Granisetron: Relating pharmacology to clinical efficacy

Supportive Care in Cancer

Volumn 11, Issue 2, 2003, Pages 93-100

  Blower, Peter R ^a  

^a Poole House   (United Kingdom)

Author keywords

5 HT3 receptor antagonist; Antiemetic; Chemotherapy; Emesis; Granisetron

Indexed keywords

ANTIEMETIC AGENT; ANTINEOPLASTIC AGENT; CISPLATIN; DOLASETRON MESILATE; GRANISETRON; METOCLOPRAMIDE; ONDANSETRON; SEROTONIN 3 ANTAGONIST;

AREA UNDER THE CURVE; BINDING AFFINITY; CANCER CHEMOTHERAPY; CANCER RADIOTHERAPY; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG TOLERABILITY; EXTRAPYRAMIDAL SYMPTOM; HUMAN; PRIORITY JOURNAL; PROPHYLAXIS; REVIEW; SIDE EFFECT; STANDARD; VERTIGO; VISUAL DISORDER; VOMITING; DRUG INTERACTION; NEOPLASM; RADIOTHERAPY;

ANTIEMETICS; ANTINEOPLASTIC AGENTS; DRUG INTERACTIONS; GRANISETRON; HUMANS; NEOPLASMS; RADIOTHERAPY; VOMITING;

EID: 0038412560     PISSN: 09414355     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00520-002-0410-z     Document Type: Review

References (81)

1. Addelman M, Erlichman C, Fine S, Warr D, Murray C (1990) Phase I/II trial of granisetron: a novel 5-hydroxytryptamine antagonist for the prevention of chemotherapy-induced nausea and vomiting. J Clin Oncol 8:337-341
2. Andrews PLR, Rapeport WG, Sanger GJ (1988) Neuropharmacology of emesis induced by anti-cancer therapy. Trends Pharmacol Sci 9:334-341
3. Andrews PLR (1992) Physiology of nausea and vomiting. Br J Anaesthesia 69 [Suppl 1]:2-19S
4. ASHP (1999) Therapeutic guidelines on the pharmacologic management of nausea and vomiting in adult and pediatric patients receiving chemotherapy or radiation therapy or undergoing surgery. Am J Health Syst Pharm 56:729-764
5. Audhuy B, Cappelaere P, Martin M, et al (1996) A double-blind, randomised comparison of the anti-emetic efficacy of two intravenous doses of dolasetron mesilate and granisetron in patients receiving high dose cisplatin chemotherapy. Eur J Cancer [A] 32:807-813
6. Balfour JA, Goa KL (1997) Dolasetron. A review of its pharmacology and therapeutic potential in the management of nausea and vomiting induced by chemotherapy, radiotherapy or surgery. Drugs 54:273-298
7. Beck TM, Hesketh PJ, Madajewicz S, et al (1992) Stratified, randomized, double-blind comparison of intravenous ondansetron administered as a multiple-dose regimen versus two single-dose regimens in the prevention of cisplatin-induced nausea and vomiting. J Clin Oncol 10:1969-1975
8. Blake JC, Palmer JL, Minton NA, Burroughs AK (1993) The pharmacokinetics of intravenous ondansetron in patients with hepatic impairment. Br J Clin Pharmacol 35:441-443
9. Bleiberg HH, Spielmann M, Falkson G, Romain D (1995) Antiemetic treatment with oral granisetron in patients receiving moderately emetogenic chemotherapy: a dose-ranging study. Clin Ther 17:38-51
10. Bloomer JC, Baldwin SJ, Smith GJ, Ayrton AD, Clarke SE, Chenery RJ (1994) Characterisation of the cytochrome P450 enzymes involved in the in vitro metabolism of granisetron. Br J Clin Pharmacol 38:557-566
11. 3 receptor antagonism in the control of cytostatic drug-induced emesis. Eur J Cancer 26 [Suppl 1]:S8-11
12. Blower P (1995) A pharmacologic profile of oral granisetron (Kytril tablets). Semin Oncol 22 [Suppl 10]:3-5
13. Blower P, Aapro M (2002) Granisetron vs ondansetron: is it a question of duration of receptor blockade? Br J Cancer 86:1665-1666
14. Boike SC, Ilson B, Zariffa N, Jorkasky DK (1997) Cardiovascular effects of i.v. granisetron at two administration rates and of ondansetron in healthy adults. Am J Health Syst Pharm 54:1172-1176
15. Boxenbaum H, Gillespie T, Heck K, Hahne W (1992) Human dolasetron pharmacokinetics. I. Disposition following single-dose intravenous administration to normal male subjects. Biopharm Drug Dispos 13:693-701
16. Boxenbaum H, Gillespie T, Heck K, Hahne W (1993) Human dolasetron pharmacokinetics: II Absorption and disposition following single-dose oral administration to normal male subjects. Biopharm Drug Dispos 14:131-141
17. Cagnoni PJ, Matthes S, Day TC, Bearman SI, Shpall EJ, Jones RB (1999) Modification of the pharmacokinetics of high-dose cyclophosphamide and cisplatin by antiemetics. Bone Marrow Transplant 24:1-4
18. 3 receptor antagonist: correlation with antiemetic response. Cancer Chemother Pharmacol 24:45-49
19. Carmichael J, Philip PA, Forfar C, Harris AL (1995) An open study to assess the safety, tolerance and pharmacokinetics of an intravenous infusion of granisetron given at 3 mg over 30 s in patients receiving chemotherapy for malignant disease. Cancer Chemother Pharmacol 37:134-138
20. Carmichael J, Keizer HJ, Cupissol D, Milliez J, Scheidel P, Schindler AE (1998) Use of granisetron in patients refractory to previous treatment with antiemetics. Anticancer Drugs 9:381-385
21. 14C-granisetron in rat, dog and man after intravenous and oral dosing. Xenobiotica 24:1119-1131
22. de Wit R, de Boer A, van de Linden G, Stoter G, Sparreboom A, Verweij J (2001) Effective crossover to granisetron after failure to ondansetron, a randomized double blind study in patients failing ondansetron plus dexamethasone during the first 24 hours following highly emetogenic chemotherapy. Br J Cancer 85:1099-1101
23. Dixon CM, Colthup PV, Serabjit-Singh CJ, et al (1995) Multiple forms of cytochrome P450 are involved in the metabolism of ondansetron in humans. Drug Metab Dispos 23:1225-1230
24. Doherty KM (1999) Closing the gap in prophylactic antiemetic therapy: patient factors in calculating the emetogenic potential of chemotherapy. Clin J Oncol Nurs 3:113-119
25. Elliott P, Seemungal BM, Wallis DI (1990) Antagonism of the effects of 5-hydroxytryptamine on the isolated rabbit vagal nerve by BRL 43694 and metoclopramide. Naunyn Schmiedebergs Arch Pharmacol 341:503-509
26. Endo T, Takahashi M, Minami M, Yoshioka M, Saito H, Parvez SH (1993) Effects of anticancer drugs on enzyme activities and serotonin release from ileal tissue in ferrets. Biogenic Amines 9:479-489
27. 3-receptor antagonist, inhibited cisplatin-induced 5-hydroxytryptamine release in the isolated ileum of ferrets. Res Commun Mol Pathol Pharmacol 100:243-253
28. Fauser AA, Duclos B, Chemaissani A, et al (1996) Therapeutic equivalence of single oral doses of dolasetron mesilate and multiple doses of ondansetron for the prevention of emesis after moderately emetogenic chemotherapy. European Dolasetron Comparative Study Group. Eur J Cancer [A] 32:1523-1529
29. Figg WD, Dukes GE, Pritchard JF, et al (1996) Pharmacokinetics of ondansetron in patients with hepatic insufficiency. J Clin Pharmacol 36:206-215
30. 3 receptor mediate cisplatin-induced emesis in dogs (abstract). Jpn J Pharmacol 55 [Suppl 1]:152P
31. Gandara DR, Roila F, Warr D, Edelman MJ, Perez EA, Gralla RJ (1998) Consensus proposal for 5-HT3 antagonists in the prevention of acute emesis related to highly emetogenic chemotherapy. Dose, schedule, and route of administration. Support Care Cancer 6:237-243
32. 4 receptors of the release of 5-hydroxytryptamine from the guinea-pig small intestine. Naunyn Schmiedebergs Arch Pharmacol 347:137-140
33. Gilbert CJ, Petros WP, Vredenburgh J, et al (1998) Pharmacokinetic interaction between ondansetron and cycle-phosphamide during high-dose chemotherapy for breast cancer. Cancer Chemother Pharmacol 42:497-503
34. Glaxo Wellcome Inc (1999) Zofran (ondansetron hydrochloride) tablets and injection. Prescribing information. Glaxo Wellcome, Research Triangle Park, NC
35. Graczyk SG, McKenzie R, Kallar S et al (1997) Intravenous dolasetron for the prevention of postoperative nausea and vomiting after outpatient laparoscopic gynecologic surgery. Anesth Analg 84:325-330
36. Gralla RJ, Navari RM, Hesketh PJ, et al (1998) Single-dose oral granisetron has equivalent antiemetic efficacy to intravenous ondansetron for highly emetogenic cisplatin-based chemotherapy. J Clin Oncol 16:1568-1573
37. Gralla RJ, Osoba D, Kris MG et al (1999) Recommendations for the use of antiemetics: evidence-based, clinical practice guidelines. An ASCO special article. J Clin Oncol 17:2971-2994
38. Gray GW, McLellan TM, Ducharme MB (1996) Granisetron shows no proarrhythmic effect in normal subjects during or after exercise in a hot environment. Aviat Space Environ Med 67:759-761
39. Gupta YK, Bhandari P, Dhar A, Seth SD. Effect of BRL 43694, a novel 5-HT-M receptor antagonist, on cisplatin-induced emesis in dogs and gastric stasis in rats. Symposium on Nausea and Vomiting: A Multidisciplinary Perspective, 8 November 1988, Ottawa, Canada, abstract 13
40. Hacking A (1992) Oral granisetron - simple and effective: a preliminary report. Eur J Cancer [A] 28 [Suppl 1]: S28-32
41. Hesketh P, Navari R, Grote T, et al (1997) Double-blind, randomized comparison of the antiemetic efficacy of intravenous dolasetron mesylate and intravenous ondansetron in the prevention of acute cisplatin-induced emesis in patients with cancer. J Clin Oncol 14:2242-2249
42. Hesketh PJ, Crews JR, Cohen R, Blackburn LM, Friedman CJ (2000) Antiemetic efficacy of single-dose oral granisetron (1 mg vs 2 mg) with moderately emetogenic chemotherapy. Cancer J 6:157-1561
43. 3 receptor antagonists injected into the area postrema inhibit cisplatin-induced emesis in the ferret. Br J Pharmacol 97:247-255
44. Hoechst Marion Roussel Inc (1999) Anzemet® (dolasetron mesylate) tablets and injection. Prescribing information. Hoechst Marion Roussel, Kansas City, Mo
45. 3 receptor antagonists in the prophylaxis of acute vomiting induced by moderately emetogenic chemotherapy - a randomised study. Eur J Cancer 12:1669-1672
46. Jantunen IT, Kataja VV, Muhonen TT, Parviainen T (1996) Effects of granisetron with doxorubicin or epirubicin on ECG intervals. Cancer Chemother Pharmacol 37:502-504
47. Koeller JM, Aapro MS, Gralla RJ, et al (2002) Antiemetic guidelines: creating a more practical treatment approach. Support Care Cancer DOI 10.1007/s00520-001-0335-y
48. Kuryshev YA, Brown AM, Wang L, Benedict CR, Rampe D (2000) Interactions of the 5-hydroxytryptamine 3 antagonist class of antiemetic drugs with human cardiac ion channels. J Pharmacol Exp Ther 295:614-620
49. 3 receptor antagonist. Anesth Analg 72:751-755
50. Lindley C, Blower P (2000) Oral serotonin type 3-receptor antagonists for prevention of chemotherapy-induced emesis. Am J Health Syst Pharm 57:1685-1697
51. Lofters WS, Peter JL, Zee B, et al (1997) Phase III double-blind comparison of dolasetron mesylate and ondansetron and an evaluation of the additive role of dexamethasone in the prevention of acute and delayed nausea and vomiting due to moderately emetogenic chemotherapy. J Clin Oncol 15:2966-2973
52. Markman M, Kennedy A, Webster K, Kulp B, Peterson G, Belinson J (1998) Low-dose oral granisetron (1 mg) plus intravenous dexamethasone: efficacy in gynecologic cancer patients receiving carboplatin-based chemotherapy. Gynecol Oncol 71:113-115
53. Marr HE, Davey PT, Boyle EA, Blower PR (1994) Further studies of the antiemetic activity of granisetron against whole body X-irradiation or cisplatin-induced emesis in the ferret. Pharmacology 48:283-292
54. Martin JK, Senecal FM, Baker TM, et al (1997) Single-dose 1 mg oral granisetron (G) is less costly and as effective as intravenous ondansetron in controlling nausea (N) and vomiting (V) from moderately emetogenic chemotherapy. Proc ASCO 16:76a (abstract 262)
55. Mendarte L, Aguas Compaired M, Martinez Bernabe E, Odena Estrade E, Rodriguez Palomar G (2000) Metaanalysis of granisetron versus ondansetron: efficacy and safety in the prevention of acute emesis induced by high dose cisplatin containing schedules. Med Clin (Barc) 115:456-460
56. 3-receptor antagonists. Br J Clin Pharmacol 37:525-530
57. Navari R, Gandara D, Hesketh P, et al (1995) Comparative clinical trial of granisetron and ondansetron in the prophylaxis of cisplatin-induced emesis. J Clin Oncol 13:1242-1248
58. Navari RM. Kaplan HG, Gralla RJ, Grunberg SM, Palmer R, Fitts D (1994) Efficacy and safety of granisetron, a selective 5-hydroxytryptamine-3 receptor antagonist, in the prevention of nausea and vomiting induced by high-dose cisplatin. J Clin Oncol 12:2204-2210
59. 3 binding sites in rat brain cortical membranes. Biochem Pharmacol 38:1693-1695
60. 3 receptors. Neuropharmacology 32:729-735
61. Palmer R (1994) Efficacy and safety of granisetron (Kytril) in two special patient populations: children and adults with impaired hepatic function. Semin Oncol 21 [Suppl 5]:22-25
62. Perez EA (1995) Review of the preclinical pharmacology and comparative efficacy of 5-hydroxytryptamine-3 receptor antagonists for chemotherapy-induced emesis. J Clin Oncol 13:1036-1043
63. Perez EA (1996) Comparative efficacy of oral and intravenous granisetron for the prevention of acute chemotherapy-induced emesis. Clin Ther 18:578-590
64. Perez EA, Hesketh P, Sandbach J, et al (1998) Comparison of single-dose oral granisetron versus intravenous ondansetron in the prevention of nausea and vomiting induced by moderately emetogenic chemotherapy: a multicenter, double-blind, randomized parallel study. J Clin Oncol 16:754-760
65. Perez EA, Lembersky B, Kaywin P, Kalman L, Yocom K, Friedman C (1998) Comparable safety and antiemetic efficacy of a brief (30-second bolus) intravenous granisetron infusion and a standard (15-minute) intravenous ondansetron infusion in breast cancer patients receiving moderately emetogenic chemotherapy. Cancer J Sci Am 4:52-58
66. Riviere A on behalf of the Granisetron Study Group (1994) Dose-finding study of granisetron in patients receiving high-dose cisplatin chemotherapy. Br J Cancer 69:967-971
67. Roche Laboratories Inc (2000) Kytril® (granisetron hydrochloride) tablets and injection. Prescribing information. Roche Laboratories, Nutley, NJ
68. Roila F, Del Favero A (1995) Ondansetron clinical pharmacokinetics. Clin Pharmacokinet 29:95-109
69. Rubenstein EB, Gralla RJ, Hainsworth JD, et al (1997) Randomized, double blind, dose-response trial across four oral doses of dolasetron for the prevention of acute emesis after moderately emetogenic chemotherapy. Oral Dolasetron Dose-Response Study Group. Cancer 76:1216-1224
70. 3 receptor antagonists (setrons) for chemotherapy-induced emesis. Pharmacoeconomics 18:533-556
71. 3 antagonists. Drug Metab Dispos 24:602-609
72. Seynaeve C, Schuller J, Buser K, et al (1992) Comparison of the antiemetic efficacy of different doses of ondansetron, given as either a continuous infusion or a single intravenous dose, in acute cisplatin-induced emesis. A multicentre, double-blind, randomised, parallel group study. Ondansetron Study Group. Br J Cancer 66:192-197
73. Scarantino CW, Ornitz RD, Hoffman LG, Anderson RF (1994) On the mechanism of radiation-induced emesis: the role of serotonin. Int J Radiat Oncol Biol Phys 30:825-830
74. Shah A, Lanman R, Bhargava V, Weir S, Hahne W (1995) Pharmacokinetics of dolasetron following single- and multiple-dose intravenous administration to normal male subjects. Biopharm Drug Dispos 16:177-189
75. Spitzer TR, Friedman CJ, Bushnell W, Frankel SR, Raschko J (2000) Double-blind, randomized, parallel-group study on the efficacy and safety of oral granisetron and oral ondansetron in the prophylaxis of nausea and vomiting in patients receiving hyperfractionated total body irradiation. Bone Marrow Transplant 26:203-210
76. Terrey J-P, Aapro MS (1996) The activity of granisetron in patients who had previously failed ondansetron antiemetic therapy. Eur J Clin Res 8:281-288
77. Tyers MB, Bunce KT, Humphrey PP (1989) Pharmacological and anti-emetic properties of ondansetron. Eur J Cancer Clin Oncol 25 [Suppl 1]:S15-19
78. 3 antagonist. Eur J Cancer 26 [Suppl 1]:S12-15
79. Van Wijngaarden I, Tulp MTM, Soudijn W (1990) The concept of selectivity in 5-HT receptor research. Eur J Pharmacol 188:301-312
80. Wilde MJ, Markham A. Ondansetron (1996) A review of its pharmacology and preliminary clinical findings in novel applications. Drugs 52:773-794
81. Wilson AJ, Diemunsch P, Lindeque BG et al (1996) Single-dose i.v. granisetron in the prevention of postoperative nausea and vomiting. Br J Anaesth 76:515-518