| Primary information |
|---|
| ThPP ID | Th1035 |
| Therapeutic Peptide/Protein Name | Glucagon recombinant |
| Sequence | HSQGTFTSDYSKYLDSRRAQDFVQWLMNT view full sequnce in fasta |
| Functional Classification | IV |
| Molecular Weight | 3767.1 |
| Chemical Formula | C165H249N49O51S1 |
| Isoelectric Point | 9.52 |
| Hydrophobicity | -1.197 |
| Melting Point (℃) | N.A. |
| Half Life | N.A. |
| Description | Glucagon is a 29 residue peptide hormone, synthesized in a special non- pathogenic laboratory strain of Escherichia coli bacteria that has been genetically altered by the addition of the gene for glucagons. |
| Indication/Disease | Used to treat severe hypoglycemia, also used in gastrointestinal imaging. |
| Pharmacodynamics | Used in the treatment of hypoglycemia and in gastric imaging, glucagon increases blood glucose concentration and is used in the treatment of hypoglycemia. Glucagon acts only on liver glycogen, converting it to glucose through the release of insulin. It also relaxes the smooth muscles of the gastrointestinal tract. |
| Mechanism of Action | Glucagon binds the glucagon receptor(G protein-coupled receptor located in the plasma membrane) which then initiates a dual signaling pathway using both adenylate cyclase activation and increased intracellular calcium. Adenylate cyclase manufactures cAMP (cyclic AMP), which activates protein kinase A (cAMP-dependent protein kinase). This enzyme, in turn, activates phosphorylase kinase, which, in turn, phosphorylates glycogen phosphorylase, converting into the active form called phosphorylase A. Phosphorylase A is the enzyme responsible for the release of glucose-1-phosphate from glycogen polymers. This yields glucose molecules to be released into the blood. Glucagon receptors are found in the liver, kidney, brain and pancreatic islet cells. The glucagon mediated signals lead to an increase in insulin excretion |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | 0.25 L/kg |
| Clearance | 13.5Â mL/min/kg [Adults with IV 1 mg] |
| Categories | Hypoglycemic Agents |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | N.A. |
| Target | Glucagon receptor,Glucagon-like peptide 2 receptor,Glucagon-like peptide 1 receptor |
| Information of corresponding available drug in the market |
|---|
| Brand Name | GlucaGen |
| Company | Novo Nordisk |
| Brand Discription | GlucaGen(29 amino acid residues, 3483 daltons, single polypeptide) is an antihypoglycemic agent and a gastrointestinal motility inhibitor. It is produced by expression of recombinant DNA in a Saccharomyces cerevisiae vector with subsequent purification. T |
| Prescribed for | GlucaGen is used to treat severe hypoglycemic (low blood sugar) reactions which may occur in patients with diabetes mellitus treated with insulin. It is also used as a diagniostic aid. GlucaGen is indicated for use during radiologic examinations to tempor |
| Chemical Name | N.A. |
| Formulation | The reconstituted solution contains glucagon as hydrochloride 1 mg/mL (1 unit/mL) and lactose monohydrate (107 mg). GlucaGen is supplied at pH 2.5-3.5 and is soluble in water. |
| Physcial Appearnce | Sterile, lyophilized white powder |
| Route of Administration | Subcutaneous, intramuSubcutaneousular, or Intraven |
| Recommended Dosage | Inject 1 mL (adults and children, weighing more than 55 lbs (25 kg)) or 0.5 mL (children weighing less than 55 lbs (25 kg)) subcutaneously, intramuscularly, or intravenously. If the weight is not known: children younger than 6 years should be given a 0.5 |
| Contraindication | Hypersensitivity |
| Side Effects | Severe side effects are very rare, although nausea and vomiting may occur occasionally especially with doses above 1 mg or with rapid injection (less than 1 minute). You may also have rapid heart beat for a short while. |
| Useful Link | http://www.novonordisk.co.in/documents/article_page/document/Glucagen.asp |
| PubMed ID | 17462598, 17620721, 17623014, 17534934, 15817468 |
| 3-D Structure | Th1035 (View) or (Download) |