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2009 | 65 | 10 |
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Farmakokinetyka tramadolu oraz jego glownych metabolitow po jednorazowym podaniu per os tabletki o przedluzonym uwalnianiu oraz czopkow per rectum u psow

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Warianty tytułu
Pharmacokinetics of tramadol and its major conjugates after a single per os administration of a sustained tablet and per rectum suppositories formulations in dogs
Języki publikacji
The aim of the present study is to evaluate the pharmacokinetics of T and its major metabolites M1, M2 and M5 after the single oral administration of an SR tablet and rectal suppositories in dogs (4-6 mg·kg⁻¹ m.c.). The plasma concentration data after SR-tablet and rectal administration were fitted on the basis of a mono- and non-compartmental model, respectively. T plasma concentration after SR tablet administration was quantitatively detected in three dogs, M1 was quantized in only one dog while M2 and M5 were quantized in all the dogs. T showed median values of Cmax, Tmax and T₁/₂ of 40 (20-170) ng·mL⁻¹, 3 (4-2) and 1.88 (2.21-1.44) hours, respectively. M5 showed median values of Cmax, Tmax and T₁/₂ of 0.1 (90-190) ng·mL⁻¹, 2 (3-1) and 4.23 (6.58-1.85) hours, respectively. M2 showed median values of Cmax, Tmax and T₁/₂ of 220 (80-330) ng·mL⁻¹, 4 (7-3) and 4.49 (6.39-1.57) hours, respectively. Following rectal administration, T was detected from 5 minutes up to 10 h in a smaller amount than M5 and M2. T median value of Cmax was 140 ± 60 ng·mL⁻¹ in 0.56 ± 0.41 h (Tmax). K₀₁ t₁/₂ and K₁₀ t₁/₂ were 0.27 ± 0.25 h and 2.24 ± 1.82 h, respectively. M1 was detectable from 5 min up to 2 h, showing low values (7-28 ng·mL⁻¹). The present findings suggest oral SR tablet and suppository rectal formulation have similar pharmacokinetic behavior and would not have suitable pharmacokinetic characteristics to be administered once-a-day as an effective and safe treatment for pain in dogs.
Opis fizyczny
  • Uniwersytet Przyrodniczy w Lublinie, ul.Akademicka 12, 20-033 Lublin
  • 1.Evangelista M.: Tramadol sustained-release capsules. Drugs. 2006, 66, 223-230.
  • 2.Gillen C., Haurand M., Kobelt D. J., Wnendt S.: Affinity, potency and efficacy of tramadol and its metabolites at the cloned human mu-opioid receptor. Naunyn Schmiedeberg Arch. Pharmacol. 2000, 362, 116-121.
  • 3.Giorgi M., Del Carlo S., Saccomanni G., Łebkowska-Wieruszewska B., Kowalski C.: Pharmacokinetic of tramadol and its major metabolites following intravenous and rectal administration in dogs. N. Z. Vet. J. w druku, 2009b.
  • 4.Giorgi M., Saccomanni G., Daniello M. R., Manera C., Soldani G., Ferrarini P. L., Giusiani M.: In vitro metabolism of tramadol in horses: preliminary data. J. Vet. Pharmacol. Therap. 2006, 29, 124.
  • 5.Giorgi M., Saccomanni G., Łebkowska-Wieruszewska B., Kowalski C.: Pharmacokinetic evaluation of tramadol and its major metabolites after single oral sustained tablet administration in the dog: a pilot study. Vet. J. 2009a, 180, 253-255.
  • 6.Giorgi M., Soldani G., Manera C., Ferrarini P. L., Sgorbini M., Saccomanni G.: Pharmacokinetics of tramadol and its metabolites M1, M2 and M5 in horses following intravenous, immediate release (fasted/fed) and sustained release single dose administration. J. Equi. Vet. Sci. 2007, 27, 481-488.
  • 7.Grond S., Lynch J., Diefenbach C., Altrock K., Lehmann K. A.: Comparison of ondansetron and droperidol in the prevention of nausea and vomiting after inpatient minor gynecologic surgery. Anesth. Analg. 1995, 81, 603-607.
  • 8.Grond S., Meuser T., Uragg H., Stahlberg H. J., Lehmann K. A.: Serum concentrations of tramadol enantiomers during patient-controlled analgesia. British J. Clin. Pharmcol. 1999, 48, 254-257.
  • 9.Grond S., Sablotzki A.: Clinical pharmacology of tramadol. Clin. Pharmacokinet. 2004, 43, 879-923.
  • 10.Hair P. I., Curran M. P., Kean S. J.: Tramadol extended-release tablets. Drugs. 2006, 66, 2017-2026.
  • 11.Henrotin Y., Sanchez C., Balligand M.: Pharmaceutical and nutraceutical management of canine osteoarthritis: present and future perspectives. Vet. J. 2005, 170, 113-123.
  • 12.Kania B. F., Kania K.: Endogenous opioid peptides: action and significance for therapy. Medycyna Wet. 2002, 58, 481-560.
  • 13.Keating G. M.: Tramadol sustained-release capsules. Drugs. 2006, 66, 223-230.
  • 14.Kogel B., Englberger W., Hennies H. H., Friderichs E.: Involvement of metabolites in the analgesic action of tramadol. 9th World Congress of Pain, 1999 Aug 22-27, Vienna, s. 523.
  • 15.Kukanich B., Papich M. G.: Pharmacokinetics of tramadol and the metabolite O-desmethyltramadol in dogs. J. Vet. Pharmacol. Therap. 2004, 27, 239-246.
  • 16.Lee C. R., McTavish D., Sorkin E. M.: Tramadol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in acute and chronic pain states. Drugs. 1993, 46, 313-340.
  • 17.Lehmann K. A., Kratzenberg U., Schroeder-Bark B., Horrichs-Haermeyer G.: Postoperative patient-controlled analgesia with tramadol: analgesic efficacy and minimum effective concentrations. Clin. J. Pain. 1990, 6, 212-220.
  • 18.Lintz W., Erlacin S., Frankus E., Uragg H.: Biotransformation of tramadol in man and animal. Arzneim. Forsch. Drug Res. 1981, 31, 1932-1943.
  • 19.Malonne H., Sonet B., Streel B., Lebrun S., De Niet S., Sereno A., Vanderbist F.: Pharmacokinetic evaluation of a new oral sustained dosage form of tramadol. Br. J. Clin. Pharmacol. 2004, 57, 270-278.
  • 20.Martignoni M., Groothuis G. M., de Kanter R.: Species differences between mouse, rat, dog, monkey and human CYP-mediated drug metabolism, inhibition and induction. Expert Opin. Drug Metab. Toxicol. 2006, 2, 875-894.
  • 21.Nicpoń J., Kubiak K., Dzimira S., Sapikowski G.: Effect of some non-steroid anti-inflammatory drugs (NSAIDs) on canine gastric mucosa. Medycyna Wet. 2000, 56, 541-612.
  • 22.Raffa R. B., Friderichs E., Reimann W., Shank R. P., Codd E. E., Vaught J. L.: Opioid and nonopioid components independently contribute to the mechanism of action of tramadol, an "atypical" opioid analgesic. J. Pharmacol. Exp. Ther. 1992, 260, 275-285.
  • 23.Raffa R. B., Friderichs E., Reimann W., Shank R. P., Codd E. E., Vaught J. L., Jacoby H. I., Selve N.: Complementary and synergistic antinociceptive interaction between the enantiomers of tramadol. Pharmacol. Exp. Ther. 1993, 267, 331-340.
  • 24.Raz A.: Is inhibition of cyclooxygenase required for the anti-tumorigenic effects of nonsteroidal, anti-inflammatory drugs (NSAIDs)? In vitro versus in vivo results and the relevance for the prevention and treatment of cancer. Biochem. Pharmacol. 2002, 63, 343-347.
  • 25.Scott L. J., Perry C. M.: Tramadol: a review of its use in perioperative pain. Drugs. 2000, 60, 139-176.
  • 26.Tuncer S., Pirbudak L., Balat O., Capar M.: Adding ketoprofen to intravenous patient-controlled analgesia with tramadol after major gynecological cancer surgery: a double-blinded, randomized, placebo-controlled clinical trial. Eur. J. Gynaecol. Oncol. 2003, 24, 181-184.
  • 27.Wilder-Smith C. H., Bettiga A.: The analgesic tramadol has minimal effect on gastrointestinal motor function. Br. J. Clin. Pharmacol. 1997, 43, 71-75.
  • 28.Zollner C., Steiner C.: Opioids. Handb. Exp. Pharmacol. 2007, 177, 31-63.
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