COX inhibitors(Cyclooxygenases inhibitors), H1 receptor antagonists(Histamine H1 receptor antagonists), α-adrenergic receptor agonists(Alpha adrenergic receptor agonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesOtorhinolaryngologic Diseases+ [1]

Active Indication

Common ColdRhinitis, Allergic, SeasonalUpper respiratory tract allergy

Inactive Indication-

Originator Organization

Pfizer Inc.

Active Organization

Haleon US Capital LLC

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (19 Dec 2002),

Common ColdRhinitis, Allergic, SeasonalUpper respiratory tract allergy

Regulation-

Structure

Molecular FormulaC13H18O2

InChIKeyHEFNNWSXXWATRW-UHFFFAOYSA-N

CAS Registry15687-27-1

View All Structures (3)

Clinical Trials associated with Chlorpheniramine Maleate/Ibuprofen/Pseudoephedrine Hydrochloride

NCT01938144 / WithdrawnPhase 3

Three-day Clinical Evaluation Of The Efficacy And Safety Of Two Ibuprofen Combination Products For The Symptomatic Treatment Of The Common Cold And Flu: A Multicenter Study

This is a multicenter, prospective, randomized, double-blind, triple-dummy, parallel group, comparative, study designed to evaluate the efficacy of Ibuprofen (IBU) 200 mg/ Phenylephrine (PE) 10 mg and IBU 200 mg/ PE 10 mg/ Chlorpheniramine (CHLOR) 4 mg on the relief of symptoms of the common cold and flu. The reference product that the active treatments will be compared to is paracetamol (PARA) 500 mg.

Start Date01 Apr 2016

Sponsor / Collaborator

Pfizer Inc.

100 Clinical Results associated with Chlorpheniramine Maleate/Ibuprofen/Pseudoephedrine Hydrochloride

100 Translational Medicine associated with Chlorpheniramine Maleate/Ibuprofen/Pseudoephedrine Hydrochloride

100 Patents (Medical) associated with Chlorpheniramine Maleate/Ibuprofen/Pseudoephedrine Hydrochloride

Literatures (Medical) associated with Chlorpheniramine Maleate/Ibuprofen/Pseudoephedrine Hydrochloride

01 Jan 2012·British Journal of PharmacologyQ2 · MEDICINE

Induction of prolonged, continuous slow‐wave sleep by blocking cerebral H₁ histamine receptors in rats

Q2 · MEDICINE

Article

Author: Ayana Hori ; Masami Ikeda-Sagara ; Yuji Matsuya ; Kazuki Honda ; Masayuki Ikeda ; Tomoya Ozaki ; Naoki Toyooka ; Kazuma Wada ; Mohammad Shahid ; Eri Morioka

BACKGROUND AND PURPOSE Classic H1 histamine receptor (H1R) antagonists are non‐selective for H1R and known to produce drowsiness. Modern antihistamines are more selective for H1R, and are ‘non‐drowsy’ presumably due to reduced permeability through the blood‐brain barrier. To characterize both histaminergic sleep regulation and the central actions of antihistamines, in the present study we analysed the effect of classic and modern antihistamines on rats' sleep using continuous i.c.v. infusions.EXPERIMENTAL APPROACH Effects of classic (d‐chlorpheniramine; d‐CPA) and second‐generation (cetirizine) antihistamines on sleep were compared after i.p. injections or continuous i.c.v. infusions into rats. Fluorescent cetirizine/DBD‐pz was synthesized to trace the approximate distribution of cerebral cetirizine. Furthermore, the effects of H1R antagonists on cultured preoptic neurons were examined using calcium imaging.KEY RESULTSd‐CPA 4 mg·kg−1 i.p. increased non‐rapid eye movement (REM) sleep whereas 10–40 mg·kg−1d‐CPA decreased non‐REM sleep at dark onset time. Nocturnal i.c.v. infusions of d‐CPA (10 µmol·100 µL−1·10 h−1) increased drowsiness but not non‐REM sleep, whereas the same i.c.v. infusions of cetirizine significantly increased non‐REM sleep, abolished REM sleep, and decreased wakefulness for more than 10 h. The medial preoptic area contained the greatest fluorescent labelling after i.c.v. cetirizine/DBD‐pz infusions. Histamine‐induced Ca2+ increases in medial preoptic neurons were blocked by d‐CPA or cetirizine, whereas d‐CPA, but not cetirizine, increased Ca2+ irrespective of antihistaminergic activity at ≥100 µM.CONCLUSION AND IMPLICATIONS The excitatory action of d‐CPA may explain the seemingly inconsistent actions of d‐CPA on sleep. Cerebral H1R inhibition by cetirizine induces synchronization of cerebral activity and prolonged, continuous slow‐wave sleep.

01 Oct 2007·Neurogastroenterology & MotilityQ3 · MEDICINE

Role of histaminergic neurons in hypnotic modulation of brain processing of visceral perception

Q3 · MEDICINE

Article

Author: S. Watanabe ; S. Fukudo ; M. Kanazawa ; M. Kano ; T. Hattori

Abstract Modulating visceral sensation of the body is important to the understanding of emotion formation. Molecules that act during hypnosis and modify visceral pain perception are not known. We tested our hypothesis that hypnotic suggestion changes electrophysiological processing of visceroafferent signals in the human brain and that these conditions are in part dependent on histaminergic neurons. Twelve healthy male subjects were studied on two separate days: a day of treatment with histamine H1 receptor antagonist (d‐chlorpheniramine 100 μg kg−1, intravenously) and another day of that with placebo (saline, the same amount) in a randomized order. We recorded cortical evoked potentials to 100 rectal electrical stimuli after neutral, hyperalgesic or analgesic hypnotic suggestions as given to modulate the visceral perception. Analgesic suggestion reduced the amplitude of the deepest positive peak of viscerosensory evoked potential. Administration of histamine H1 antagonist diminished the attenuation of viscerosensory evoked potential by analgesic suggestion. Our results suggest that central pain modulatory system in the brain is activated by hypnotic suggestion and that brain histamine is a mediator in the hypnotic modulation of visceral sensory pathway as well as in the control of consciousness level. These findings lead us to possible new treatment for control of visceral perception.

01 Dec 2003·Human Psychopharmacology: Clinical and ExperimentalQ4 · MEDICINE

Comparative study of acute effects of single doses of fexofenadine, olopatadine, d‐chlorpheniramine and placebo on psychomotor function in healthy volunteers

Q4 · MEDICINE

Article

Author: Hiroyuki Kamei ; Toshitaka Nabeshima ; Ian Hindmarch ; Kazuhiro Ishikawa ; Koji Senzaki ; Yukihiro Noda ; Isao Muraoka ; Yoshinori Hasegawa

AbstractSince most classical (first‐generation) antihistamines have undesirable sedative effects on the central nervous system (CNS), newer (second‐generation) antihistamines have been developed to relieve the sedative effects and to improve the patient's quality of life. However, the psychomotor profiles of second‐generation antihistamines are not fully elucidated. In this randomized, double‐blind, crossover study, the acute effects of single doses of second‐generation antihistamines, fexofenadine (120 mg) and olopatadine (10 mg), on cognitive and psychomotor performance were investigated in comparison with those of placebo and d‐chlorpheniramine (4 mg), a first‐generation antihistamine, using objective and subjective assessments, in 11 healthy Japanese volunteers. In a battery of psychomotor tests, d‐chlorpheniramine impaired tracking ability in the compensatory tracking task and caused a reduction in behavioural activity as continuously measured by wrist actigraphy. Olopatadine, like d‐chlorpheniramine, reduced the behavioural activity, while fexofenadine had no effect in any of the tests. No significant changes in the subjects' self‐ratings of drowsiness were found with the three antihistamines. These results suggest that d‐chlorpheniramine and olopatadine, but not fexofenadine, produce sedative effects on psychomotor performance, and that the CNS profile of fexofenadine is different from that of olopatadine. Copyright © 2003 John Wiley & Sons, Ltd.

100 Deals associated with Chlorpheniramine Maleate/Ibuprofen/Pseudoephedrine Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	R06AB54 R01BA52 M01AE51	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Common Cold	US	Haleon US Capital LLC	19 Dec 2002
Rhinitis, Allergic, Seasonal	US	Haleon US Capital LLC	19 Dec 2002
Upper respiratory tract allergy	US	Haleon US Capital LLC	19 Dec 2002

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