Brand name: Vesicare
Drug class: Antimuscarinics
Chemical name: (1S)-(3R)-1-azabicyclo[2.2.2]oct-3-yl-3,4-dihydro-1-phenyl-2(1H)-isoquinolinecarboxylate cmpd. with butanedioic acid (1:1)
Molecular formula: C₂₃H₂₆N₂O₂•C₄H₆O₄
CAS number: 242478-38-2

Medically reviewed by Drugs.com on Aug 16, 2023. Written by ASHP.

Introduction

Genitourinary antispasmodic agent; an antimuscarinic agent.

Uses for Solifenacin

Overactive Bladder

Relief of symptoms associated with voiding (e.g., urge urinary incontinence, urgency, frequency).

Solifenacin Dosage and Administration

Administration

Oral Administration

Administer orally once daily with liquids without regard to meals.

Swallow tablets whole.

Dosage

Available as solifenacin succinate; dosage expressed in terms of the salt.

Adults

Overactive Bladder

Oral

Initially, 5 mg once daily. If well tolerated, may increase to 10 mg once daily.

Prescribing Limits

Adults

Overactive Bladder

Oral

Maximum 10 mg daily.

Special Populations

Hepatic Impairment

Maximum 5 mg daily in patients with moderate hepatic impairment (Child-Pugh class B). (See Elimination: Special Populations, under Pharmacokinetics.)

Use not recommended in patients with severe hepatic impairment (Child-Pugh class C).

Renal Impairment

Maximum 5 mg daily in patients with severe renal impairment (Cl_cr <30 mL/minute). (See Elimination: Special Populations, under Pharmacokinetics.)

Cautions for Solifenacin

Contraindications

• Urinary retention, gastric retention, or uncontrolled angle-closure glaucoma.

• Known hypersensitivity to solifenacin succinate or any ingredient in the formulation.

Warnings/Precautions

Sensitivity Reactions

Angioedema

Angioedema reported in at least 1 patient.

General Precautions

Urinary Retention

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

Decreased GI Motility

Use with caution in patients with decreased GI motility (e.g., patients with severe constipation, ulcerative colitis, or myasthenia gravis) or obstructive GI disorders.

Fecal impaction, colonic obstruction, and intestinal obstruction reported rarely with 10-mg daily dosage.

Prolongation of QT Interval

30-mg daily dosage associated with more pronounced prolongation of QT interval than 10-mg daily dosage. (See Prescribing Limits under Dosage and Administration.) Consider this observation when deciding to use solifenacin in patients with history of QT interval prolongation or receiving drugs that prolong QT interval.

Controlled Angle-closure Glaucoma

Use with caution in patients being treated for angle-closure glaucoma. (See Contraindications under Cautions.)

Specific Populations

Pregnancy

Category C.

Lactation

Distributed into milk in mice; not known whether distributed into human milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established in children <18 years of age.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults. (See Elimination: Special Populations, under Pharmacokinetics.)

Hepatic Impairment

Use with caution. (See Hepatic Impairment under Dosage and Administration and see Elimination: Special Populations, under Pharmacokinetics.)

Use not recommended in patients with severe hepatic impairment (Child-Pugh class C).

Renal Impairment

Use with caution. (See Renal Impairment under Dosage and Administration and see Elimination: Special Populations, under Pharmacokinetics.)

Common Adverse Effects

Dry mouth, constipation.

Drug Interactions

Metabolized principally by CYP3A4. Does not inhibit CYP1A1/2, 2C9, 2C19, 2D6, or 3A4.

Drugs Affecting Hepatic Microsomal Enzymes

Inhibitors of CYP3A4: Potential pharmacokinetic interaction (increased plasma solifenacin concentrations). Do not exceed 5 mg daily when used concomitantly with potent inhibitors of CYP3A4. (See Specific Drugs under Interactions.)

Inducers of CYP3A4: Potential pharmacokinetic interaction (altered solifenacin pharmacokinetics).

Drugs Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP1A1/2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4: Pharmacokinetic interaction unlikely

Drugs Affected by GI Motility

Potential pharmacokinetic interaction (altered absorption because of decreased GI motility). (See Decreased GI Motility under Cautions.)

Specific Drugs

Solifenacin Pharmacokinetics

Absorption

Bioavailability

Absolute bioavailability is approximately 90%.

Peak plasma concentrations achieved within 3–8 hours after administration.

Food

Food does not affect pharmacokinetics of solifenacin.

Special Populations

Increased plasma concentrations reported in geriatric patients, patients with moderate hepatic impairment (Child-Pugh class B), and patients with severe renal impairment (Cl_cr <30 mL/minute). (See Special Populations under Dosage and Administration and see Elimination: Special Populations, under Pharmacokinetics.)

Distribution

Extent

Highly distributed to tissues outside the CNS.

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

Plasma Protein Binding

Approximately 98% (mainly to α₁-acid glycoprotein).

Elimination

Metabolism

Extensively metabolized in the liver, mainly via CYP3A4.

Elimination Route

Excreted in urine (approximately 69%) and in feces (approximately 23%); unchanged drug accounts for <15% of recovered radioactivity.

Half-life

45–68 hours following long-term administration.

Special Populations

Prolonged half-life in geriatric patients, patients with moderate hepatic impairment (Child-Pugh class B), and patients with severe renal impairment (Cl_cr <30 mL/minute). (See Special Populations under Dosage and Administration.)

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).

Actions

• Potent and selective antimuscarinic agent.

• Inhibits contraction of the detrusor muscle of the bladder, resulting in decreased bladder activity.

• Demonstrates binding specificity for muscarinic M₃ receptors in vitro and functional selectivity for urinary bladder over secretory (e.g., salivary) glands.

• Risk of blurred vision, constipation, dry mouth, and heat prostration (when used in a hot environment). Use caution when driving or performing dangerous activities until effects on vision are known. Consult a clinician if severe abdominal pain occurs or if constipation persists for ≥3 days.

• Importance of taking solifenacin succinate with liquids and swallowing the tablet whole. If a dose is skipped, resume therapy the next day; do not take 2 doses in the same day.

• Importance of reading manufacturer’s patient information leaflet before initiating therapy.

• 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 women informing their clinician if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing 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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