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Tolterodine tartrate
Tolterodine tartrate (Detrol)
Tolterodine tartrate
(tohl-TER-oh-deen)
Pregnancy Category: C Detrol (Rx)

Classification: Urinary tract drug

Action/Kinetics: Acts as a competitive muscarinic receptor antagonist in the bladder to cause increased bladder control. Metabolized by first pass effect in the liver to the active 5-hydroxymethyl derivative, which has similar activity as tolterodine. Rapidly absorbed with peak serum levels within 1-2 hr. Food increases bioavialability. Highly bound to plasma proteins. Excreted in the urine.

Uses: Treat overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence.

Contraindications: Urinary retention, gastric retention, uncontrolled narrow-angle glaucoma, lactation.

Special Concerns: Use with caution in renal impairment, in bladder outflow obstruction, in GI obstructive disorders (e.g., pyloric stenosis), and in those being treated for narrow-angle glaucoma. Doses greater than 1 mg b.i.d. not to be given to those with significantly decreased hepatic function. Safety and efficacy have not been determined in children.

Side Effects: GI: Dry mouth (common), dyspepsia, constipation, abdominal pain, N&V;, diarrhea, flatulence. CNS: Headache, vertigo, dizziness, somnolence, paresthesia, nervousness. Respiratory: URI, bronchitis, coughing, pharyngitis, rhinitis, sinusitis. Dermatologic: Rash, erythema, dry skin, pruritus. GU: UTI, dysuria, micturition frequency, urinary retention. Ophthalmic: Abnormalities with vision, including accommodation. Musculoskeletal: Arthralgia, back pain, chest pain. Miscellaneous: Fatigue, flu-like symptoms, infection, hypertension, weight gain, fall, fungal infection.

Overdose Management: Symptoms: Significant anticholinergic symptoms. Treatment: Symptomatic. Monitor ECG.

Drug Interactions: Clarithromycin / Tolterodine plasma levels R/T liver metabolism; do not give tolterodine >1 mg b.i.d. Erythromycin / Tolterodine plasma levels R/T liver metabolism; do not give tolterodine >1 mg b.i.d. Itraconazole / Tolterodine plasma levels R/T liver metabolism; do not give tolterodine >1 mg b.i.d. Ketoconazole / Tolterodine plasma levels R/T liver metabolism; do not give tolterodine >1 mg b.i.d. Miconazole / Tolterodine plasma levels R/T liver metabolism; do not give tolterodine >1 mg b.i.d.

How Supplied: Tablets: 1 mg, 2 mg

Dosage
•Tablets Treat overactive bladder.
Initial: 2 mg b.i.d. Dose may be lowered to 1 mg b.i.d. based on individual response and side effects. Adjust dose to 1 mg b.i.d. in those with significantly reduced hepatic funtion or who are currently taking drugs that are inhibitors of cytochrome P450 3A4 (see Drug Interactions).