^a   Vaidyanathan, S ^a   Yeh, C M ^a   Bizot, M N ^b   Dieterich, H A ^a   Dole, W P ^c   Howard, D ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b NOVARTIS PHARMA K K   (Japan)

^c NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

Acenocoumarol; Aliskiren; Antihypertensive; Bioavailability; Drug drug interactions; Prothrombin time

Indexed keywords

ACENOCOUMAROL; ALISKIREN; PLACEBO; RENIN INHIBITOR;

ADULT; ANTICOAGULANT THERAPY; ANTICOAGULATION; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CLINICAL TRIAL; COMBINATION CHEMOTHERAPY; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG POTENTIATION; DRUG SAFETY; DRUG TOLERABILITY; FEMALE; FLATULENCE; GASTROINTESTINAL DISEASE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; INTERNATIONAL NORMALIZED RATIO; LIQUID CHROMATOGRAPHY; LOOSE FECES; LOW DRUG DOSE; MALE; MASS SPECTROMETRY; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; NORMAL HUMAN; PHARMACODYNAMICS; PROTHROMBIN TIME; RANDOMIZED CONTROLLED TRIAL; RECOMMENDED DRUG DOSE; SINGLE DRUG DOSE; THERAPY EFFECT; TIME TO MAXIMUM PLASMA CONCENTRATION;

ACENOCOUMAROL; ADMINISTRATION, ORAL; AMIDES; ANTICOAGULANTS; AREA UNDER CURVE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CROSS-OVER STUDIES; DOUBLE-BLIND METHOD; FEMALE; FUMARATES; HISTORY, 16TH CENTURY; HUMANS; MALE; RENIN; SPECTROPHOTOMETRY, ULTRAVIOLET;

EID: 53349090037     PISSN: 03007995     EISSN: None     Source Type: Journal    
DOI: 10.1185/03007990802285763     Document Type: Article

References (28)

1. Wood JM, Maibaum J, Rahuel J, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun 2003;308:698-705
2. Nussberger J, Wuerzner G, Jensen C, et al. Angiotensin II suppression in humans by the orally active renin inhibitor Aliskiren (SPP100): comparison with enalapril. Hypertension 2002;39:E1-8
3. Gradman AH, Schmieder RE, Lins RL, et al. Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation 2005;111:1012-18
4. Oh BH, Mitchell J, Herron JR, et al. Aliskiren, an oral renin inhibitor, provides dose-dependent efficacy and sustained 24-hour blood pressure control in patients with hypertension. J Am Coll Cardiol 2007;49:1157-63
5. Weir MR, Bush C, Anderson DR, et al. Antihypertensive efficacy, safety and tolerability of the oral direct renin inhibitor aliskiren in patients with hypertension: a pooled analysis. J Am Soc Hypertens 2007;1:264-77
6. Andersen K, Weinberger MH, Egan B, et al. Comparative efficacy and safety of aliskiren, an oral direct renin inhibitor, and ramipril in hypertension: a 6-month, randomized, double-blind trial. J Hypertens 2008;26:589-99
7. Sica D, Gradman AH, Lederballe O, et al. Aliskiren, a novel renin inhibitor, is well tolerated and has sustained BP-lowering effects alone or in combination with HCTZ during long-term (52 weeks) treatment of hypertension. Eur Heart J 2006;27(Suppl):121 P-797
8. Schmieder RE, Philipp T, Guerediaga J, et al. Aliskiren-based therapy lowers blood pressure more effectively than hydrochlorothiazide-based therapy in patients with hypertension. J Clin Hypertens 2007;9(Suppl A):A182 P-436
9. Dieterle W, Faigle JW, Montigel C, et al. Biotransformation and pharmacokinetics of acenocoumarol (Sintrom) in man. Eur J Clin Pharmacol 1977;11:367-75
10. Thijssen HH, Janssen GM, Baars LG. Lack of effect of cimetidine on pharmacodynamics and kinetics of single oral doses of R- and S-acenocoumarol. Eur J Clin Pharmacol 1986;30:619-23
11. Meinertz T, Kasper W, Kahl C, et al. Anticoagulant activity of the enantiomers of acenocoumarol. Br J Clin Pharmacol 1978; 5:187-8
12. Godbillon J, Richard J, Gerardin A, et al. Pharmacokinetics of the enantiomers of acenocoumarol in man. Br J Clin Pharmacol 1981;12:621-9
13. Harder S, Thurmann P. Clinically important drug interactions with anticoagulants. An update. Clin Pharmacokinet 1996; 30:416-44
14. Dieterle W, Corynen S, Mann J. Effect of the oral renin inhibitor aliskiren on the pharmacokinetics and pharmacodynamics of a single dose of warfarin in healthy subjects. Br J Clin Pharmacol 2004;58:433-6
15. Ufer M. Comparative pharmacokinetics of vitamin K antagonists: warfarin, phenprocoumon and acenocoumarol. Clin Pharmacokinet 2005;44:1227-46
16. Penning-van Beest FJ, Koerselman J, Herings RM. Quantity and quality of potential drug interactions with coumarin anticoagulants in the Netherlands. Pharm World Sci 2007;29:671-5
17. Metropolitan Life Insurance Company. 1983 Metropolitan height and weight tables. Stat Bull Metrop Life Found 1983; 64:3-9
18. Sunkara G, Bigler H, Wang Y, et al. The effect of nateglinide on the pharmacokinetics and pharmacodynamics of acenocoumarol. Curr Med Res Opin 2004;20:41-8
19. Azizi M, Webb R, Nussberger J, et al. Renin inhibition with aliskiren: where are we now, and where are we going? J Hypertens 2006;24:243-56
20. Thijssen HH, Flinois JP, Beaune PH. Cytochrome P4502C9 is principal catalyst of racemic acenocoumarol hydroxylation reactions in human liver microsomes. Drug Metab Dispos 2000;28:1284-90
21. Vaidyanathan S. Aliskiren, a novel oral renin inhibitor, has no interaction with cytochrome P450 isoenzymes in vitro. Basic Res Pharmcol Toxicol 2005;97(Suppl 1):239
22. Kroon C, de Boer A, Hoogkamer JF, et al. Detection of drug interactions with single dose acenocoumarol: new screening method? Int J Clin Pharmacol Ther Toxicol 1990; 28:355-60
23. Bonnabry P, Desmeules J, Rudaz S, et al. Stereoselective interaction between piroxicam and acenocoumarol. Br J Clin Pharmacol 1996;41:525-30
24. Yates RA, Wong J, Seiberling M, et al. The effect of anastrozole on the single-dose pharmacokinetics and anticoagulant activity of warfarin in healthy volunteers. Br J Clin Pharmacol 2001; 51:429-35
25. Rolan P, Terpstra IJ, Clarke C, et al. A placebo-controlled pharmacodynamic and pharmacokinetic interaction study between tamsulosin and acenocoumarol. Br J Clin Pharmacol 2003;55:314-16
26. Vaidyanathan S, Jarugula V, Dieterich H-A, et al. Clinical pharmacokinetics and pharmacodynamics of aliskiren. Clin Pharmacokinet 2008:47:515-31
27. Dieterle W, Corynen S, Vaidyanathan S, et al. Pharmacokinetic interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol, celecoxib and cimetidine. Int J Clin Pharmacol Ther 2005;43:527-35
28. Vaidyanathan S, Valencia J, Kemp C, et al. Lack of pharmacokinetic interactions of aliskiren, a novel direct renin inhibitor for the treatment of hypertension, with the antihypertensives amlodipine, valsartan, hydrochlorothiazide (HCTZ) and ramipril in healthy volunteers. Int J Clin Pract 2006;60: 1343-56