The H1 histamine receptor blocker, chlorpheniramine, completely prevents the increase in REM sleep induced by immobilization stress in rats

Rojas-Zamorano, José Ángel; Esqueda-León, Enrique; Jiménez-Anguiano, Anabel; Cintra-McGlone, L.; Meléndez, Margarita; Moctezuma, Javier Velázquez

doi:10.1016/j.pbb.2008.07.011

Cited by 19 publications

(9 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…[1112] When taken at night, first-generation H 1 -antihistamines increase the latency to the onset of rapid eye movement (REM) sleep and reduce the duration of REM sleep. [13–15] The residual effects of poor sleep, including impairment of attention, vigilance, working memory, and sensory motor performance, are still present in the next morning. [1416] This is especially problematical with drugs with a long half-life [Table 1].…”

Section: Introductionmentioning

confidence: 99%

Pharmacology of antihistamines

Church

Church²

2013

Indian J Dermatol

152

103

View full text Add to dashboard Cite

H1-antihistamines, the mainstay of treatment for urticaria, were developed from anticholinergic drugs more than 70 years ago. They act as inverse agonists rather than antagonists of histamine H1-receptors which are members of the G-protein family. The older first generation H1-antihistamines penetrate readily into the brain to cause sedation, drowsiness, fatigue and impaired concentration and memory causing detrimental effects on learning and examination performance in children and on impairment of the ability of adults to work and drive. Their use should be discouraged. The newer second-generation H1-antihistamines are safer, cause less sedation and are more efficacious. Three drugs widely used for symptomatic relief in urticaria, desloratadine, levocetirizine and fexofenadine are highlighted in this review. Of these levocetirizine and fexofenadine are the most potent in humans in vivo. However, levocetirizine may cause somnolence in susceptible individuals, whereas fexofenadine has a relatively short duration of action and may be required to be given twice daily for all round daily protection. Although desloratadine is less potent, it has the advantages of rarely causing somnolence and having a long duration of action.

show abstract

Section: Introductionmentioning

confidence: 99%

Pharmacology of antihistamines

Church

Church²

2013

Indian J Dermatol

152

103

View full text Add to dashboard Cite

show abstract

“…In rats, sex differences in the ability of stress to augment acetylcholine release in the dorsal hippocampus, a regulator of REMS (Jouvet, 1998), are completely dependent on gonadal hormones (Mitsushima et al, 2009) suggesting that sex may interact with cholinergic regulation of REMS. Alternatively, inhibition of the histamine H1 receptor in male rats also prevents the ability of restraint stress to increase REMS (Rojas-Zamorano et al, 2009). Furthermore, the ability of stress to impair histamine release from hypothalamic neurons in rats is greater in males than in females.…”

Section: Discussionmentioning

confidence: 99%

The ability of stress to alter sleep in mice is sensitive to reproductive hormones

et al. 2009

View full text Add to dashboard Cite

Though stress causes complex sleep disruptions that are different in females and males, little is known about how sex influences the ability of stress to alter sleep. To date there have been no comprehensive examinations of whether effects of stress on sleep are sensitive to determinants of sex, such as reproductive hormones. Since restraint stress produces a sexually dimorphic increase in rapid eye movement sleep (REMS) amount in mice that is greater in males than females, in the current study we sought to determine whether estrogens and androgens influence the ability of restraint stress to alter sleep states. We removed the gonads from adult female and male C57BL/6J mice and implanted the mice with recording electrodes to monitor sleep-wake states. Gonadectomized females and males exhibited similar amounts of REMS in response to restraint stress. Mice were then implanted with continuous release hormone pellets. Females received 17β-estradiol and males received testosterone. Hormone replacement (HR) in females decreased the REMS response to restraint stress while HR in males increased the REMS response to restraint stress. The combined effects of HR in females and males restored the sex difference in the ability of restraint stress to alter REMS. These results demonstrate that sex differences in the effects of stress on REMS are dependent on reproductive hormones and support the view that endogenous or exogenous changes in the reproductive hormone environment influence sleep responses to stress.

show abstract

“…When taken during the day, firstgeneration H 1 antihistamines, even in the manufacturers' recommended doses, frequently cause daytime somnolence, sedation, drowsiness, fatigue, and impaired concentration and memory [27,28] . When taken at night, first-generation H 1 antihistamines increase the latency to the onset of rapid eye movement (REM) sleep and reduce the duration of REM sleep [29][30][31] . The residual effects of poor sleep, including impairment of attention, vigilance, working memory and sensorimotor performance, are still present the next morning [30,32] .…”

Section: H 1 Antihistamines and The Central Nervous Systemmentioning

confidence: 99%

Antihistamines

Church¹,

Maurer²

2014

History of Allergy

View full text Add to dashboard Cite

The discovery of histamine, its physiological role and reversal of its pharmacological effects by antihistamines takes us on a journey through the origins of modern physiology and the rising understanding of pharmacology at the end of the 19th and the early part of the 20th centuries. This journey, which has been traced in the excellent historical review by Michael Emanuel [Clin Exp Allergy 1999;29:1-11], is populated by some of the greatest scientists of the era, including six Nobel laureates - Bovet, Dale, Ehrlich, Richet, Windaus and Black. In addition, it laid the basis of medicinal chemistry not only for antihistamines, but also for the discovery of a plethora of drugs still in use today.

show abstract

The H1 histamine receptor blocker, chlorpheniramine, completely prevents the increase in REM sleep induced by immobilization stress in rats

Cited by 19 publications

References 34 publications

Pharmacology of antihistamines

Pharmacology of antihistamines

The ability of stress to alter sleep in mice is sensitive to reproductive hormones

Antihistamines

Contact Info

Product

Resources

About