H1-Receptor Antagonists

Fe, Simons

doi:10.2165/00002018-199410050-00002

Cited by 196 publications

(7 citation statements)

References 205 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…They are also consistent with findings reported for the recommended daily doses of most second generation histamine H1-receptor antagonists [26]. These results indicated an incidence of objective and subjective CNS side effects similar to that observed after the administration of placebo and significantly lower than those reported for first generation antihistamines.…”

Section: Discussionsupporting

confidence: 90%

Rupatadine does not potentiate the CNS depressant effects of lorazepam: randomized, double‐blind, crossover, repeated dose, placebo‐controlled study

García-Gea

Ballester

Martínez

et al. 2010

Brit J Clinical Pharma

View full text Add to dashboard Cite

WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• Although one defining characteristic of second generation H1-antihistamines is their lack of CNS effects, it has been proved that some compounds of this group are not devoid of such effects.• There is evidence that second generation H1-antihistamine compounds without relevant CNS effects at therapeutic doses could increase the behavioural impairment produced by sedating drugs when both are taken concomitantly.• The evaluation of possible drug interactions is crucial, especially when both compounds could have CNS effects, due to the possible consequences at the patient safety level. WHAT THIS STUDY ADDS• The study demonstrates the lack of CNS effects after repeated administration at therapeutic doses of the unique second generation H1-antihistamine with anti-PAF activity.• The study demonstrates the lack of interaction between repeated administration of rupatadine 10 mg and a single oral dose of lorazepam 2 mg.• The study presents a useful design to evaluate the interaction between two compounds saving time and the exposure of the volunteers to medication. AIMThe main objective was to assess whether benzodiazepine intake when rupatadine plasma concentrations were at steady-state would increase the CNS depressant effects. Rupatadine is a new H1-antihistamine which also inhibits platelet activating factor (PAF) release and has been shown to be clinically effective at doses of 10 mg. METHODSSixteen healthy young volunteers took part in a crossover, randomized, double-blind, placebo controlled trial comprising two experimental periods (repeated administration for 7 days of rupatadine 10 mg or placebo as single oral daily doses, separated by a washout of 14 days). On days 5 and 7, according to a fully balanced design, a single oral dose of lorazepam 2 mg or placebo was added. CNS effects were evaluated on these days by seven objective tests of psychomotor performance and eight subjective visual analogue scales (VAS) at pre-dose and several times after drug intake. Four treatment conditions were evaluated: placebo, rupatadine 10 mg, lorazepam 2 mg and rupatadine 10 mg + lorazepam 2 mg. RESULTSSignificant CNS effects, either impairment of psychomotor performance or subjective sedation, were observed when lorazepam was administered, either alone or in combination with steady state concentrations of rupatadine. No significant differences were found between these two conditions. In addition, rupatadine was not different from placebo. All treatments were well tolerated. CONCLUSIONRepeated doses of rupatadine (10 mg orally) did not enhance the CNS depressant effects of lorazepam (2 mg orally, single dose) either in objective psychomotor tasks or in subjective evaluations.

show abstract

Section: Discussionsupporting

confidence: 90%

Rupatadine does not potentiate the CNS depressant effects of lorazepam: randomized, double‐blind, crossover, repeated dose, placebo‐controlled study

García-Gea

Ballester

Martínez

et al. 2010

Brit J Clinical Pharma

View full text Add to dashboard Cite

show abstract

“…[12] Furthermore, the reaction also proceeds successfully with a number of other primary amines. The transformation of substituted anilines with benzyl alcohol afforded the corresponding secondary amines in high yields (entries 12-16).…”

mentioning

confidence: 93%

Efficient and Clean Gold‐Catalyzed One‐Pot Selective N‐Alkylation of Amines with Alcohols

Lou

Liu

et al. 2010

Chemistry A European J

168

View full text Add to dashboard Cite

show abstract

“…Diphenhydramine and chloropheniramine maleate are histamine H 1 -receptor antagonists, while diphenhydramine also coupled with antimuscarinic activity [9]. Cimetidine possesses histamine H 2 receptor antagonistic activity [10]. It is suggested that the relaxation effects elicited by BDPBI were through activation of the histaminergic substances from the aortic vessels.…”

Section: Discussionmentioning

confidence: 99%

A New Isoquinolinone Derivative with Noble Vasorelaxation Activity

Lin¹,

Lin

Lin³

et al. 2003

Pharmacology

View full text Add to dashboard Cite

The pharmacological effects of BDPBI (7-bromo-1,4-dihydro-2-phenyl-4,4-bis(4-pyridinylmethyl)2H-isoquinolin-3-one dihydrochloride) were tested on isolated endothelium-containing or denuded aorta of the guinea pig. BDPBI with the formula C₂₇H₂₄BrCl₂N₃O was synthesized starting with 3-isochromanone. In the endothelium-containing preparations of the aortic rings, phenylephrine (PHE; 10 µmol/l) elicited contracture and acetylcholine (ACh; 10 µmol/l) or BDPBI (0.01–10 µmol/l) elicited relaxation effects on the PHE-precontracted preparations. The BDPBI-elicited effect on the PHE-precontracted aortic rings was not altered in the presence of adrenergic blockers (propranolol or yohimbine; 1 µmol/l) or pretreated preparations with aspirin, indomethacin (10 µmol/l) or L-NAME (1 mmol/l). However, the relaxation effects of BDPBI were blocked if the preparations were pretreated with diphenhydramine (10 µmol/l) or chloropheniramine maleate (10 µmol/l). In contrast to lower concentrations of atropine (1 µmol/l), higher concentrations of atropine (30 µmol/l) did block the effects of BDPBI on the PHE-precontracted aortic rings. HTMT dimaleate (0.01–10 µmol/l), a histamine H₁ receptor agonist, also elicited relaxation effects on the PHE-precontracted preparation, and the effects were blocked if the preparations were pretreated with diphenhydramine or chloropheniramine maleate. On isolated denuded aorta of the guinea pig, BDPBI did not elicit relaxation effects on the PHE-precontracted aortic rings. These results demonstrated that the vasorelaxation effect of BDPBI on PHE-precontracted aortic rings is partly dependent on the activation of a histaminergic receptor from the vascular endothelium. We suggested that BDPBI would be an effective vasorelaxant for cardiovascular systems.

show abstract

H1-Receptor Antagonists

Cited by 196 publications

References 205 publications

Rupatadine does not potentiate the CNS depressant effects of lorazepam: randomized, double‐blind, crossover, repeated dose, placebo‐controlled study

Rupatadine does not potentiate the CNS depressant effects of lorazepam: randomized, double‐blind, crossover, repeated dose, placebo‐controlled study

Efficient and Clean Gold‐Catalyzed One‐Pot Selective N‐Alkylation of Amines with Alcohols

A New Isoquinolinone Derivative with Noble Vasorelaxation Activity

Contact Info

Product

Resources

About