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Trospium

Trospium structure

Trospium 

structure
  • CAS No:

    47608-32-2

  • Formula:

    C25H30NO3

  • Chemical Name:

    Trospium

  • Synonyms:

    Spiro[8-azoniabicyclo[3.2.1]octane-8,1′-pyrrolidinium],3-[(2-hydroxy-2,2-diphenylacetyl)oxy]-,(1α,3α,5α)-;Spiro[8-azoniabicyclo[3.2.1]octane-8,1′-pyrrolidinium],3-[(hydroxydiphenylacetyl)oxy]-,(1α,3α,5α)-;(1α,3α,5α)-3-[(2-Hydroxy-2,2-diphenylacetyl)oxy]spiro[8-azoniabicyclo[3.2.1]octane-8,1′-pyrrolidinium];Trospium;Trospium cation;112726-87-1;50857-35-7;1001382-35-9;1008557-44-5

Description

Trospium is a carboxylic ester resulting from the formal condensation of the carboxy group of hydroxy(diphenyl)acetic acid with the hydroxy group of (1S,3R,5R)-3-hydroxy-8lambda(5)-azaspiro[bicyclo[3.2.1]octane-8,1'-pyrrolidin]-8-ylium. Its chloride salt is used to treat overactive bladder. It has a role as a muscarinic antagonist and an antispasmodic drug. It is a carboxylic ester, an azabicycloalkane, a tertiary alcohol and a quaternary ammonium ion.|Trospium is an antispasmodic agent used to treat the symptoms of overactive bladder, a condition that causes the bladder muscles to contract uncontrollably. An overactive bladder leads to an increased urge to urinate, frequent urination, and sometimes, loss of control over urination. Trospium is manufactured by Indevus Pharmaceutical Inc. and was granted FDA approval in 2007.|Trospium is a Cholinergic Muscarinic Antagonist. The mechanism of action of trospium is as a Cholinergic Muscarinic Antagonist.|Trospium is an antispasmotic and anticholinergic agent used to treat urinary incontinence and overactive bladder syndrome. Trospium has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.

Trospium Basic Attributes

392.5 g/mol

392.22256882 g/mol

T4Y8ORK057

DTXSID6048337

G04BD09|G - Genito urinary system and sex hormones

Characteristics

46.5 Ų

Toxicity

Like other anticholinergic agents, trospium has not been linked to episodes of liver enzyme elevations or clinically apparent liver injury. A major reason for its safety may relate to the low daily dose. Trospium is probably metabolized in the liver but its metabolic pathways have not been defined.

50-85%

Drug Information

For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency, detrusor instability and frequency of micturition.|FDA Label

Trospium is an antispasmotic and anticholinergic agent used to treat urinary incontinence and overactive bladder syndrome. Trospium has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.

Anticholinergic Agents

Trospium is an antispasmodic, antimuscarinic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. According to receptor assays, it displays higher affinity towards muscarininc receptors compared to nicotinic receptors at therapeutic concentrations.

9.6%|After administration of oral 14C-trospium chloride, the majority of the dose (85.2%) was recovered in feces and a smaller amount (5.8% of the dose) was recovered in urine; 60% of the radioactivity excreted in urine was unchanged trospium. Trospium mainly undergoes elimination via active tubular secretion, as indicated by the mean renal clearance of 29.07 L/hour, which is about 4-fold higher than average glomerular filtration rate. Trospium is metabolized by ester hydrolysis and excreted by the kidneys by a combination of tubular secretion and glomerular filtration.|395 ± 140 L|Renal cl=29.07 L/hour

Not fully defined

20 hours

Trospium antagonizes the effect of acetylcholine on muscarinic receptors in cholinergically innervated organs. Its parasympatholytic action reduces the tonus of smooth muscle in the bladder.

Computed Properties

Molecular Weight:392.5
XLogP3:4.4
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:5
Exact Mass:392.22256882
Monoisotopic Mass:392.22256882
Topological Polar Surface Area:46.5
Heavy Atom Count:29
Formal Charge:1
Complexity:553
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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