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Solifenacin

Pronunciation

Pronunciation

(sol i FEN a sin)

Index Terms

  • Solifenacin Succinate
  • YM905

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as succinate:

VESIcare: 5 mg, 10 mg

Brand Names: U.S.

  • VESIcare

Pharmacologic Category

  • Anticholinergic Agent

Pharmacology

Inhibits muscarinic receptors resulting in decreased urinary bladder contraction, increased residual urine volume, and decreased detrusor muscle pressure.

Distribution

Vd: ~600 L

Metabolism

Extensively hepatic; via N-oxidation and 4 R-hydroxylation, forms 1 active and 3 inactive metabolites; primary pathway for elimination is via CYP3A4

Excretion

Urine (69%; <15% as unchanged drug); feces (23%)

Time to Peak

Plasma: 3-8 hours

Half-Life Elimination

45-68 hours following chronic dosing; prolonged in severe renal (CrCl <30 mL/minute) or moderate hepatic (Child-Pugh class B) impairment

Protein Binding

~98% bound primarily to alpha1-acid glycoprotein

Special Populations: Renal Function Impairment

There is a 2.1-fold increase in AUC and 1.6-fold increase in half-life of solifenacin in patients with severe renal impairment.

Special Populations: Hepatic Function Impairment

There is a 2-fold increase in the half-life and 35% increase in AUC of solifenacin in patients with moderate hepatic impairment.

Special Populations: Elderly

Elderly volunteers (65 to 80 y of age) showed that Cmax, AUC, and half-life values were 20% to 25% higher compared with younger volunteers (18 to 55 y of age).

Use: Labeled Indications

Treatment of overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence

Contraindications

Hypersensitivity to solifenacin or any component of the formulation; urinary retention; gastric retention; uncontrolled narrow-angle glaucoma.

Dosing: Adult

Overactive bladder: Oral: 5 mg once daily; if tolerated, may increase to 10 mg once daily

Dosage adjustment with concomitant CYP3A4 inhibitors: Maximum solifenacin dose: 5 mg/day

Dosing: Geriatric

Base dosing on renal/hepatic function.

Dosing: Renal Impairment

Use with caution in reduced renal function; CrCl <30 mL/minute: Maximum dose: 5 mg/day

Dosing: Hepatic Impairment

Use with caution in reduced hepatic function:

Moderate (Child-Pugh class B): Maximum dose: 5 mg/day

Severe (Child-Pugh class C): Use is not recommended

Administration

Swallow tablet whole; administer with liquids; may be administered without regard to meals.

Dietary Considerations

May be taken without regard to meals.

Storage

Store at controlled room temperature of 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

Acetylcholinesterase Inhibitors: Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Acetylcholinesterase Inhibitors may diminish the therapeutic effect of Anticholinergic Agents. Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics (Opioid). Specifically, the risk for constipation and urinary retention may be increased with this combination. Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Monitor therapy

Antifungal Agents (Azole Derivatives, Systemic): May decrease the metabolism of Solifenacin. Applicable Isavuconazonium considerations are addressed in separate monographs. Exceptions: Isavuconazonium Sulfate. Consider therapy modification

Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates. Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Avoid combination

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination

Highest Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification

MiFEPRIStone: May enhance the QTc-prolonging effect of QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying). Management: Though the drugs listed here have uncertain QT-prolonging effects, they all have some possible association with QT prolongation and should generally be avoided when possible. Consider therapy modification

Mirabegron: May enhance the adverse/toxic effect of Solifenacin. Specifically, the risk of acute urinary retention may be enhanced. Mirabegron may increase the serum concentration of Solifenacin. Monitor therapy

Mitotane: May decrease the serum concentration of CYP3A4 Substrates. Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Moderate Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Monitor therapy

Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Avoid combination

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor closely for a diminished response to secretin. Consider therapy modification

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

St John's Wort: May decrease the serum concentration of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Adverse Reactions

>10%: Gastrointestinal: Xerostomia (11% to 28%; dose-related), constipation (5% to 13%; dose-related)

1% to 10%:

Cardiovascular: Edema (≤1%), hypertension (≤1%)

Central nervous system: Fatigue (1% to 2%), depression (≤1%)

Gastrointestinal: Dyspepsia (1% to 4%), nausea (2% to 3%), upper abdominal pain (1% to 2%)

Genitourinary: Urinary tract infection (3% to 5%), urinary retention (≤1%)

Ophthalmic: Blurred vision (4% to 5%), dry eye syndrome (≤2%)

Respiratory: Cough (≤1%)

Miscellaneous: Influenza (≤2%)

<1% (Limited to important or life-threatening): Abnormal hepatic function tests, anaphylaxis, angioedema, atrial fibrillation, confusion, delirium, erythema multiforme, exfoliative dermatitis, fecal impaction, gastroesophageal reflux disease, gastrointestinal obstruction, glaucoma, hallucination, hyperkalemia, hypersensitivity reactions, intestinal obstruction, palpitations, prolonged Q-T interval on ECG, renal insufficiency, tachycardia, torsades de pointes, voice disorder

Warnings/Precautions

Concerns related to adverse effects:

• Angioedema: Cases of angioedema involving the face, lips, tongue, and/or larynx have been reported during treatment; some cases have occurred after the first dose. May be life-threatening. Immediately discontinue and institute supportive care if tongue, hypopharynx, or larynx is involved.

• CNS effects: Central nervous system effects have been reported (eg, headache, confusion, hallucinations, somnolence); monitor, particularly at treatment initiation or dose increase, reduce dose or discontinue if necessary. May cause drowsiness and/or blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

• Heat prostration: May occur in the presence of increased environmental temperature; use caution in hot weather and/or exercise.

• Hypersensitivity reactions: Anaphylactic reactions have been reported rarely with solifenacin; immediately discontinue therapy if anaphylactic reaction develops. Do not use in patients with a known or suspected hypersensitivity.

Disease-related concerns:

• Bladder outflow obstruction: Use with caution in patients with bladder outflow obstruction; increased risk of urinary retention.

• Gastrointestinal disease: Use with caution in patients with gastrointestinal obstructive disorders or decreased gastrointestinal motility.

• Glaucoma: Use with caution in patients with controlled (treated) narrow-angle glaucoma; use is contraindicated in uncontrolled narrow-angle glaucoma.

• Hepatic impairment: Use with caution in patients with moderate hepatic impairment (Child-Pugh class B); dosage adjustment is required; use is not recommended in patients with severe hepatic impairment (Child-Pugh class C).

• QT prolongation: Use with caution in patients with a known history of QT prolongation or other risk factors for QT prolongation (eg, concomitant use of medications known to prolong QT interval and/or electrolyte abnormalities).The risk for QT prolongation is dose-related.

• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment is required for severe renal impairment (CrCl <30 mL/minute).

Concurrent drug therapy issues:

• High potential for interactions: Patients on potent CYP3A4 inhibitors require the lower dose of solifenacin.

Monitoring Parameters

Anticholinergic effects (eg, fixed and dilated pupils, blurred vision, tremors, or dry skin); creatinine clearance (prior to treatment for dosing adjustment); liver function

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience dry eyes, blurred vision, nausea, dry mouth, or fatigue. Have patient report immediately to prescriber severe dizziness, passing out, severe loss of strength and energy, difficulty breathing, confusion, hallucinations, severe abdominal pain, severe constipation, lack of sweat, urinary retention, painful urination, bradycardia, tachycardia, arrhythmia, or severe headache (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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