Trospium

Thuốc Gốc

Small Molecule

CAS: 10405-02-4

ATC: G04BD09

ĐG : Allergan Inc. , http://www.allergan.com

CTHH: C₂₅H₃₀NO₃

PTK: 392.5106

Trospium is a urinary antispasmodic. It is sold under the brand name Sanctura in the US, and as Trosec in Canada. [Wikipedia]

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₂₅H₃₀NO₃

Phân tử khối

392.5106

Monoisotopic mass

392.222568831

InChI

InChI=1S/C25H30NO3/c27-24(25(28,19-9-3-1-4-10-19)20-11-5-2-6-12-20)29-23-17-21-13-14-22(18-23)26(21)15-7-8-16-26/h1-6,9-12,21-23,28H,7-8,13-18H2/q+1

InChI Key

InChIKey=OYYDSUSKLWTMMQ-UHFFFAOYSA-N

IUPAC Name

3-[(2-hydroxy-2,2-diphenylacetyl)oxy]-8$l^{5}-azaspiro[bicyclo[3.2.1]octane-8,1'-pyrrolidin]-8-ylium

Traditional IUPAC Name

3-[(2-hydroxy-2,2-diphenylacetyl)oxy]-8$l^{5}-azaspiro[bicyclo[3.2.1]octane-8,1'-pyrrolidin]-8-ylium

SMILES

OC(C(=O)OC1CC2CCC(C1)[N+]21CCCC1)(C1=CC=CC=C1)C1=CC=CC=C1

Độ hòa tan

6.68e-05 g/l

logP

-0.5

logS

-6.8

pKa (strongest acidic)

11.05

pKa (Strongest Basic)

-4.5

PSA

46.53 Å²

Refractivity

124.04 m³·mol^-1

Polarizability

43.18 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Dược Lực Học : Trospium is an antispasmodic, antimuscarinic agent indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Receptor assays showed that trospium has negligible affinity for nicotinic receptors as compared to muscarinic receptors at concentrations obtained from therapeutic doses.

Cơ Chế Tác Dụng : Trospium is a urinary antispasmodic. It is sold under the brand name Sanctura in the US, and as Trosec in Canada. [Wikipedia] 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.

Dược Động Học :

▧ Absorption :
9.6%
▧ Volume of Distribution :
* 395 ± 140 L
▧ Protein binding :
50-85%
▧ Metabolism :
Not fully defined
▧ Route of Elimination :
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. The mean renal clearance for trospium (29.07 L/hour) is 4-fold higher than average glomerular filtration rate, indicating that active tubular secretion is a major route of elimination for trospium. SANCTURA ® is metabolized by ester hydrolysis and excreted by the kidneys by a combination of tubular secretion and glomerular filtration.
▧ Half Life :
20 hours
▧ Clearance :
* Renal cl=29.07 L/hour

Chỉ Định : For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency, detrusor instability and frequency of micturition.

Tương Tác Thuốc :

Acetophenazine Trospium and Acetophenazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Alimemazine Trospium and Trimeprazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Amitriptyline Trospium and Amitriptyline, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Amoxapine Trospium and Amoxapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Atropine Trospium and Atropine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Azelastine Trospium and Azelastine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Benzatropine Trospium and Benztropine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Biperiden Trospium and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Bromodiphenhydramine Trospium and Bromodiphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Brompheniramine Trospium and Brompheniramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Carbinoxamine Trospium and Carbinoxamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Chlorphenamine Trospium and Chlorpheniramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Chlorpromazine Trospium and Chlorpromazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Clemastine Trospium and Clemastine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Clidinium Trospium and Clidinium, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Clomipramine Trospium and Clomipramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Clozapine Trospium and Clozapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Cyclizine Trospium and Cyclizine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Cyclobenzaprine Trospium and Cyclobenzaprine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Cyclopentolate Trospium and Cyclopentolate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Cyproheptadine Trospium and Cyproheptadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Darifenacin Trospium and Darifenacin, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Desipramine Trospium and Desipramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Desloratadine Trospium and Desloratadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Dexbrompheniramine Trospium and Dexbrompheniramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Dicyclomine Trospium and Dicyclomine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Dimenhydrinate Trospium and Dimenhydrinate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Diphenhydramine Trospium and Diphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Donepezil The therapeutic effects of the anticholinergic, Trospium, and/or the acetylcholinesterase inhibitor (central), Donepezil, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
Doxepin Trospium and Doxepin, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Doxylamine Trospium and Doxylamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Dronabinol Anticholinergics, such as Trospium, may increase the tachycardic effect of cannabinoids such as Marinol. Close monitoring of cardiovascular effects is recommended.
Droperidol Trospium and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Fexofenadine Trospium and Fexofenadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Flavoxate Trospium and Flavoxate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Flupentixol Trospium and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Fluphenazine Trospium and Fluphenazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Galantamine The therapeutic effects of the anticholinergic, Trospium, and/or the acetylcholinesterase inhibitor (central), Galantamine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
Glycopyrrolate Trospium and Glycopyrrolate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Haloperidol Trospium and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Homatropine Methylbromide Trospium and Homatropine Methylbromide, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Hydroxyzine Trospium and Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Hyoscyamine Trospium and Hyoscyamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Imipramine Trospium and Imipramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Ipratropium bromide Trospium and Ipratropium, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Isocarboxazid Trospium and Isocarboxazid, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Ketotifen Trospium and Ketotifen, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Loratadine Trospium and Loratadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Loxapine Trospium and Loxapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Maprotiline Trospium and Maprotiline, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Meclizine Trospium and Meclizine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Mepenzolate Trospium and Mepenzolate, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Mesoridazine Trospium and Mesoridazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Methantheline Trospium and Methantheline, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Methylscopolamine bromide Trospium and Methylscopolamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Moclobemide Trospium and Moclobemide, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Molindone Trospium and Molindone, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Nabilone Anticholinergics, such as Trospium, may increase the tachycardic effect of cannabinoids such as Nabilone. Close monitoring of cardiovascular effects is recommended.
Nortriptyline Trospium and Nortriptyline, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Olanzapine Trospium and Olanzapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Orphenadrine Trospium and Orphenadrine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Oxybutynin Trospium and Oxybutynin, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Perphenazine Trospium and Perphenazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Phenelzine Trospium and Phenelzine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Phenindamine Trospium and Phenindamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Pimozide Trospium and Pimozide, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Pizotifen Trospium and Pizotifen, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Potassium Chloride The ulcerative effects of solid oral dosage forms of KCl may be enhanced by Trospium, an anticholinergic. Anticholinergics slow gastric emptying, increasing the contact time between the gastrointestinal mucosa and KCl. Prolonged exposure to KCl increases the risk of gastric and intestinal irritation and ulceration. Solid oral dosage forms of KCl should be avoided; alternatives include liquid or effervescent potassium preparations.
Pramlintide The anticholinergic effects of Trospium may be enhanced by Pramlintide. Additive effects of reduced GI motility may occur. Pramlintide slows gastic emptying and should not be used with drugs that alter GI motility (e.g. anticholinergics). Consider alternative treatments or use caution during concomitant therapy.
Prochlorperazine Trospium and Prochlorperazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Procyclidine Trospium and Procyclidine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Promethazine Trospium and Promethazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Propantheline Trospium and Propantheline, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Protriptyline Trospium and Protriptyline, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Quetiapine Trospium and Quetiapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Risperidone Trospium and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Rivastigmine The therapeutic effects of the anticholinergic, Trospium, and/or the acetylcholinesterase inhibitor (central), Rivastigmine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
Scopolamine Trospium and Scopolamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Secretin The stimulatory effect of Secretin may be reduced by anticholinergics such as Trospium. Concomitant use of Secretin and drugs with substantial anticholinergic effects should be avoided. If combination therapy must be used, Secretin efficacy should be closely monitored.
Solifenacin Trospium and Solifenacin, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Trospium, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Thioridazine Trospium and Thioridazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Thiothixene Trospium and Thiothixene, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Tiotropium Trospium and Tiotropium, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Tolterodine Trospium and Tolterodine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Tranylcypromine Trospium and Tranylcypromine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trifluoperazine Trospium and Trifluoperazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trihexyphenidyl Trospium and Trihexyphenidyl, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trimethobenzamide Trospium and Trimethobenzamide, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trimipramine Trospium and Trimipramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Trospium and Triprolidine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Zuclopenthixol Trospium and Zuclopenthixol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.

Liều Lượng & Cách Dùng : Tablet - Oral

Dữ Kiện Thương Mại

Giá thị trường

Biệt dược thương mại : Sanctura 20 mg tablet

Giá bán buôn : USD >3.12

Đơn vị tính : tablet
Biệt dược thương mại : Sanctura xr 60 mg capsule

Giá bán buôn : USD >5.02

Đơn vị tính : capsule
Biệt dược thương mại : Sanctura XR 60 mg 24 Hour Capsule

Giá bán buôn : USD >5.17

Đơn vị tính : capsule

Nhà Sản Xuất

Công ty :

Sản phẩm biệt dược : Flotros
Công ty :

Sản phẩm biệt dược : Regurin
Công ty :

Sản phẩm biệt dược : Sanctura
Công ty :

Sản phẩm biệt dược : Spasmex
Công ty :

Sản phẩm biệt dược : Spasmolyt
Công ty :

Sản phẩm biệt dược : Spasmoplex
Công ty :

Sản phẩm biệt dược : Tropez OD
Công ty :

Sản phẩm biệt dược : Trosec

Đóng gói

Công ty : Allergan Inc.

Website : http://www.allergan.com
Công ty : Catalent Pharma Solutions

Website : http://www.catalent.com
Công ty : Endo Pharmaceuticals Inc.

Website : http://www.endo.com
Công ty : Esprit Pharma Inc.
Công ty : Madaus GmbH

Website : http://www.madaus.de
Công ty : Murfreesboro Pharmaceutical Nursing Supply

Website : http://www.unitdosesupply.com
Công ty : Odyssey Pharmaceuticals Inc.
Công ty : Redpharm Drug

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00209

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5596

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506398

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D01103

ChemSpider

http://www.chemspider.com/Chemical-Structure.5394.html

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0023-3513-60

PharmGKB

http://www.pharmgkb.org/drug/PA164748976

Wikipedia

http://en.wikipedia.org/wiki/Trospium

RxList

http://www.rxlist.com/cgi/generic/sanctura.htm

Drugs.com

http://www.drugs.com/cdi/trospium.html

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