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Pronunciation: TROSE-pee-um KLOR-ide
- Tablets 20 mg
- Tablets, extended-release 60 mg
Antagonizes effect of acetylcholine on muscarinic receptors in cholinergically innervated organs. Its parasympatholytic action reduces tonus of smooth muscle in the bladder.
Less than 10% absorbed after oral dose (bioavailability 9.6%). C max occurs 5 to 6 h postdose. Dose increases from 20 mg to 40 mg or 60 mg result in an increase in C max of 3- or 4-fold, respectively. There is a diurnal variability with a decrease in C max and AUC of up to 59% and 33%, respectively, for evening compared with morning doses. Because high-fat meals reduce absorption, it is recommended that trospium be taken at least 1 h before meals or on an empty stomach.Extended-release
Following a single 60 mg dose, C max is 2 ng/mL; T max is 5 h.
Vd is 395 L after a 20 mg dose. Protein binding is 50% to 85%.
Of 10% absorbed, metabolites account for about 40% of excreted dose. Hypothesized metabolic pathway is ester hydrolysis with subsequent conjugation of benzylic acid.
Plasma t ½ is approximately 20 h. Majority of dose (85.2%) recovered in feces and 5.8% in urine.Extended-release
Following a single 60 mg dose, t ½ is 35 h.
Special PopulationsRenal Function Impairment
In patients with severe renal function impairment, there is a 4.5- and 2-fold increase in mean AUC and C max , respectively, and prolonged elimination t ½ .Hepatic Function Impairment
In patients with mild or moderate hepatic function impairment, the C max increased 12% and 63%, respectively. There is no information regarding the effect of severe hepatic function impairment on the pharmacokinetics.Elderly
Pharmacokinetics were similar in elderly (65 yr of age and older) patients compared with younger (younger than 65 yr of age) patients.Gender
Pharmacokinetic data are conflicting.Race
Pharmacokinetics have not been studied.
Indications and Usage
Treatment of overactive bladder with symptoms of urinary incontinence, urgency, and urinary frequency.
Patients with or at risk of urinary retention; gastric retention; uncontrolled narrow-angle glaucoma; hypersensitivity to any component of product.
Dosage and AdministrationAdults
PO Immediate-release: 20 mg twice daily on an empty stomach or at least 1 h before meals.
PO Extended-release: 60 mg daily in the morning on an empty stomach, at least 1 h before a meal.Severe Renal Function Impairment (CrCl less than 30 mL/min)
PO Immediate-release: 20 mg once daily at bedtime.
Extended-release: Do not administer to patients with severe renal function impairment (ie, CrCl less than 30 mL/min).Elderly (75 yr of age and older)
PO Titrate dosage down to 20 mg once daily based on tolerability.
Store at controlled room temperature (68° to 77°F).
Do not consume within 2 h of taking trospium. In addition, risk of drowsiness may be enhanced.Anticholinergics
Additive effects, leading to increased dry mouth, constipation, and other anticholinergic effects.Drugs eliminated by active tubular secretion (eg, metformin, morphine, pancuronium, procainamide, tenofovir, vancomycin)
Serum concentrations of these agents as well as of trospium may be increased.
Laboratory Test Interactions
None well documented.
Tachycardia (less than 2%); chest pain, hypertensive crisis, palpitations, supraventricular tachycardia, syncope (postmarketing).
Headache (4%); fatigue (2%); delirium, hallucinations (postmarketing).
Rash (less than 2%); Stevens-Johnson syndrome (postmarketing).
Nasopharyngitis (3%); dry eyes (2%); nasal dryness (1%); abnormal vision (postmarketing).
Dry mouth (20%); constipation (10%); flatulence, upper abdominal pain (2%); abdominal distention, aggravated constipation, dyspepsia, nausea (1%); gastritis (postmarketing).
UTI (7%); urinary retention (1%).
Anaphylactic reactions (postmarketing).
Category C .
Safety and efficacy not established.
May have increased sensitivity to effects of anticholinergic agents.
Dose modification is recommended in patients with CrCl less than 30 mL/min.
Special Risk Patients
Use with caution in patients with GI obstruction (risk of gastric retention), hepatic function impairment, or clinically important bladder overflow obstruction (risk of urinary retention).
Controlled narrow-angle glaucoma
Use only if benefits outweigh risks.
Severe anticholinergic effects.
- Advise patient to take prescribed dose on an empty stomach at least 1 h before or 2 h after a meal.
- Advise patient if a dose is missed to skip that dose and take the next dose at least 1 h before the next meal.
- Advise patient to contact health care provider if urinary symptoms do not improve or if they worsen while taking this medication.
- Advise patient to take sips of water, chew sugarless gum, or suck on sugarless candy to relieve symptoms of dry mouth.
- Advise patient to avoid strenuous activity during periods of high temperature or humidity.
- Advise patient to avoid alcoholic beverages within 2 h of taking trospium.
- Advise patient that drug may cause dizziness or blurred vision and to use caution while driving or performing other tasks requiring coordination and mental alertness until tolerance is determined.
Copyright © 2009 Wolters Kluwer Health.