Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations

International Journal of Clinical Pharmacology and Therapeutics

Volumn 51, Issue 4, 2013, Pages 338-348

  Göhler, Karin ^a   Brett, Martin ^a   Smit, Johan W ^b   Rengelshausen, Jens ^a   Terlinden, Rolf ^a  

^a GRÜNENTHAL GMBH   (Germany)

^b JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

Bioavail ability; Formulations; Pharmacokinetics; Tapentadol

Indexed keywords

TAPENTADOL;

ADULT; AREA UNDER THE CURVE; ARTICLE; BIOCHEMISTRY; BIOEQUIVALENCE; CONTROLLED STUDY; CROSSOVER PROCEDURE; DISTRIBUTION VOLUME; DIZZINESS; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG DOSAGE FORM COMPARISON; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG FATALITY; DRUG FORMULATION; DRUG HALF LIFE; DRUG SAFETY; DRUG TOLERABILITY; ELECTROCARDIOGRAM; FATIGUE; HALF VALUE DURATION; HEADACHE; HEMATOLOGY; HUMAN; HUMAN EXPERIMENT; IMMEDIATE RELEASE FORMULATION; MALE; MAXIMUM PLASMA CONCENTRATION; MEAN RESIDENCE TIME; NAUSEA AND VOMITING; NORMAL HUMAN; OPEN STUDY; PHARMACOLOGICAL PARAMETERS; PROLONGED RELEASE FORMULATION; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; SINGLE DRUG DOSE; SOMNOLENCE; TIME TO MAXIMUM PLASMA CONCENTRATION; URINALYSIS; VITAL SIGN; XEROSTOMIA;

ADMINISTRATION, ORAL; ADOLESCENT; ADULT; ANALGESICS, OPIOID; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CROSS-OVER STUDIES; DELAYED-ACTION PREPARATIONS; HALF-LIFE; HUMANS; INJECTIONS, INTRAVENOUS; MALE; PHENOLS; TISSUE DISTRIBUTION; YOUNG ADULT;

EID: 84876547199     PISSN: 09461965     EISSN: None     Source Type: Journal    
DOI: 10.5414/CP201722     Document Type: Article

References (27)

1. Tzschentke TM, Christoph T, Kögel B, Schiene K, Hennies H-H, Englberger W, Haurand M, Jahnel U, Cremers TI, Friderichs E, De Vry J. (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel μ-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007; 323: 265-276. doi:10.1124/jpet.107.126052
2. Palexia® (tapentadol) oral film-coated tablets [summary of product characteristics]. Aachen, Germany: Grünenthal GmbH; 2011.
3. Palexia® SR (tapentadol) prolonged-release oral tablets [summary of product characteristics]. Aachen, Germany: Grünenthal GmbH; 2011.
4. Nucynta. Nucynta® ER (tapentadol) extended-release oral tablets C-II [prescribing information]. Raritan, NJ: Janssen Pharmaceuticals, Inc.; 2011. 2011.
5. Daniels S, Casson E, Stegmann JU, Oh C, Okamoto A, Rauschkolb C, Upmalis D. A randomized, double-blind, placebo-controlled phase 3 study of the relative efficacy and tolerability of tapentadol IR and oxycodone IR for acute pain. Curr Med Res Opin. 2009; 25: 1551-1561. doi:10.1185/03007990902952825
6. Daniels SE, Upmalis D, Okamoto A, Lange C, Häeussler J. A randomized, double-blind, phase III study comparing multiple doses of tapentadol IR, oxycodone IR, and placebo for postoperative (bunionectomy) pain. Curr Med Res Opin. 2009; 25: 765-776. doi:10.1185/03007990902728183
7. Hartrick C, Van Hove I, Stegmann J-U, Oh C, Upmalis D. Efficacy and tolerability of tapentadol immediate release and oxycodone HCl immediate release in patients awaiting primary joint replacement surgery for end-stage joint disease: a 10-day, phase III, randomized, double-blind, active - and placebo-controlled study. Clin Ther. 2009; 31: 260-271. doi:10.1016/j.clinthera. 2009.02.009
8. Afilalo M, Etropolski MS, Kuperwasser B, Kelly K, Okamoto A, Van Hove I, Steup A, Lange B, Rauschkolb C, Haeussler J. Efficacy and safety of tapentadol extended release compared with oxycodone controlled release for the management of moderate to severe chronic pain related to osteoarthritis of the knee: a randomized, double-blind, placebo- and active-controlled phase III study. Clin Drug Investig. 2010; 30: 489-505. doi:10.2165/11533440-000000000-00000
9. Lange B, Kuperwasser B, Okamoto A, Steup A, Häufel T, Ashworth J, Etropolski M. Efficacy and safety of tapentadol prolonged release for chronic osteoarthritis pain and low back pain. Adv Ther. 2010; 27: 381-399. doi:10.1007/s12325-010-0036-3
10. Buynak R, Shapiro D Y, Okamoto A, Van Hove I, Rauschkolb C, Steup A, Lange B, Lange C, Etropolski M. Efficacy and safety of tapentadol extended release for the management of chronic low back pain: results of a prospective, randomized, double-blind, placebo- and active-controlled Phase III study. Expert Opin Pharmacother. 2010; 11: 1787-1804. doi:10.1517/14656566.2010.4977 20
11. Schwartz S, Etropolski M, Shapiro D Y, Okamoto A, Lange R, Haeussler J, Rauschkolb C. Safety and efficacy of tapentadol ER in patients with painful diabetic peripheral neuropathy: results of a randomized-withdrawal, placebo-controlled trial. Curr Med Res Opin. 2011; 27: 151-162. doi:1 0.1185/03007995.2010.537589
12. Etropolski M, Kelly K, Okamoto A, Rauschkolb C. Comparable efficacy and superior gastrointestinal tolerability (nausea, vomiting, constipation) of tapentadol compared with oxycodone hydrochloride. Adv Ther. 2011; 28: 401-417. doi:10.1007/s12325-011-0018-0
13. Hale M, Upmalis D, Okamoto A, Lange C, Rauschkolb C. Tolerability of tapentadol immediate release in patients with lower back pain or osteoarthritis of the hip or knee over 90 days: a randomized, double-blind study. Curr Med Res Opin. 2009; 25: 1095-1104. doi:10.1185/03007990902816970
14. 14C-labeled tapentadol HCl in healthy male subjects. Eur J Drug Metab Pharmacokinet. 2007; 32: 163-169. doi:10.1007/BF03190478
15. Smit J W, Oh C, Rengelshausen J, Terlinden R, Ravenstijn PGM, Wang S-S, Upmalis D, Mangold B. Effects of acetaminophen, naproxen, and ace-tylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Pharmacotherapy. 2010; 30: 25-34. doi:10.1592/phco.30.1.25
16. Xu XS, Smit J W, Lin R, Stuyckens K, Terlinden R, Nandy P. Population pharmacokinetics of tapentadol immediate release (IR) in healthy subjects and patients with moderate or severe pain. Clin Pharmacokinet. 2010; 49: 671-682. doi:10.2165/11535390-000000000-00000
17. Terlinden R, Kögel B Y, Englberger W, Tzschentke TM. In vitro and in vivo characterization of tapentadol metabolites. Methods Find Exp Clin Pharmacol. 2010; 32: 31-38. doi:10.1358/mf.2010.32.1.1434165
18. Gibaldi M, Perrier D. Drugs and the Pharmaceutical Sciences. Volume 15: Pharmacokinetics. New York: Marcel Dekker, Inc; 1982.
19. SAS Institute Inc. SAS/STAT User's-Guide, Release 6.03 Edition. The GLM Procedure. Cary, NC: SAS Institute Inc.; 1988. p. 519.
20. Zacny J P, Conley K, Galinkin J. Comparing the subjective, psychomotor and physiological effects of intravenous buprenorphine and morphine in healthy volunteers. J Pharmacol Exp Ther. 1997; 282: 1187-1197.
21. Terlinden R, Ossig J, Fliegert F, Gohler K. Pharmacokinetics, excretion, and metabolism of tapentadol HCl, a novel centrally acting analgesic, in healthy subjects. J Pain. 2006; 7 (suppl 1): S26. doi:10.1016/j.jpain.2006.01. 091Abstract689.
22. Osborne R, Joel S, Trew D, Slevin M. Morphine and metabolite behavior after different routes of morphine administration: demonstration of the importance of the active metabolite morphine-6-glucuronide. Clin Pharmacol Ther. 1990; 47: 12-19. doi:10.1038/clpt.1990.2
23. Lugo RA, Kern SE. The pharmacokinetics of oxycodone. J Pain Palliat Care Pharmacother. 2004; 18: 17-30. doi:10.1080/J354v18n04-03
24. Glare P A, Walsh TD. Clinical pharmacokinetics of morphine. Ther Drug Monit. 1991; 13: 1-23. doi:10.1097/00007691-199101000-00001
25. Hoskin PJ, Hanks G W, Aherne G W, Chapman D, Littleton P, Filshie J. The bioavailability and pharmacokinetics of morphine after intravenous, oral and buccal administration in healthy volunteers. Br J Clin Pharmacol. 1989; 27: 499-505. doi:10.1111/j.1365-2125.1989.tb05399.x
26. Tzschentke TM, De Vry J, Terlinden R, Hennies HH, Lange C, Strassburger W, Haurand M, Kolb J, Schneider J, Buschmann H, Finkam M, Jahnel U, Friderichs E. Tapentadol HCl. Drugs Future. 2006; 31: 1053-1061. doi:10.1358/dof.2006.031. 12.1047744
27. Stuart-Harris R, Joel S P, McDonald P, Currow D, Slevin ML. The pharmacokinetics of morphine and morphine glucuronide metabolites after subcutaneous bolus injection and subcutaneous infusion of morphine. Br J Clin Pharmacol. 2000; 49: 207-214. doi:10.1046/j.1365-2125.2000.00141.x.