Trospium Chloride

Title: Trospium Chloride
CAS Registry Number: 10405-02-4
CAS Name: (1a,3b,5a)-3-[(Hydroxydiphenylacetyl)oxy]spiro[8-azoniabicyclo[3.2.1]octane-8,1¢-pyrrolidinium] chloride
Additional Names: 3a-hydroxyspiro[1aH,5aH-nortropane-8,1¢-pyrrolidinium] chloride benzilate; azoniaspiro(3a-benziloyloxynortropane-8,1¢-pyrrolidine) chloride; azoniaspiro(3a-diphenylglycoloyloxynortropan-8,1¢-pyrrolidine) chloride; 3a-benziloyloxyspiro(nortropane-8,1¢-pyrrolidinium) chloride
Trademarks: Regurin (Galen); Relaspium (Isei); Sanctura (Indevus); Spasmex (Pfleger); Spasmolyt (Madaus)
Molecular Formula: C25H30ClNO3
Molecular Weight: 427.96
Percent Composition: C 70.16%, H 7.07%, Cl 8.28%, N 3.27%, O 11.22%
Literature References: Tropine derivative with anticholinergic activity. Prepn: NL 6402155; R. Pfleger et al., US 3480626 (1964, 1969 both to Pfleger); H. Bertholdt et al., Arzneim.-Forsch. 17, 719 (1967). Pharmacology and toxicology in animals: H. Antweiler et al., ibid. 16, 1581 (1966). Inhibition of gastric motility and acid secretion in humans: G. Lux, P. Frühmorgen, Fortschr. Med. 96, 2113 (1978). Fluorimetric determn in plasma and urine: G. Schladitz-Keil et al., J. Chromatogr. 345, 99 (1985). Bioavailability: eidem, Arzneim.-Forsch. 36, 984 (1986). Clinical trial in bladder hyper-reflexia: H. Madersbacher et al., Br. J. Urol. 75, 452 (1995). Review in overactive bladder: N. R. Zinner, Expert Opin. Pharmacother. 6, 1409-1420 (2005).
Properties: Crystals from ethanol-ether, mp 255-257° (dec). Soly in water: ~1 g/2 ml. LD50 in mice (mg/kg): 12.3 i.v. (Antweiler).
Melting point: mp 255-257° (dec)
Toxicity data: Soly in water: ~1 g/2 ml. LD50 in mice (mg/kg): 12.3 i.v. (Antweiler)
Therap-Cat: Antispasmodic; in treatment of urinary incontinence.
Keywords: Antimuscarinic; Antispasmodic.
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