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
Synonyms: 3a-hydroxyspiro[1a
H,5a
H-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.