Dosing & Uses
Dosage Forms & Strengths
tablet
- 5mg (VESIcare)
- 10mg (VESIcare)
Overactive Bladder
VESIcare only
Indicated for treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency
5 mg PO qDay, may increase to 10 mg/day if well tolerated
Dosing Modifications
Renal impairment
- Mild-to-moderate (CrCl ≥30 mL/min): No dosage adjustment necessary
- Severe (CrCl <30 mL/min): Not to exceed 5 mg/day
Hepatic impairment
- Mild (Child-Pugh A): No dosage adjustment necessary
- Moderate (Child-Pugh B): Not to exceed 5 mg/day
- Severe (Child-Pugh class C): Not recommended
CYP3A4 inhibitors
- Coadministration with strong CYP3A4 (eg, ketoconazole): Solifenacin dose not to exceed 5 mg/day
Dosage Forms & Strengths
oral suspension
- 1mg/mL (VESIcare LS)
Neurogenic Detrusor Overactivity
VESIcare LS only
Indicated for treatment of neurogenic detrusor overactivity (NDO) in pediatric patients aged ≥2 years
<2 years: Safety and efficacy not established
≥2 years
- Oral suspension concentration 1 mg/mL
- 9 to 15 kg: 2 mL PO qDay initially; not to exceed 4 mL/day
- >15 to 30 kg: 3 mL PO qDay initially; not to exceed 5 mL/day
- >30 to 45 kg: 3 mL PO qDay initially; not to exceed 6 mL/day
- >45 to 60 kg: 4 mL PO qDay initially; not to exceed 8 mL/day
- >60 kg: 5 mL PO qDay initially; not to exceed 10 mL/day
Dosage Modifications
Renal impairment
- Mild-to-moderate (CrCl ≥30 mL/min): No dosage adjustment necessary
- Severe (CrCl <30 mL/min): Not to exceed starting dose for weight range
Hepatic impairment
- Mild (Child-Pugh A): No dosage adjustment necessary
- Moderate (Child-Pugh B): Not to exceed starting dose for weight range
- Severe (Child-Pugh class C): Not recommended
Strong CYP3A4 inhibitors
- Coadministration with strong CYP3A4 (eg, ketoconazole): Solifenacin dose not to exceed starting dose for weight range
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
tablets
- Dry mouth (10.6-27.6%)
- Constipation (5.4-13.4%)
1-10%
tablets
- Blurred vision (3.8-4.8%)
- Urinary tract infection NOS (2.8-4.8%)
- Dyspepsia (1.4-3.9%)
- Nausea (1.7-3.3%)
- Influenza (0.9-2.2%)
- Fatigue (1-2.1%)
- Dizziness (1.8-1.9%)
- Upper abdominal pain (1.2-1.9%)
- Dry eyes NOS (0.3-1.6%)
- Urinary retention (1.4%)
- Hypertension NOS (0.5-1.4%)
- Depression NOS (0.8-1.2%)
- Edema lower limb (0.3-1.1%)
- Vomiting (0.2-1.1%)
- Cough (0.2-1.1%)
Oral suspension
- Constipation (7.4%)
- Dry mouth (3.2%)
- Urinary tract infection (2.1%)
- Abdominal pain (1.1%)
- Positive urinalysis bacterial test (1.1%)
- Somnolence (1.1%)
Postmarketing Reports
General disorders and administration site conditions: Peripheral edema, hypersensitivity reactions (including angioedema with airway obstruction, rash, pruritus, urticaria, anaphylactic reaction)
Nervous system disorders: Dizziness, headache, confusion, hallucinations, delirium, somnolence
Cardiac disorders: QT prolongation, torsade de pointes, atrial fibrillation, tachycardia, palpitations
Hepatobiliary disorders: Liver disorders mostly characterized by abnormal liver function tests (ie, AST, ALT, GGT)
Renal and urinary disorders: renal impairment, urinary retention
Metabolism and nutrition disorders: Decreased appetite, hyperkalemia
Skin and subcutaneous tissue disorders: Exfoliative dermatitis, erythema multiforme, dry skin
Eye disorders: Glaucoma
Gastrointestinal disorders: Gastroesophageal reflux disease, ileus, vomiting, abdominal pain, dysgeusia, sialadenitis
Respiratory, thoracic and mediastinal disorders: Dysphonia, nasal dryness
Musculoskeletal and connective tissue disorders: Muscular weakness
Warnings
Contraindications
Hypersensitivity
Gastric retention
Uncontrolled narrow-angle glaucoma
tablets only
- Urinary retention
Cautions
Reports of angioedema of face, lips and/or larynx, in some cases occurring after the first dose, described; anaphylactic reactions reported rarely
Administer with caution with clinically significant bladder outflow obstruction
Caution with decreased gastrointestinal motility
Somnolence reported; advise patients not to drive or operate heavy machinery until they know how therapy affects them
Caution in patients being treated for narrow-angle glaucoma
Caution with a known history of QT prolongation or patients who are taking medications known to prolong the QT interval
Associated with antimuscarinic CNS adverse reactions; monitor for signs of antimuscarinic CNS adverse reactions, particularly after beginning treatment or increasing the dose
Drug interaction overview
- Solifenacin is a CYP3A4 substrate
- Coadministration of ketoconazole, a strong CYP3A4 inhibitor, significantly increased the exposure of solifenacin; modify solifenacin dose if coadministered with strong CYP3A4 inhibitors
Pregnancy & Lactation
Pregnancy
There are no studies on use in pregnant females
Animal data
- No adverse developmental outcomes were observed in animal reproduction studies with oral solifenacin succinate to pregnant mice during organogenesis at a 10 mg/day dose (1.2x the maximum recommended human dose [MRHD])
- Administration of doses ≥3.6x the MRHD during organogenesis produced maternal toxicity in the pregnant mice and resulted in developmental toxicity and reduced fetal body weights in offspring
Lactation
No information available
Solifenacin is present in mouse milk
When a drug is present in animal milk, it is likely to be present in human milk
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Competitive muscarinic-receptor antagonist
Absorption
Peak plasma concentration
- Tablets: 32.3 ng/mL (5-mg dose); 62.9 ng/mL (10-mg dose)
- Solution: 2.5-29 ng/mL
Peak plasma time
- Tablets: 3 hr (5-mg dose); 8 hr (10-mg dose)
- Solution: 2-6 hr
Bioavailability
- Tablets or solution: ~90%
Distribution
Protein bound: 98%
Metabolism
Extensively metabolized by the liver, primarily CYP3A4
Metabolites: 4R-hydroxy solifenacin (active); N-glucuronide, N-oxide, and 4R-hydroxyN-oxide of solifenacin (inactive)
Elimination
Excretion: Urine (69%), feces (23%)
Half-life
- Adults: 45-68 hr
- Children and adolescents: ~26 hr
Administration
Oral Administration
Tablets
- May take with or without food
- Administer with water and swallow whole
Oral suspension
- Shake bottle well before administration of each dose
- Take once daily, followed by liquid (eg, water or milk) after each dose
-
Missed dose
- Missed dose <12 hr: Take as soon as possible
- Missed dose >12 hr: Skip dose and wait for next scheduled dose
Storage
Tablets
- Store at 25ºC (68-77ºF) with excursions permitted to 15-30ºC (59-86ºF)
Oral suspension
- Store at 20-25ºC (68-77ºF) with excursions permitted to 15-30ºC (59-86ºF)
- Store in original bottle to protect from degradation; discard any unused product 28 days after opening the original bottle
- Dispense in a tight, light-resistant container
Images
Patient Handout
Formulary
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Adding plans allows you to:
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- Compare formulary status to other drugs in the same class.
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