Names and pronunciation
(toll-tehr′oh-deen) Detrol, Detrol LA
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Drug reference
(toll-tehr′oh-deen) Detrol, Detrol LA
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Func. class.: Overactive bladder product
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Chem. class.: Muscarinic receptor antagonist
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ACTION: Relaxes smooth muscles in urinary tract by inhibiting acetylcholine at postganglionic sites
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USES: Overactive bladder (urinary frequency, urgency), urinary inconti- nence
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CONTRAINDICATIONS: Hyper- sensitivity, uncontrolled closed-angle glaucoma, urinary retention, gastric retention Precautions: Pregnancy, breastfeeding, children, renal disease, controlled closed-angle glaucoma, bladder obstruc- tion, QT prolongation, decreased GI motility
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SIDE EFFECTS CNS: Anxiety, paresthesia, fatigue, dizzi- ness, headache; increasing dementia, memory impairment CV: Chest pain, hypertension, QT prolongation EENT: Vision abnormalities, xerophthalmia GI: Nausea, vomiting, anorexia, abdominal pain, constipation, dry mouth, dyspepsia GU: Dysuria, urinary retention, fre- quency, UTI INTEG: Rash, pruritus RESP: Bronchitis, cough, pharyngitis, upper respiratory tract infection SYST: Angioedema, Stevens-Johnson syndrome
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INTERACTIONS • Do not use in those with known hyper sensitivity to fesoterodine • Increase: QT prolongation—class IA/ III antidysrhythmics, some phenothiazines, β-agonists, local anesthetics, tricyclics, halo peridol, methadone, chloroquine, clarithromy cin, droperidol, erythromycin, pentamidine Increase: action of tolterodine—antiret- roviral protease inhibitors, macrolide antiinfectives, azole antifungals Increase: anticholinergic effect— antimuscarinics Increase: urinary frequency—diuretics Drug/Food • Food increases bioavailability of tol terodine Drug/Lab Increase: LFTs, bilirubin
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Black Box Warning: Fatal hepatic in- jury: increased LFTs, bilirubin during first 18 mo of therapy in those with autoso- mal dominant polycystic kidney disease; assess for fatigue, anorexia, right upper abdominal pain, dark urine, jaundice; if these occur, discontinue product and do not restart if cause is liver injury • Beers: avoid in older adults with de- lirium or at high risk for delirium; moni- tor for confusion, delirium frequently
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DOSAGE AND ROUTES Overactive bladder • Adult and geriatric: PO 2 mg bid; may decrease to 1 mg bid; EXT REL 4 mg/ day, may decrease to 2 mg/day if needed, max 4 mg/day Hepatic/renal dose • Adult: PO 1 mg bid (50% dose) or EXT REL 2 mg/day; CCr ≤30 mL/min, reduce by 50% CYP3A4 inhibitor dose • Adult: PO 1 mg bid; EXT REL 2 mg/day
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Available forms: Tabs 1, 2 mg; ext rel caps 2, 4 mg
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Administer: • Whole; take with liquids; do not crush, chew, or break ext rel product; without regard to meals
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Assess: • Urinary patterns: distention, nocturia, frequency, urgency, incontinence, resid- ual urine • Serious skin disorders: angioedema, Stevens-Johnson syndrome; allergic reac tions: rash; if this occurs, product should be discontinued; usually occurs in first few doses • QT prolongation: ECG, ejection frac tion; assess for chest pain, palpitations, dyspnea; may be compounded in those taking class IA/III dysrhythmics
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Evaluate: • Decreasing dysuria, frequency, noctu- ria, incontinence
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To avoid hazardous activities; dizziness may occur • Not to drink liquids before bedtime; to swallow ext rel product whole • About the importance of bladder maintenance • Not to breastfeed; to notify prescriber if pregnancy is planned or suspected • To report signs of infection, skin effects, shortness of breath, urinary retention
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PHARMACOKINETICS T Rapidly absorbed; highly protein bound; extensively metabolized by CYP2D6; a portion of the population may be poor metabolizers; excreted in urine, feces half-life 2-3.7 hr
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• Adult and geriatric: PO 2 mg bid; may decrease to 1 mg bid; EXT REL 4 mg/ day, may decrease to 2 mg/day if needed, max 4 mg/day Hepatic/renal dose
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