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Pronunciation
(sol i FEN a sin)
Generic Available (U.S.)
No
Index Terms
Brand Names: U.S.
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence
Pregnancy Risk Factor
C
Pregnancy Considerations
Decreased fetal weight, increased incidence of cleft palate, and delayed physical development were observed in some animal studies. There are no adequate or well-controlled studies in pregnant women. Use during pregnancy only if the benefit to the mother outweighs the potential risk to the fetus.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Hypersensitivity to solifenacin or any component of the formulation; urinary retention; gastric retention; uncontrolled narrow-angle glaucoma.
Warnings/Precautions
Concerns related to adverse effects:
• Angioedema: Cases of angioedema involving the face, lips, tongue, and/or larynx have been reported. Immediately discontinue if tongue, hypopharynx, or larynx are involved.
• CNS effects: 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.
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 (Clcr <30 mL/minute).
Concurrent drug therapy issues:
• High potential for interactions: Patients on potent CYP3A4 inhibitors require the lower dose of solifenacin.
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: Headache (3% to 6%), 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%)
Ocular: Blurred vision (4% to 5%), dry eyes (≤2%)
Respiratory: Cough (≤1%)
Miscellaneous: Influenza (≤2%)
<1%, postmarketing, and/or case reports: Anaphylaxis, angioedema, confusion, erythema multiforme, exfoliative dermatitis, fecal impaction, gastrointestinal obstruction, hallucinations, hypersensitivity reactions, pruritus, QTc prolongation, rash, somnolence, torsade de pointes, urticaria
Metabolism/Transport Effects
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Drug Interactions
AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Risk C: Monitor therapy
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Antifungal Agents (Azole Derivatives, Systemic): May decrease the metabolism of Solifenacin. Risk D: Consider therapy modification
Cannabinoids: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoids. Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid combination
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Herbs (CYP3A4 Inducers): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Risk C: Monitor therapy
Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Risk D: Consider therapy modification
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Risk C: Monitor therapy
Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Risk D: Consider therapy modification
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Food: Grapefruit juice may increase the serum level effects of solifenacin.
Herb/Nutraceutical: St John's wort (Hypericum) may decrease the levels/effects of solifenacin.
Storage
Store at controlled room temperature of 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Mechanism of Action
Inhibits muscarinic receptors resulting in decreased urinary bladder contraction, increased residual urine volume, and decreased detrusor muscle pressure.
Pharmacodynamics/Kinetics
Distribution: Vd: 600 L
Protein binding: ~98% bound primarily to alpha1-acid glycoprotein
Metabolism: Extensively hepatic; via N-oxidation and 4 R-hydroxylation, forms 1 active and 3 inactive metabolites; primary pathway for elimination is via CYP3A4
Bioavailability: ~90%
Half-life elimination: 45-68 hours following chronic dosing; prolonged in severe renal (Clcr <30 mL/minute) or moderate hepatic (Child-Pugh class B) impairment
Time to peak, plasma: 3-8 hours
Excretion: Urine 69% (<15% as unchanged drug); feces 23%
Dosage
Oral: Adults: 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
Dosage adjustment in renal impairment: Use with caution in reduced renal function
Clcr <30 mL/minute: Maximum dose: 5 mg/day
Dosage adjustment in 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: Oral
Swallow tablet whole; administer with liquids; may be administered without regard to meals.
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
Dietary Considerations
May be taken without regard to meals.
Patient Education
Maintain adequate hydration unless instructed to restrict fluid intake by prescriber. This medication may cause dry mouth. You may be more susceptible to heat prostration due to decreased ability to sweat. Use caution in hot weather. You may experience constipation, nausea, vomiting, blurred vision, and dry eyes. Report difficulty, pain, or burning on urination.
Geriatric Considerations
In patients with Clcr <30 mL/minute, doses >5 mg/day are not recommended. Similar safety and effectiveness were observed in elderly and younger patients.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation). Prolonged xerostomia may contribute to discomfort and dental disease (eg, caries, periodontal disease, and oral candidiasis).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause depression, sedation, or dizziness
Mental Health: Effects on Psychiatric Treatment
Dry mouth and constipation are common; concomitant use with psychotropic agents may produce additive effects; monitor. Carbamazepine, phenobarbital, phenytoin, and St John's wort may decrease levels of solifenacin while nefazodone may increase the levels of solifenacin; monitor.
Nursing: Physical Assessment/Monitoring
Monitor urination pattern.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, oral, as succinate:
VESIcare®: 5 mg, 10 mg
Pricing: U.S. (www.drugstore.com)
Tablets (VESIcare)
5 mg (30): $170.98
10 mg (30): $170.09
References
Cardozo L, Lisec M, Millard R, et al, “Randomized, Double-Blind Placebo Controlled Trial of the Once Daily Antimuscarinic Agent Solifenacin Succinate in Patients With Overactive Bladder,” J Urol, 2004, 172(5 Pt 1):1919-24.
Chapple CR, Arano P, Bosch JL, et al, “Solifenacin Appears Effective and Well Tolerated in Patients With Symptomatic Idiopathic Detrusor Overactivity in a Placebo- and Tolterodine-Controlled Phase 2 Dose-Finding Study,” BJU Int, 2004, 93(1):71-7.
Garely AD, Kaufman JM, Sand PK, et al, “Symptom Bother and Health-Related Quality of Life Outcomes Following Solifenacin Treatment for Overactive Bladder: The VESIcare Open-Label Trial (VOLT),” Clin Ther, 2006, 28(11):1935-46.
International Brand Names
Lexi-Comp.com
Last full review/revision February 2012
Content last modified February 2012
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