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Tolterodine
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DRUG INFO
Tolterodine
Drug Name:
Tolterodine
Indication: For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence)
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.
Drug Category: Antispasmodics; Anti-Incontinence Agents; Genitourinary Smooth Muscle Relaxants; ATC:G04BD07
Brand Names/Synonyms: CHEMBANK1673; Detrol; Detrol La; Tolterodina [Inn-Spanish]; Tolterodine; Tolterodine L-Tartrate; Tolterodine Tartrate; Tolterodine [Inn]; Tolterodinum [Inn-Latin]; Tolterondine Tartrate
Dosage Forms: CAPSULE (SUSTAINED-RELEASE)
Absorption: Not Available
Interactions:
DrugBank: Interactions for Tolterodine
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.
Chemical IUPAC Name: 2-[3-[bis(1-methylethyl)amino]-1-phenyl-propyl]-4-methyl-phenol
Chemical Formula: C22H31NO
Half Life: 1.9-3.7 hours
Drug Type: Approved Drug
# Accession No: APRD00146
CAS Registry Number: 124937-51-5
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Tolterodine News
(When available)
DETROL LA Significantly Reduced Daytime and Nighttime Urinary ... Dec 15, 2005
Market Wire (press release) NEW YORK, NY -- (MARKET WIRE) -- 12/15/2005 -- Pfizer Inc's Detrol® LA (tolterodine tartrate extended release capsules) significantly improved lower urinary ...
FINDING RIGHT TREATMENT FOR OVERACTIVE BLADDER OFTEN REQUIRES A ... Dec 12, 2005
Charlotte Sun-Herald, ...dashing for years. My doctor put me on Detrol, which did not work and gave me the worst dry mouth I have ever experienced. He recently ...
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