Effects of gender and moderate smoking on the pharmacokinetics and effects of the CYP1A2 substrate tizanidine

European Journal of Clinical Pharmacology

Volumn 64, Issue 1, 2008, Pages 17-24

  Backman, Janne T ^a   Schröder, Marika T ^a   Neuvonen, Pertti J ^a  

^a UNIVERSITY OF HELSINKI   (Finland)

Author keywords

Caffeine test; CYP1A2; Gender; Smoking; Tizanidine

Indexed keywords

CAFFEINE; CYTOCHROME P450 1A2; PARAXANTHINE; TIZANIDINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; BLOOD PRESSURE; BODY MASS; BODY WEIGHT; DROWSINESS; DRUG BLOOD LEVEL; DRUG HALF LIFE; FEMALE; GENDER; HUMAN; HUMAN EXPERIMENT; HYPOTENSION; MALE; NORMAL HUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; PSYCHOMOTOR ACTIVITY; SMOKING; STATISTICAL ANALYSIS; VOLUNTEER;

ADRENERGIC ALPHA-AGONISTS; ADULT; AREA UNDER CURVE; BLOOD PRESSURE; BODY WEIGHT; CAFFEINE; CLONIDINE; CYTOCHROME P-450 CYP1A2; DRUG INTERACTIONS; FEMALE; HALF-LIFE; HUMANS; MALE; SEX FACTORS; SLEEP STAGES; SMOKING; THEOPHYLLINE;

EID: 38049035557     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00228-007-0389-y     Document Type: Article

References (48)

1. Relling MV, Lin JS, Ayers GD, Evans WE (1992) Racial and gender differences in N-acetyltransferase, xanthine oxidase, and CYP1A2 activities. Clin Pharmacol Ther 52:643-658
2. Fletcher CV, Acosta EP, Strykowski JM (1994) Gender differences in human pharmacokinetics and pharmacodynamics. J Adolesc Health 15:619-629
3. Meibohm B, Beierle I, Derendorf H (2002) How important are gender differences in pharmacokinetics? Clin Pharmacokinet 41:329-342
4. Gandhi M, Aweeka F, Greenblatt RM, Blaschke TF (2004) Sex differences in pharmacokinetics and pharmacodynamics. Annu Rev Pharmacol Toxicol 44:499-523
5. Bies RR, Bigos KL, Pollock BG (2003) Gender differences in the pharmacokinetics and pharmacodynamics of antidepressants. J Gend Specif Med 6:12-20
6. Rasmussen BB, Brix TH, Kyvik KO, Brøsen K (2002) The interindividual differences in the 3-demethylation of caffeine alias CYP1A2 is determined by both genetic and environmental factors. Pharmacogenetics 12:473-478
7. Schwartz JB (2003) The influence of sex on pharmacokinetics. Clin Pharmacokinet 42:107-121
8. Cotreau MM, von Moltke LL, Greenblatt DJ (2005) The influence of age and sex on the clearance of cytochrome P450 3A substrates. Clin Pharmacokinet 44:33-60
9. Morris ME, Lee HJ, Predko LM (2003) Gender differences in the membrane transport of endogenous and exogenous compounds. Pharmacol Rev 55:229-240
10. Niemi M, Pasanen MK, Neuvonen PJ (2006) SLCO1B1 polymorphism and sex affect the pharmacokinetics of pravastatin but not fluvastatin. Clin Pharmacol Ther 80:356-366
11. Parsons WD, Neims AH (1978) Effect of smoking on caffeine clearance. Clin Pharmacol Ther 24:40-45
12. Sesardic D, Boobis AR, Edwards RJ, Davies DS (1988) A form of cytochrome P450 in man, orthologous to form d in the rat, catalyses the O-deethylation of phenacetin and is inducible by cigarette smoking. Br J Clin Pharmacol 26:363-372
13. Kalow W, Tang BK (1991) Caffeine as a metabolic probe: exploration of the enzyme-inducing effect of cigarette smoking. Clin Pharmacol Ther 49:44-48
14. Vistisen K, Loft S, Poulsen HE (1991) Cytochrome P450 IA2 activity in man measured by caffeine metabolism: effect of smoking, broccoli and exercise. Adv Exp Med Biol 283:407-411
15. Rasmussen BB, Brøsen K (1996) Determination of urinary metabolites of caffeine for the assessment of cytochrome P4501A2, xanthine oxidase, and N-acetyltransferase activity in humans. Ther Drug Monit 18:254-262
16. Zevin S, Benowitz NL (1999) Drug interactions with tobacco smoking. An update. Clin Pharmacokinet 36:425-438
17. Tantcheva-Poor I, Zaigler M, Rietbrock S, Fuhr U (1999) Estimation of cytochrome P-450 CYP1A2 activity in 863 healthy Caucasians using a saliva-based caffeine test. Pharmacogenetics 9:131-144
18. Faber MS, Fuhr U (2004) Time response of cytochrome P450 1A2 activity on cessation of heavy smoking. Clin Pharmacol Ther 76:178-184
19. Faber MS, Jetter A, Fuhr U (2005) Assessment of CYP1A2 activity in clinical practice: why, how, and when? Basic Clin Pharmacol Toxicol 97:125-134
20. Petersen MS, Halling J, Damkier P, Nielsen F, Grandjean P, Weihe P, Brøsen K (2006) Caffeine N3-demethylation (CYP1A2) in a population with an increased exposure to polychlorinated biphenyls. Eur J Clin Pharmacol 62:1041-1048
21. Jokinen MJ, Olkkola KT, Ahonen J, Neuvonen PJ (2001) Effect of rifampin and tobacco smoking on the pharmacokinetics of ropivacaine. Clin Pharmacol Ther 70:344-350
22. Ursing C, von Bahr C, Brismar K, Röjdmark S (2005) Influence of cigarette smoking on melatonin levels in man. Eur J Clin Pharmacol 61:197-201
23. Rostami-Hodjegan A, Amin AM, Spencer EP, Lennard MS, Tucker GT, Flanagan RJ (2004) Influence of dose, cigarette smoking, age, sex, and metabolic activity on plasma clozapine concentrations: a predictive model and nomograms to aid clozapine dose adjustment and to assess compliance in individual patients. J Clin Psychopharmacol 24:70-78
24. Seppälä NH, Leinonen EV, Lehtonen ML, Kivistö KT (1999) Clozapine serum concentrations are lower in smoking than in nonsmoking schizophrenic patients. Pharmacol Toxicol 85:244-246
25. Gardner MJ, Tornatore KM, Jusko WJ, Kanarkowski R (1983) Effects of tobacco smoking and oral contraceptive use on theophylline disposition. Br J Clin Pharmacol 16:271-280
26. Grygiel JJ, Birkett DJ (1981) Cigarette smoking and theophylline clearance and metabolism. Clin Pharmacol Ther 30:491-496
27. Koch P, Hirst DR, von Wartburg BR (1989) Biological fate of sirdalud in animals and man. Xenobiotica 19:1255-1265
28. Granfors MT, Backman JT, Laitila J, Neuvonen PJ (2004) Tizanidine is mainly metabolized by cytochrome p450 1A2 in vitro. Br J Clin Pharmacol 57:349-353
29. Granfors MT, Backman JT, Neuvonen M, Ahonen J, Neuvonen PJ (2004) Fluvoxamine drastically increases concentrations and effects of tizanidine: a potentially hazardous interaction. Clin Pharmacol Ther 75:331-341
30. Granfors MT, Backman JT, Neuvonen M, Neuvonen PJ (2004) Ciprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism. Clin Pharmacol Ther 76:598-606
31. Backman JT, Karjalainen MJ, Neuvonen M, Laitila J, Neuvonen PJ (2006) Rofecoxib is a potent inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine in healthy subjects. Br J Clin Pharmacol 62:345-357
32. Karjalainen MJ, Neuvonen PJ, Backman JT (2006) Rofecoxib is a potent, metabolism-dependent inhibitor of CYP1A2: implications for in vitro prediction of drug interactions. Drug Metab Dispos 34:2091-2096
33. Harder S, Fuhr U, Staib AH, Wolff T (1989) Ciprofloxacin-caffeine: a drug interaction established using in vivo and in vitro investigations. Am J Med 87:89S-91S
34. Fuhr U, Wolff T, Harder S, Schymanski P, Staib AH (1990) Quinolone inhibition of cytochrome P-450-dependent caffeine metabolism in human liver microsomes. Drug Metab Dispos 18:1005-1010
35. Brøsen K, Skjelbo E, Rasmussen BB, Poulsen HE, Loft S (1993) Fluvoxamine is a potent inhibitor of cytochrome P4501A2. Biochem Pharmacol 45:1211-1214
36. Wang JS, Backman JT, Wen X, Taavitsainen P, Neuvonen PJ, Kivistö KT (1999) Fluvoxamine is a more potent inhibitor of lidocaine metabolism than ketoconazole and erythromycin in vitro. Pharmacol Toxicol 85:201-205
37. Kalow W, Tang BK (1991) Use of caffeine metabolite ratios to explore CYP1A2 and xanthine oxidase activities. Clin Pharmacol Ther 50:508-519
38. Backman JT, Granfors MT, Neuvonen PJ (2006) Rifampicin is only a weak inducer of CYP1A2-mediated presystemic and systemic metabolism: studies with tizanidine and caffeine. Eur J Clin Pharmacol 62:451-461
39. Granfors MT, Backman JT, Laitila J, Neuvonen PJ (2005) Oral contraceptives containing ethinyl estradiol and gestodene markedly increase plasma concentrations and effects of tizanidine by inhibiting cytochrome P450 1A2. Clin Pharmacol Ther 78:400-411
40. Holland DT, Godfredsen KA, Page T, Connor JD (1998) Simple high-performance liquid chromatography method for the simultaneous determination of serum caffeine and paraxanthine following rapid sample preparation. J Chromatogr B Biomed Sci Appl 707:105-110
41. Pickard CE, Stewart AD, Hartley R, Lucock MD (1986) A rapid HPLC method for monitoring plasma levels of caffeine and theophylline using solid phase extraction columns. Ann Clin Biochem 23(Pt 4):440-446
42. Dollery C (1999) Caffeine. In: Dollery C (ed) Therapeutic drugs. Churchill Livingstone, Edinburgh, pp C4-C6
43. Bebia Z, Buch SC, Wilson JW, Frye RF, Romkes M, Cecchetti A, Chaves-Gnecco D, Branch RA (2004) Bioequivalence revisited: influence of age and sex on CYP enzymes. Clin Pharmacol Ther 76:618-627
44. Oztekin S, Mavioglu O, Elar Z, Guven H, Kalkan S, Gurpinar T (2005) The effects of gender and menopause on serum lidocaine levels in smokers. Eur J Drug Metab Pharmacokinet 30:231-234
45. Bruno R, Vivier N, Montay G, Le Liboux A, Powe LK, Delumeau JC, Rhodes GR (1997) Population pharmacokinetics of riluzole in patients with amyotrophic lateral sclerosis. Clin Pharmacol Ther 62:518-526
46. Schrenk D, Brockmeier D, Mörike K, Bock KW, Eichelbaum M (1998) A distribution study of CYP1A2 phenotypes among smokers and non-smokers in a cohort of healthy Caucasian volunteers. Eur J Clin Pharmacol 53:361-367
47. Bock KW, Schrenk D, Forster A, Griese EU, Mörike K, Brockmeier D, Eichelbaum M (1994) The influence of environmental and genetic factors on CYP2D6, CYP1A2 and UDP-glucuronosyltransferases in man using sparteine, caffeine, and paracetamol as probes. Pharmacogenetics 4:209-218
48. Laine K, Palovaara S, Tapanainen P, Manninen P (1999) Plasma tacrine concentrations are significantly increased by concomitant hormone replacement therapy. Clin Pharmacol Ther 66:602-608