Tolterodine drug data and news

Tolterodine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name

Tolterodine

Brand Names/Synonyms

CHEMBANK1673; Detrol; Detrol La; Tolterodina [Inn-Spanish]; Tolterodine; Tolterodine L-Tartrate; Tolterodine Tartrate; Tolterodine [Inn]; Tolterodinum [Inn-Latin]; Tolterondine Tartrate

Indication

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence)

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Description

Not Available

Pharmacology

Tolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract.

Mechanism Of Action

Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, act as competitive antagonists at muscarinic receptors. This results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.

Tolterodine News
(When available)

EAU 2006: The Star Study: Analysis of Symptom Severity and ... Apr 18, 2006
The STAR study, a double-blind, randomised study designed as a head-to-head comparison between solifenacin and tolterodine ER administered according to ... - UroToday,

EAU 2006: SUNRISE* Study Backgrounder Apr 18, 2006
3 . The head-to-head STAR study, demonstrated solifenacin 5 and 10 mg od is superior to tolterodine ER 4mg in reducing urgency episodes Solifenacin provided a ... - UroToday,

EAU 2006: Major New Study Confirms Solifenacin Effectively Treats ... Apr 18, 2006
...opted for a dose increase from 5 to 1 Omg was strikingly similar to another recent solifenacin study, the STAR Study 3 (solifenacin versus tolterodine ER 4mg). ... - UroToday,

EAU 2006: Fesoterodine in Non-Neurogenic Voiding Dysfunction ... Apr 18, 2006
After a 2-week placebo run-in, subjects were randomized to receive either placebo, 4 mg or 8mg of fesoterodine or 4mg tolterodine ER once daily for 12 weeks. ... - UroToday,

Dosage Forms

CAPSULE (SUSTAINED-RELEASE)

Drug_Category

Antispasmodics; Anti-Incontinence Agents; Genitourinary Smooth Muscle Relaxants; ATC:G04BD07

Absorption

Not Available

Interactions

-->Interactions for Tolterodine:

CYP3A4 Inhibitors: Ketoconazole, an inhibitor of the drug metabolizing enzyme CYP3A4, significantly increased plasma concentrations of tolterodine when coadministered to subjects who were poor metabolizers (see CLINICAL PHARMACOLOGY, Variability in Metabolism and Drug-Drug Interactions). For patients receiving ketoconazole or other potent CYP3A4 inhibitors such as other azole antifungals (eg, itraconazole, miconazole) or macrolide antibiotics (eg, erythromycin, clarithromycin) or cyclosporine or vinblastine, the recommended dose of DETROL LA is 2 mg daily.

Drug-Laboratory-Test Interactions

Interactions between tolterodine and laboratory tests have not been studied.

Toxicity

Not Available

Organisms Affected

Humans and other mammals

Chemical IUPAC Name

2-[3-[bis(1-methylethyl)amino]-1-phenyl-propyl]-4-methyl-phenol

Chemical Formula

C22H31NO

Molecular Weight

325.488 g/mol

Smiles String

CC1=CC(=C(C=C1)O)C(CCN(C(C)C)C(C)C)C2=CC=CC=C2

Melting Point

Not Available

Water Solubility

Not Available

State

Solid

LogP/Hphobicity

6.076

Isoelectric Point

Not Available

Biotransformation

Not Available

Half Life

1.9-3.7 hours

Protein Binding [%]

~96.3%

RxList Link

RXlist

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Drug Reference

http://www.drugs.com/cons/Tolterodine.html
http://www.rxlist.com/cgi/generic2/tolter.htm

Drug Type

Approved Drug

Accession No

APRD00146

CAS Registry Number

124937-51-5

KEGG Compound ID

C07750

PubChem ID

SID:197020

PharmGKB ID

PA451724

SwissProt ID

Not Available

GenBank ID

Not Available

Drug ID Number [DIN]

2244612