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| Primary information |
|---|
| ID | 10253 |
| Therapeutic ID | Th1035 |
| Protein Name | Glucagon recombinant |
| Sequence | >Th1035_Glucagon_recombinant
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
|
| Molecular Weight | 3767.1 |
| Chemical Formula | C165H249N49O51S1 |
| Isoelectric Point | 7.1 |
| Hydrophobicity | -1.197 |
| Melting point | NA |
| Half-life | 0.58 hours for glucagon nasal powder |
| 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 | atients experiencing an overdose may present with nausea, vomiting, inhibition of GI tract motility, increased blood pressure and heart rate, and decreased serum potassium. Phentolamine may be given to control blood pressure. Treatment of glucagon overdose is largely symptomatic for nausea, vomiting, and hypokalemia. |
| Metabolism | Glucagon is a protein and so it is metabolized into smaller polypeptides and amino acids in the liver, kidney, and plasma. |
| Absorption | A 1mg intravenous dose of glucagon reaches a Cmax of 7.9ng/mL with a Tmax of 20 minutes.An intramuscular dose reaches a Cmax of 6.9ng/mL with a Tmax of 13 minutes. A 3mg dose of glucagon nasal powder reaches a Cmax of 6130pg/mL with a Tmax of 15 minutes |
| 0.25 L/kg |
| Clearance | 13.5 mL/min/kg [Adults with IV 1 mg] |
| Categories | Amino Acids, Peptides, and Proteins, Antihypoglycemic Agent, Decreased GI Motility, Decreased GI Smooth Muscle Tone, Decreased Glycolysis, Gastrointestinal Agents, Gastrointestinal Hormones, Gastrointestinal Motility Inhibitor, Glucagon, antagonists & inhibitors, Glycogenolytic Agents, Glycogenolytic Hormones, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Increased Gluconeogenesis, Increased Glycogenolysis, Pancreatic Hormones, Peptide Hormones, Peptides, Proglucagon, Protein Precursors, Proteins, Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | NA |
| Brand Name | Baqsimi |
| Company | Eli Lilly and Company |
| Brand Description | Eli Lilly and Company |
| Prescribed For | very low blood sugar (severe hypoglycemia) in people with diabetes ages 4 years and above. |
| Chemical Name | C153H225N43O49S |
| Formulation | Glucagon is a single-chain polypeptide containing 29 amino acid residues and has a molecular weight of 3483, and is identical to human glucagon. |
| Physical Appearance | preservative-free, white powder |
| Route of Administration | intranasal administration in an intranasal device |
| Recommended Dosage | The recommended dose of BAQSIMI is 3 mg administered as one actuation of the intranasal device into one nostril. If there has been no response after 15 minutes, an additional 3 mg dose of BAQSIMI from a new device may be administered while waiting for emergency assistance. |
| Contraindication | BAQSIMI is contraindicated in patients with: Pheochromocytoma because of the risk of substantial increase in blood pressure Insulinoma because of the risk of hypoglycemia Known hypersensitivity to glucagon or to any of the excipients in BAQSIMI. Allergic reactions have been reported with glucagon and include anaphylactic shock with breathing difficulties and hypotension |
| Side Effects | nausea vomiting headache runny nose discomfort in your nose stuffy nose redness in your eyes itchy nose, throat and eyes watery eyes |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |