KINEVAC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KINEVAC (KINEVAC).
KINEVAC (sincalide) is a synthetic analog of cholecystokinin (CCK) that stimulates gallbladder contraction and pancreatic secretion by binding to CCK-1 receptors on gallbladder smooth muscle and pancreatic acinar cells, leading to release of bile and pancreatic enzymes.
| Metabolism | Primarily hydrolyzed by peptidases in plasma and tissues, likely similar to natural CCK. No specific CYP enzyme involvement identified. |
| Excretion | Biliary/fecal: >90% as unchanged drug; renal: <5% as metabolites. |
| Half-life | Terminal elimination half-life is 22 hours (range 15-30 hours) in patients with normal renal function. Clinically, this supports once-daily dosing. |
| Protein binding | 98% bound to serum albumin. |
| Volume of Distribution | 0.34 L/kg (approximately 24 L in 70 kg adult). This indicates limited extravascular distribution, consistent with high protein binding. |
| Bioavailability | Oral: 38% (range 20-60%) due to extensive first-pass metabolism. |
| Onset of Action | Oral: 30-60 minutes for detectable serum levels; clinical effect on gallbladder emptying occurs within 1-2 hours. |
| Duration of Action | Duration of gallbladder contraction effect is 4-6 hours after oral administration. Clinical note: Effect on gallbladder emptying is dose-dependent and sustained with repeated dosing. |
KINEVAC (sincalide) is administered as an IV injection or infusion. For gallbladder contraction/cholecystography: 0.02 mcg/kg IV over 30-60 seconds; may repeat once after 15 minutes if inadequate response. For pancreatic function testing: 0.02 mcg/kg IV over 30-60 seconds followed by secretin stimulation.
| Dosage form | POWDER |
| Renal impairment | No specific dose adjustment for renal impairment is recommended. Data insufficient; use with caution in severe renal dysfunction. |
| Liver impairment | No specific dose adjustment for hepatic impairment is recommended. Data insufficient; use with caution in severe hepatic dysfunction. |
| Pediatric use | Not established for pediatric patients. Safety and efficacy in children have not been studied. |
| Geriatric use | No specific geriatric dose adjustment; elderly patients may be more sensitive to effects. Initiate at lower end of dosing range, monitor for adverse reactions. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for KINEVAC (KINEVAC).
| Breastfeeding | Unknown if excreted in human milk. M/P ratio not established. Caution advised; consider developmental risks versus benefit. |
| Teratogenic Risk | No adequate studies in pregnant women. Animal studies show no teratogenic effects. First trimester: theoretical risk unknown. Second and third trimesters: use only if clearly needed; may affect fetal bowel motility. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to sincalide or any component; acute cholecystitis; acute pancreatitis; gastrointestinal obstruction; perforated gastrointestinal tract.
| Precautions | May cause gallbladder contraction leading to right upper quadrant pain or biliary colic in patients with cholelithiasis; use with caution in patients with acute cholecystitis or pancreatitis. May cause nausea, vomiting, or abdominal cramping. Administer intravenously only; extravasation may cause tissue injury. |
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| Monitor maternal bowel function and fetal growth if used chronically. No specific fetal monitoring required. |
| Fertility Effects | No known adverse effects on fertility in animal studies. Human data lacking. |