Drugs online research references
Int J Clin Pharmacol Res. 1988;8(6):463-70.
Single dose pharmacokinetics of cetirizine in young and elderly volunteers.
Lefebvre RA, Rosseel MT, Bernheim J.
Heymans Institute of Pharmacology, University of Gent Medical School, Belgium.
The pharmacokinetics of the H1-receptor antagonist cetirizine were studied from 0 to 48 h after a single oral intake of 10 mg in 10 elderly volunteers (60 to 90 years) and in 10 young healthy volunteers (21 to 29 years). In young healthy volunteers about 60% of an oral dose of cetirizine was excreted in the urine in unchanged form. Mean plasma concentrations were slightly higher in the elderly subjects. Cmax (362 ng/ml), Tmax (1.30 h), terminal half-life (11.8 h) and AUC infinity (4316 ng.h/ml) in the elderly subjects were somewhat higher than in the young subjects (Cmax: 337 ng/ml, Tmax: 1.12 h, terminal half-life: 10.6 h, AUC: 3721 ng.h/ml), but the difference was not significant. The mean cumulative urinary excretion at 32 h was significantly lower in the elderly subjects. It is concluded that the slight differences in pharmacokinetics of cetirizine between young and elderly subjects after single oral intake can be attributed to the decreased renal clearance in the elderly.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2908109&dopt=Abstract
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Ann Allergy. 1987 Oct;59(4):278-82.
Inhibition of histamine and allergen skin wheal by cetirizine in four animal species.
De Vos C, Maleux MR, Baltes E, Gobert J.
Research Centre, UCB Pharmaceutical Sector, Chemin du Foriest, Belgium.
Histamine-induced skin reactions were studied in four animal species. Cetirizine displayed very potent oral antihistaminic activity in this model. In rats, the dose that reduced the reaction by 50% in comparison to controls was 4.2 mumol/kg and between 0.1 and 0.4 mumol/kg for the other species (mice, guinea pigs, and dogs). Cetirizine also inhibited the immediate hypersensitivity reaction induced by Ascaris extract in dogs. By the oral route, cetirizine had a more potent and longer acting activity than mepyramine, clemastine, terfenadine, astemizole, and hydroxyzine.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2959177&dopt=Abstract
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Int Arch Allergy Appl Immunol. 1988;87(1):9-13.
Inhibition of eosinophil chemotaxis by a new antiallergic compound (cetirizine).
Leprevost C, Capron M, De Vos C, Tomassini M, Capron A.
Centre d'Immunologie et de Biologie Parasitaire, Unite mixte INSERM U167-CNRS 624, Institut Pasteur, Lille, France.
The in vivo inhibitory effect of a new antiallergic, anti-H1 drug, cetirizine, on eosinophil attraction at skin sites challenged with various stimuli has been recently suggested. In the present work, we confirmed that this molecule, at therapeutical concentration, has a potent inhibitory action on eosinophil response to different chemoattractant mediators such as platelet-activating factor (PAF acether) and N-formyl methionyl leucyl phenyl alanyl in vitro. Another anti-H1 drug, polaramine, did not show this effect at the same concentration. These findings suggest that cetirizine in addition to its antihistaminic effect could also play a direct inhibitory effect on eosinophil recruitment. Moreover, cetirizine was not toxic for eosinophils and did not induce degranulation, as shown by the absence of peroxidase release. Comparison between cetirizine and a PAF acether antagonist (BN 52021) suggested that cetirizine did not act by a PAF receptor-blocking activity.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2971624&dopt=Abstract
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