Brain histamine H1 receptor occupancy of orally administered antihistamines measured by positron emission tomography with 11 C-doxepin in a placebo-controlled crossover study design in healthy subjects: A comparison of olopatadine and ketotifen

British Journal of Clinical Pharmacology

Volumn 61, Issue 1, 2006, Pages 16-26

  Tashiro, Manabu ^a,c   Mochizuki, Hideki ^a   Sakurada, Yumiko ^a   Ishii, Kenji ^b   Oda, Keiichi ^b   Kimura, Yuichi ^b   Sasaki, Toru ^b   Ishiwata, Kiichi ^b   Yanai, Kazuhiko ^a  

^a TOHOKU UNIVERSITY GRADUATE SCHOOL OF MEDICINE   (Japan)

^b TOKYO METROPOLITAN INSTITUTE OF GERONTOLOGY   (Japan)

^c TOHOKU UNIVERSITY   (Japan)

Author keywords

First generation antihistamine; Histamine H1 receptor (H1R); Histamine H1 receptor occupancy; Ketotifen; Olopatadine; Positron emission tomography (PET); Second generation antihistamine

Indexed keywords

ANTIHISTAMINIC AGENT; BRAIN RECEPTOR; DOXEPIN; HISTAMINE H1 RECEPTOR; KETOTIFEN; OLOPATADINE; PLACEBO;

ADULT; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; BLOOD BRAIN BARRIER; BRAIN REGION; CALCULATION; CINGULATE GYRUS; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG RECEPTOR BINDING; HUMAN; HUMAN EXPERIMENT; INSULA; MALE; NEUROIMAGING; NORMAL HUMAN; OCCIPITAL CORTEX; PARIETAL LOBE; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RECEPTOR OCCUPANCY; SEDATION; TEMPORAL CORTEX;

ADMINISTRATION, ORAL; ADULT; AREA UNDER CURVE; BRAIN; CROSS-OVER STUDIES; DIBENZOXEPINS; DOXEPIN; HISTAMINE ANTAGONISTS; HISTAMINE H1 ANTAGONISTS; HUMANS; KETOTIFEN; MALE; POSITRON-EMISSION TOMOGRAPHY; RECEPTORS, HISTAMINE H1;

EID: 33644987428     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2005.02514.x     Document Type: Article

References (54)

1. Haas H Panula P The role of histamine and the tuberomamillary nucleus in the nervous system Nat Rev Neurosci 2003 4 2 121 30
2. Holgate ST Canonica GW Simons FE Taglialatela M Tharp M Timmerman H Yanai K Consensus Group on New-Generation Antihistamines (CONGA): present status and recommendations Clin Exp Allergy 2003 33 9 1305 24
3. Casale TB Blaiss MS Gelfand E Gilmore T Harvey PD Hindmarch I Simons FE Spangler DL Szefler SJ Terndrup TE Waldman SA Weiler J Wong DF First do no harm: managing antihistamine impairment in patients with allergic rhinitis J Allergy Clin Immunol 2003 111 5 S835 42
4. Yanai K Ryu JH Watanabe T Iwata R Ido T Sawai Y Ito K Itoh M Histamine H1 receptor occupancy in human brains after single oral doses of histamine H1 antagonists measured by positron emission tomography Br J Pharmacol 1995 116 1 1649 55
5. Yanai K Ryu JH Watanabe T Iwata R Ido T Asakura M Matsumura R Itoh M Positron emission tomographic study of central histamine H1-receptor occupancy in human subjects treated with epinastine, a second-generation antihistamine Meth Find Exp Clin Pharmacol 1995 17 Suppl C 64 9
6. Yanai K Okamura N Tagawa M Itoh M Watanabe T New findings in pharmacological effects induced by antihistamines: from PET studies to knock-out mice Clin Exp Allergy 1999 29 Suppl 3 29 36 ; discussion 37 8
7. Okamura N Yanai K Higuchi M Sakai J Iwata R Ido T Sasaki H Watanabe T Itoh M Functional neuroimaging of cognition impaired by a classical antihistamine, d-chlorpheniramine Br J Pharmacol 2000 129 1 115 23
8. Tagawa M Kano M Okamura N Higuchi M Matsuda M Mizuki Y Arai H Iwata R Fujii T Komemushi S Ido T Itoh M Sasaki H Watanabe T Yanai K Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)- chlorpheniramine, a classical antihistamine Br J Clin Pharmacol 2001 52 5 501 9
9. 11C-doxepin positron emission tomography J Clin Pharmacol 2004 44 8 890 900
10. Karlsson P Farde L Halldin C Sedvall G Ynddal L Sloth-Nielsen M Oral administration of NNC 756 - a placebo controlled PET study of D1-dopamine receptor occupancy and pharmacodynamics in man Psychopharmacology (Berl) 1995 119 1 1 8
11. 2 receptor occupancy in patients with recent-onset schizophrenia treated with low-dose olanzapine or haloperidol: a randomized, double-blind study Am J Psychiatry 2003 160 2 303 9
12. 2 receptor occupancy during treatment with the atypical antipsychotic sertindole Psychopharmacology (Berl) 2002 162 1 37 41
13. 2 and 5-HT2A receptor occupancy in schizophrenic patients Am J Psychiatry 1999 156 6 869 75
14. 2 dopamine receptor blockade in schizophrenic patients: a baseline-endpoint Psychiatry Res 2001 107 2 87 97
15. Kapur S Zipursky R Jones C Remington G Houle S Relationship between dopamine D(2) occupancy, clinical response, and side effects: a double-blind PET study of first-episode schizophrenia Am J Psychiatry 2000 157 4 514 20
16. 2 receptor occupancy by amisulpride in schizophrenia Psychopharmacology (Berl) 1996 124 1-2 154 8
17. 2-dopamine receptor occupancy in relation to antipsychotic drug effects: a double-blind PET study of schizophrenic patients Biol Psychiatry 1993 33 4 227 35
18. 11C]WAY 100635 and positron emission tomography in humans Neuropsychopharmacology 2001 24 3 209 29
19. Rabiner EA Bhagwagar Z Gunn RN Sargent PA Bench CJ Cowen PJ Grasby PM Pindolol augmentation of selective serotonin reuptake inhibitors: PET evidence that the dose used in clinical trials is too low Am J Psychiatry 2001 158 12 2080 2
20. 11C][O-methyl-3H]-N-(2- (4-(2-methoxyphenyl) -1-piperazinyl) ethyl) -N-(2-py ridinyl) cyclohexanecarboxamide trihydrochloride (WAY-100635) positron emission tomography study in humans J Pharmacol Exp Ther 2002 301 3 1144 50
21. Nakayama T Suhara T Okubo Y Ichimiya T Yasuno F Maeda J Takano A Saijo T Suzuki K In vivo drug action of tandospirone at 5-HT1A receptor examined using positron emission tomography and neuroendocrine response Psychopharmacology (Berl) 2002 165 1 37 42
22. Andree B Nyberg S Ito H Ginovart N Brunner F Jaquet F Halldin C Farde L Positron emission tomographic analysis of dose-dependent MDL 100, 907 binding to 5-hydroxytryptamine-2A receptors in the human brain J Clin Psychopharmacol 1998; 18 4 317 23
23. Abelson MB Spitalny L Combined analysis of two studies using the conjunctival allergen challenge model to evaluate olopatadine hydrochloride, a new ophthalmic antiallergic agent with dual activity Am J Ophthalmol 1998 125 6 797 804
24. Katelaris CH Ciprandi G Missotten L Turner FD Bertin D Berdeaux G A comparison of the efficacy and tolerability of olopatadine hydrochloride 0.1% ophthalmic solution and cromolyn sodium 2% ophthalmic solution in seasonal allergic conjunctivitis Clin Ther 2002 24 10 1561 75
25. Spangler DL Bensch G Berdy GJ Evaluation of the efficacy of olopatadine hydrochloride 0.1% ophthalmic solution and azelastine hydrochloride 0.05% ophthalmic solution in the conjunctival allergen challenge model Clin Ther 2001 23 8 1272 80
26. Berdy GJ Spangler DL Bensch G Berdy SS Brusatti RC A comparison of the relative efficacy and clinical performance of olopatadine hydrochloride 0.1% ophthalmic solution and ketotifen fumarate 0.025% ophthalmic solution in the conjunctival antigen challenge model Clin Ther 2000 22 7 826 33
27. Artal MN Luna JD Discepola M A forced choice comfort study of olopatadine hydrochloride 0.1% versus ketotifen fumarate 0.05% Acta Ophthalmol Scand Suppl 2000 230 64 5
28. Aguilar AJ Comparative study of clinical efficacy and tolerance in seasonal allergic conjunctivitis management with 0.1% olopatadine hydrochloride versus 0.05% ketotifen fumarate Acta Ophthalmol Scand Suppl 2000 230 52 5
29. Butrus S Greiner JV Discepola M Finegold I Comparison of the clinical efficacy and comfort of olopatadine hydrochloride 0.1% ophthalmic solution and nedocromil sodium 2% ophthalmic solution in the human conjunctival allergen challenge model Clin Ther 2000 22 12 1462 72
30. Abelson MB Welch DL An evaluation of onset and duration of action of patanol (olopatadine hydrochloride ophthalmic solution 0.1%) compared to Claritin (loratadine 10 mg) tablets in acute allergic conjunctivitis in the conjunctival allergen challenge model Acta Ophthalmol Scand Suppl 2000; 230 60 3
31. Yanni JM Weimer LK Sharif NA Xu SX Gamache DA Spellman JM Inhibition of histamine-induced human conjunctival epithelial cell responses by ocular allergy drugs Arch Ophthalmol 1999 117 5 643 7
32. Ohmori K Hayashi K Kaise T Ohshima E Kobayashi S Yamazaki T Mukouyama A Pharmacological pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug Jpn J Pharmacol 2002 88 4 379 97
33. Ishii H Sasaki Y Manabe H Ikemura T Sato H Ichikawa S Shiozaki S Kitamura S Ohmori K [General pharmacology of KW-4679, an antiallergic drug (1st report): effects on central nervous system, autonomic nervous system and peripheral nervous system] Clin Pharmacol Ther 1995 5 8 1421 40. in Japanese.
34. Hamilton SA Duddle J Herdman MJ Trigg CJ Davies RJ Comparison of a new antihistaminic and antiallergic compound KW 4679 with terfenadine and placebo on skin and nasal provocation in atopic individuals Clin Exp Allergy 1994 24 10 955 9
35. Morita K Koga T Moroi Y Urabe K Furue M Rapid effects of olopatadine hydrochloride on the histamine-induced skin responses J Dermatol 2002 29 11 709 12
36. Kamei C Ichiki C Izumo T Ohishi H Yoshida T Tsujimoto S Effect of the new antiallergic agent olopatadine on EEG spectral powers in conscious rats Arzneimittelforschung 1996 46 8 789 93
37. Kamei C Nishiga M Shigemoto Y Konishi M Shinomiya K [Effect of epinastine hydrochloride (Alesion) on the central nervous system ] Jpn Pharmacol Ther 2002 30 2 91 5
38. Nishiga M Fujii Y Konishi M Hossen MA Effects of second-generation histamine H1 receptor antagonists on the active avoidance response in rats Clin Exp Pharmacol Physiol 2003 30 1-2 60 3
39. Kamei H Noda Y Ishikawa K Senzaki K Muraoka I Hasegawa Y Hindmarch I Nabeshima T Comparative study of acute effects of single doses of fexofenadine, olopatadine, d-chlorpheniramine and placebo on psychomotor function in healthy volunteers Hum Psychopharmacol 2003 18 8 611 8
40. Grant SM Goa KL Fitton A Sorkin EM Ketotifen. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma and allergic disorders Drugs 1990 40 3 412 48
41. Simons FE Fraser TG Reggin JD Simons KJ Comparison of the central nervous system effects produced by six H1-receptor antagonists Clin Exp Allergy 1996 26 9 1092 7
42. Matejcek M Irwin P Neff G Abt K Wehrli W Determination of the central effects of the asthma prophylactic ketotifen, the bronchodilator theophylline, and both in combination: an application of quantitative electroencephalography to the study of drug interactions Int J Clin Pharmacol Ther Toxicol 1985 23 5 258 66
43. Vollmer R Matejcek M Greenwood C Grisold W Jellinger K Correlation between EEG changes indicative of sedation and subjective responses Neuropsychobiology 1983 10 4 249 53
44. Tagawa M Kano M Okamura N Higuchi M Matsuda M Mizuki Y Arai H Fujii T Komemushi S Itoh M Sasaki H Watanabe T Yanai K Differential cognitive effects of ebastine and (+) -chlorpheniramine in healthy subjects: correlation between cognitive impairment and plasma drug concentration Br J Clin Pharmacol 2002 53 3 296 304
45. 11C) methyl triflate Appl Radiat Isot 2001 55 1 17 22
46. 11C]doxepin Nucl Med Biol 2004 31 2 165 71
47. 11C labelled radiopharmaceuticals from external measurement with thermoluminescent dosimeters Phys Med Biol 1998 43 2 389 405
48. 11C]doxepin Nucl Med Biol 2004 31 8 1005 11
49. Fujiwara T Watanuki S Yamamoto S Miyake M Seo S Itoh M Ishii K Orihara H Fukuda H Satoh T Kitamura K Tanaka K Takahashi S Performance evaluation of a large axial field-of-view PET scanner SET-2400w Ann Nucl Med 1997 11 4 307 13
50. Friston KJ Holmes AP Worsley KJ Poline JP Frith CD Frackowiak RSJ Statistical parametric maps in functional imaging: a general linear approach Hum Brain Mapp 1995 2 189 210
51. Talairach J Tournoux P Co-Planar Stereotaxic Atlas of the Human Brain Stuttgart. Germany Georg Thieme Verlag 1988
52. Drescher S Schaeffeler E Hitzl M Hofmann U Schwab M Brinkmann U Eichelbaum M Fromm MF MDR1 gene polymorphisms and disposition of the P-glycoprotein substrate fexofenadine Br J Clin Pharmacol 2002 53 5 526 34
53. Spaeth J Klimek L Mosges R Sedation in allergic rhinitis is caused by the condition and not by antihistamine treatment Allergy 1996 51 12 893 906
54. 11C-raclopride Psychopharmacology (Berl) 1993 112 2-3 308 14