Drugs online research references
Int Arch Allergy Appl Immunol. 1989;88(1-2):212-5.
Inhibition of human eosinophil chemotaxis and of the IgE-dependent stimulation of human blood platelets by cetirizine.
De Vos C, Joseph M, Leprevost C, Vorng H, Tomassini M, Capron M, Capron A.
Centre d'Immunologie et de Biologie Parasitaire, Unite mixte INSERM 167-CNRS 624-Institut Pasteur, Lille, France.
Cetirizine is a new anti-allergic compound with a potent, long-acting, and specific antihistaminic property. Strongly active in the therapy of urticaria and seasonal or perennial rhinitis, it has been shown to inhibit the in vivo eosinophil attraction at skin sites challenged with allergen in atopic patients. In the present work, we confirmed that, at a therapeutical concentration, this molecule had a potent inhibitory action in vitro on eosinophil chemotaxis induced either by N-formyl-Met-Leu-Phe or platelet-activating factor and also on the IgE-dependent stimulation of platelets. These observations appear in favour of a possible role for cetirizine in the modulation of inflammatory cell interactions in allergic processes.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2523357&dopt=Abstract
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J Clin Pharmacol. 1989 Sep;29(9):809-15.
The pharmacokinetics and pharmacodynamics of hydroxyzine in patients with primary biliary cirrhosis.
Simons FE, Watson WT, Chen XY, Minuk GY, Simons KJ.
Health Sciences Clinical Research Centre, Faculty of Medicine, University of Manitoba, Canada.
Hydroxyzine, a potent H1-receptor antagonist often used for relief of pruritus in patients with hepatic dysfunction, was studied in eight patients, mean age 53.4 +/- SD 11.2 years, with primary biliary cirrhosis. The patients ingested a single dose of hydroxyzine, 0.7 mg/kg (mean dose 43.9 +/- 6.6 mg). Before the dose, then hourly for 6 hours, every 2 hours from 6-12 hours, at 24 hours, and every 24 hours for 6 days, serum hydroxyzine and cetirizine were measured and an intradermal injection of 0.01 mL of a 0.1 mg/mL solution of histamine phosphate was performed. Wheals and flares were traced at 10 minutes and the areas were calculated. Mean peak hydroxyzine levels of 116.5 +/- 60.6 ng/mL occurred at 2.3 +/- 0.7 hours and mean peak cetirizine levels of 500.4 +/- 302.0 ng/mL occurred at 4.8 +/- 2.8 hours. The mean serum elimination half-life of hydroxyzine was 36.6 +/- 13.1 hours, and the mean serum elimination half-life of cetirizine was 25.0 +/- 8.2 hours. The mean hydroxyzine clearance rate was 8.65 +/- 7.46 mL/min/kg, and the mean volume of distribution was 22.7 +/- 13.3 L/kg. The mean wheal area was suppressed (P less than 0.01) from 1 to 120 hours, with maximal suppression from 2 to 48 hours. The mean flare area was suppressed from 1 to 144 hours, with maximal suppression from 3 to 24 hours (P less than 0.01). All patients became sleepy from 0.5 to 6 hours. Blurred vision, dizziness and dry mouth each occurred in two patients. Hydroxyzine elimination is impaired in patients with primary biliary cirrhosis.(ABSTRACT TRUNCATED AT 250 WORDS)
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Ann Allergy. 1987 Dec;59(6 Pt 2):13-9.
In vitro effects of cetirizine and histamine on human neutrophil function.
Van Epps DE, Kutvirt SG, Potter JW.
Department of Medicine, University of New Mexico, Albuquerque.
IgE-mediated hypersensitivity reactions are characterized by an immediate or early-phase response within the first 30 minutes of exposure to allergen, followed by a late-phase response that begins two to six hours later. Histamine is released during both the early- and late-phase responses and inhibits a variety of neutrophil functions, including superoxide anion generation, chemotaxis, and enzyme secretion. There is some debate as to whether histamine's action on neutrophils is mediated through H1 or H2 receptors, or through a single receptor that recognizes both H1 and H2 agonists. In an effort to understand the mechanism of action of the H1-antagonist cetirizine, we studied its effects on a variety of neutrophil functions. We found that at concentrations up to 35 micrograms/mL), it does not affect superoxide anion production or degranulation. However, at higher concentrations (greater than 35 micrograms/mL), a concentration-dependent inhibition of superoxide anion production is observed. This inhibition is most apparent with responses stimulated by chemotactic factors. Limited inhibition of degranulation and chemotaxis is also seen at high concentrations, but at a level far below that seen with superoxide anion production. These studies indicate that neutrophil function is not altered by the circulating concentrations of cetirizine attained during therapy (less than 10 micrograms/mL), but may be suppressed at higher concentrations. Additional effects of cetirizine on neutrophil function, possible influences of the drug on the inflammatory response, and histamine's modulation of neutrophil function are discussed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2892444&dopt=Abstract
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