Trospium Chloride

Pronunciation: TROSE-pee-um KLOR-ide
Class: Anticholinergic

Trade Names

Sanctura
- Tablets 20 mg

Sanctura XR
- Tablets, extended-release 60 mg

Pharmacology

Antagonizes effect of acetylcholine on muscarinic receptors in cholinergically innervated organs. Its parasympatholytic action reduces tonus of smooth muscle in the bladder.

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Pharmacokinetics

Absorption

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.

Following a single 60 mg dose, C _max is 2 ng/mL; T _max is 5 h.

Distribution

Vd is 395 L after a 20 mg dose. Protein binding is 50% to 85%.

Metabolism

Of 10% absorbed, metabolites account for about 40% of excreted dose. Hypothesized metabolic pathway is ester hydrolysis with subsequent conjugation of benzylic acid.

Elimination

Plasma t _½ is approximately 20 h. Majority of dose (85.2%) recovered in feces and 5.8% in urine.

Following a single 60 mg dose, t _½ is 35 h.

Special Populations

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 .

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.

Pharmacokinetics were similar in elderly (65 yr of age and older) patients compared with younger (younger than 65 yr of age) patients.

Pharmacokinetic data are conflicting.

Pharmacokinetics have not been studied.

Indications and Usage

Treatment of overactive bladder with symptoms of urinary incontinence, urgency, and urinary frequency.

Contraindications

Patients with or at risk of urinary retention; gastric retention; uncontrolled narrow-angle glaucoma; hypersensitivity to any component of product.

Dosage and Administration

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.

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).

PO Titrate dosage down to 20 mg once daily based on tolerability.

Storage/Stability

Store at controlled room temperature (68° to 77°F).

Drug Interactions

Do not consume within 2 h of taking trospium. In addition, risk of drowsiness may be enhanced.

Additive effects, leading to increased dry mouth, constipation, and other anticholinergic effects.

Serum concentrations of these agents as well as of trospium may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Tachycardia (less than 2%); chest pain, hypertensive crisis, palpitations, supraventricular tachycardia, syncope (postmarketing).

CNS

Headache (4%); fatigue (2%); delirium, hallucinations (postmarketing).

Dermatologic

Rash (less than 2%); Stevens-Johnson syndrome (postmarketing).

EENT

Nasopharyngitis (3%); dry eyes (2%); nasal dryness (1%); abnormal vision (postmarketing).

GI

Dry mouth (20%); constipation (10%); flatulence, upper abdominal pain (2%); abdominal distention, aggravated constipation, dyspepsia, nausea (1%); gastritis (postmarketing).

Genitourinary

UTI (7%); urinary retention (1%).

Hypersensitivity

Anaphylactic reactions (postmarketing).

Musculoskeletal

Rhabdomyolysis (postmarketing).

Miscellaneous

Influenza (2%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

May have increased sensitivity to effects of anticholinergic agents.

Renal Function

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.

Overdosage

Symptoms

Severe anticholinergic effects.

Patient Information

• 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.