SANCTURA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SANCTURA (SANCTURA).
Trospium chloride is an antimuscarinic agent that competitively inhibits acetylcholine at muscarinic receptors, thereby reducing detrusor muscle contractions and increasing bladder capacity.
| Metabolism | Trospium undergoes minimal hepatic metabolism via ester hydrolysis and conjugation; less than 10% is metabolized. It is primarily excreted unchanged in urine (60%) and feces (40%). CYP450 enzymes are not significantly involved. |
| Excretion | Primarily renal (approximately 60% as unchanged drug and metabolites); biliary/fecal elimination accounts for ~30%. |
| Half-life | Terminal elimination half-life is approximately 12–20 hours in healthy adults, allowing twice-daily dosing. |
| Protein binding | ~80% bound primarily to albumin. |
| Volume of Distribution | Approximately 2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: ~30% due to first-pass metabolism. |
| Onset of Action | Oral: Onset of anticholinergic effect occurs within 1 hour. |
| Duration of Action | Duration of action is 8–12 hours, supporting twice-daily administration for overactive bladder symptoms. |
| Molecular Weight | 593.75 |
20 mg orally twice daily, with or without food. Maximum dose 20 mg twice daily.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in patients with GFR <30 mL/min/1.73 m² (severe renal impairment). No dose adjustment recommended for mild-to-moderate renal impairment (GFR 30-89 mL/min/1.73 m²). |
| Liver impairment | Contraindicated in patients with Child-Pugh class C (severe hepatic impairment). For Child-Pugh class A or B, no dose adjustment recommended due to limited data; use with caution. |
| Pediatric use | Not approved for pediatric use; safety and efficacy not established. |
| Geriatric use | Elderly patients may be more sensitive to anticholinergic effects. No specific dose adjustment recommended, but initiate at lowest effective dose and monitor closely. Avoid in patients with significant impairment of renal or hepatic function. |
| 1st trimester | Limited human data; animal studies show no teratogenic effects at clinically relevant doses. Use only if benefit outweighs risk. |
| 2nd trimester | No known risk; however, anticholinergic effects may cause fetal tachycardia. Use with caution. |
| 3rd trimester | May cause neonatal anticholinergic effects (e.g., ileus, respiratory depression). Avoid near term. |
Clinical note
Comprehensive clinical and safety monograph for SANCTURA (SANCTURA).
| Placental transfer | Undetermined; molecular weight suggests likely placental transfer, but no quantitative data available. |
| Breastfeeding | Minimal excretion into breast milk; anticholinergic effects in infant unlikely at therapeutic doses. Monitor infant for dry mouth, constipation, or tachycardia. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Urinary retentionGastric retentionUncontrolled narrow-angle glaucomaHypersensitivity to any component
| Precautions | Angioedema has been reported with trospium; if occurs, discontinue and manage appropriately., May cause urinary retention; use with caution in patients with bladder outflow obstruction., May aggravate symptoms in patients with gastrointestinal obstructive disorders., May decrease gastric motility; use with caution in patients with severe constipation or ulcerative colitis., May cause blurred vision and dizziness; advise patients not to drive or operate machinery until effects are known., Use with caution in patients with myasthenia gravis., Use with caution in patients with moderate to severe renal impairment (dose adjustment required)., May cause heat prostration in hot environments due to decreased sweating. |
| Food/Dietary | Take SANCTURA on an empty stomach at least one hour before meals. High-fat meals may reduce absorption. Avoid grapefruit juice as it may increase drug levels. Alcohol can exacerbate drowsiness and should be limited. |
Loading safety data…
| Lactation Rating |
| L2 (Safe) |
| Teratogenic Risk | Pregnancy Category C. Animal studies have shown adverse effects (fetal resorption, reduced fetal weight) at doses 1.6 times the maximum recommended human dose. No adequate human studies in pregnant women. Risk cannot be ruled out. First trimester: potential for teratogenicity, avoid unless clearly needed. Second and third trimesters: potential for fetal anticholinergic effects (tachycardia, constipation). |
| Fetal Monitoring | Monitor for maternal anticholinergic side effects (dry mouth, constipation, blurred vision, tachycardia, urinary retention). Fetal monitoring: consider fetal heart rate monitoring if used near term due to potential for fetal tachycardia. |
| Fertility Effects | Reduced fertility observed in animal studies. In humans: no controlled studies; anticholinergic effects may theoretically affect reproductive function, but clinical significance unknown. |
| Clinical Pearls | SANCTURA (trospium chloride) is a quaternary ammonium anticholinergic that does not cross the blood-brain barrier, resulting in fewer central nervous system side effects compared to other anticholinergics. It is primarily used for overactive bladder with symptoms of urge incontinence, urgency, and frequency. Because of its low lipophilicity, it has minimal drug-drug interactions via CYP450. Tablets should be taken at least one hour before meals on an empty stomach to maximize absorption. Dosage adjustment is required in severe renal impairment (CrCl <30 mL/min): 20 mg once daily at bedtime. |
| Patient Advice | Take SANCTURA on an empty stomach at least one hour before meals. · Swallow the tablet whole with water; do not crush, chew, or split. · Avoid driving or operating heavy machinery until you know how SANCTURA affects you, as it may cause drowsiness or blurred vision. · Drink plenty of fluids unless otherwise instructed by your doctor, but avoid excessive alcohol consumption. · Contact your doctor if you experience severe constipation, difficulty urinating, or signs of heat stroke (e.g., hot, dry skin with no sweating). · Do not take with other anticholinergic medications without consulting your healthcare provider. |