VESICARE LS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VESICARE LS (VESICARE LS).
Competitive antagonist at muscarinic acetylcholine receptors (M1–M5), with high selectivity for M3 receptors in the bladder detrusor muscle. Reduces involuntary bladder contractions and increases bladder capacity.
| Metabolism | Primarily hepatic via CYP3A4; undergoes extensive metabolism to inactive metabolites. Minor pathways include N-dealkylation and glucuronidation. |
| Excretion | Renal: 68% (unchanged drug ~59%, metabolites ~9%), Fecal: 24% (metabolites), Biliary: negligible. |
| Half-life | Terminal elimination half-life: 45 hours (range 32–68 h). Extended half-life allows once-daily dosing; steady-state reached in ~10 days. |
| Protein binding | ~50–60%, primarily to alpha-1-acid glycoprotein (AAG) and albumin. |
| Volume of Distribution | ~113 L (approx. 1.9 L/kg for a 60 kg adult). Large Vd indicates extensive tissue distribution. |
| Bioavailability | Oral: ~60–70% (extended-release formulation). |
| Onset of Action | Oral: Therapeutic effects on urinary frequency and urgency may be observed within 1–2 weeks of initiation. |
| Duration of Action | Oral: 24 hours (sustained over dosing interval due to extended-release formulation and long half-life). |
5 mg orally once daily; may increase to 10 mg once daily.
| Dosage form | SUSPENSION |
| Renal impairment | No dose adjustment for GFR >=30 mL/min. For GFR 15-29 mL/min: maximum dose 5 mg once daily. Not recommended for GFR <15 mL/min. |
| 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; consider dose reduction to 5 mg once daily due to increased anticholinergic sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VESICARE LS (VESICARE LS).
| Breastfeeding | It is not known whether solifenacin is excreted in human milk. M/P ratio not available. Due to potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. |
| Teratogenic Risk | Pregnancy Category C. No adequate well-controlled studies in pregnant women. In animal studies, solifenacin succinate (active ingredient) caused decreased fetal weight, increased incidence of fetal death, and delayed skeletal ossification at doses 1.6–10 times the human AUC. Risk cannot be ruled out; use only if potential benefit justifies risk to fetus. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to solifenacin or any excipient; urinary retention; gastric retention; uncontrolled narrow-angle glaucoma.
| Precautions | Risk of urinary retention (especially in patients with bladder outflow obstruction), decreased gastrointestinal motility (use with caution in patients with constipation or ulcerative colitis), blurred vision, dizziness, and drowsiness. Monitor for signs of angioedema. Use with caution in patients with impaired renal or hepatic function, or with conditions predisposing to QT prolongation. |
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| Fetal Monitoring | Monitor for anticholinergic effects in mother (dry mouth, constipation, blurred vision, urinary retention). Fetal monitoring per routine prenatal care; no specific fetal monitoring required. Observe newborn for anticholinergic symptoms if exposed in utero. |
| Fertility Effects | No human data on fertility. In animal studies, solifenacin had no effect on male or female fertility at doses up to 10 times the MRHD. |