Influence of simulated weightlessness on the intramuscular and oral pharmacokinetics of promethazine in 12 human volunteers

Journal of Clinical Pharmacology

Volumn 46, Issue 9, 2006, Pages 1008-1016

  Gandia, Peggy ^a   Saivin, Sylvie ^a   Le Traon, Anne Pavy ^b   Guell, Antonio ^b   Houin, Georges ^a  

^a CHU PURPAN   (France)

^b CHU RANGUEIL   (France)

Author keywords

Bed rest; Pharmacokinetics; Promethazine; Weightlessness

Indexed keywords

PROMETHAZINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; BED REST; BIOEQUIVALENCE; BODY POSITION; BRADYCARDIA; DRUG BLOOD LEVEL; HUMAN; HYPOTENSION; INTESTINE TRANSIT TIME; INTESTINE WALL; LIPOTHYMIC SENSATION; MALE; MEASUREMENT; MOBILIZATION; MOTION SICKNESS; NEUROTOXICITY; NORMAL HUMAN; SIDE EFFECT; SIMULATION; SPACE FLIGHT; TACHYCARDIA; VOLUNTEER; WEIGHTLESSNESS;

ADMINISTRATION, ORAL; ADULT; HUMANS; INJECTIONS, INTRAMUSCULAR; MALE; PROMETHAZINE; WEIGHTLESSNESS SIMULATION;

EID: 33747050908     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270006291032     Document Type: Article

References (73)

1. Davis JR, Jennings RT, Beck BG. Comparison of treatment strategies for Space Motion Sickness. Microgravity Q. 1992;2:173-177.
2. Oman CM. Spacelab experiments on space motion sickness. Acta Astronaut. 1987;15:55-66.
3. Davis JR, Vanderploeg JM, Santy PA, Jennings RT, Stewart DF. Space motion sickness during 24 flights of the space shuttle. Aviat Space Environ Med. 1988;59:1185-1189.
4. Bagian JP. First intramuscular administration in the U.S. Space Program. J Clin Pharmacol. 1991;31:920.
5. Graybiel A, Lackner JR. Treatment of severe motion sickness with antimotion sickness drug injections. Aviat Space Environ Med. 1987;58:773-776.
6. Hordinsky JR, Schwartz E, Beier J, Martin J, Aust G. Relative efficacy of the proposed Space Shuttle antimotion sickness medications. Acta Astronaut. 1982;9:375-383.
7. Graybiel A, Wood CD, Miller EF, Cramer DB. Diagnostic criteria for grading the severity of acute motion sickness. Aerosp Med. 1968;39:453-455.
8. Graybiel A. Coping with space motion sickness in Spacelab missions. Acta Astronaut. 1981;8:1015-1018.
9. Kakurin LI, Lobachik VI, Mikhailov M, Senkevich YA. Antiorthostatic hypokinesia as a method of weightlessness simulation. Aviat Space Environ Med. 1976;47:1083-1086.
10. Nixon JV, Gordon Murray R, Bryant C, et al. Early cardiovascular adaptation to simulated zero gravity. J Appl Physiol. 1979;46:541-548.
11. Gaffney FA, Nixon JW, Karlsson ES, Campbell W, Dowdey ABC, Blomqvist CG. Cardiovascular deconditioning produced by 20 hours of bedrest with head-down tilt (-5°) in middle-aged healthy men. Am J Cardiol. 1985;56:634-638.
12. Dictionnaire Vidal. Paris, France: Vidal; 2000.
13. Ramanathan R, Geary RS, Bourne DW, Putcha L. Bioavailability of intranasal promethazine dosage forms in dogs. Pharmacol Res. 1998;38:35-39.
14. DiGregorio GJ, Ruch E. Human whole blood and parotid saliva concentrations of oral and intramuscular promethazine. J Pharm Sci. 1980;69:1457-1459.
15. Shah VP, Midha KK, Findlay JW, et al. Bioanalytical method validation - a revisit with a decade of progress. Pharm Res. 2000;17:1551-1557.
16. Rowland M, Tozer TN. Clinical Pharmacokinetics: Concepts and Applications. Philadelphia, Pa: Lea and Fehiger; 1980.
17. Lellouch J, Lazar P. Méthodes statistiques en expé rimentation biologique. Paris, France: Flammarion; 1996.
18. Zaman R, Honigherg IL, Francisco GE, et al. Bioequivalency and dose proportionality of three tahleted promethazine products. Biopharm Drug Dispos. 1986;7:281-291.
19. Koytchev R, Alken RG, Kirkov V, Neshev G, Vagaday M, Kunter U. Absolute bioavailability of chlorpromazine, promazine and promethazine. Arzneimittelforschung. 1994;44:121-125.
20. Paton DM, Webster DR. Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet. 1985;10:477-497.
21. Saivin S, Pavy-Le Traon A, Cornac A, Guell A, Houin G. Impact of a four-day head-down tilt (-6 degrees) on lidocaine pharmacokinetics used as probe to evaluate hepatic blood flow. J Clin Pharmacol. 1995;35:697-704.
22. Cheymol G, Jaillon P. The effect of cardiac insufficiency on pharmacokinetics. Archives des maladies du coeur et des Vaisseaux. 1989;82:391-397.
23. Blyden G, Silverstein F, Epstein M, et al. Lidocaine pharmacokinetics during water immersion in normal humans. J Appl Physiol. 1989;66:57-60.
24. Richard C, Berdeaux A, Delion F, et al. Effect of mechanical ventilation on hepatic drug pharmacokinetics. Chest. 1986;90:837-841.
25. Montgomery LD. Body volume changes during simulated microgravity, II: comparison of horizontal and head-down bed rest. Aviat Space Environ Med. 1993;64:899-904.
26. Thornton WE, Hedge V, Coleman E, Uri JJ, Moore TP. Changes in leg volume during microgravity simulation. Aviat Space Environ Med. 1992;63:789-794.
27. Leach CS, Inners LD, Charles JB. Changes in total body water during spaceflight. J Clin Pharmacol. 1991;31:1001-1006.
28. Montastruc J-L, Senard J-M, Verwaerde P, Montastruc P. Mécanismes physiologiques de l'adaptation cardiovasculaire à l'orthostatisme. Therapie. 1994;49:81-87.
29. Drummer C, Hesse C, Baisch F, et al. Water and sodium balances and their relation to body mass changes in microgravity. Eur J Clin Invest. 2000;30:1066-1075.
30. Norsk P, Epstein M. Manned space flights and the kidney. Am J Nephrol. 1991;11:81-97.
31. Ertl AC, Diedrich A, Biaggioni I, et al. Human muscle sympathetic nerve activity and plasma noradrenaline kinetics in space. J Physiol. 2002;538:321-329.
32. Houin G. Pharmacocinetique. Paris, France: Ellipse; 1990.
33. 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.
34. Petring OU, Flachs H. Inter- and intrasubject variability of gastric emptying in healthy volunteers measured by scintigraphy and paracetamol absorption. Br J Pharmacol. 1990;29:703-708.
35. Heading RC, Nimmo J, Prescott LF, Tothill P. The dependence of paracetamol absorption on the rate of gastric emptying. Br J Pharmacol. 1973;47:415-421.
36. Sanaka M, Koike Y, Yamamoto T, et al. A reliable and convenient parameter of the rate of paracetamol absorption to measure gastric emptying rate of liquids. Int J Clin Pharmacol Ther. 1997;35:509-513.
37. Sanaka M, Kuyama Y, Nishinakagawa S, Mineshita S. Use of salivary acetaminophen concentration to assess gastric emptying rate of liquids. J Gastroenterol. 2000;35:429-433.
38. Doherty TJ, Andrews FM, Provenza MK, Frazier DL. Acetaminophen as a marker of gastric emptying in ponies. Equine Vet J. 1998;30:349-351.
39. Lohmann KL, Roussel AJ, Cohen ND, Boothe DM, Rakestraw PC, Walker MA. Comparison of nuclear scintigraphy and acetaminophen absorption as a means of studying gastric emptying in horses. Am J Vet Res. 2000;61:310-315.
40. Renwick AG, Ahsan CH, Challenor VF, et al. The influence of posture on the pharmacokinetics of orally administered nifedipine. Br J Clin Pharmacol. 1992;34:332-336.
41. Backon J, Hoffman A. The lateral decubitus position may affect gastric emptying through an autonomic mechanism: the skin pressure-vegetative reflex. Br J Clin Pharmacol. 1991;32:138-139.
42. Anvari M, Horowitz M, Fraser R, et al. Effects of posture on gastric emptying of non-nutrient liquids and antropyloroduodenal motility. Am J Physiol. 1995;268:G868-G871.
43. Villanueva-Meyer J, Swischuk LE, Cesani F, Ali SA, Briscoe E. Pediatric gastric emptying: value of right lateral and upright positioning. J Nucl Med. 1996;37:1356-1358.
44. Lathers CM, Charles JB, Bungo MW. Humans in space: NASA's contributions to medical technology and health care. J Clin Pharmacol. 1990;30:223-225.
45. Mulvagh SL, Charles JB, Riddle JM, Rehhein TL, Bungo MW. Echographic evaluation of the cardiovascular effects of shortduration spaceflight. J Clin Pharmacol. 1991;31:1024-1026.
46. Bassett Frey MA, Tomaselli CM, Hoffler WG. Cardiovascular responses to postural changes: differences with age for women and men. J Clin Pharmacol. 1994;34:394-402.
47. Smith JJ, Porth CM, Erickson M. Hemodynamic response to the upright posture. J Clin Pharmacol. 1994;34:375-386.
48. Lathers CM, Diamandis PH, Riddle JM, et al. Acute and intermediate cardiovascular responses to zero gravity and to fractional gravity levels induced by head-down or head-up tilt. J Clin Pharmacol. 1990;30:494-523.
49. Lathers CM, Riddle JM, Mulvagh SL, et al. Echocardiograms during six hours of bedrest at head-down and head-up tilt and during space flight. J Clin Pharmacol. 1993;33:535-543.
50. Lathers CM, Charles JB, Bungo MW. Pharmacology in space, I: influence of adaptive changes on pharmacokinetics. Trends Pharmacol Sci. 1989;10:193-200.
51. Lathers CM, Diamandis PH, Riddle JM, et al. Orthostatic function during a stand test before and after head-up or head-down bed-rest. J Clin Pharmacol. 1991;31:893-903.
52. Rawlins MD, Henderson DB, Hijab AR. Pharmacokinetics of paracetamol (acetaminophen) after intravenous and oral administration. Eur J Clin Pharmacol. 1977;11:283-286.
53. Bagnall WE, Kelleher J, Walker BE, Losowsky MS. The gastrointestinal absorption of paracetamol in the rat. J Pharm Pharmacol. 1979;31:157-160.
54. von Richter O, Burk O, Fromm MF, Thon KP, Eichelbaum M, Kivisto KT. Cytochrome P450 3A4 and P-glycoprotein expression in human small intestinal enterocytes and hepatocytes: a comparative analysis in paired tissue specimens. Clin Pharmacol Ther. 2004;75:172-183.
55. Yang J, Tucker GT, Rostami-Hodjegan A. Cytochrome P450 3A expression and activity in the human small intestine. Clin Pharmacol Ther. 2004;76:391.
56. Kharasch ED, Hoffer C, Whittington D, Sheffels P. Role of hepatic and intestinal cytochrome P450 3A and 2B6 in the metabolism, disposition, and miotic effects of methadone. Clin Pharmacol Ther. 2004;76:250-269.
57. Tietze KJ, Putcha L. Factors affecting drug bioavailability in space. J Clin Pharmacol. 1994;34:671-676.
58. Grybäck P, Jacobsson H, Blomquist L, Schnell PO, Hellström P. Scintigraphy of the small intestine: a simplified standard for study of transit with reference to normal values. Eur J Nucl Med. 2002;29:39-45.
59. Rao KA, Yazaki E, Evans DF, Carbon R. Objective evaluation of small bowel and colonic transit time using pH telemetry in athletes with gastrointestinal symptoms. Br J Sports Med. 2004;38:482-487.
60. Brun B, Hegedus V. Radiography of the small intestine with large amounts of cold contrast medium. Acta Radiol Diagn (Stockh). 1980;21:65-70.
61. Hu Z, Mawatari S, Shibata N, et al. Application of a biomagnetic measurement system (BMS) to the evaluation of gastrointestinal transit of intestinal pressure-controlled colon delivery capsules (PCDCs) in human subjects. Pharm Res. 2000;17:160-167.
62. Dainese R, Serra J, Azpiroz F, Malagelada JR. Influence of body posture on intestinal transit of gas. Gut. 2003;52:971-974.
63. Jonmarker C, Castor R, Drefeldt B, Werner O. An analyzer for in-line measurement of expiratory sulfur hexafluoride concentration. Anesthesiology. 1985;63:84-88.
64. Miller MA, Parkman HP, Urbain JL, et al. Comparison of scintigraphy and lactulose breath hydrogen test for assessment of orocecal transit: lactulose accelerates small bowel transit. Dig Dis Sci. 1997;42:10-18.
65. Saitoh H, Hasegawa N, Kawai S, Miyazaki K, Arita T. Interaction of tertiary amines and quaternary ammonium compounds with gastrointestinal mucin. J Pharmacobiodyn. 1986;9:1008-1014.
66. Santy PA, Bungo MW. Pharmacologic considerations for Shuttle astronauts. J Clin Pharmacol. 1991;31:931-933.
67. Bagian JP, Ward DF. A retrospective study of promethazine and its failure to produce the expected incidence of sedation during space flight. J Clin Pharmacol. 1994;34:649-651.
68. Wood CD, Manno JE, Manno BR, Redetzki HM, Wood MJ, Mims ME. Evaluation of antimotion sickness drug side effects on performance. Aviat Space Environ Med. 1985;56:310-316.
69. Keats AS, Telford J, Kurosu Y. "Potentiation" of meperidine by promethazine. Anesthesiology. 1961;22:34-41.
70. Eckberg DL. Bursting into space: alterations of sympathetic control by space travel. Acta Physiol Scand. 2003;177:299-311.
71. Macho L, Koska J, Ksinantova L, et al. The response of endocrine system to stress loads during space flight in human subject. Adv Drug Res. 2003;31:1605-1610.
72. Schwinghammer TL, Juhl RP, Dittert LW, Melethil SK, Kroboth FJ, Chung VS. Comparison of the bioavailability of oral, rectal and intramuscular promethazine. Biopharm Drug Dispos. 1984;5:185-194.
73. Taylor G, Houston JB, Shaffer J, Mawer G. Pharmacokinetics of promethazine and its sulphoxide metabolite after intravenous and oral administration to man. Br J Clin Pharmacol. 1983;15:287-293.