Brand name: Sanctura
Drug class: Genitourinary Smooth Muscle Relaxants
VA class: GU201
Chemical name: spiro[8-azoniabicyclo[3,2,1]octane-8,1’-pyrrolidinium]-3-[(hydroxydiphenyl-acetyl)- oxy]chloride,(1α, 3β, 5α)
Molecular formula: C₂₅H₃₀C_lNO₃
CAS number: 10405-02-4

Medically reviewed by Drugs.com on Sep 23, 2024. Written by ASHP.

Introduction

Genitourinary antispasmodic; quaternary ammonium antimuscarinic.

Uses for Trospium

Overactive Bladder

Management of overactive bladder for the relief of symptoms associated with voiding (e.g., urge urinary incontinence, urgency, frequency).

Appears to be as effective as immediate-release preparations of oxybutynin or tolterodine in decreasing urinary frequency; may be more effective than immediate-release preparations of tolterodine in decreasing urgency incontinence.

May offer no advantage over extended-release anticholinergic preparations for the treatment of overactive bladder.

Trospium Dosage and Administration

Administration

Oral Administration

Administer orally twice daily, at least 1 hour before meals or on an empty stomach.

Dosage

Available as trospium chloride; dosage expressed in terms of the salt.

Adults

Overactive Bladder

Oral

20 mg twice daily.

Special Populations

Hepatic Impairment

Use caution in patients with moderate or severe hepatic impairment. (See Special Populations under Pharmacokinetics.)

Renal Impairment

In patients with severe renal impairment (Cl_cr <30 mL/minute), decrease dosage to 20 mg once daily at bedtime.

Geriatric Patients

In geriatric patients ≥75 years of age, may decrease dosage to 20 mg once daily based on patient tolerance. (See Geriatric Use under Cautions.)

Cautions for Trospium

Contraindications

• Presence or risk of urinary retention.

• Presence or risk of gastric retention.

• Presence or risk of risk of uncontrolled angle-closure glaucoma.

• Known hypersensitivity to trospium or any ingredient in the formulation.

Warnings/Precautions

General Precautions

Urinary Retention

Risk of urinary retention; use with caution in patients with clinically important bladder outflow obstruction.

Decreased GI Motility

Risk of gastric retention; use caution with obstructive GI disorders.

May decrease GI motility; use with caution in patients with ulcerative colitis, intestinal atony, or myasthenia gravis.

Controlled Angle-closure Glaucoma

Use only if potential benefits outweigh the risks; use with caution and monitor carefully.

Specific Populations

Pregnancy

Category C.

Lactation

Distributed into milk in rats; not known whether distributed into human milk. Use with caution and only if potential benefit justifies the risk to the infant.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

In patients ≥75 years of age, possible increased incidence of adverse anticholinergic effects compared with younger adults. (See Geriatric Patients under Dosage and Administration.)

Hepatic Impairment

Use with caution in patients with moderate or severe hepatic impairment. (See Special Populations under Pharmacokinetics.)

Renal Impairment

Dosage reduction necessary in patients with severe renal impairment (Cl_cr<30 mL/per minute); not studied in patients with mild or moderate renal impairment (See Renal Impairment under Dosage and Administration and see Special Populations under Pharmacokinetics.)

Common Adverse Effects

Dry mouth, constipation.

Drug Interactions

Minimally metabolized by CYP isoenzymes; does not inhibit CYP1A2, 3A4, 2A6, 2C9, 2C19, 2D6, or 2E1 in vitro. Pharmacokinetic interactions unlikely with drugs metabolized by CYP isoenzymes or with CYP enzyme inducers or inhibitors.

Drugs Eliminated by Active Tubular Secretion

Possible competition for renal secretion, decreased renal elimination, and increased serum concentrations of trospium and/or other drug. Use concomitantly with caution; monitor carefully.

Drugs Affected by GI Motility

Potential for altered absorption because of decreased GI motility.

Specific Drugs

Trospium Pharmacokinetics

Absorption

Bioavailability

Absorption from GI tract is incomplete.

Mean absolute oral bioavailability is about 9.6%.

Food

High-fat meal reduces AUC and peak plasma concentrations by about 70–80%.

Distribution

Extent

In blood, plasma to whole blood ratio is 1.6 to 1.

Hydrophilic; theoretically should not cross the blood-brain barrier.

Distributed into milk in rats; not known whether distributed into human milk.

Plasma Protein Binding

50–85%.

Elimination

Metabolism

Metabolism not fully elucidated; major pathway may be ester hydrolysis and subsequent glucuronidation to form inactive metabolites. Minimally metabolized by CYP isoenzymes.

Elimination Route

Excreted principally in feces (about 85%) and in urine (5.8%), mainly as unchanged drug.

Active tubular secretion is a major elimination route.

Half-life

About 20 hours.

Special Populations

In patients with severe renal impairment (Cl_cr<30 mL/per minute), peak plasma concentrations and AUC increased 2-fold and 4.5-fold, respectively, and an additional elimination phase (half-life of about 33 hours) occurred.

In patients with mild or moderate hepatic impairment, peak plasma concentrations increased (12 or 63%, respectively); AUC was similarly increased.

Stability

Storage

Oral

Tablets

20–25°C.

Actions

• Antagonizes acetylcholine at muscarinic receptors in cholinergically innervated organs.

• Parasympatholytic action reduces the tonus of smooth muscle in the urinary bladder.

• Increases maximum cystometric capacity and volume at first detrusor contraction in patients with involuntary detrusor contractions.

• Little or no affinity for nicotinic receptors compared with muscarinic receptors at concentrations achieved following usual therapeutic doses.

• Importance of informing patients of potential adverse anticholinergic effects (e.g., dizziness, blurred vision, heat prostration when used in a hot environment).

• Importance of taking trospium chloride on an empty stomach or at least 1 hour before meals, and if a dose is skipped, taking the next scheduled dose at least 1 hour before the next meal.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, and dietary or herbal supplements as well as any concomitant illnesses.

• Importance of using alcohol with caution, since it may enhance drowsiness caused by trospium.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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