URECHOLINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for URECHOLINE (URECHOLINE).
Bethanechol is a synthetic choline ester that directly stimulates muscarinic acetylcholine receptors, primarily M2 and M3 subtypes, leading to increased gastrointestinal motility, bladder contraction, and other parasympathetic effects. It has minimal nicotinic activity.
| Metabolism | Primarily metabolized by plasma and tissue esterases via hydrolysis; negligible hepatic metabolism. |
| Excretion | Primarily renal excretion of unchanged drug and metabolites; approximately 50-60% excreted in urine within 24 hours, with negligible biliary or fecal elimination. |
| Half-life | Terminal elimination half-life is approximately 1.5-2 hours. Due to its short half-life, continuous or frequent dosing is required for sustained cholinergic effects. |
| Protein binding | Minimal (<5%) binding to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.3-0.5 L/kg, indicating distribution primarily into extracellular fluid with limited tissue penetration. |
| Bioavailability | Oral: 10-20% due to extensive first-pass metabolism; Subcutaneous: near 100% bioavailable. |
| Onset of Action | Oral: 30-90 minutes; Subcutaneous: 5-15 minutes. Intravenous administration is contraindicated due to risk of severe cholinergic crisis. |
| Duration of Action | Oral: 4-6 hours; Subcutaneous: 2-4 hours. Duration may be dose-dependent and shorter in patients with rapid gastrointestinal transit. |
10-50 mg orally two to four times daily; alternatively, 5 mg subcutaneously three to four times daily. Maximum oral dose: 200 mg daily.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in patients with significant renal impairment (CrCl < 30 mL/min). Use with caution in mild to moderate impairment, with dose reduction as needed. |
| Liver impairment | No specific adjustment recommended for Child-Pugh classification; use with caution in severe hepatic impairment. |
| Pediatric use | Safety and efficacy not established for children under 8 years. For older children, oral dose of 0.6 mg/kg three times daily, or subcutaneous dose of 0.15 mg/kg three to four times daily. Maximum single dose: 5 mg. |
| Geriatric use | Initiate at low end of dosing range (e.g., 5-10 mg orally) due to increased sensitivity to cholinergic effects and risk of bradycardia, hypotension, and falls. Titrate slowly based on response and tolerability. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for URECHOLINE (URECHOLINE).
| Breastfeeding | No data on excretion in human milk; M/P ratio unknown. Caution recommended due to potential for cholinergic effects in the infant. |
| Teratogenic Risk | Pregnancy Category C. First trimester: No adequate human studies; animal studies not available. Second and third trimesters: Potential to induce uterine hypertonicity and fetal bradycardia if used near term. Avoid use during pregnancy unless clearly necessary. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to bethanechol or any component.","Hyperthyroidism, asthma, peptic ulcer disease, or significant gastrointestinal obstruction.","Mechanical intestinal or urinary tract obstruction.","Recent gastrointestinal surgery, bladder wall instability, or concurrent use of anticholinergic agents.","Bradycardia, hypotension, or coronary insufficiency."]
| Precautions | ["Risk of severe cholinergic adverse effects, including hypotension, bradycardia, and bronchospasm.","Use with caution in patients with epilepsy, hyperthyroidism, asthma, coronary artery disease, or peptic ulcer disease.","May exacerbate urinary obstruction if anatomical obstruction is present.","Administer subcutaneously only; not for intramuscular or intravenous use (risk of severe cholinergic crisis)."] |
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| Monitor maternal heart rate, blood pressure, and signs of cholinergic excess. Fetal heart rate monitoring if used near term. |
| Fertility Effects | No data on effects on human fertility. Animal studies not available. |