Effects of terbinafine and itraconazole on the pharmacokinetics of orally administered tramadol

European Journal of Clinical Pharmacology

Volumn 71, Issue 3, 2015, Pages 321-327

  Saarikoski, Tuukka ^a   Saari, Teijo I ^a   Hagelberg, Nora M ^a   Backman, Janne T ^b   Neuvonen, Pertti J ^b   Scheinin, Mika ^a,c   Olkkola, Klaus T ^b   Laine, Kari ^c,d  

^a TURKU UNIVERSITY HOSPITAL   (Finland)

^b HELSINKI UNIVERSITY CENTRAL HOSPITAL   (Finland)

^c UNIVERSITY OF TURKU   (Finland)

^d Medbase Ltd   (Finland)

Author keywords

Interaction; Itraconazole; O desmethyltramadol; Pharmacokinetics; Terbinafine; Tramadol

Indexed keywords

CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; ITRACONAZOLE; O NORTRAMADOL; PLACEBO; TERBINAFINE; TRAMADOL; ANTIFUNGAL AGENT; CYTOCHROME P450 2D6 INHIBITOR; CYTOCHROME P450 3A INHIBITOR; NAPHTHALENE DERIVATIVE; NARCOTIC ANALGESIC AGENT;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CROSSOVER PROCEDURE; DROWSINESS; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG HALF LIFE; DRUG METABOLISM; ELIMINATION HALF-LIFE; ELIMINATION RATE CONSTANT; FEMALE; GENOTYPE; HUMAN; HUMAN EXPERIMENT; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PHARMACODYNAMICS; PHARMACOKINETICS; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; TIME TO MAXIMUM PLASMA CONCENTRATION; XEROSTOMIA; BLOOD; DRUG INTERACTION; GENETICS; NEUROPSYCHOLOGICAL TEST; ORAL DRUG ADMINISTRATION; YOUNG ADULT;

ADMINISTRATION, ORAL; ADULT; ANALGESICS, OPIOID; ANTIFUNGAL AGENTS; CROSS-OVER STUDIES; CYTOCHROME P-450 CYP2D6; CYTOCHROME P-450 CYP2D6 INHIBITORS; CYTOCHROME P-450 CYP3A INHIBITORS; DRUG INTERACTIONS; FEMALE; GENOTYPE; HUMANS; ITRACONAZOLE; MALE; NAPHTHALENES; NEUROPSYCHOLOGICAL TESTS; TRAMADOL; YOUNG ADULT;

EID: 84925490782     PISSN: 00316970     EISSN: 14321041     Source Type: Journal    
DOI: 10.1007/s00228-014-1799-2     Document Type: Article

References (40)

1. Moore RA, McQuay HJ (1997) Single-patient data meta-analysis of 3453 postoperative patients: oral tramadol versus placebo, codeine and combination analgesics. Pain 69(3):287-294
2. Harati Y, Gooch C, Swenson M, Edelman S, Greene D, Raskin P, Donofrio P, Cornblath D, Sachdeo R, Siu CO, Kamin M (1998) Double-blind randomized trial of tramadol for the treatment of the pain of diabetic neuropathy. Neurology 50(6):1842-1846
3. Boureau F, Legallicier P, Kabir-Ahmadi M (2003) Tramadol in post-herpetic neuralgia: a randomized, double-blind, placebo-controlled trial. Pain 104(1-2):323-331
4. Malonne H, Coffiner M, Sonet B, Sereno A, Vanderbist F (2004) Efficacy and tolerability of sustained-release tramadol in the treatment of symptomatic osteoarthritis of the hip or knee: a multicenter, randomized, double-blind, placebo-controlled study. Clin Ther 26(11):1774-1782. doi: 10.1016/j.clinthera.2004.11.005
5. Grond S, Sablotzki A (2004) Clinical pharmacology of tramadol. Clin Pharmacokinet 43(13):879-923
6. Gillen C, Haurand M, Kobelt DJ, Wnendt S (2000) Affinity, potency and efficacy of tramadol and its metabolites at the cloned human mu-opioid receptor. Naunyn Schmiedebergs Arch Pharmacol 362(2):116-121
7. Raffa RB, Friderichs E, Reimann W, Shank RP, Codd EE, Vaught JL, Jacoby HI, Selve N (1993) Complementary and synergistic antinociceptive interaction between the enantiomers of tramadol. J Pharmacol Exp Ther 267(1):331-340
8. Saarikoski T, Saari TI, Hagelberg NM, Neuvonen M, Neuvonen PJ, Scheinin M, Olkkola KT, Laine K (2013) Rifampicin markedly decreases the exposure to oral and intravenous tramadol. Eur J Clin Pharmacol 69(6):1293-1301. doi: 10.1007/s00228-012-1460-x
9. Lintz W, Barth H, Osterloh G, Schmidt-Bothelt E (1986) Bioavailability of enteral tramadol formulations. 1st communication: capsules. Arzneimittelforschung 36(8):1278-1283
10. Wu WN, McKown LA, Liao S (2002) Metabolism of the analgesic drug ULTRAM (tramadol hydrochloride) in humans: API-MS and MS/MS characterization of metabolites. Xenobiotica 32(5):411-425. doi: 10.1080/00498250110113230
11. Subrahmanyam V, Renwick AB, Walters DG, Young PJ, Price RJ, Tonelli AP, Lake BG (2001) Identification of cytochrome P-450 isoforms responsible for cis-tramadol metabolism in human liver microsomes. Drug Metab Dispos 29(8):1146-1155
12. Poulsen L, Arendt-Nielsen L, Brosen K, Sindrup SH (1996) The hypoalgesic effect of tramadol in relation to CYP2D6. Clin Pharmacol Ther 60(6):636-644. doi: 10.1016/S0009-9236(96)90211-8
13. Abdel-Rahman SM, Nahata MC (1997) Oral terbinafine: a new antifungal agent. Ann Pharmacother 31(4):445-456
14. Ahonen J, Olkkola KT, Neuvonen PJ (1995) Effect of itraconazole and terbinafine on the pharmacokinetics and pharmacodynamics of midazolam in healthy volunteers. Br J Clin Pharmacol 40(3):270-272
15. Abdel-Rahman SM, Gotschall RR, Kauffman RE, Leeder JS, Kearns GL (1999) Investigation of terbinafine as a CYP2D6 inhibitor in vivo. Clin Pharmacol Ther 65(5):465-472. doi: 10.1016/S0009-9236(99)70065-2
16. Hynninen VV, Olkkola KT, Bertilsson L, Kurkinen K, Neuvonen PJ, Laine K (2008) Effect of terbinafine and voriconazole on the pharmacokinetics of the antidepressant venlafaxine. Clin Pharmacol Ther 83(2):342-348. doi: 10.1038/sj.clpt.6100311
17. Olkkola KT, Ahonen J, Neuvonen PJ (1996) The effects of the systemic antimycotics, itraconazole and fluconazole, on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Anesth Analg 82(3):511-516
18. Kaukonen KM, Olkkola KT, Neuvonen PJ (1997) Itraconazole increases plasma concentrations of quinidine. Clin Pharmacol Ther 62(5):510-517. doi: 10.1016/S0009-9236(97)90046-1
19. Walsky RL, Astuccio AV, Obach RS (2006) Evaluation of 227 drugs for in vitro inhibition of cytochrome P450 2B6. J Clin Pharmacol 46(12):1426-1438. doi: 10.1177/0091270006293753
20. Tirkkonen T, Laine K (2004) Drug interactions with the potential to prevent prodrug activation as a common source of irrational prescribing in hospital inpatients. Clin Pharmacol Ther 76(6):639-647. doi: 10.1016/j.clpt.2004.08.017
21. Michna E, Ross EL, Hynes WL, Nedeljkovic SS, Soumekh S, Janfaza D, Palombi D, Jamison RN (2004) Predicting aberrant drug behavior in patients treated for chronic pain: importance of abuse history. J Pain Symptom Manag 28(3):250-258. doi: 10.1016/j.jpainsymman.2004.04.007
22. Madani S, Barilla D, Cramer J, Wang Y, Paul C (2002) Effect of terbinafine on the pharmacokinetics and pharmacodynamics of desipramine in healthy volunteers identified as cytochrome P450 2D6 (CYP2D6) extensive metabolizers. J Clin Pharmacol 42(11):1211-1218
23. Stone BM (1984) Pencil and paper tests - sensitivity to psychotropic drugs. Br J Clin Pharmacol 18(Suppl 1):15S-20S
24. Cogan DG (1941) Simplified entoptic pupillometer. Am J Ophthalmol 24:1431-1433
25. Hannington-Kiff JG (1970) Measurement of recovery from outpatient general anaesthesia with a simple ocular test. Br Med J 3(5715):132-135
26. Grach M, Massalha W, Pud D, Adler R, Eisenberg E (2004) Can coadministration of oxycodone and morphine produce analgesic synergy in humans? An experimental cold pain study. Br J Clin Pharmacol 58(3):235-242. doi: 10.1111/j.1365-2125.2004.02141.x
27. Kharasch ED, Hoffer C, Whittington D, Sheffels P (2003) Role of P-glycoprotein in the intestinal absorption and clinical effects of morphine. Clin Pharmacol Ther 74(6):543-554. doi: 10.1016/j.clpt.2003.08.011
28. Kharasch ED, Hoffer C, Altuntas TG, Whittington D (2004) Quinidine as a probe for the role of p-glycoprotein in the intestinal absorption and clinical effects of fentanyl. J Clin Pharmacol 44(3):224-233. doi: 10.1177/0091270003262075
29. Kalvass JC, Olson ER, Pollack GM (2007) Pharmacokinetics and pharmacodynamics of alfentanil in P-glycoprotein-competent and P-glycoprotein-deficient mice: P-glycoprotein efflux alters alfentanil brain disposition and antinociception. Drug Metab Dispos 35(3):455-459. doi: 10.1124/dmd.106.011445
30. DuBuske LM (2005) The role of P-glycoprotein and organic anion-transporting polypeptides in drug interactions. Drug Saf 28(9):789-801
31. Kanaan M, Daali Y, Dayer P, Desmeules J (2009) Uptake/efflux transport of tramadol enantiomers and O-desmethyl-tramadol: focus on P-glycoprotein. Basic Clin Pharmacol Toxicol 105(3):199-206. doi: 10.1111/j.1742-7843.2009.00428.x
32. Tzvetkov MV, Saadatmand AR, Lotsch J, Tegeder I, Stingl JC, Brockmoller J (2011) Genetically polymorphic OCT1: another piece in the puzzle of the variable pharmacokinetics and pharmacodynamics of the opioidergic drug tramadol. Clin Pharmacol Ther 90(1):143-150. doi: 10.1038/clpt.2011.56
33. Stamer UM, Musshoff F, Kobilay M, Madea B, Hoeft A, Stuber F (2007) Concentrations of tramadol and O-desmethyltramadol enantiomers in different CYP2D6 genotypes. Clin Pharmacol Ther 82(1):41-47. doi: 10.1038/sj.clpt.6100152
34. Hagelberg NM, Saarikoski T, Saari TI, Neuvonen M, Neuvonen PJ, Turpeinen M, Scheinin M, Laine K, Olkkola KT (2013) Ticlopidine inhibits both O-demethylation and renal clearance of tramadol, increasing the exposure to it, but itraconazole has no marked effect on the ticlopidine-tramadol interaction. Eur J Clin Pharmacol 69(4):867-875. doi: 10.1007/s00228-012-1433-0
35. Gronlund J, Saari T, Hagelberg N, Martikainen IK, Neuvonen PJ, Olkkola KT, Laine K (2010) Effect of telithromycin on the pharmacokinetics and pharmacodynamics of oral oxycodone. J Clin Pharmacol 50(1):101-108. doi: 10.1177/0091270009336444
36. Hughes CW, Petty F, Sheikha S, Kramer GL (1996) Whole-blood serotonin in children and adolescents with mood and behavior disorders. Psychiatry Res 65(2):79-95
37. Epperson N, Czarkowski KA, Ward-O'Brien D, Weiss E, Gueorguieva R, Jatlow P, Anderson GM (2001) Maternal sertraline treatment and serotonin transport in breast-feeding mother-infant pairs. Am J Psychiatry 158(10):1631-1637
38. Maurer-Spurej E, Pittendreigh C, Solomons K (2004) The influence of selective serotonin reuptake inhibitors on human platelet serotonin. Thromb Haemost 91(1):119-128. doi: 10.1267/THRO04010119
39. Enggaard TP, Poulsen L, Arendt-Nielsen L, Brosen K, Ossig J, Sindrup SH (2006) The analgesic effect of tramadol after intravenous injection in healthy volunteers in relation to CYP2D6. Anesth Analg 102(1):146-150. doi: 10.1213/01.ane.0000189613.61910.32
40. Desmeules J, Gascon MP, Dayer P, Magistris M (1991) Impact of environmental and genetic factors on codeine analgesia. Eur J Clin Pharmacol 41(1):23-26. doi: 10.1007/BF00280101