Unique ID issued by UMIN | UMIN000011372 |
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Receipt number | R000013278 |
Scientific Title | Brain histamine H1 receptor occupancy of sedating OTC antihistamines: Time-course of receptor occupancy measured by PET in normal volunteers |
Date of disclosure of the study information | 2013/08/05 |
Last modified on | 2017/10/25 13:22:58 |
Brain histamine H1 receptor occupancy of sedating OTC antihistamines: Time-course of receptor occupancy measured by PET in normal volunteers
Histamine H1 receptor occupancy of OTC antihistamines
Brain histamine H1 receptor occupancy of sedating OTC antihistamines: Time-course of receptor occupancy measured by PET in normal volunteers
Histamine H1 receptor occupancy of OTC antihistamines
Japan |
Normal volunteers
Adult |
Others
NO
Sedating H1 antihistamines are often used in the medication for allergic diseases, coughs and colds, and insomnia, without prescription, even though their sedative properties are a potentially dangerous unwanted side effect that is not properly recognized. These sedative properties have been evaluated using the incidence of subjective sleepiness, objective cognitive and psychomotor functions, and positron emission tomography (PET) measurement of H1 receptor occupancy. This study is designed to evaluate brain histamine H1 receptor occupancy sequentially using carbon-11 doxepin after oral administration of OTC antihistamines containing ketotifen 1.38 mg and diphenhydramine 50 mg in normal volunteers.
Safety
Confirmatory
Explanatory
Phase IV
Brain histamine H1 receptor occupancy 3 and 23 hours after oral administration of ketotifen 1.38 mg and diphenhydramine 50 mg.
Subjective sleepiness scale 3 and 23 hours after oral administration of ketotifen 1.38 mg and diphenhydramine 50 mg.
Interventional
Cross-over
Randomized
Individual
Single blind -participants are blinded
Placebo
NO
NO
Institution is not considered as adjustment factor.
NO
Numbered container method
2
Treatment
Medicine |
Ketotifen 1.38 mg
Diphenhydramine 50 mg
20 | years-old | <= |
30 | years-old | >= |
Male
1. Normal volunteers with his own free will. There is no subordinate relation.
2. Male healthy volunteers aged 20-30 years old, who understand the purpose of this study.
3. Subjects who can take enough sleep and rest at the previous night of PET scans
4. Subjects who can read documents attached with e-mail.
5. Subjects who can communicate with mobile phones.
6. Subjects who can take 3 PET-sacns examination and 1 MRI scan.
1. Subjects who take no medication including antihistamines at present.
2. Subjects who do not take any PET scans within the recent 2 years.
3. No serious allergy
4. No convulsion at past
5. No frequent medical addmission
6. No glaucoma and prostatic hypertrophy
7. Subjects who can not take any anticholinergic and antihistaminergic drugs from medical points of view.
8. No brain MRI abnormality
9. Inadequate subjects from the point of medical view of the investigators.
8
1st name | |
Middle name | |
Last name | Yanai Kazuhiko |
Tohoku University Graduate School of Medicine
Pharmacology
2-1 Seiryo-machi, Aoba-ku, Sendai 980-8575 Japan
022-717-8055
yanai@med.tohoku.ac.jp
1st name | |
Middle name | |
Last name | Yanai Kazuhiko |
Tohoku University Graduate School of Medicine
Pharmacology
2-1 Seiryo-machi, Aoba-ku, Sendai 980-8575 Japan
022-717-8055
yanai@med.tohoku.ac.jp
Department of Pharmacology, Tohoku University Graduate School of Medicine
Department of Pharmacology, Tohoku University Graduate School of Medicine
NEDO microdose project
Self funding
Japan
NO
東北大学大学院医学系研究科機能薬理学分野
Tohoku University Graduate School of Medicine, Department of Pharmacology
2013 | Year | 08 | Month | 05 | Day |
Partially published
Brain histamine H1 receptors were measured using PET and [11C]doxepin at 3 hours and 23 hours consecutively after diphenhydramine (50 mg) or ketotifen (1 mg) intake in healthy, young male subjects. The half-life of
diphenhydramine and ketotifen in the brain was estimated to be ~30 hours and 45 hours, respectively.
Completed
2011 | Year | 02 | Month | 01 | Day |
2013 | Year | 08 | Month | 01 | Day |
2015 | Year | 03 | Month | 31 | Day |
2015 | Year | 03 | Month | 31 | Day |
2015 | Year | 03 | Month | 31 | Day |
2016 | Year | 03 | Month | 31 | Day |
Yanai K, et al. Histamine H1 Receptor Occupancy in Human Brain. In: Histamine Receptors:Preclinical and Clinical Aspects.Springer 2016: pp311-325. ISBN: 978-3-319-40306-9
2013 | Year | 08 | Month | 05 | Day |
2017 | Year | 10 | Month | 25 | Day |
Value
https://center6.umin.ac.jp/cgi-open-bin/ctr_e/ctr_view.cgi?recptno=R000013278
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