sincalide

Action and Spectrum

Actions and Spectrum: 

The mechanism of action of sincalide involves binding to the CCK receptors in the gastrointestinal tract, particularly the CCK-A receptors. By activating these receptors, sincalide stimulates the contraction of the gallbladder and relaxation of the sphincter of Oddi, which allows the release of bile into the small intestine. It also promotes the secretion of pancreatic enzymes such as amylase, lipase, and trypsin. 

The spectrum of activity of sincalide is primarily focused on the gallbladder and pancreas. sincalide helps assess the gallbladder’s functionality, evaluate biliary patency, and diagnose disorders such as gallstones, gallbladder dyskinesia, and acute acalculous cholecystitis by stimulating gallbladder contraction and bile release. In pancreatic function tests, sincalide can measure pancreatic exocrine secretion and assess pancreatic duct patency. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Nausea (20%) 

Abdominal discomfort or pain (20%) 

1-10% 

Dizziness (2%) 

<1% 

Flushing 

Rash 

Hypertension 

Shortness of breath 

Headache 

Diarrhea 

Sneezing 

Numbness 

Vomiting 

Sweating 

Hypotension 

Urge to defecate 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

Obstruction of intestine 

Hypersensitivity 

Caution: 

• Allergy or hypersensitivity: Allergic reactions may include symptoms such as rash, itching, swelling, dizziness, or difficulty breathing.  
• Gallbladder or pancreatic disorders: sincalide may not be appropriate for individuals with specific pre-existing gallbladder or pancreatic conditions 
• Adverse effects: While sincalide is generally well-tolerated, some individuals may experience mild adverse effects such as abdominal discomfort, nausea, vomiting, diarrhea, flushing, dizziness, or headache.

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

• Gallbladder Contraction: sincalide stimulates the contraction of the gallbladder by binding to CCK-A receptors located on smooth muscle cells in the gallbladder wall. This leads to increased gallbladder emptying and the release of bile into the small intestine. 
• Sphincter of Oddi Relaxation: sincalide also induces relaxation of the sphincter of Oddi, which is the muscle that controls the flow of bile and pancreatic enzymes into the small intestine. Relaxation of this muscle allows the free flow of bile and pancreatic secretions. 
• Pancreatic Enzyme Secretion: sincalide stimulates the secretion of pancreatic enzymes such as amylase, lipase, and trypsin from the acinar cells of the pancreas. This leads to increased pancreatic enzyme activity and the digestion of nutrients in the small intestine. 

Pharmacodynamics: 

The pharmacodynamics of sincalide involves its interactions with cholecystokinin (CCK) receptors and the resulting physiological effects. sincalide primarily acts on CCK receptors in the gastrointestinal tract. The two main types of CCK receptors are CCK-A and CCK-B receptors. sincalide has a higher affinity for CCK-A receptors. 

Pharmacokinetics: 

Absorption 

sincalide is typically administered intravenously, which ensures its rapid and complete absorption into the bloodstream. Intravenous administration allows for immediate availability of the drug and bypasses any absorption barriers in the gastrointestinal tract. 

Distribution 

Following intravenous administration, sincalide distributes throughout the body, including the gastrointestinal tract, where it exerts its effects. The exact distribution pattern of sincalide in various tissues and organs is not extensively studied, but it is expected to be relatively widespread due to its systemic effects. 

Metabolism 

sincalide is metabolized primarily by peptidases, enzymes responsible for the breakdown of peptides and proteins. It is broken down into smaller peptide fragments and individual amino acids. The specific metabolites generated from sincalide have yet to be extensively characterized. 

Elimination and Excretion 

The metabolites of sincalide, resulting from its metabolism, are primarily eliminated from the body through the kidneys via urine. The exact route and extent of excretion may vary depending on the specific metabolic pathways involved. sincalide has a short elimination half-life, typically ranging from a few minutes to several hours. 

Adminstartion

Administration: 

sincalide is administered intravenously, which means it is directly injected into a vein. The intravenous route ensures rapid and complete medication absorption into the bloodstream. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: sincalide 

Why do we use sincalide? 

sincalide is primarily used in medical diagnostics to evaluate the gallbladder and pancreas function. It is employed in various procedures to assess and diagnose conditions related to these organs.  

• Gallbladder Function Assessment: sincalide is commonly used in cholescintigraphy, also known as a hepatobiliary iminodiacetic acid (HIDA) scan. sincalide stimulates gallbladder contraction, aiding in evaluating gallbladder function, biliary system patency, and gallstones or gallbladder dyskinesia. 
• Pancreatic Function Testing: sincalide can be used in pancreatic function tests, particularly those involving the measurement of pancreatic exocrine secretion. It is commonly used in secretin-stimulated pancreatic function tests.