SINCALIDE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SINCALIDE (SINCALIDE).
Sincalide is a synthetic carboxyl-terminal octapeptide of cholecystokinin (CCK). It acts as a CCK-A receptor agonist in the gallbladder and small intestine, causing contraction of the gallbladder and stimulation of pancreatic and gastric secretions. It also stimulates peristalsis and delays gastric emptying.
| Metabolism | Sincalide is rapidly metabolized in the liver and plasma by aminopeptidases and endopeptidases, producing inactive fragments. Primary enzyme responsible is neutral endopeptidase (neprilysin). |
| Excretion | Biliary (80-90% as parent drug and metabolites), renal (<5% unchanged) |
| Half-life | 4-6 minutes (rapid elimination, requires continuous infusion for sustained effect) |
| Protein binding | ~90% (primarily albumin) |
| Volume of Distribution | 0.2 L/kg (confined to extracellular fluid, consistent with low tissue penetration) |
| Bioavailability | Not applicable (administered IV or IM; no oral bioavailability due to GI degradation) |
| Onset of Action | IV: 15-30 seconds; IM: 5-10 minutes |
| Duration of Action | IV: 15-30 minutes (biliary effects persist up to 1 hour); IM: 1-2 hours |
0.02 mcg/kg IV bolus over 30-60 seconds, may repeat once after 5 minutes if gallbladder contraction inadequate; maximum total dose 1 mcg.
| Dosage form | POWDER |
| Renal impairment | No specific dose adjustment recommended; limited data in severe renal impairment (CrCl <30 mL/min); use with caution. |
| Liver impairment | No specific dose adjustment recommended; use with caution in Child-Pugh class B or C due to altered drug metabolism; monitor for prolonged effect. |
| Pediatric use | 0.02 mcg/kg IV bolus over 30-60 seconds; maximum single dose 1 mcg; safety and efficacy not established in children <18 years; off-label use with caution. |
| Geriatric use | Monitor renal function; consider starting at lower end of dosing range due to age-related decreased renal function; no specific dose adjustment required. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SINCALIDE (SINCALIDE).
| Breastfeeding | No data on excretion into human milk. M/P ratio unknown. Consider risk-benefit; use cautiously in nursing mothers due to potential for gastrointestinal effects in infant if absorbed. |
| Teratogenic Risk | Sincalide is a synthetic cholecystokinin analog used diagnostically. No adequate and well-controlled studies in pregnant women. Animal reproduction studies have not been conducted. Risk cannot be ruled out. Avoid use in first trimester if possible; use only if clearly needed in second and third trimesters with consideration of maternal benefit versus unknown fetal risk. |
■ FDA Black Box Warning
None
| Serious Effects |
["Known hypersensitivity to sincalide or any component of the formulation","Obstruction of the gastrointestinal or biliary tract","Acute pancreatitis","Perforated viscus","Hemorrhagic pancreatitis"]
| Precautions | ["May cause gallbladder contraction leading to stone impaction, acute cholecystitis, or pancreatitis","Use with caution in patients with suspected obstruction of the common bile duct or gallbladder","May cause transient hypotension or tachycardia","May induce abdominal pain or nausea","Use in pregnancy only if clearly needed"] |
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| Fetal Monitoring |
| Monitor maternal vital signs during infusion, including blood pressure and heart rate, due to potential vasovagal reactions or hypotension. Fetal monitoring not typically required; may consider ultrasound if used near term due to unknown effects. |
| Fertility Effects | No studies on fertility effects. Theoretical risk of alteration in reproductive hormone levels due to cholecystokinin receptor activity, but clinical significance unknown. |