Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamics of tolterodine

Clinical Pharmacology and Therapeutics

Volumn 63, Issue 5, 1998, Pages 529-539

  Brynne, Niclas ^a   Dalén, Per ^a   Alván, Gunnar ^a   Bertilsson, Leif ^a   Gabrielsson, Johan ^a  

^a Pharmacia and Upjohn AB ^*

Author keywords

[No Author keywords available]

Indexed keywords

DEBRISOQUINE; DEBRISOQUINE 4 HYDROXYLASE; DRUG METABOLITE; PNU 200577; TOLTERODINE; UNCLASSIFIED DRUG;

ACCOMMODATION; ADULT; ARTICLE; CLINICAL TRIAL; DOSE RESPONSE; DRUG CLEARANCE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; ENZYME POLYMORPHISM; EYE DISEASE; HEADACHE; HUMAN; HUMAN EXPERIMENT; INTRAVENOUS DRUG ADMINISTRATION; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; SALIVATION; TACHYCARDIA; URGE INCONTINENCE; XEROSTOMIA;

ADMINISTRATION, ORAL; ADULT; AREA UNDER CURVE; BENZHYDRYL COMPOUNDS; CRESOLS; CYTOCHROME P-450 CYP2D6; DEBRISOQUIN; HALF-LIFE; HEART RATE; HUMANS; INFUSIONS, INTRAVENOUS; MALE; METABOLIC CLEARANCE RATE; MUSCARINIC ANTAGONISTS; PHENOTYPE; PHENYLPROPANOLAMINE; POLYMORPHISM, GENETIC; SALIVATION;

EID: 0031836669     PISSN: 00099236     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0009-9236(98)90104-7     Document Type: Article

References (26)

1. Alván G, Bechtel P, Iselius L, Gundert-Remy U. Hydroxylation polymorphisms of debrisoquine and mephenytoin in European populations. Eur J Clin Pharmacol 1990; 39:533-7.
2. Alván G. Clinical consequences of polymorphic drug oxidation. Fundam Clin Pharmacol 1991;5:209-28.
3. Bertilsson L. Geographical/interracial differences in polymorphic drug oxidation: current state of knowledge of cytochromes P450 (CYP) 2D6 and 2C19. Clin Pharmacokinet 1995;29:192-209.
4. Bertilsson L, Dahl ML. Polymorphic drug oxidation: relevance to the treatment of psychiatric disorders. CNS Drugs 1996;5:200-23.
5. Dayer P, Desmeules J, Leemann T, Striberni R. Bioactivation of the narcotic drug codeine in human liver is mediated by the polymorphic monooxygenase catalysing debrisoquine 4-hydroxylation. Biochem Biophys Res Commun 1988;152:411-6.
6. Woosley RL, Wood AJJ, Roden DM. Drug therapy: encainide. N Engl J Med 1988;318:1107-15.
7. Jonas U, Höfner K, Madersbacher H, Holmdahl TH, et al. Efficacy and safety of two doses of tolterodine versus placebo in patients with detrusor overactivity and symptoms of frequency, urge incontinence, and urgency: urodynamic evaluation. World J Urol 1997; 15:144-51.
8. Nilvebrant L, Andersson KE, Gillberg PG, Stahl M, Sparf B. Tolterodine: a new bladder-selective antimuscarinic agent. Eur J Pharmacol 1997;327:195-207.
9. Stahl MMS, Ekström B, Sparf B, Mattiasson A, Andersson KE. Urodynamic and other effects of tolterodine: a novel antimuscarinic drug for treatment of detrusor overactivity. Neurourol Urodyn 1995;14:647-55.
10. Rentzhog L, Stanton SL, Cardozo L, Nelson E, Fall M, Abrams P. Efficacy and safety of tolterodine in patients with detrusor instability: a dose-ranging study. Br J Urol 1998;81:42-8.
11. Brynne N, Stahl MMS, Hallén B, Edlund PO, Palmér L, Gabrielsson J. Pharmacokinetics and pharmacodynamics of tolterodine in man: a new drug for the treatment of urinary bladder overactivity. Int J Clin Pharmacol Ther 1997;35:287-95.
12. Nilvebrant L, Gillberg PG, Sparf B. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol 1997;81: 169-72.
13. Bertilsson L, Lou YQ, Du YL, Liu Y, Kuang TY, Liao XM, et al. Pronounced differences between native Chinese and Swedish populations in the polymorphic hydroxylations of debrisoquin and S-mephenytoin. Clin Pharmacol Ther 1992;51:388-97.
14. Nordin C, Bertilsson L, Otani K, Widmark A. Little anti-cholinergic effect of E-10-hydroxynortriptyline compared with nortriptyline in healthy subjects. Clin Pharmacol Ther 1987;41:97-102.
15. Palmér L, Andersson L, Andersson T, Stenberg U. Determination of tolterodine and the 5-hydroxymethyl metabolite in plasma, serum and urine using gas chromatography-mass spectrometry. J Pharm Biomed Anal 1997;16:155-65.
16. Statistical Consultants Inc. PCNONLIN and NONLIN84: software for the statistical analysis of nonlinear models. Am Stat 1986;40:52.
17. Gibaldi M, Perrier D. Pharmacokinetics. 2nd ed. New York: Marcel Dekker; 1982.
18. Rowland M, Tozer TN. Clinical pharmacokinetics: concepts and applications. 3rd ed. Philadelphia: Williams & Wilkins; 1995.
19. Gozzi P, Påhlman I. Serum protein binding of tolterodine and its 5-hydroxymethyl metabolite in different species. Presented at the Sixth European Meeting of the International Society for the Study of Xenobiotics; June 30-July 3, 1997; Gothenberg, Sweden.
20. Wolff T, Distlerath LM, Worthington MT, Groopman JD, Hammons GJ, Kadlubar FF, et al. Substrate specificity of human liver cytochrome P-450 debrisoquine 4-hydroxylase probed using immunochemical inhibition and chemical modeling. Cancer Res 1985;45:2116-22.
21. Meyer UA, Gut J, Kronbach T, Skoda C, Meier UT, Catin T, et al. The molecular mechanisms of two common polymorphisms of drug oxidation: evidence for functional changes in cytochrome P-450 isozymes catalysing bufuralol and mephenytoin oxidation. Xenobiotica 1986;16: 449-64.
22. Kramer Nielsen K, Brøsen K, Gram LF. Steady-state plasma levels of clomipramine and its metabolites: impact of the sparteine/debrisoquine polymorphism. Danish University Antidepressant Group. Eur J Clin Pharmacol 1992;43:405-11.
23. Sindrup SH, Brøsen K, Gram LF, Hallas J, Skjelbo E, Allen A, et al. The relationship between paroxetine and the sparteine oxidation polymorphism. Clin Pharmacol Ther 1992;51:278-87.
24. Siddoway LA, Thompson KA, McAllister CB, Wang T, Wilkinson GR, Roden DM, et al. Polymorphism of propafenone metabolism and disposition in man: clinical and pharmacokinetic consequences. Circulation 1987;75: 785-91.
25. Spina E, Martines C, Caputi AP, Cobaleda J, Pinas B, Carrillo JA, et al. Debrisoquine oxidation phenotype during neuroleptic monotherapy. Eur Clin Pharmacol 1991; 41:467-70.
26. Postlind H, Danielsson A, Lindgren A, Andersson SHG. Tolterodine, a new muscarinic receptor antagonist, is metabolized by cytochromes P450 2D6 and 3A in human liver microsomes. Drug Metab Dispos 1998;26:289-93.