Biomaterial Database

The inhibitory effect of glycopyrrolate on human plasma-cholinesterase. 1985

E K Zsigmond, and A P Winnie, and E Barabas, and X Y Wang

The in vitro inhibitory effect of glycopyrrolate and atropine on the hydrolysis of benzoylcholine at 50.0 microM concentration was determined in the plasma of 6 healthy volunteers at 37 degrees C and at 240 nm by the ultraviolet spectrophotometric method of Kalow. The 50 per cent inhibitory concentration (I50) of glycopyrrolate was found to be 1.0 mM and the I50 of atropine was 0.9 mM. This inhibitory effect of glycopyrrolate and atropine is moderate but its interaction with the in vivo hydrolysis of succinylcholine or that of ester-type of local anaesthetics in patients should be further studied. Although both glycopyrrolate and atropine inhibit PChE to the same extent, glycopyrrolate should be utilized in patients in whom inhibition of brain PChE or central effects ought to be avoided, since glycopyrrolate does not penetrate the blood-brain barrier.

UI	MeSH Term	Description	Entries
D011759	Pyrrolidines	Compounds also known as tetrahydropyridines with general molecular formula (CH2)4NH.	Tetrahydropyridine,Tetrahydropyridines
D002800	Cholinesterase Inhibitors	Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.	Acetylcholinesterase Inhibitor,Acetylcholinesterase Inhibitors,Anti-Cholinesterase,Anticholinesterase,Anticholinesterase Agent,Anticholinesterase Agents,Anticholinesterase Drug,Cholinesterase Inhibitor,Anti-Cholinesterases,Anticholinesterase Drugs,Anticholinesterases,Cholinesterase Inhibitors, Irreversible,Cholinesterase Inhibitors, Reversible,Agent, Anticholinesterase,Agents, Anticholinesterase,Anti Cholinesterase,Anti Cholinesterases,Drug, Anticholinesterase,Drugs, Anticholinesterase,Inhibitor, Acetylcholinesterase,Inhibitor, Cholinesterase,Inhibitors, Acetylcholinesterase,Inhibitors, Cholinesterase,Inhibitors, Irreversible Cholinesterase,Inhibitors, Reversible Cholinesterase,Irreversible Cholinesterase Inhibitors,Reversible Cholinesterase Inhibitors
D002802	Cholinesterases		Acylcholineacylhydrolase,Cholase,Cholinesterase
D006024	Glycopyrrolate	A muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.	Glycopyrronium,Glycopyrronium Bromide,NVA 237,NVA-237,NVA237,Pyrrolidinium, 3-((cyclopentylhydroxyphenylacetyl)oxy)-1,1-dimethyl-, bromide,Bromide, Glycopyrronium
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D006868	Hydrolysis	The process of cleaving a chemical compound by the addition of a molecule of water.
D001285	Atropine	An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.	AtroPen,Atropin Augenöl,Atropine Sulfate,Atropine Sulfate Anhydrous,Atropinol,Anhydrous, Atropine Sulfate,Augenöl, Atropin,Sulfate Anhydrous, Atropine,Sulfate, Atropine
D001588	Benzoylcholine	The benzoic acid ester of choline.
D066298	In Vitro Techniques	Methods to study reactions or processes taking place in an artificial environment outside the living organism.	In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In