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| Primary information |
|---|
| ID | 15050 |
| Therapeutic ID | Th1565 |
| Protein Name | Pancrelipase lipase |
| Sequence | >Th1565_Pancrelipase_lipase
SEVCFPRLGCFSDDAPWAGIVQRPLKILPWSPKDVDTRFLLYTNQNQNNYQELVADPSTITNSNFRMDRKTRFIIHGFIDKGEEDWLSNICKNLFKVESVNCICVDWKGGSRTGYTQASQNIRIVGAEVAYFVEVLKSSLGYSPSNVHVIGHSLGSHAAGEAGRRTNGTIERITGLDPAEPCFQGTPELVRLDPSDAKFVDVIHTDAAPIIPNLGFGMSQTVGHLDFFPNGGKQMPGCQKNILSQIVDIDGIWEGTRDFVACNHLRSYKYYADSILNPDGFAGFPCDSYNVFTANKCFPCPSEGCPQMGHYADRFPGKTNGVSQVFYLNTGDASNFARWRYKVSVTLSGKKVTGHILVSLFGNEGNSRQYEIYKGTLQPDNTHSDEFDSDVEVGDLQKVKFIWYNNNVINPTLPRVGASKITVERNDGKVYDFCSQETVREEVLLTLNPC
|
| Molecular Weight | 48000 |
| Chemical Formula | NA |
| Isoelectric Point | 7.4 |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the elimination half-life is not relevant.105 |
| Description | Pancrelipase, in general, is composed of a mixture of pancreatic enzymes which include amylases, lipases, and proteases. These enzymes are extracted from porcine pancreatic glands.[L2509] The amylases are enzymes that help in the chemical process of digestion by hydrolizing starch into more available saccharide forms.[T177] The pancrelipase amylase is a single polypeptide chain containing two SH groups and four disulfide bridges.[L2512] The pancrelipase mixture, including pancrelipase amylase, was developed by Ortho-McNeil-Janssen Pharmaceuticals, Inc and FDA approved on April 12, 2010.[L2510] |
| Indication/Disease | The use of pancrelipase amylase is part of the pancreatic enzyme replacement therapy. This therapy is indicated for the treatment of pancreatic insufficiency attributed to cystic fibrosis, chronic pancreatitis or any other medically defined pancreatic disease that might require it. Pancreatic diseases are associated with the deterioration of pancreatic parenchyma and of the dual physiological functions of the pancreas. Once established, pancreatic insufficiency results in malnutrition, weight loss, and steatorrhea. |
| Pharmacodynamics | The major maldigestion/malabsorption problems arise from incomplete fat digestion. In clinical trials, the administration of pancrelipase as a mixture of amylase, lipase, and protease demonstrated a significant improvement in the coefficient of fat absorption and nitrogen absorption. These effects are accompanied by increased in body weight and body mass index. |
| Mechanism of Action | Pancrelipase lipase catalyzes the hydrolysis of triglycerides to monoglycerides, glycerol, and fatty acids. This activity is performed by the hydrolyzation of the esters of fatty acids. The hydrolysis is started by the action of colipase which helps to anchor lipase to the lipid-water membrane of the micelle producing a surface change on lipase. The hydrophobic active site is exposed for the binding of triglycerides and further interaction with the catalytic triad. In this triad, the function of the three amino acids allows the formation of a deprotonated serine which becomes a nucleophile and act on the ester carbonyl of the fatty acids for the later formation of monoglyceride and fatty acid monomers.[A32750] |
| Toxicity | The studies of the toxicology of pancrelipase are not needed as this drug has been used clinically for a long time. Clinical overdose studies proved no effect on lungs, pancreas, liver and kidneys but it can produce symptoms such as diarrhea or stomach upset. Carcinogenicity studies have not shown any increased incidence with the use of pancrelipase. As pancrelipase is not absorbed, the effect on fetal development or reproduction is not expected. |
| Metabolism | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the metabolism is not relevant. |
| Absorption | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount. |
| Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the volume of distribution is not relevant. |
| Clearance | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the clearance rate is not relevant. |
| Categories | Enzymes |
| Patents Number | 8562979 |
| Date of Issue | 22-10-2013 |
| Date of Expiry | 20-02-2028 |
| Drug Interaction | NA |
| Target | Dietary fat |
| Brand Name | Cotazym |
| Company | Organon Canada Inc. |
| Brand Description | Organon Canada Inc. |
| Prescribed For | Oral |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | Abnormal feces anxiety bloated feeling chills cold sweats confusion cool, pale skin depression excess air or gas in the stomach or intestines feeling of fullness fever frequent bowel movements loss of consciousness muscle aches nightmares passing gas runny nose seizures shakiness slurred speech sore throat |
| Route of Administration | NA |
| Recommended Dosage | NA |
| Contraindication | NA |
| Side Effects | NA |
| Useful Link 1 | Link |
| Useful Link 2 | Link |
| Remarks | NA |