Functional Neuroimaging of Cognition Impaired by a Classical Antihistamine, D-chlorpheniramine

Overview

Journal Br J Pharmacol

Publisher Wiley

Specialty Pharmacology

Date 2000 Feb 29

PMID 10694210

Citations 23

Authors

N Okamura

K Yanai

M Higuchi

J Sakai

R Iwata

T Ido

H Sasaki

T Watanabe

M Itoh

Affiliations

Soon will be listed here.

Abstract

Antihistamine induced cognitive decline was evaluated using positron emission tomography (PET) measurement of histamine H1 receptor (H1R) occupancy and regional cerebral blood flow (rCBF). Cognitive performance in attention-demanding task deteriorated dose-dependently and the effects were statistically significant after the treatment of 2 mg of d-chlorpheniramine. There was no significant change in subjective sleepiness in the same dose. The regional blockade of H1R was observed mainly in the frontal, temporal and anterior cingulate cortices, and the intravenous administration of d-chlorpheniramine as a therapeutic dose (2 mg) blocked over 60% of H1R in the frontal cortices. The results from activation study using visual discrimination tasks demonstrated that enhanced activity in the right prefrontal and anterior cingulate cortices as well as a decreased activity in the left temporal and frontal cortices and midbrain after the treatment of d-chlorpheniramine. There were no changes in global CBF for the subjects treated with 2 mg d-chlorpheniramine (pre; 44.8+/-3.3 ml dl(-1) min(-1) vs post; 44.4+/-4.7 ml dl(-1) min(-1)). The results indicated that the attention system of human brain could be altered by therapeutic doses of H1R antagonists. These findings provide the information as to the potential risk of antihistamines in our daily activities. British Journal of Pharmacology (2000) 129, 115 - 123

Citing Articles

Targeting Histamine and Histamine Receptors for Memory Regulation: An Emotional Perspective.

Fang Z, Chen J, Zheng Y, Chen Z Curr Neuropharmacol. 2024; 22(11):1846-1869.

PMID: 38288837 PMC: 11284729. DOI: 10.2174/1570159X22666240128003108.

Molecular mechanism of antihistamines recognition and regulation of the histamine H receptor.

Wang D, Guo Q, Wu Z, Li M, He B, Du Y Nat Commun. 2024; 15(1):84.

PMID: 38167898 PMC: 10762250. DOI: 10.1038/s41467-023-44477-4.

Old versus new antihistamines: Effects on cognition and psychomotor functions.

Shamil K, Prakruti P, Anuradha M, Bela J, Chetna K J Family Med Prim Care. 2023; 11(10):5909-5917.

PMID: 36618177 PMC: 9810909. DOI: 10.4103/jfmpc.jfmpc_77_22.

Migraine Pharmacological Treatment and Cognitive Impairment: Risks and Benefits.

Russo M, De Rosa M, Calisi D, Consoli S, Evangelista G, Dono F Int J Mol Sci. 2022; 23(19).

PMID: 36232720 PMC: 9569564. DOI: 10.3390/ijms231911418.

Histamine H receptor on astrocytes and neurons controls distinct aspects of mouse behaviour.

Karpati A, Yoshikawa T, Naganuma F, Matsuzawa T, Kitano H, Yamada Y Sci Rep. 2019; 9(1):16451.

PMID: 31712580 PMC: 6848115. DOI: 10.1038/s41598-019-52623-6.

References

Watanabe T, Taguchi Y, Shiosaka S, Tanaka J, Kubota H, Terano Y . Distribution of the histaminergic neuron system in the central nervous system of rats; a fluorescent immunohistochemical analysis with histidine decarboxylase as a marker. Brain Res. 1984; 295(1):13-25. DOI: 10.1016/0006-8993(84)90811-4. View

Raichle M, Martin W, Herscovitch P, Mintun M, Markham J . Brain blood flow measured with intravenous H2(15)O. II. Implementation and validation. J Nucl Med. 1983; 24(9):790-8. View

Kemp J, Buckley C, Gershwin M, Buchman E, Cascio F, Chretien J . Multicenter, double-blind, placebo-controlled trial of terfenadine in seasonal allergic rhinitis and conjunctivitis. Ann Allergy. 1985; 54(6):502-9. View

Seidel W, Cohen S, Bliwise N, Dement W . Cetirizine effects on objective measures of daytime sleepiness and performance. Ann Allergy. 1987; 59(6 Pt 2):58-62. View

Lin J, Sakai K, Jouvet M . Evidence for histaminergic arousal mechanisms in the hypothalamus of cat. Neuropharmacology. 1988; 27(2):111-22. DOI: 10.1016/0028-3908(88)90159-1. View

Goldman-Rakic P . Topography of cognition: parallel distributed networks in primate association cortex. Annu Rev Neurosci. 1988; 11:137-56. DOI: 10.1146/annurev.ne.11.030188.001033. View

Goetz D, Jacobson J, Murnane J, Reid M, Repperger D, Goodyear C . Prolongation of simple and choice reaction times in a double-blind comparison of twice-daily hydroxyzine versus terfenadine. J Allergy Clin Immunol. 1989; 84(3):316-22. DOI: 10.1016/0091-6749(89)90414-4. View

Meador K, Loring D, Thompson E, THOMPSON W . Differential cognitive effects of terfenadine and chlorpheniramine. J Allergy Clin Immunol. 1989; 84(3):322-5. DOI: 10.1016/0091-6749(89)90415-6. View

Posner M, Petersen S . The attention system of the human brain. Annu Rev Neurosci. 1990; 13:25-42. DOI: 10.1146/annurev.ne.13.030190.000325. View

10.

Logan J, Fowler J, Volkow N, Wolf A, Dewey S, Schlyer D . Graphical analysis of reversible radioligand binding from time-activity measurements applied to [N-11C-methyl]-(-)-cocaine PET studies in human subjects. J Cereb Blood Flow Metab. 1990; 10(5):740-7. DOI: 10.1038/jcbfm.1990.127. View

11.

Meltzer E . Performance effects of antihistamines. J Allergy Clin Immunol. 1990; 86(4 Pt 2):613-9. DOI: 10.1016/s0091-6749(05)80225-8. View

12.

Pardo J, Fox P, Raichle M . Localization of a human system for sustained attention by positron emission tomography. Nature. 1991; 349(6304):61-4. DOI: 10.1038/349061a0. View

13.

Schwartz J, Arrang J, Garbarg M, Pollard H, Ruat M . Histaminergic transmission in the mammalian brain. Physiol Rev. 1991; 71(1):1-51. DOI: 10.1152/physrev.1991.71.1.1. View

14.

Wada H, Inagaki N, Yamatodani A, Watanabe T . Is the histaminergic neuron system a regulatory center for whole-brain activity?. Trends Neurosci. 1991; 14(9):415-8. DOI: 10.1016/0166-2236(91)90034-r. View

15.

Yanai K, Watanabe T, Yokoyama H, Meguro K, Hatazawa J, Itoh M . Histamine H1 receptors in human brain visualized in vivo by [11C]doxepin and positron emission tomography. Neurosci Lett. 1992; 137(2):145-8. DOI: 10.1016/0304-3940(92)90390-s. View

16.

Hendeles L . Efficacy and safety of antihistamines and expectorants in nonprescription cough and cold preparations. Pharmacotherapy. 1993; 13(2):154-8. View

17.

Smith M, Feldman W . Over-the-counter cold medications. A critical review of clinical trials between 1950 and 1991. JAMA. 1993; 269(17):2258-63. DOI: 10.1001/jama.269.17.2258. View

18.

Rice V, Snyder H . The effects of Benadryl and Hismanal on psychomotor performance and perceived performance. Aviat Space Environ Med. 1993; 64(8):726-34. View

19.

Tasaka K, Chung Y, Mio M, Kamei C . The pathway responsible for EEG synchronization and effect of histamine on this system. Brain Res Bull. 1993; 32(4):365-71. DOI: 10.1016/0361-9230(93)90201-l. View

20.

Simons F, Simons K . The pharmacology and use of H1-receptor-antagonist drugs. N Engl J Med. 1994; 330(23):1663-70. DOI: 10.1056/NEJM199406093302307. View