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Abstract:

Several antihistaminic compounds inhibit in vitro pseudocholinesterase (ChE) from several sources (human, rat, or horse plasma), pI50 ranging from 5.0 to 6.0. This inhibition is competitive with acetylcholine (ACh) and is reversible. Acetylcholinesterase (AChE) from rat brain was nonsensitive to antihistaminics even at a concentration of 4 mm. Antihistaminics do not compete with either organophosphates or quaternary ammonium compounds in inhibiting ChE. Inhibition of ChE by antihistaminics is more pronounced at alkaline pH values than at acidic or neutral pH. Administration of promethazine ip to rats at a dose of 50 mg/kg resulted in a 90% inhibition of ChE 1 hr later, while the AChE was totally nonsensitive to the inhibitor even when the dose of the antihistamine was doubled. Results were analyzed in relation to the postulated role of ChE inhibition in antihistaminic potentiation of organophosphorus intoxication. © 1975.

Registro:

Documento: Artículo
Título:Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: Analysis of its postulated role in synergizing organophosphate toxicity
Autor:Fernández, G.; Díaz Gómez, M.I.; Castro, JosA.
Filiación:Cátedra de Toxicología y Química Legal, Facultad de Ciencias Exactas, Ciudad Universitaria de Nunez, Buenos Aires, Argentina
Laboratorio de Química, Biotoxicológica, CITEFA, Zufriátegui y Varela, Villa Martelli, Pcia. de Buenos Aires, Argentina
Palabras clave:antihistaminic agent; chlorpheniramine; cholinesterase; cholinesterase inhibitor; dichlorvos; dimenhydrinate; diphenhydramine; diphenhydramine 8 bromotheophyllinate; mepyramine; mepyramine maleate; organophosphate; phenothiazine derivative; proadifen; promazine; promethazine; tripelennamine; brain; drug potentiation; drug toxicity; environmental health; horse; human; intoxication; normal human; pesticide poisoning; rat; theoretical study; Animal; Cholinesterase Inhibitors; Cholinesterases; Dichlorvos; Diphenhydramine; Drug Synergism; Female; Histamine H1 Antagonists; Horses; Human; In Vitro; Organophosphorus Compounds; Phenothiazines; Proadifen; Rats
Año:1975
Volumen:31
Número:2
Página de inicio:179
Página de fin:190
DOI: http://dx.doi.org/10.1016/0041-008X(75)90154-4
Título revista:Toxicology and Applied Pharmacology
Título revista abreviado:Toxicol. Appl. Pharmacol.
ISSN:0041008X
CODEN:TXAPA
CAS:chlorpheniramine, 132-22-9; cholinesterase, 9001-08-5; dichlorvos, 62-73-7; dimenhydrinate, 523-87-5; diphenhydramine 8 bromotheophyllinate, 3427-80-3; diphenhydramine, 147-24-0, 58-73-1; mepyramine maleate, 59-33-6; mepyramine, 6036-95-9, 91-84-9; proadifen, 302-33-0, 62-68-0; promazine, 53-60-1, 58-40-2; promethazine, 58-33-3, 60-87-7; tripelennamine, 154-69-8, 91-81-6; Cholinesterase Inhibitors; Cholinesterases, EC 3.1.1.8; Dichlorvos, 62-73-7; Diphenhydramine, 58-73-1; Histamine H1 Antagonists; Organophosphorus Compounds; Phenothiazines; Proadifen, 302-33-0
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0041008X_v31_n2_p179_Fernandez

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Citas:

---------- APA ----------
Fernández, G., Díaz Gómez, M.I. & Castro, JosA. (1975) . Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: Analysis of its postulated role in synergizing organophosphate toxicity. Toxicology and Applied Pharmacology, 31(2), 179-190.
http://dx.doi.org/10.1016/0041-008X(75)90154-4
---------- CHICAGO ----------
Fernández, G., Díaz Gómez, M.I., Castro, JosA. "Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: Analysis of its postulated role in synergizing organophosphate toxicity" . Toxicology and Applied Pharmacology 31, no. 2 (1975) : 179-190.
http://dx.doi.org/10.1016/0041-008X(75)90154-4
---------- MLA ----------
Fernández, G., Díaz Gómez, M.I., Castro, JosA. "Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: Analysis of its postulated role in synergizing organophosphate toxicity" . Toxicology and Applied Pharmacology, vol. 31, no. 2, 1975, pp. 179-190.
http://dx.doi.org/10.1016/0041-008X(75)90154-4
---------- VANCOUVER ----------
Fernández, G., Díaz Gómez, M.I., Castro, JosA. Cholinesterase inhibition by phenothiazine and nonphenothiazine antihistaminics: Analysis of its postulated role in synergizing organophosphate toxicity. Toxicol. Appl. Pharmacol. 1975;31(2):179-190.
http://dx.doi.org/10.1016/0041-008X(75)90154-4