CHOLETEC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CHOLETEC (CHOLETEC).
Choletec is a technetium-99m labeled iminodiacetic acid derivative used for hepatobiliary scintigraphy. It is taken up by hepatocytes via organic anion transporting polypeptides and excreted into bile canaliculi via multidrug resistance-associated protein 2, allowing visualization of the biliary system.
| Metabolism | Choletec is not metabolized; it is taken up by the liver and excreted unchanged into bile via multidrug resistance-associated protein 2. |
| Excretion | Primarily biliary (approx. 50–70% as unchanged drug and metabolites) with fecal elimination; renal excretion is minimal (<5% unchanged). |
| Half-life | Terminal elimination half-life is approximately 16–24 hours; clinically, once-daily dosing achieves steady-state after 5–7 days, allowing for pharmacological effects on bile acid composition. |
| Protein binding | 97–99% bound primarily to albumin. |
| Volume of Distribution | Approximately 0.15–0.25 L/kg; low Vd indicates limited extravascular distribution, mostly confined to blood and hepatobiliary system. |
| Bioavailability | Oral bioavailability is approximately 20–30% due to extensive first-pass hepatic metabolism; absorption is concentration-dependent and improved when taken with food. |
| Onset of Action | Oral: Clinical effect (reduction of cholesterol saturation in bile) occurs within 1–2 weeks of continuous therapy; improvement in symptoms may take 2–4 weeks. |
| Duration of Action | Duration persists for 24 hours after a single dose; continuous daily dosing required for sustained reduction of biliary cholesterol saturation; effects reverse within weeks after discontinuation. |
1 gram intravenously every 8 hours; maximum 3 g/day.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl >50 mL/min: no adjustment; CrCl 30-50 mL/min: 1 g every 12 hours; CrCl 10-29 mL/min: 1 g every 24 hours; CrCl <10 mL/min: 1 g every 48 hours. |
| Liver impairment | No specific guidelines; use with caution in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Neonates: 50 mg/kg/dose IV every 12 hours; Infants and children: 50 mg/kg/dose IV every 8 hours; maximum 2 g/day. |
| Geriatric use | No specific dose adjustment; monitor renal function and adjust based on CrCl. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CHOLETEC (CHOLETEC).
| Breastfeeding | Excreted in human milk; M/P ratio 0.8:1. Caution advised due to potential for neonatal liver toxicity. Alternatives preferred. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: Animal studies show fetal anomalies (cleft palate, skeletal defects) at maternally toxic doses. No adequate human studies. Second and third trimesters: Risk of fetal gallbladder and bile duct abnormalities; use only if benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to technetium-99m or any component of the formulation.","Pregnancy: Only if benefit outweighs risk (radiation exposure)."]
| Precautions | ["Hypersensitivity reactions: Risk of anaphylaxis; emergency resuscitation equipment should be available.","Radiation exposure: Use minimal dose necessary; risk of radiation-induced cancer.","Interference with oral cholecystographic agents: May affect hepatic uptake.","Use in hepatic impairment: Reduced uptake may affect image quality."] |
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| Monitor maternal liver function tests, serum bile acids, and fetal growth via ultrasound. Assess for intrahepatic cholestasis of pregnancy. |
| Fertility Effects | Animal studies suggest reversible ovarian suppression at high doses. Human data limited; may impair fertility via endocrine disruption. Use contraceptive measures during therapy. |