VESICARE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VESICARE (VESICARE).
Competitive antagonist at muscarinic acetylcholine receptors (M1-M5), with selectivity for M3 receptors over M2. Inhibits bladder detrusor muscle contraction, increasing bladder capacity and reducing urinary urgency.
| Metabolism | Extensively metabolized in the liver via cytochrome P450 isoenzyme CYP3A4; minor pathways include CYP2D6. The major metabolite is active (R)-desethylsolifenacin (M1 and M2). |
| Excretion | Approximately 70% of an oral dose is excreted in urine (mainly as metabolites, <15% unchanged) and 25% in feces. |
| Half-life | Terminal elimination half-life is approximately 45 hours (range 33–57 hours), supporting once-daily dosing. |
| Protein binding | Approximately 50–70% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is about 600 L (approximately 8.6 L/kg for a 70 kg adult), indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 90%, with no significant food effect. |
| Onset of Action | Oral: Onset of therapeutic effect is observed within 3–5 hours post-dose, with peak serum concentrations at 3–8 hours. |
| Duration of Action | Duration of action is approximately 24 hours, allowing once-daily administration. |
| Molecular Weight | 362.46 Da |
5 mg orally once daily; may increase to 10 mg once daily if needed.
| Dosage form | TABLET |
| Renal impairment | GFR 30-89 mL/min: no adjustment. GFR <30 mL/min: maximum dose 5 mg once daily. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: maximum dose 5 mg once daily. Child-Pugh C: not recommended. |
| Pediatric use | Not approved for pediatric use. |
| Geriatric use | Start at 5 mg once daily; monitor anticholinergic effects. |
| 1st trimester | No adequate studies in pregnant women. Animal studies show risk at doses 2-4 times the maximum recommended human dose. Use only if potential benefit justifies potential risk to fetus. |
| 2nd trimester | Same as T1. Consider alternative therapy in pregnant women with urinary incontinence due to potential anticholinergic effects. |
| 3rd trimester | Same as T1. May cause adverse effects in neonate including constipation, urinary retention, and anticholinergic symptoms. |
Clinical note
Comprehensive clinical and safety monograph for VESICARE (VESICARE).
| Placental transfer | Maternal-fetal transfer occurs in animal models; limited human data. Molecular size and lipophilicity suggest potential placental crossing. |
| Breastfeeding | Excreted into breast milk in animal studies; unknown in humans. Caution due to potential anticholinergic effects in infant, including constipation, urinary retention, and blurred vision. Consider alternatives, especially for preterm infants or those with compromised renal function. |
■ FDA Black Box Warning
None
| Serious Effects |
Urinary retentionGastric retentionUncontrolled narrow-angle glaucomaHypersensitivity to solifenacin succinate or any component of the formulation
| Precautions | Angioedema and anaphylactic reactions, Urinary retention risk, especially in patients with bladder outflow obstruction, Gastric retention risk in patients with gastrointestinal obstructive disorders, Decreased gastrointestinal motility (use caution in severe constipation or ulcerative colitis), Central nervous system effects (dizziness, somnolence); may impair ability to drive or operate machinery, Angle-closure glaucoma precipitation (use caution in patients being treated for glaucoma), QT prolongation at high doses; avoid in patients with known QT prolongation or concurrent use of potent CYP3A4 inhibitors, Renal and hepatic impairment: dose adjustment needed for severe renal impairment (CrCl <30 mL/min) or moderate hepatic impairment (Child-Pugh B); not recommended in severe hepatic impairment (Child-Pugh C) |
| Food/Dietary | Grapefruit and grapefruit juice may increase solifenacin exposure; avoid concurrent use. No other significant food interactions. May take without regard to meals. |
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| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | FDA Pregnancy Category B. No evidence of teratogenicity in animal studies. No adequate human studies in first trimester; risk cannot be excluded. Use only if clearly needed. |
| Fetal Monitoring | Monitor for anticholinergic effects (dry mouth, constipation, blurred vision, urinary retention) and potential fetal effects via ultrasound if prolonged use. |
| Fertility Effects | No known significant effects on human fertility. Animal studies show no impairment. |
| Clinical Pearls | VESICARE (solifenacin succinate) is an antimuscarinic agent for overactive bladder. Onset of action may be delayed; assess efficacy after 4-8 weeks. Use cautiously in patients with narrow-angle glaucoma, GI obstructive disorders, decreased GI motility, or urinary retention. May prolong QT interval; avoid in patients with known QT prolongation or concurrent use of QT-prolonging drugs. Monitor for anticholinergic side effects (dry mouth, constipation, blurred vision). Dose adjustment required for severe renal impairment (CrCl <30 mL/min) or moderate hepatic impairment (Child-Pugh B); not recommended in severe hepatic impairment (Child-Pugh C). |
| Patient Advice | Take VESICARE exactly as prescribed, usually once daily with or without food. · Swallow tablet whole with water; do not crush or chew. · May cause dry mouth, constipation, blurred vision, or drowsiness; avoid driving if affected. · Avoid excessive alcohol intake as it may exacerbate side effects. · Report worsening symptoms, difficulty urinating, or signs of allergic reaction. · Do not take with other anticholinergic medications without consulting your doctor. · Store at room temperature away from moisture and heat. |