TOLTERODINE TARTRATE
| TOLTERODINE TARTRATe (tol-ter'o-deen tar'trate) Detrol, Detrol LA Classifications: anticholinergic agent; muscarinic receptor antagonist; Therapeutic: anticholinergic agent; antimuscarinic agent; muscarinic receptor antagonist Prototype: Atropine Pregnancy Category: C |
Availability
1 mg, 2 mg tablets; 2 mg, 4 mg sustained release
Action
Selective muscarinic urinary bladder receptor antagonist. Reduces urinary incontinence, urgency, and frequency.
Therapeutic Effect
Controls urinary bladder incontinence by controlling contractions.
Uses
Overactive bladder (urinary frequency, urgency, urge incontinence).
Contraindications
Gastric retention; hypersensitivity to tolterodine; uncontrolled narrow-angle glaucoma; urinary retention; pregnancy (category C); lactation.
Cautious Use
Cardiovascular disease; liver disease; controlled narrow-angle glaucoma; urinary retention; severe hepatic impairment; obstructive GI disease; obstructive uropathy; paralytic ileus or intestinal atony; renal impairment; ulcerative colitis.
Route & Dosage
| Overactive Bladder Adult: PO 2 mg b.i.d. or 4 mg sustained release q.d. Hepatic Impairment May decrease to 1 mg b.i.d. or 2 mg sustained release q.d. in those with significantly reduced liver function. |
Administration
Oral- Do not crush or chew sustained release tablets. These must be swallowed whole.
- Do not give doses >1 mg b.i.d. to those with significantly reduced liver function or concurrently receiving macrolide antibiotics, azole antifungal agents, or other cytochrome P450 3A4 inhibitors.
- Store at 20°–25° C (68°–77° F) in a tightly closed container.
Adverse Effects (≥1%)
Body as a Whole: Back pain, fatigue, flu-like syndrome, falls, arthralgia, weight gain. CNS: Headache, paresthesias, vertigo, dizziness, nervousness, somnolence. CV: Chest pain, hypertension. GI: Dry mouth, dyspepsia, constipation, abdominal pain, diarrhea, flatulence, nausea, vomiting. Urogenital: Dysuria, micturition frequency, urinary retention, UTI. Respiratory: Bronchitis, cough, pharyngitis, rhinitis, sinusitis, URI. Skin: Pruritus, rash, erythema, dry skin. Special Senses: Dry eyes, vision abnormalities.Interactions
Drug: Additive anticholinergic effects with amantadine, amoxapine, bupropion, clozapine, cyclobenzaprine, disopyramide, maprotiline, olanzapine, orphenadrine, sedating h1-blockers, phenothiazines, tricyclic antidepressants. Increased effects with clarithromycin, cyclosporine, erythromycin, itraconazole, or ketoconazole. Food: Grapefruit juice may increase tolterodine levels in some patients.Pharmacokinetics
Absorption: 77% absorbed, significantly decreased with food. Peak: 1–2 h. Distribution: 96% protein bound. Metabolism: In liver by cytochrome P450 2D6 enzymes to active metabolite. Elimination: 77% in urine, 17% in feces. Half-Life: 1.9–3.7 h.Nursing Implications
Assessment & Drug Effects
- Monitor intraocular pressure more frequently with glaucoma patients.
- Monitor vital signs carefully (HR and BP), especially in those with cardiovascular disease.
Patient & Family Education
- Notify physician promptly if you experience eye pain, rapid heartbeat, difficulty breathing, skin rash or hives, confusion, or incoordination.
- Report blurred vision, sensitivity to light, and dry mouth (all common adverse effects) to physician if bothersome.
- Avoid the use of alcohol or OTC antihistamines.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug