Sanctura

Pronunciation

Generic Name: Trospium Chloride
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: C25H30ClNO3
CAS Number: 10405-02-4

Introduction

Genitourinary antispasmodic; quaternary ammonium antimuscarinic.1 3

Uses for Sanctura

Overactive Bladder

Management of overactive bladder for the relief of symptoms associated with voiding (e.g., urge urinary incontinence, urgency, frequency).1 3 5

Slideshow: How to Manage Your Overactive Bladder

Appears to be as effective as immediate-release preparations of oxybutynin or tolterodine in decreasing urinary frequency;2 4 5 6 may be more effective than immediate-release preparations of tolterodine in decreasing urgency incontinence.5 6

May offer no advantage over extended-release anticholinergic preparations for the treatment of overactive bladder.3

Sanctura Dosage and Administration

Administration

Oral Administration

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

Dosage

Available as trospium chloride; dosage expressed in terms of the salt.1

Adults

Overactive Bladder
Oral

20 mg twice daily.1

Special Populations

Hepatic Impairment

Use caution in patients with moderate or severe hepatic impairment.1 (See Special Populations under Pharmacokinetics.)

Renal Impairment

In patients with severe renal impairment (Clcr <30 mL/minute), decrease dosage to 20 mg once daily at bedtime.1

Geriatric Patients

In geriatric patients ≥75 years of age, may decrease dosage to 20 mg once daily based on patient tolerance.1 (See Geriatric Use under Cautions.)

Cautions for Sanctura

Contraindications

  • Presence or risk of urinary retention.1

  • Presence or risk of gastric retention.1

  • Presence or risk of risk of uncontrolled angle-closure glaucoma.1

  • Known hypersensitivity to trospium or any ingredient in the formulation.1

Warnings/Precautions

General Precautions

Urinary Retention

Risk of urinary retention; use with caution in patients with clinically important bladder outflow obstruction.1

Decreased GI Motility

Risk of gastric retention; use caution with obstructive GI disorders.1

May decrease GI motility; use with caution in patients with ulcerative colitis, intestinal atony, or myasthenia gravis.1

Controlled Angle-closure Glaucoma

Use only if potential benefits outweigh the risks; use with caution and monitor carefully.1

Specific Populations

Pregnancy

Category C.1

Lactation

Distributed into milk in rats; not known whether distributed into human milk.1 Use with caution and only if potential benefit justifies the risk to the infant.1

Pediatric Use

Safety and efficacy not established.1

Geriatric Use

In patients ≥75 years of age, possible increased incidence of adverse anticholinergic effects compared with younger adults.1 (See Geriatric Patients under Dosage and Administration.)

Hepatic Impairment

Use with caution in patients with moderate or severe hepatic impairment.1 (See Special Populations under Pharmacokinetics.)

Renal Impairment

Dosage reduction necessary in patients with severe renal impairment (Clcr<30 mL/per minute); not studied in patients with mild or moderate renal impairment1 (See Renal Impairment under Dosage and Administration and see Special Populations under Pharmacokinetics.) 1

Common Adverse Effects

Dry mouth,1 2 3 constipation.1 2

Interactions for Sanctura

Minimally metabolized by CYP isoenzymes; does not inhibit CYP1A2, 3A4, 2A6, 2C9, 2C19, 2D6, or 2E1 in vitro.1 2 7 Pharmacokinetic interactions unlikely with drugs metabolized by CYP isoenzymes or with CYP enzyme inducers or inhibitors.1 2 7

Drugs Eliminated by Active Tubular Secretion

Possible competition for renal secretion, decreased renal elimination, and increased serum concentrations of trospium and/or other drug.1 Use concomitantly with caution; monitor carefully.1

Drugs Affected by GI Motility

Potential for altered absorption because of decreased GI motility.1

Specific Drugs

Drug

Interaction

Comment

Alcohol

Potential for additive sedative effects1

Anticholinergic agents

Potential for additive anticholinergic effects1

Digoxin

Potential for decreased renal elimination and increased serum concentrations of trospium and/or digoxin1 3

Use concomitantly with caution; monitor carefully1

Metformin

Potential decreased renal elimination and increased serum concentrations of trospium and/or metformin1 3

Use concomitantly with caution; monitor carefully1

Morphine

Potential for decreased renal elimination and increased serum concentrations of trospium and/or morphine 1 3

Use concomitantly with caution; monitor carefully1

Pancuronium

Potential for decreased renal elimination and increased serum concentrations of trospium and/or pancuronium1

Use concomitantly with caution; monitor carefully1

Procainamide

Potential for decreased renal elimination and increased serum concentrations of trospium and/or procainamide1 3

Use concomitantly with caution; monitor carefully1

Tenofovir

Potential for decreased renal elimination and increased serum concentrations of trospium and/or tenofovir1

Use concomitantly with caution; monitor carefully1

Vancomycin

Potential for decreased renal elimination and increased serum concentrations of trospium and/or vancomycin1

Use concomitantly with caution; monitor carefully1

Sanctura Pharmacokinetics

Absorption

Bioavailability

Absorption from GI tract is incomplete.1 3 5 7

Mean absolute oral bioavailability is about 9.6%.1

Food

High-fat meal reduces AUC and peak plasma concentrations by about 70–80%.1 3

Distribution

Extent

In blood, plasma to whole blood ratio is 1.6 to 1.1

Hydrophilic; theoretically should not cross the blood-brain barrier.5 7

Distributed into milk in rats; not known whether distributed into human milk.1

Plasma Protein Binding

50–85%.1

Elimination

Metabolism

Metabolism not fully elucidated;1 2 7 major pathway may be ester hydrolysis and subsequent glucuronidation to form inactive metabolites.1 7 Minimally metabolized by CYP isoenzymes.1 2 7

Elimination Route

Excreted principally in feces (about 85%) and in urine (5.8%), mainly as unchanged drug.1 2 3 5 7

Active tubular secretion is a major elimination route.1

Half-life

About 20 hours.1 7

Special Populations

In patients with severe renal impairment (Clcr<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.1 7

In patients with mild or moderate hepatic impairment, peak plasma concentrations increased (12 or 63%, respectively); AUC was similarly increased.1

Stability

Storage

Oral

Tablets

20–25°C.1

Actions

  • Antagonizes acetylcholine at muscarinic receptors in cholinergically innervated organs.1 3 5

  • Parasympatholytic action reduces the tonus of smooth muscle in the urinary bladder.1 3

  • Increases maximum cystometric capacity and volume at first detrusor contraction in patients with involuntary detrusor contractions.1 5

  • Little or no affinity for nicotinic receptors compared with muscarinic receptors at concentrations achieved following usual therapeutic doses.1 7

Advice to Patients

  • Importance of informing patients of potential adverse anticholinergic effects (e.g., dizziness, blurred vision, heat prostration when used in a hot environment).1

  • 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.1

  • 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.1

  • Importance of using alcohol with caution, since it may enhance drowsiness caused by trospium.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of advising patients of other important precautionary information.1 (See Cautions.)

Preparations

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

Trospium Chloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

20 mg

Sanctura

Odyssey

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Sanctura 20MG Tablets (ALLERGAN DERMATOLOGICS): 30/$99.99 or 90/$275.99

Sanctura XR 60MG 24-hr Capsules (ALLERGAN DERMATOLOGICS): 30/$196.00 or 90/$560.96

Trospium Chloride 20MG Tablets (GLENMARK PHARMACEUTICALS): 30/$82.99 or 90/$235.97

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions October 1, 2012. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Odyssey Pharmaceuticals. Sanctura™ (trospium chloride) tablets prescribing information. East Hanover, NJ; 2004. From Sanctura website (http://www.sanctura.com/Sanctura_Prescribing_Information.pdf).

2. Zinner N, Gittelman M, Harris R et al. Trospium chloride improves overactive bladder symptoms: a multicenter phase II trial. J Urol. 2004; 171:2311-5. [IDIS 519949] [PubMed 15126811]

3. Anon. Trospium Chloride (Sanctura): Another anticholinergic for overactive bladder. Med Lett Drugs Ther. 2004; 46:63-4. [PubMed 15289745]

4. Halaska M, Ralph G, Wiedemann A et al. Controlled, double-blind, multicentre clinical trial to investigate long-term tolerability and efficacy of trospium chloride in patients with detrusor instability. World J Urol. 2003; 20:392-9. [IDIS 519866] [PubMed 12811500]

5. Hashim H, Abrams P. Drug treatment of overactive bladder. Efficacy, cost and quality-of-life considerations. Drugs. 2004; 64:1643-56. [PubMed 15257626]

6. UK Medicines Information Pharmacists Group. Trospium. New Medicines on the market. Evaluated Information for the NHS. 2002 Feb. From UKMi website (http://www.ukmi.nhs.uk/NewMaterial/html/docs/trospium.pdf)

7. Rovner ES. Trospium chloride in the management of overactive bladder. Drugs. 2004; 64:2433-2446. [PubMed 15482001]

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