Evaluation of Efficacy and Sedative Profiles of H1 Antihistamines by Large-Scale Surveillance Using the Visual Analogue Scale (VAS)

Izumi, Norimasa; Mizuguchi, Hiroyuki; Umehara, Hayato; Ogino, Satoshi; Fukui, Hirokazu

doi:10.2332/allergolint.o-07-525

Cited by 20 publications

(12 citation statements)

References 17 publications

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“…Our data are consistent with the finding that antihistaminic drugs control hormones release and with the previous data evidencing that the release of hormones in response to altered stimuli is subjected to various regulatory pathways [13].…”

Section: Discussionsupporting

confidence: 82%

Clemastine, the H1 Histamine Receptor Antagonist, Alters the Human Sex and Thyroid Hormonal Profiles

Abdrabou

Ahmed

Eskander

2017

Asian J Pharm Clin Res

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Objective: Clemastine is widely used as an antihistaminic drug. However, clemastine effectively acts as an antagonist of H1 histamine receptor, it has significant burden adverse effects causing common nervous system, psychiatric, and gastrointestinal ailments, as well as rare cardiac and immune system disorders. The objective of this study is to investigate whether there is a remarkable impact of clemastine administration on the human hormonal pituitary-thyroid-adrenal axis.Methods: To achieve that, hormonal profile was tested in the sera of males and females treated and untreated individuals with clemastine. This is to measure serum estradiol, follicle-stimulating hormone, luteinizing hormone, prolactin, progesterone, dehydroepiandrosterone sulfate, thyroidstimulating hormone, triiodothyronine, thyroxine, fasting insulin, and cortisol levels. The circulating hormonal levels were measured quantitatively using enzyme-link immunosorbent assay. Results:We resulted that there were significant differences of the human hormonal profile on clemastine treatment. Conclusion:Hormonal profiling showed that there were remarkable signatures could be of great interest to underline some recommendations and guidelines optimizing the clemastine dosage to avoid burdens associated with the administration of this drug as well as maintain the physiological and psychological performances of both sexes exposing to clemastine during the period of allergic treatment.

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Section: Discussionsupporting

confidence: 82%

Clemastine, the H1 Histamine Receptor Antagonist, Alters the Human Sex and Thyroid Hormonal Profiles

Abdrabou

Ahmed

Eskander

2017

Asian J Pharm Clin Res

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“…Error bars, S.E. brain barrier, then causing sedative side effects of the drug (30). Thus, an intracellular binding site could not be excluded a priori.…”

Section: Potentiating Effect Of Clemastine On Hp2x7 Is Voltage-indepementioning

confidence: 99%

Clemastine Potentiates the Human P2X7 Receptor by Sensitizing It to Lower ATP Concentrations

Nörenberg¹,

Hempel²,

Urban

et al. 2011

Journal of Biological Chemistry

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P2X7 receptors have emerged as potential drug targets for the treatment of medical conditions such as e.g. rheumatoid arthritis and neuropathic pain. To assess the impact of pharmaceuticals on P2X7, we screened a compound library comprising approved or clinically tested drugs and identified several compounds that augment the ATP-triggered P2X7 activity in a stably transfected HEK293 cell line. Of these, clemastine markedly sensitized Ca 2؉ entry through P2X7 to lower ATP concentrations. Extracellularly but not intracellularly applied clemastine rapidly and reversibly augmented P2X7-mediated whole-cell currents evoked by non-saturating ATP concentrations. Clemastine also accelerated the ATP-induced pore formation and Yo-Pro-1 uptake, increased the fractional NMDG ؉ permeability, and stabilized the open channel conformation of P2X7. Thus, clemastine is an extracellularly binding allosteric modulator of P2X7 that sensitizes P2X7 to lower ATP concentrations and facilitates its pore dilation. The activity of clemastine on native P2X7 receptors, Ca 2؉ entry, and whole-cell currents was confirmed in human monocyte-derived macrophages. Similar effects were observed in murine bone marrow-derived macrophages. Consistent with the data on recombinant P2X7, clemastine augmented the ATP-induced cation entry and Yo-Pro-1 uptake. In accordance with the observation that P2X7 controls the cytokine release from LPS-primed macrophages, we found that clemastine augmented the IL-1␤ release from LPS-primed human macrophages. Collectively, these data point to a sensitization of the recombinantly or natively expressed human P2X7 receptor toward its physiological activator, ATP, possibly leading to a modulation of macrophage-dependent immune responses.

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“…It can induce possible paradoxical excitement (e.g., restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures), especially in children, but in general it is well tolerated in patients and clemastine-related adverse reactions are considerably milder compared to other drugs in the same group such as chlorpheniramine or ebastine [5]. Details are shown in Table 1.…”

Section: Discussionmentioning

confidence: 99%

Safety of Oral Clemastine – Analysis of Data from Spontaneous Reporting System in Poland

Han¹,

Karłowicz-Bodalska²,

Miœkiewicz³

et al. 2015

Trop. J. Pharm Res

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Evaluation of Efficacy and Sedative Profiles of H1 Antihistamines by Large-Scale Surveillance Using the Visual Analogue Scale (VAS)

Cited by 20 publications

References 17 publications

Clemastine, the H1 Histamine Receptor Antagonist, Alters the Human Sex and Thyroid Hormonal Profiles

Clemastine, the H1 Histamine Receptor Antagonist, Alters the Human Sex and Thyroid Hormonal Profiles

Clemastine Potentiates the Human P2X7 Receptor by Sensitizing It to Lower ATP Concentrations

Safety of Oral Clemastine – Analysis of Data from Spontaneous Reporting System in Poland

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