"In vivo" and "in vitro" evaluation of four antihistamines (astemizole, azatadine, mequitazine, terfenadine). 1989

A Malet i Casajuana, and J Ruiz de León, and A Valero Santiago, and J Sanosa Valls, and M Zamorano Calderón, and P A García Calderón
Inmunolab, Barcelona, Spain.

A group of 32 patients with perennial allergic rhinitis sensitized exclusively to house dust and mites were evaluated for "in vivo" modifications (skin tests for histamine, house dust and mites) and "in vitro" alterations (seric IgE, specific IgE, histamine release curve to different concentrations of Dermatophagoides pteronyssinus and histamine release curve to this pneumoallergen after incubation with H1 receptor antagonists) to four antihistamines (astemizole, azatadine, mequitazine and terfenadine). The patients were divided into 4 groups of 8 and the "in vivo" and "in vitro" tests were performed on days -1, +15 and +30 of administration of these drugs. The reduction in the size of the wheal (prick test) for histamine when comparing days -1 and +15 and -1 and +30 was 69% and 79% (astemizole), 64% and 71% (azatadine), 69% and 64% (mequitazine) and 61% and 64% (terfenadine), respectively. The difference in the mean size of the wheal in mm2 for house dust, Dermatophagoides pteronyssinus and farinae was statistically significant (p less than 0.001) except when comparing the results obtained for mequitazine on days -1 and +15. This was also the case on days -1 and +30 for terfenadine. The values of the serum IgE and specific IgE did not attain statistical significance (p greater than 0.05) in the various tests carried out. After incubation with H1 receptor antagonists an inhibition curve of the histamine release in the presence of Dermatophagoides pteronyssinus was obtained. The inhibition of this curve on day -1 was higher for terfenadine and mequitazine than for azatadine and astemizole.(ABSTRACT TRUNCATED AT 250 WORDS)

UI MeSH Term Description Entries
D007962 Leukocytes White blood cells. These include granular leukocytes (BASOPHILS; EOSINOPHILS; and NEUTROPHILS) as well as non-granular leukocytes (LYMPHOCYTES and MONOCYTES). Blood Cells, White,Blood Corpuscles, White,White Blood Cells,White Blood Corpuscles,Blood Cell, White,Blood Corpuscle, White,Corpuscle, White Blood,Corpuscles, White Blood,Leukocyte,White Blood Cell,White Blood Corpuscle
D008297 Male Males
D008925 Mites Any arthropod of the subclass ACARI except the TICKS. They are minute animals related to the spiders, usually having transparent or semitransparent bodies. They may be parasitic on humans and domestic animals, producing various irritations of the skin (MITE INFESTATIONS). Many mite species are important to human and veterinary medicine as both parasite and vector. Mites also infest plants. Acarus,Mite
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D002648 Child A person 6 to 12 years of age. An individual 2 to 5 years old is CHILD, PRESCHOOL. Children
D004341 Drug Evaluation Any process by which toxicity, metabolism, absorption, elimination, preferred route of administration, safe dosage range, etc., for a drug or group of drugs is determined through clinical assessment in humans or veterinary animals. Evaluation Studies, Drug,Drug Evaluation Studies,Drug Evaluation Study,Drug Evaluations,Evaluation Study, Drug,Evaluation, Drug,Evaluations, Drug,Studies, Drug Evaluation,Study, Drug Evaluation
D004391 Dust Earth or other matter in fine, dry particles. (Random House Unabridged Dictionary, 2d ed) House Dust,Housedust,Dust, House
D005260 Female Females
D006632 Histamine An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter. Ceplene,Histamine Dihydrochloride,Histamine Hydrochloride,Peremin
D006634 Histamine H1 Antagonists Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. Antihistamines, Classical,Antihistaminics, Classical,Antihistaminics, H1,Histamine H1 Antagonist,Histamine H1 Receptor Antagonist,Histamine H1 Receptor Antagonists,Histamine H1 Receptor Blockaders,Antagonists, Histamine H1,Antagonists, Histamine H1 Receptor,Antihistamines, Sedating,Blockaders, Histamine H1 Receptor,First Generation H1 Antagonists,H1 Receptor Blockaders,Histamine H1 Blockers,Receptor Blockaders, H1,Antagonist, Histamine H1,Classical Antihistamines,Classical Antihistaminics,H1 Antagonist, Histamine,H1 Antagonists, Histamine,H1 Antihistaminics,Sedating Antihistamines

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