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Detrol

Detrol - General Information

Detrol is an antimuscarinic drug that is used to treat urinary incontinence. Detrol acts on M2 and M3 subtypes of muscarinic receptors.

 

Pharmacology of Detrol

Detrol 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. Detrol 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.

 

Detrol for patients

 

Detrol Interactions

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.

 

Detrol Contraindications

DETROL LA Capsules are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. DETROL LA is also contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients.

 

Additional information about Detrol

Detrol Indication: For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).
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 Interactions: Not Available
Food Interactions: Take with food.
Generic Name: Tolterodine
Synonyms: Tolterodina [Inn-Spanish]; Tolterodine L-Tartrate; Tolterodine Tartrate; Tolterodine [Inn]; Tolterodinum [Inn-Latin]; Tolterondine Tartrate
Drug Category: Antispasmodics; Anti-Incontinence Agents; Genitourinary Smooth Muscle Relaxants
Drug Type: Small Molecule; Approved; Investigational

Other Brand Names containing Tolterodine: Detrol; Detrol LA;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Approximately 96.3%.
Biotransformation: Not Available
Half Life: 1.9-3.7 hours
Dosage Forms of Detrol: Tablet Oral
Capsule, extended release Oral
Chemical IUPAC Name: 2-[(1S)-3-(di(propan-2-yl)amino)-1-phenylpropyl]-4-methylphenol
Chemical Formula: C22H31NO
Tolterodine on Wikipedia: https://en.wikipedia.org/wiki/Tolterodine
Organisms Affected: Humans and other mammals