title: Cetirizine inhibits the in vitro and ex vivo chemotactic response of T lymphocytes and monocytes.
abstract: We have studied the effect of a nonsedating antihistamine, cetirizine dihydrochloride, on the in vitro chemotaxis of leukocytes from human peripheral blood. We observed that 0.25 microgram/ml of cetirizine dihydrochloride in vitro significantly inhibited the chemotaxis of monocytes toward N-formyl-methionyl-leucyl-phenylalanine and leukotriene B4. Higher concentrations of cetirizine, 1.0 and 2.5 micrograms/ml, completely inhibited monocyte chemotaxis without affecting cell viability. T-lymphocyte migration was also significantly depressed but not abolished. Pyrilamine (mepyramine) was not inhibitory in equimolar concentrations. According to these in vitro observations, we extended our studies to measure monocyte and T-lymphocyte chemotaxis in an open study, where four healthy volunteers and six patients with atopic dermatitis took 10 and 20 mg/day cetirizine 3 days. We observed a reduction in ex vivo monocyte and T-lymphocyte chemotaxis toward N-formyl-methionyl-leucyl-phenylalanine and leukotriene B4 without a reduction of the blood cell count. The results were confirmed in an ensuing double-blind, placebo-controlled study of 16 healthy subjects and 14 adult patients with atopic dermatitis, where ex vivo monocyte chemotaxis was reduced or abolished during cetirizine therapy. Serum levels of the two eosinophil-derived granule proteins, eosinophilcationic protein P and eosinophil protein X, were not changed during the treatment period of 7 days. The results show that cetirizine dihydrochloride has an inhibitory effect on monocytes and T lymphocytes in vitro and ex vivo. Our findings support the clinical observations that cetirizine dihydrochloride has an antiinflammatory effect besides its H1-blocking activity.
authors.affiliation: Department of Dermatology, Marselisborg Hospital, Aarhus C., Denmark.
authors.forename: T
authors.initials: T
authors.lastname: Jinquan
authors.forename: C M
authors.initials: CM
authors.lastname: Reimert
authors.forename: B
authors.initials: B
authors.lastname: Deleuran
authors.forename: C
authors.initials: C
authors.lastname: Zachariae
authors.forename: C
authors.initials: C
authors.lastname: Simonsen
authors.forename: K
authors.initials: K
authors.lastname: Thestrup-Pedersen
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001798:Blood Proteins / Q000032:analysis; D017332:Cetirizine / Q000494:pharmacology*; D002634:Chemotaxis, Leukocyte / Q000187:drug effects*; D003876:Dermatitis, Atopic / Q000276:immunology*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D047091:Eosinophil Granule Proteins; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000187:drug effects*; D007975:Leukotriene B4 / Q000494:pharmacology; D009000:Monocytes / Q000187:drug effects; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000494:pharmacology; D015990:Placebo Effect; D011738:Pyrilamine / Q000494:pharmacology; D012260:Ribonucleases; D013601:T-Lymphocytes / Q000187:drug effects
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D001798:Blood Proteins; D047091:Eosinophil Granule Proteins; D007975:Leukotriene B4; D009240:N-Formylmethionine Leucyl-Phenylalanine; D012260:Ribonucleases; D011738:Pyrilamine; D017332:Cetirizine