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| Primary information |
|---|
| ID | 10424 |
| Therapeutic ID | Th1071 |
| Protein Name | Pancrelipase |
| Sequence | >Th1071_Pancrelipase
QYSPNTQQGRTSIVHLFEWRWVDI
|
| Molecular Weight | 131000 |
| Chemical Formula | C5850H8902N1606O1739S49 |
| Isoelectric Point | 8.44 |
| Hydrophobicity | NA |
| Melting point | 48-50 |
| Half-life | Pancrelipase is not significantly absorbed from the gastrointestinal tract and acts locally, so limination half-life is not relevant |
| Description | Pancrelipase is an enzyme mixture isolated from porcine or bovine pancreas, sometimes called pancreatin. It contains 3 enzymes: amylase, lipase, and a protease (chymotrypsin). Pancrelipase is marketed under several brand names such as Ultresa and Viokace. |
| Indication/Disease | For treatment of exocrine pancreatic insufficiency in cystic fibrosis (Ultresa), chronic pancreatitis (Viokace in combination with a proton pump inhibitor), and pancreatectomy (Viokace in combination with a proton pump inhibitor) |
| Pharmacodynamics | Used in the treatment of cystic fibrosis or pancreatic dysfunction, pancrelipase helps improve fat digestion in the small intestine. Specifically, the lipase, protease and amylase components break down fat, protein, and starches, respectively, in the small intestine. Lipase hydrolyzes fats into glycerol and fatty acids. Protease converts proteins into proteoses and derived substances, while amylase converts starches into dextrins and sugars. Pancreatic enzymes are used to correct maldigestion, malabsorption and pain associated with pancreatic insufficiency. The major maldigestion/malabsorption problems arise from incomplete fat digestion. Exogenous pancrelipase reduces the amount of nitrogen and fat excreted in the stool. |
| Mechanism of Action | The lipase, protease and amylase components of pancrelipase break down fat, protein, and starches, respectively, in the small intestine. Lipase hydrolyzes fats into glycerol and fatty acids. Protease converts proteins into proteoses and derived substances, while amylase converts starches into dextrins and sugars. |
| Toxicity | Overdose symptoms may include diarrhea or stomach upset. The most common adverse reactions seen are ear, neck, and abdominal pain; headache, nasal congestion, and beta-hemolytic streptococcal infection. |
| Metabolism | Pancrelipase acts locally, so there is minimal metabolism. |
| Absorption | Pancrelipase is not significantly absorbed from the gastrointestinal tract. |
| NA |
| Clearance | Pancrelipase is not significantly absorbed, so there is minimal clearance from the body. |
| Categories | Alimentary Tract and Metabolism, Carboxylic Ester Hydrolases, Complex Mixtures, Digestives, Incl. Enzymes, Enzyme Preparations, Enzymes, Enzymes and Coenzymes, Esterases, Gastrointestinal Agents, Hydrolases, Lipase, Pancreatic Extracts, Tissue Extracts |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Synaptosomal-associated protein 25,Rho-related GTP-binding protein RhoB |
| Brand Name | ULTRESA |
| Company | Aptalis Pharma US, Inc. |
| Brand Description | Aptalis Pharma US, Inc. |
| Prescribed For | ULTRESA (pancrelipase) is indicated for the treatment of exocrinepancreatic insufficiency due to cystic fibrosis or other conditions. |
| Chemical Name | NA |
| Formulation | Each delayed-release capsule for oral administration contains enteric-coatedbeads (1.7 mm in diameter and 1.9 mm thick for 4,000 USP lipase units, approximately 2.0 mm in diameter and 2.0 – 2.4 mm thick for 13,800, 20,700, and 23,000 USP lipase units). it also contains colloidal silicon dioxide, croscarmellose sodium, hydrogenated castor oil, hypromellose phthalate, magnesium stearate, microcrystalline cellulose, talc, and triethyl citrate. |
| Physical Appearance | Pancrelipase is a beige-white amorphous powder. It is miscible in water and practically insoluble or insoluble in alcohol and ether and converted to Delayed-Release Capsules |
| Route of Administration | Oral route |
| Recommended Dosage | Enzyme dosing should begin with 500 lipase units/kg of body weight per meal for those older than age 4 years to a maximum of 2,500 lipase units/kg of body weight per meal (or less than or equal to 10,000 lipase units/kg of body weight per day), or less than 4,000 lipase units/g fat ingested per day. |
| Contraindication | None |
| Side Effects | The most serious adverse reactions reported with different pancreatic enzyme products of the same active ingredient (pancrelipase) that are described elsewhere in the label include fibrosing colonopathy,hyperuricemia and allergic reactions. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |