Pharmacokinetic-pharmacodynamic modelling of S(-)-atenolol in rats: Reduction of isoprenaline-induced tachycardia as a continuous pharmacodynamic endpoint

British Journal of Pharmacology

Volumn 151, Issue 3, 2007, Pages 356-366

  Van Steeg, T J ^a   Freijer, J ^b   Danhof, M ^a   De Lange, E C M ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

^b LAP and P Consultants BV   (Netherlands)

Author keywords

blockers; Heart rate; Isoprenaline; NONMEM; PK PD modelling; Rats; S( ) atenolol; Tachycardia

Indexed keywords

ATENOLOL; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; ISOPRENALINE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLOOD SAMPLING; CONTROLLED STUDY; HEART RATE; HYSTERESIS; IN VIVO STUDY; MALE; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; RAT; TACHYCARDIA; WISTAR KYOTO RAT;

ADRENERGIC BETA-AGONISTS; ADRENERGIC BETA-ANTAGONISTS; ALGORITHMS; ANIMALS; ATENOLOL; DOSE-RESPONSE RELATIONSHIP, DRUG; HEART RATE; INFUSIONS, INTRAVENOUS; ISOPROTERENOL; MALE; MODELS, BIOLOGICAL; RATS; RATS, INBRED WKY; STEREOISOMERISM; TACHYCARDIA;

EID: 34249688254     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707234     Document Type: Article

References (44)

1. Akaike (1974). A new look at the statistical model identification. IEEE Trans Automatic Control 19: 716-723.
2. Anderson JL, Patterson E, Conlon M, Pasyk S, Pitt B, Lucchesi BR (1980). Kinetics of antifibrillatory effects of bretylium: correlation with myocardial drug concentrations. Am J Cardiol 46: 583-592.
3. Beal SL, Sheiner LB (1999). NONMEM Users Guide. University of California at San Fransisco, San Fransisco, CA.
4. Belpaire FM, De Smet F, Vynckier LJ, Vermeulen AM, Rosseel MT, Bogaert MG et al. (1990). Effect of aging on the pharmcokinetics of atenolol, metoprolol and propranolol in the rat. J Pharmacol Exp Ther 254: 116-122.
5. Belpaire FM, Rosseel MT, Vermeulen AM, De Smet F, Bogaert MG (1993). Stereoselective pharmacokinetics of atenolol in the rat: influence of aging and of renal failure. Mech Ageing Dev 67: 201-210.
6. Black JW, Leff P (1983). Operational models of pharmacological agonism. Proc R Soc Lond B Biol Sci 220: 141-162.
7. Breimer DD, Danhof M (1997). Relevance of the application of pharmacokinetic-pharmacodynamic modelling concepts in drug development - The 'Wooden Shoe' paradigm. Clin Pharmacokinet 32: 259-267.
8. Brynne L, Paalzow LK, Karlsson MO (2000). Consequence of exercise on the cardiovascular effects of l-propranolol in spontaneously hypertensive rats. J Pharmacol Exp Ther 294: 1201-1208.
9. Chiu CC, Lin YT, Tsai CH, Liang JC, Chiang LC, Wu JR et al. (2000). Pharmacological effects of an aldehyde type alpha/beta-adrenoceptor blocking agent with vasodilating properties. Gen Pharmacol 34: 391-400.
10. Cox EH, Kerbusch T, Van Der Graaf PH, Danhof M (1998). Pharmacokinetic-pharmacodynamic modeling of the electroence-phalogram effect of synthetic opioids in the rat: correlation with the interaction at the mu-opioid receptor. J Pharmacol Exp Ther 284: 1095-1103.
11. de Lange EC, Danhof M, de Boer AG, Breimer DD (1994). Critical factors of intracerebral microdialysis as a technique to determine the pharmacokinetics of drugs in rat brain. Brain Res 666: 1-8.
12. Dingemanse J, Danhof M, Breimer DD (1988). Pharmacokinetic- pharmacodynamic modeling of CNS drug effects: an overview. Pharmacol Ther 38: 1-52.
13. Doggrell SA, Surman AJ (1994). Functional beta-adrenoceptors in the left atrium of normotensive and hypertensive rats. J Auton Pharmacol 14: 425-436.
14. Gabrielsson J, Weiner D (1997). Pharmacokinetic and Pharmacodynamic Data Analysis: Concepts and Applications. Swedish Pharmaceutical Press: Stockholm.
15. Gabrielsson J, Jusko WJ, Alari L (2000). Modeling of dose-response-time data: four examples of estimating the turnover parameters and generating kinetic functions from response profiles. Biopharm Drug Dispos 21: 41-52.
16. Hocht C, Di Verniero C, Opezzo JA, Bramuglia GF, Taira CA (2006). Pharmacokinetic-pharmacodynamic (PK-PD) modeling of cardiovascular effects of metoprolol in spontaneously hypertensive rats: a microdialysis study. Naunyn Schmiedebergs Arch Pharmacol 373: 310-318.
17. Hocht C, Di Verniero C, Opezzo JAW, Taira CA (2004). Pharmacokinetic- pharmacodynamic properties of metoprolol in chronic aortic coarctated rats. Naunyn-Schmiedebergs Archives of Pharmacology 370: 1-8.
18. Hoffman BB, Lefkowitz RJ (1996). Catecholamines, sympathomimetic drugs, and adrenergic receptor antagonists. In: Hardman JG, Limbird LE, Molinoff PB, Ruddon RW, Goodman Gillman G (eds). Goodman & Gilman's The Pharmacological Basis of Therapeutics. McGraw-Hill: New York, pp 199-248.
19. Johnsson G, Regardh CG (1976). Clinical pharmacokinetics of beta-adrenoreceptor blocking drugs. Clin Pharmacokinet 1: 233-263.
20. Kendall MJ (1997). Clinical relevance of pharmacokinetic differences between beta blockers. Am J Cardiol 80: 15J-19J.
21. Kirch W, Gorg KG (1982). Clinical pharmacokinetics of atenolol - a review. Eur J Drug Metab Pharmacokinet 7: 81-91.
22. Lacchini S, Ferlin EL, Moraes RS, Ribeiro JP, Irigoyen MC (2001). Contribution of nitric oxide to arterial pressure and heart rate variability in rats submitted to high-sodium intake. Hypertension 38: 326-331.
23. Lipworth BJ, Irvine NA, McDevitt DG (1991). A dose-ranging study to evaluate the beta 1-adrenoceptor selectivity of bisoprolol. Eur J Clin Pharmacol 40: 135-139.
24. Mehvar R, Brocks DR (2001). Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humans. J Pharm Sci 4: 185-200.
25. Mehvar R, Gross ME, Kreamer RN (1990). Pharmacokinetics of atenolol enantiomers in humans and rats. J Pharm Sci 79: 881-885.
26. Nandakumar K, Bansal SK, Singh R, Bodhankar SL, Jindal DP, Coumar MS et al. (2005). Selective beta(1)-adrenoreceptor blocking activity of newly synthesized acyl amino-substituted aryloxypropanolamine derivatives, DPJ 955 and DPJ 890, in rats. J Pharm Pharmacol 57: 515-520.
27. Oliveira EL, Cardoso LM, Pedrosa ML, Silva ME, Dun NJ, Colombari E et al. (2004). A low protein diet causes an increase in the basal levels and variability of mean arterial pressure and heart rate in Fisher rats. Nutr Neurosci 7: 201-205.
28. Piercy V (1988). Method for assessing the activity of drugs at beta 1-and beta 2-adrenoceptors in the same animal. J Pharmacol Methods 20: 125-133.
29. Rang H, Dale M, Ritter J (1999). Pharmacology 4th edn. Philadelphia: Lippincott.
30. Reeves PR, Barnfield DJ, Longshaw S, McIntosh DA, Winrow MJ (1978a). Disposition and metabolism of atenolol in animals. Xenobiotica 8: 305-311.
31. Reeves PR, McAinsh J, McIntosh DA, Winrow MJ (1978b). Metabolism of atenolol in man. Xenobiotica 8: 313-320.
32. Reiter MJ (2004). Cardiovascular drug class specificity: beta-blockers. Prog Cardiovasc Dis 47: 11-33.
33. Riddell JG, Harron DW, Shanks RG (1987). Clinical pharmacokinetics of beta-adrenoceptor antagonists. An update. Clin Pharmacokinet 12: 305-320.
34. Ritchie RH, Morgan DJ, Horowitz JD (1998). Myocardial effect compartment modeling of metoprolol and sotalol: importance of myocardial subsite drug concentration. J Pharm Sci 87: 177-182.
35. Schafers RF, Karl I, Mennicke K, Daul AE, Philipp T, Brodde OE (1999). Ketotifen and cardiovascular effects of xamoterol following single and chronic dosing in healthy volunteers. Br J Clin Pharmacol 47: 59-66.
36. Singh BN (2005). Beta-Adrenergic blockers as antiarrhythmic and antifibrillatory compounds: an overview. J Cardiovasc Pharmacol Ther 10 (Suppl 1): S3-S14.
37. Smedes F, Kraak JC, Poppe H (1982). Simple and fast solvent extraction system for selective and quantitative isolation of adrenaline, noradrenaline and dopamine from plasma and urine. J Chromatogr 231: 25-39.
38. Van Bortel LM, de Hoon JN, Kool MJ, Wijnen JA, Vertommen CI, Van Nueten LG (1997). Pharmacological properties of nebivolol in man. Eur J Clin Pharmacol 51: 379-384.
39. Van Der Graaf PH, Danhof M (1997). Analysis of drug-receptor interactions in vivo: a new approach in pharmacokinetic-pharmacodynamic modelling. Int J Clin Pharmacol Ther 35: 442-446.
40. Van Der Graaf PH, Van Schaick EA, Mathôt RA, Ijzerman AP, Danhof M (1997). Mechanism-based pharmacokinetic-pharmacodynamic modeling of the effects of N6-cyclopentyladenosine analogs on heart rate in rat: estimation of in vivo operational affinity and efficacy at adenosine A1 receptors. J Pharmacol Exp Ther 283: 809-816.
41. Van Der Graaf PH, Van Schaick EA, Visser SA, De Greef HJ, Ijzerman AP, Danhof M (1999). Mechanism-based pharmacokinetic-pharmacodynamic modeling of antilipolytic effects of adenosine A(1) receptor agonists in rats: prediction of tissue-dependent efficacy in vivo. J Pharmacol Exp Ther 290: 702-709.
42. Waldeck B (2002). Beta-adrenoceptor agonists and asthma - 100 years of development. Eur J Pharmacol 445: 1-12.
43. Wellstein A, Palm D, Belz GG, Butzer R, Polsak R, Pett B (1987). Reduction of exercise tachycardia in man after propranolol, atenolol and bisoprolol in comparison to beta-adrenoceptor occupancy. Eur Heart J 8 (Suppl): M:3-M:8.
44. Zuideveld KP, Van Der Graaf PH, Newgreen D, Thurlow R, Petty N, Jordan P et al. (2004). Mechanism-based pharmacokinetic-pharmacodynamic modeling of 5-HT1A receptor agonists: estimation of in vivo affinity and intrinsic efficacy on body temperature in rats. J Pharmacol Exp Ther 308: 1012-1020.