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

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