Pharmacology, Clinical Uses, and Adverse Effects of Ceruletide, A Cholecystokinetic Agent

Abstract

Ceruletide, a decapeptide, is a potent cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts in humans and animals. It was recently approved by the Food and Drug Administration for use as an adjunct in x-ray examination of the gallbladder and small bowel. The drug causes a coordinated propulsive activity from the duodenum to the ileum and segmenting activity in the colon. Because of this stimulatory effect, ceruletide is useful not only diagnostically as an aid in x-ray examination of the small bowel, but also therapeutically for treatment of postoperative ileus, intestinal atonia, and chronic fecal statis. Because of its pancreatic stimulatory action, it is useful in evaluation of exocrine pancreatic function. In therapeutic doses the adverse effects noted are mild, transient extensions of the drug's pharmacologic actions and are manifest as nausea, vomiting, abdominal pain, and rarely hypotension and tachycardia. On the basis of current evidence, ceruletide is a safe and effective cholecystokinetic agent and small bowel and exocrine pancreatic stimulant.

Review of the Pathophysiology and Management of Postoperative Ileus

“…It has since been removed from the market because potentially fatal arrhythmias were associated with its use, and no substitute for the drug has become available. Clinical trials in the 1980s revealed some benefit of the synthetic cholecystokinin agonist ceruletide; however, adverse effects such as nausea and vomiting have limited its clinical usefulness and may account for the lack of more recent studies 45,46. Unfortunately, there is currently no prokinetic drug that has been found to be safe and effective for the treatment of postoperative ileus.…”

Repetitive Cerulein-Induced Chronic Pancreatitis in Growing Pigs—A Pilot Study

“…As previously mentioned, pancreatitis, one of the most common problems in gastroenterology, is linked to serious complications and high patient mortality [16][17][18][19]. Cerulein, a decapeptide, is an analogue of CCK and a potent stimulant of the musculature of the gallbladder and the intestine, as well as a powerful stimulant of pancreatic secretion and moderate stimulant of gastric secretion [20][21][22][23]. Cerulein is used in rodent and non-rodent studies to induce secretory effects or pancreatic injury in a time-, species-, dose-and routdependent manner [20,[24][25][26][27].…”

Ceruletide, an Analog of Cholecystokinin Octapeptide: New Perspectives on Its Efficacy

“…Early studies reported that ceruletide attenuates anxiety associated with histamine-induced headache in patients with psychogenic headache compared to placebo (6). When used in cholecystography, ceruletide often causes nausea and abdominal discomfort and occasionally produces flushing, tachycardia, and dizziness (100). The latter symptoms might be consistent with the criteria for panic attack.…”

“…1) and possesses a virtually identical spectrum of biological activities. Because ceruletide induces a variety of CCK-8-like effects on the digestive organs (e.g., stimulation of gallbladder contraction, pancreatic enzyme secretion, and intestinal motility), it was initially thought to be potentially useful for examining digestive functions and treating intestinal disease (100). Actually, ceruletide has been clinically used in cholecystography (80).…”