Pharmacokinetics of an oral drug (acetaminophen) administered at various times in relation to subcutaneous injection of exenatide (exendin-4) in healthy subjects

Journal of Clinical Pharmacology

Volumn 45, Issue 5, 2005, Pages 570-577

  Blase, Erich ^a   Taylor, Kristin ^a   Gao, Hong Ye ^a   Wintle, Matthew ^a   Fineman, Mark ^a  

^a AMYLIN PHARMACEUTICALS INC   (United States)

Author keywords

Exenatide; Exendin 4; Pharmacokinetics; Type 2 diabetes

Indexed keywords

EXENDIN 4; PARACETAMOL; PLACEBO;

ADULT; AGED; AREA UNDER THE CURVE; ARTICLE; CARDIOTOXICITY; CARDIOVASCULAR DISEASE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG EFFECT; FEMALE; HUMAN; HYPOGLYCEMIA; LIVER TOXICITY; LUNG TOXICITY; MALE; NAUSEA AND VOMITING; NEPHROTOXICITY; NORMAL HUMAN; PHASE 2 CLINICAL TRIAL; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; SINGLE BLIND PROCEDURE;

ACETAMINOPHEN; ADMINISTRATION, ORAL; ADOLESCENT; ADULT; AGED; ANALGESICS, NON-NARCOTIC; AREA UNDER CURVE; CROSS-OVER STUDIES; DRUG INTERACTIONS; FEMALE; HUMANS; HYPOGLYCEMIC AGENTS; INJECTIONS, SUBCUTANEOUS; MALE; MIDDLE AGED; PEPTIDES; SINGLE-BLIND METHOD; VENOMS;

EID: 17644401388     PISSN: 00912700     EISSN: None     Source Type: Journal    
DOI: 10.1177/0091270004274432     Document Type: Article

References (47)

1. UK Prospective Diabetes Study Group. UK Prospective Diabetes Study 16. Overview of 6 years' therapy of type II diabetes: a progressive disease. Diabetes. 1995;44:1249-1258.
2. UK Prospective Diabetes Study Group. Intensive blood-glucose control with sulfonylureas or insulin compared with conventional treatment and risk of complications in subjects with type 2 diabetes (UKPDS 33). Lancet. 1998;352:837-853.
3. Inzucchi SE. Oral antihyperglycemic therapy for type 2 diabetes: scientific review. JAMA. 2002;287:360-372.
4. DeFronzo RA. Pharmacologic therapy for type 2 diabetes mellitus. Ann Intern Med. 1999;131:281-303.
5. Kolterman OG, Buse JB, Fineman MS, et al. Synthetic exendin-4 (exenatide) significantly reduces postprandial and fasting plasma glucose in subjects with type 2 diabetes. J Clin Endocrinol Metab. 2003;88:3082-3089.
6. Nielsen LL, Baron AD. Pharmacology of exenatide (synthetic exendin-4) for the treatment of type 2 diabetes. Curr Opin Investig Drugs. 2003;4:401-405.
7. Parkes DG, Pittner R, Jodka C, Smith P, Young A. Insulinotropic actions of exendin-4 and glucagon-like peptide-1 in vivo and in vitro. Metabolism. 2001;50:583-589.
8. Nielsen LL, Young AA, Parkes DG. Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetes. Regul Pept. 2004;117:77-88.
9. Egan JM, Clocquet AR, Elahi D. The insulinotropic effect of acute exendin-4 administered to humans: comparison of nondiabetic state to type 2 diabetes. J Clin Endocrinol Metab. 2002;87:1282-1290.
10. Holst JJ. Therapy of type 2 diabetes mellitus based on the actions of glucagon-like peptide-1. Diabetes Metab Res Rev. 2002;18:430-441.
11. Nauck MA, Kleine N, Orskov C, Holst JJ, Willms B, Creutzfeldt W. Normalization of fasting hyperglycaemia by exogenous glucagon-like peptide 1 (7-38 amide) in type 2 (non-insulin-dependent) diabetic patients. Diabetologia. 1993;36:741-744.
12. Edwards CM, Stanley SA, Davis R, et al. Exendin-4 reduces fasting and postprandial glucose and decreases energy intake in healthy volunteers. Am J Physiol Endocrinol Metab. 2001;281:E155-E161.
13. Zander M, Madsbad S, Madsen JL, Holst JJ. Effect of 6-week course of glucagon-like peptide-1 on glycaemic control, insulin sensitivity, and β-cell function in type 2 diabetes: a parallel-group study. Lancet. 2002;359:824-830.
14. Young AA, Gedulin BR, Bhavsar S, et al. Glucose-lowering and insulin-sensitizing actions of exendin-4: studies in obese diabetic (ob/ob, db/db) mice, diabetic fatty Zucker rats, and diabetic rhesus monkeys (Macaco mulatta). Diabetes. 1999;48:1026-1034.
15. Szayna M, Doyle ME, Betkey JA, et al. Exendin-4 decelerates food intake, weight gain, and fat deposition in Zucker rats. Endocrinology. 2000;141:1936-1941.
16. Fineman MS, Bicsak TA, Shen LZ, et al. Effect on glycemic control of exenatide (synthetic exendin-4) additive to existing metformin and/or sulfonylurea treatment in patients with type 2 diabetes. Diabetes Care. 2003;26:2370-2377.
17. Wettergren A, Schjoldager B, Mortensen PE, Myhre J, Christiansen J, Holst JJ. Truncated GLP-1 (proglucagon 78-107-amide) inhibits gastric and pancreatic functions in man. Dig Dis Sci. 1993;38:665-673.
18. Naslund E, Bogefors J, Skogar S, et al. GLP-1 slows solid gastric emptying and inhibits insulin, glucagon, and PYY release in humans. Am J Physiol. 1999;277:R910-R916.
19. Naslund E, Bogefors J, Gryback P, et al. GLP-1 inhibits gastric emptying of water but does not influence plasma. Scand J Gastroenterol. 2001;36:156-162.
20. Jodka C, Gedulin BR, Young AA. Exendin-4 potently stimulates gastric emptying in rats [abstract]. Diabetes. 1998;47:A403.
21. Marathe PH, Wen Y, Norton J, Greene DS, Barbhaiya RH, Wilding IR. Effect of altered gastric emptying and gastrointestinal motility on metformin absorption. Br J Clin Pharmacol. 2000;50:325-332.
22. Sanchez J, Martinez L, Garcia-Barbal J, Roser R, Bartlett A, Sagarra R. The influence of gastric emptying on droxicam pharmacokinetics. J Clin Pharmacol. 1989;29:739-745.
23. Bateman DN. The action of cisapride on gastric emptying and the pharmacodynamics and pharmacokinetics of oral diazepam. Eur J Clin Pharmacol. 1986;30:205-208.
24. Riley SA, Sutcliffe F, Kim M, Kapas M, Rowland M, Turnberg LA. The influence of gastrointestinal transit on drug absorption in healthy volunteers. Br J Clin Pharmacol. 1992;34:32-39.
25. Gandia P, Bareille MP, Saivin S, et al. Influence of simulated weightlessness on the oral pharmacokinetics of acetaminophen as a gastric emptying probe in man: a plasma and a saliva study. J Clin Pharmacol. 2003;43:1235-1243.
26. Naslund E, Bogefors J, Gryback P, Jacobsson H, Hellstrom PM. Gastric emptying: comparison of scintigraphic, polyethylene glycol dilution, and paracetamol tracer assessment techniques. Scand J Gastroenterol. 2000;35:375-379.
27. Declaration of Helsinki: recommendations guiding medical physicians in biomedical research involving human subjects. JAMA. 1997;277:925-926.
28. Forrest, JA, Clements, JA, Prescott LF. Clinical pharmacokinetics of paracetamol. Clin Pharmacokinet. 1982;7:93-107.
29. Horowitz M, Edelbroek MA, Wishart JM, Straathof JW. Relationship between oral glucose tolerance and gastric emptying in normal healthy subjects. Diabetologia. 1993;36:857-862.
30. Mourot J, Thouvenot P, Couet C, Antoine JM, Krobicka A, Debry G. Relationship between the rate of gastric emptying and glucose and insulin responses to starchy foods in young healthy adults. Am J Clin Nutr. 1988;48:1035-1040.
31. Horowitz M, O'Donovan D, Jones KL, Feinle C, Rayner CK, Samsom M. Gastric emptying in diabetes: clinical significance and treatment. Diabetic Med. 2002;19:177-194.
32. Schvarcz E, Palmer M, Aman J, Horowitz M, Stridsberg M, Berne C. Physiological hyperglycemia slows gastric emptying in normal subjects and patients with insulin-dependent diabetes mellitus. Gastroenterology. 1997;113:60-66.
33. Kong MF, Macdonald IA, Tattersall RB. Gastric emptying in diabetes. Diabetic Med. 1996;13:112-119.
34. Horowitz M, Maddox AF, Wishart JM, Harding PE, Chatterton BE, Shearman DJ. Relationships between oesophageal transit and solid and liquid gastric emptying in diabetes mellitus. Eur J Nucl Med. 1991;18:229-234.
35. Horowitz M, Harding PE, Maddox AF, et al. Gastric and oesophageal emptying in patients with type 2 (non-insulin-dependent) diabetes mellitus. Diabetologia. 1989;32:151-159.
36. Keshavarzian A, Iber FL, Vaeth J. Gastric emptying in patients with insulin-requiring diabetes mellitus. Am J Gastroenterol. 1987;82:29-35.
37. Wegener M, Borsch G, Schaffstein J, Luerweg C, Leverkus F. Gastrointestinal transit disorders in patients with insulin-treated diabetes mellitus. Dig Dis. 1990;8:23-36.
38. Lyrenas EB, Olsson EH, Arvidsson UC, Orn TJ, Spjuth JH. Prevalence and determinants of solid and liquid gastric emptying in unstable type I diabetes: relationship to postprandial blood glucose concentrations. Diabetes Care. 1997;20:413-418.
39. Nowak TV, Johnson CP, Kalbfleisch JH, et al. Highly variable gastric emptying in patients with insulin dependent diabetes mellitus. Gut. 1995;37:23-29.
40. Kong MF, Horowitz M. Gastric emptying in diabetes mellitus: relationship to blood-glucose control. Clin Geriatr Med. 1999;15:321-338.
41. Greiff JM, Rowbotham D. Pharmacokinetic drug interactions with gastrointestinal motility modifying agents. Clin Pharmacokinet. 1994;27:447-461.
42. Janssens J, Peeters TL, Vantrappen G, et al. Improvement of gastric emptying in diabetic gastroparesis by erythromycin: preliminary studies. N Engl J Med. 1990;322:1028-1031.
43. Gonlachanvit S, Hsu C-W, Boden GH, et al. Effect of altering gastric emptying on postprandial plasma glucose concentrations following a physiologic meal in type-II diabetic patients. Dig Dis Sci. 2003;48:488-497.
44. Phillips WT, Schwartz JG, McMahan CA. Reduced postprandial blood glucose levels in recently diagnosed non-insulin-dependent diabetics secondary to pharmacologically induced delayed gastric emptying. Dig Dis Sci. 1993;38:51-58.
45. Chaudhuri TK, Fink S. Update: pharmaceuticals and gastric emptying. Am J Gastroenterol. 1990;85:223-230.
46. Soon D, Linnebjerg H, Chan C, et al. Effect of exenatide on digoxin pharmacokinetics. Clin Exp Pharmacol Physiol, 2004;31:A65.
47. Kolterman OG, Kim D, Shen L, Ruggles JA, Nielsen LL, Fineman MS. Pharmacokinetics, pharmacodynamics, and safety of a range of subcutaneous exenatide in patients with type 2 diabetes mellitus. Am J Health-Sys Pharmacy. 2005;15:173-181.