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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VESICARE (VESICARE).
| Breastfeeding | Excreted in animal milk; unknown in human milk. Caution advised. M/P ratio not determined. |
| 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. |
■ FDA Black Box Warning
None
| Serious Effects |
["Urinary retention","Gastric retention","Uncontrolled narrow-angle glaucoma","Hypersensitivity to solifenacin or any component of the formulation","Severe hepatic impairment (Child-Pugh C)"]
| 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)"] |
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| Fertility Effects | No known significant effects on human fertility. Animal studies show no impairment. |