Modeling drug- and system-related changes in body temperature: Application to clomethiazole-induced hypothermia, long-lasting tolerance development, and circadian rhythm in rats

Journal of Pharmacology and Experimental Therapeutics

Volumn 317, Issue 1, 2006, Pages 209-219

  Visser, Sandra A G ^a   Sällström, Björn ^e   Forsberg, Tomas ^a   Peletier, Lambertus A ^b,c   Gabrielsson, Johan ^d  

^a ASTRAZENECA R AND D   (Sweden)

^b LEIDEN UNIVERSITY   (Netherlands)

^c CWI   (Netherlands)

^d ASTRAZENECA R AND D   (Sweden)

^e NONE

Author keywords

[No Author keywords available]

Indexed keywords

CLOMETHIAZOLE;

ANIMAL EXPERIMENT; ARTICLE; BODY TEMPERATURE; CATHETERIZATION; CIRCADIAN RHYTHM; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DOSE REGIMEN; DRUG POTENCY; DRUG TOLERANCE; HYPOTHERMIA; MALE; NEGATIVE FEEDBACK; NONHUMAN; OSMOTIC PUMP; PRIORITY JOURNAL; RAT; TELEMETRY; THERMOREGULATION; TURNOVER TIME;

EID: 33645115632     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.105.095224     Document Type: Article

References (40)

1. Achermann P and Kunz H (1999) Modeling circadian rhythm generation in the suprachiasmatic nucleus with locally coupled self-sustained oscillators: phase shifts and phase response curves. J Biol Rhythms 14:460-468.
2. Ackerman E, Rosevear JW, and McGuckin WF (1964) A mathematical model of the glucose-tolerance test. Phys Med Biol 9:203-213.
3. Bauer JA, Balthasar JP, and Fung HL (1997) Application of pharmacodynamic modeling for designing time-variant dosing regimens to overcome nitroglycerin tolerance in experimental heart failure. Pharm Res 14:1140-1145.
4. Benstaali C, Mailloux A, Bogdan A, Auzeby A, and Touitou Y (2001) Circadian rhythms of body temperature and motor activity in rodents their relationships with the light-dark cycle. Life Sci 68:2645-2656.
5. Blatteis CM (2000) Thermoregulation in complex situations: combined heat exposure, infectious fever and water deprivation. Int J Biometeorol 44:31-43.
6. Briese E (1998) Normal body temperature of rats: the set point controversy. Neurosci Biobehav Rev 22:427-436.
7. Chakraborty A, Krzyzanski W, and Jusko WJ (1999) Mathematical modeling of circadian cortisol concentrations using indirect response models: comparison of several methods. J Pharmacokinet Biopharm 27:23-43.
8. Chaulk D, Wells J, Evans S, Jackson D, and Corbett D (2003) Long-term effects of clomethiazole in a model of global ischemia. Exp Neurol 182:476-482.
9. Corbett D, Evans S, Thomas C, Wang D, and Jonas RA (1990) MK-801 reduced cerebral ischemic injury by inducing hypothermia. Brain Res 514:300-304.
10. Cross AJ, Jones JA, Baldwin HA, and Green AR (1991) Neuroprotective activity of chlormethiazole following transient forebrain ischaemia in the gerbil. Br J Pharmacol 104:406-411.
11. Dayneka NL, Garg V, and Jusko WJ (1993) Comparison of four basic models of indirect pharmacodynamic responses. J Pharmacokinet Biopharm 21:457-478.
12. Ekblad EB and Licko V (1984) Invariant relation between total acid secretion and secretagogue exposure: secretory dynamics in bullfrog. Am J Physiol 246:G325-G330.
13. Fattinger K, Verotta D, and Benowitz NL (1997) Pharmacodynamics of acute tolerance to multiple nicotinic effects in humans. J Pharmacol Exp Ther 281:1238-1246.
14. Gabrielsson J and Weiner D (1997) Pharmacokinetic and Pharmacodynamic Data Analysis, Concepts and Applications. Swedish Pharmaceutical Press, Stockholm.
15. Gardmark M, Brynne L, Hammarlund-Udenaes M, and Karlsson MO (1999) Interchangeability and predictive performance of empirical tolerance models. Clin Pharmacokinet 36:145-167.
16. Green AR (1998) Clomethiazole (Zendra) in acute ischemic stroke: basic pharmacology and biochemistry and clinical efficacy. Pharmacol Ther 80:123-147.
17. Green AR, Murray TK, Misra A, Snape MF, Jones JA, and Cross AJ (2000) The metabolism of clomethiazole in gerbils and the neuroprotective and sedative activity of the metabolites. Br J Pharmacol 129:95-100.
18. Hempel G, Karlsson MO, de Alwis DP, Toublanc N, McNay J, and Schaefer HG (1998) Population pharmacokinetic-pharmacodynamic modeling of moxonidine using 24-hour ambulatory blood pressure measurements. Clin Pharmacol Ther 64:622-635.
19. Holford NH and Sheiner LB (1982) Kinetics of pharmacologic response. Pharmacol Ther 16:143-166.
20. Kleinbloesem CH, van Brummelen P, and Breimer DD (1987) Nifedipine: relationship between pharmacokinetics and pharmacodynamics. Clin Pharmacokinet 12:12-29.
21. Lemmer B (1999) Chronopharmacokinetics: implications for drug treatment. J Pharm Pharmacol 51:887-890.
22. Lobo LL, Claustrat B, Debilly G, Paut-Pagano L, Jouvet M, and Valatx JL (1999) Hypoprolactinemic rats under conditions of constant darkness or constant light: effects on the sleep-wake cycle, cerebral temperature and sulfatoxymelatonin levels. Brain Res 835:282-289.
23. Mager DE and Jusko WJ (2001) Pharmacodynamic modeling of time-dependent transduction systems. Clin Pharmacol Ther 70:210-216.
24. Mandema JW and Wada DR (1995) Pharmacodynamic model for acute tolerance development to the electroencephalographic effects of alfentanil in the rat. J Pharmacol Exp Ther 275:1185-1194.
25. Movin-Osswald G and Hammarlund-Udenaes M (1995) Prolactin release after remoxipride by an integrated pharmacokinetic-pharmacodynamic model with intra and interindividual aspects. J Pharmacol Exp Ther 274:921-927.
26. Perachon S, Betancur C, Pilon C, Rostene W, Schwartz JC, and Sokoloff P (2000) Role of dopamine D3 receptors in thermoregulation: a reappraisal. Neuroreport 11:221-225.
27. Porchet HC, Benowitz NL, and Sheiner LB (1988) Pharmacodynamic model of tolerance: application to nicotine. J Pharmacol Exp Ther 244:231-236.
28. Prudian F, Gantenbein M, Pelissier AL, Attolini L, and Bruguerolle B (1997) Daily rhythms of heart rate, temperature and locomotor activity are modified by anaesthetics in rats: a telemetric study. Naunyn-Schmiedeberg's Arch Pharmacol 355:774-778.
29. Sällström B, Visser SAG, Forsberg T, Ericson AC, Peletier LA, and Gabrielsson J (2005) A new pharmacodynamic turnover model capturing asymmetric circadian baseline of body temperature, heart rate and blood pressure in rats: Challenges in terms of tolerance and animal handling effects. J Pharmacokin Pharmacodyn 32:835-859 DOI: 10.1007/s10928-005-0087-2.
30. Salmi P and Ahlenius S (1998) Evidence for functional interactions between 5-HT1A and 5-HT2A receptors in rat thermoregulatory mechanisms. Pharmacol Toxicol 82:122-127.
31. Sheiner LB, Stanski DR, Vozeh S, Miller RD, and Ham J (1979) Simultaneous modeling of pharmacokinetics and pharmacodynamics: application to dtubocurarine. Clin Pharmacol Ther 25:358-371.
32. Shimada S, Nakajima Y, Yamamoto K, Sawada Y, and Iga T (1996) Comparative pharmaco-dynamics of eight calcium channel blocking agents in Japanese essential hypertensive patients. Biol Pharm Bull 19:430-437.
33. Simon E, Pierau FK, and Taylor DC (1986) Central and peripheral thermal control of effectors in homeothermic temperature regulation. Physiol Rev 66:235-300.
34. Sun YN and Jusko WJ (1998) Transit compartments versus gamma distribution function to model signal transduction processes in pharmacodynamics. J Pharm Sci 87:732-737.
35. Visser SAG, Pozarek S, Martinsson S, Forsberg T, Ross SB, and Gabrielsson J (2005) Rapid and long-lasting tolerance to clomethiazole-induced hypothermia in the rat. Eur J Pharmacol 512:139-151.
36. Wakelkamp M, Alvan G, Gabrielsson J, and Paintaud G (1996) Pharmacodynamic modeling of furosemide tolerance after multiple intravenous administration. Clin Pharmacol Ther 60:75-88.
37. Wang EQ, Balthasar JP, and Fung HL (2004) Pharmacodynamics of in vivo nitroglycerin tolerance in normal conscious rats: effects of dose and dosing protocol. Pharm Res 21:114-120.
38. Zarrindast MR and Oveissi Y (1988) GABAA and GABAB receptor sites involvement in rat thermoregulation. Gen Pharmacol 19:223-226.
39. Zuideveld KP, Maas HJ, Treijtel N, Hulshof J, van der Graaf PH, Peletier LA, and Danhof M (2001) A set-point model with oscillatory behavior predicts the time course of 8-OH-DPAT-induced hypothermia. Am J Physiol 281:R2059-R2071.
40. Zuideveld KP, van der Graaf PH, Newgreen D, Thurlow R, Petty N, Jordan P, Peletier LA, and Danhof M (2004) Mechanism-based pharmacokineticpharmacodynamic 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.