Biomaterial Database

Pharmacological modulation of cutaneous reactivity to histamine: a double-blind acute comparative study between cetirizine, terfenadine and astemizole. 1989

L Ghys, and J P Rihoux

UCB sa, Chemin du Foriest, Braine l'Alleud, Belgium.

In a double-blind study performed in 81 healthy volunteers, 10 mg cetirizine and 60 mg terfenadine given orally in a single administration significantly inhibited skin reactivity to histamine. Astemizole (10 mg) was completely ineffective. The inhibitory effect of cetirizine was potent and regular whereas 6/28 (21%) volunteers did not respond to terfenadine. The difference observed between cetirizine and terfenadine might be due to differences in the metabolism of the two drugs after administration: terfenadine is rapidly and extensively metabolized whereas cetirizine is directly active without the need for biotransformation and, indeed is poorly metabolized.

UI	MeSH Term	Description	Entries
D004311	Double-Blind Method	A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.	Double-Masked Study,Double-Blind Study,Double-Masked Method,Double Blind Method,Double Blind Study,Double Masked Method,Double Masked Study,Double-Blind Methods,Double-Blind Studies,Double-Masked Methods,Double-Masked Studies,Method, Double-Blind,Method, Double-Masked,Methods, Double-Blind,Methods, Double-Masked,Studies, Double-Blind,Studies, Double-Masked,Study, Double-Blind,Study, Double-Masked
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
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D006919	Hydroxyzine	A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.	2-(2-(4-((4-Chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)ethanol,Atarax,Durrax,Hydroxyzine Dihydrochloride,Hydroxyzine Hydrochloride,Hydroxyzine Pamoate,Orgatrax,Vistaril,Pamoate, Hydroxyzine
D000328	Adult	A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available.	Adults
D001559	Benzhydryl Compounds	Compounds which contain the methyl radical substituted with two benzene rings. Permitted are any substituents, but ring fusion to any of the benzene rings is not allowed.	Diphenylmethyl Compounds,Compounds, Benzhydryl,Compounds, Diphenylmethyl
D001562	Benzimidazoles	Compounds with a BENZENE fused to IMIDAZOLES.
D012867	Skin	The outer covering of the body that protects it from the environment. It is composed of the DERMIS and the EPIDERMIS.
D016589	Astemizole	Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.	Alermizol,Astemina,Astemizol Alonga,Astemizol Ratiopharm,Astesen,Emdar,Esmacen,Fustermizol,Hismanal,Histaminos,Hubermizol,Laridal,Paralergin,R-43-512,Retolen,Rifedot,Rimbol,Romadin,Simprox,Urdrim,Alonga, Astemizol,R 43 512,R43512,Ratiopharm, Astemizol