Drugs online research references
Clin Pharmacol Ther. 1993 Apr;53(4):431-5.
A pharmacokinetic evaluation of the second-generation H1-receptor antagonist cetirizine in very young children.
Desager JP, Dab I, Horsmans Y, Harvengt C.
Department of Internal Medicine, Universite Catholique de Louvain, Belgium.
The pharmacokinetics of the second-generation H1-receptor antagonist cetirizine was studied in eight children younger than 4 years of age who were treated with a single dose of cetirizine solution (5 mg). These children were hospitalized with suspected allergic respiratory problems or recurrent respiratory tract infections. Blood samples were collected at 1/2, 1, 1 1/2, 2, 4, 6, 8, 12, and 24 hours, and a 24-hour urine collection was performed in five of the samples. The findings obtained in children were compared with those obtained in 16 healthy young adults (mean +/- SD, 24.6 +/- 4.1 years) who received a single 20 mg dose. Cetirizine was absorbed more slowly in children (p = 0.006; mean +/- SD, 1.44 +/- 1.12 hours) than in adults (0.62 +/- 0.22 hours). The plasma elimination half-life of cetirizine was significantly shorter in children (p < 0.001; 4.91 +/- 0.6 hours) than in adults (8.6 +/- 2.1 hours), and the clearance rate was significantly higher in children (p < 0.001; 1.48 +/- 0.41 ml/min/kg) than in adults (0.80 +/- 0.17 ml/min/kg). Urinary excretion of unchanged cetirizine was significantly lower in children (p < 0.001; 37.8% +/- 5.2%; n = 5) than in adults (57.7% +/- 11.8%). Therefore the metabolism of cetirizine is faster in young children than in adults. This effect must be taken into account in future pharmacodynamic studies in this age group.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8477559&dopt=Abstract
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Allergy. 2000 Mar;55(3):226-31.
Quantitative flow cytometric analysis of the effects of cetirizine on the expression of ICAM-1/CD54 on primary cultured nasal cells.
Mincarini M, Cagnoni F, Canonica GW, Cordone G, Sismondini A, Semino C, Pietra G, Melioli G.
Servizio di Allergologia ed Immunologia Clinica, DIMI, Universita di Genoa, Italy.
An in vitro flow cytometric model has been developed to evaluate the effects of antiallergic drugs such as cetirizine (CTZ) on the expression of surface molecules on primary cultured normal cells. Quantitative analysis demonstrated that HLA class I and ICAM-1/CD54 molecules are present on both epithelial and stromal cells, and that their expression is strongly enhanced by treatment with interferon-gamma (IFN-gamma). Nevertheless, the IFN-gamma-mediated upregulation of ICAM-1/CD54 was inhibited by treatment with CTZ, demonstrating a direct effect on both cell types. This finding is particularly interesting because ICAM-1/CD54 is the main rhinovirus receptor, and rhinoviruses are the principal cause of asthma exacerbation in children. Thus, according to data derived from this in vitro model, CTZ should have an important role in the reduction of infectious exacerbation of asthma in atopic patients.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10753012&dopt=Abstract
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Int Arch Allergy Immunol. 1996 May;110(1):52-6.
Cetirizine exerts anti-inflammatory effects on human neutrophils.
Koller M, Hilger RA, Rihoux JP, Konig W.
Medizinische Mikrobiologie und Immunologie, AG Infektabwehrmechanismen, Ruhr-Universitat Bochum, Germany.
Leukotrienes are potent lipid mediators involved in acute and chronic inflammatory processes and allergic inflammation. Cetirizine is an H1-receptor antagonist used in the treatment of allergic symptoms. We analyzed the effect of cetirizine on the formation of leukotriene B4 (LTB4) after stimulation of human peripheral blood neutrophils. The inflammatory mediators were analyzed after cellular activation with different stimuli: the Ca ionophore A23187, which bypasses membranous signal transduction elements; the bacterial peptide formyl-methionine-leucyl-phenylalanine (fMLP), which activates cells by binding to a GTP-protein (G-protein)-coupled receptor, and with sodium fluoride (NaF), which directly activates G-proteins. After cellular preincubation with cetirizine, the amounts of LTB4 generated from neutrophil granulocytes decreased significantly when the cells were subsequently stimulated with either fMLP or NaF, in contrast to stimulations with the Ca ionophore. The data provide evidence that cetirizine exerts anti-inflammatory effects apart from H1 antagonism.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8645978&dopt=Abstract
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