Clidiniumbromid Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R22:Gesundheitssch?dlich beim Verschlucken.
S-S?tze Betriebsanweisung:
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Clidinium is a gastrointestinal muscarinic receptor antagonist (K
i = 3 nM against [
3H]quinuclidinyl benzilate binding in rat colonic enterocytes). Administration of clidinium, at a dose of 1 mg/kg, slows intestinal transit and induces constipation in mice. This clidinium-induced constipation induces serum hyperammonemia and decreases clonic, myoclonic, and tonic seizure thresholds in a murine pentylenetetrazole-induced epilepsy model.
Chemische Eigenschaften
White Crystalline Solid
Verwenden
Clidinium inhibits muscarinic action of acetylcholine on postganglionic parasympathetic
effector regions. It is used for treating stomach ulcers.
Application
The United States Food and Drug Administration (FDA) approved the use of this combination, clidinium/chlordiazepoxide, as an adjunct therapy for the treatment of peptic ulcer, irritable bowel syndrome (IBS), and acute enterocolitis.
Definition
ChEBI: The bromide salt of clinidium. It is used for the symptomatic treatment of peptic ulcer disease and also to help relieve abdominal or stomach spasms or cramps due to colicky abdominal pain, diverticulitis, and irritable bowel syndrome.
Allgemeine Beschreibung
Clidinium bromide, 3-hydroxy-1-methylquinuclidinium bromide benzilate (Quarzan),is a white or nearly white, almost odorless, crystalline powderthat is optically inactive. It is soluble in water and alcohol butonly very slightly soluble in ether and benzene.
Clinical Use
This anticholinergic agent is marketed alone and in combinationwith the minor tranquilizer chlordiazepoxide (Librium)in a product known as Librax. The rationale of the combinationfor the treatment of GI complaints is the use of an anxiety-reducing agent together with an anticholinergic agent,based on the recognized contribution of anxiety to the developmentof the diseased condition. It is suggested for pepticulcer, hyperchlorhydria, ulcerative or spastic colon, anxietystates with GI manifestations, nervous stomach, irritable orspastic colon, and others. Clidinium bromide is contraindicatedin glaucoma and other conditions that may be aggravatedby the parasympatholytic action, such as prostatic hypertrophyin elderly men, which could lead to urinary retention.
Synthese
Clidinium, 3-benzyloyloxy-1-methylcynuclidinium bromide (14.1.19), is
synthesized by reacting 3-hydroxycynuclidine (14.1.17) with the of benzilic acid chloride
producing the ester (14.1.18), which if further alkylated at the nitrogen atom by methylbromide, giving clidinium (14.1.19) [16].
Clidiniumbromid Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
