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| Primary information |
|---|
| ID | 11429 |
| Therapeutic ID | Th1247 |
| Protein Name | Glucagon |
| Sequence | >Th1247_Glucagon
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
|
| Molecular Weight | 3767.1 |
| Chemical Formula | C165H249N49O51S1 |
| Isoelectric Point | 7.1 |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | The half life of glucagon is 26 minutes for an intramuscular dose.[L7634] The half life of glucagon nasal powder is approximately 35 minutes.[L7643] The half life of glucagon by a subcutaneous auto-injector or pre-filled syringe is 32 minutes.[L8519] |
| Description | Glucagon is a 29 amino acid hormone used as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and to treat severe hypoglycemia.[L7634,L7637,L7640,L7643,L8519] Glucagon raises blood sugar through activation of hepatic glucagon receptors, stimulating glycogenolysis and the release of glucose.[L7640,L7643] Glucagon was granted FDA approval on 14 November 1960.[L7631] |
| Indication/Disease | Glucagon is indicated as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and to treat severe hypoglycemia.[L7634,L7637,L7640,L7643,L8519] |
| Pharmacodynamics | Glucagon is indicated as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and severe hypoglycemia.[A19402,L7634,L7637,L7640,L7643,L8519] Glucagon raises blood sugar through activation of hepatic glucagon receptors, stimulating glycogenolysis and the release of glucose.[L7640,L7643] Glucagon has a short duration of action.[L7634,L7637,L7640,L7643] Glucagon may cause hyperglycemia in diabetic patients.[L7634,L7637,L7640,L7643] |
| Mechanism of Action | Glucagon binds to the glucagon receptor activating Gsa and Gq.[A19402] This activation activates adenylate cyclase, which increases intracellular cyclic AMP and activates protein kinase A.[A19402] Activating Gq activates phospholipase C, increases production of inositol 1,4,5-triphosphate, and releases intracellular calcium.[A19402] Protein kinase A phosphorylates glycogen phosphorylase kinase, which phosphorylates glycogen phosphorylase, which phosphorylates glycogen, causing its breakdown.[A19402] Glucagon also relaxes smooth muscle of the stomach, duodenum, small bowel, and colon.[L7634,L7643] |
| Toxicity | Patients experiencing an overdose may present with nausea, vomiting, inhibition of GI tract motility, increased blood pressure and heart rate, and decreased serum potassium.[L7634,L7637,L7640,L7643] Phentolamine may be given to control blood pressure.[L7634,L7637,L7640,L7643] Treatment of glucagon overdose is largely symptomatic for nausea, vomiting, and hypokalemia.[L7637] The LD50 for intravenous glucagon in mice is 300mg/kg and in rats is 38.6mg/kg.[L7637] |
| Metabolism | Glucagon is a protein and so it is metabolized into smaller polypeptides and amino acids in the liver, kidney, and plasma.[L7634,L7643] |
| Absorption | A 1mg intravenous dose of glucagon reaches a Cmax of 7.9ng/mL with a Tmax of 20 minutes.[L7637] An intramuscular dose reaches a Cmax of 6.9ng/mL with a Tmax of 13 minutes.[L7637] A 3mg dose of glucagon nasal powder reaches a Cmax of 6130pg/mL with a Tmax of 15 minutes.[L7643] |
| The volume of distribution of glucagon is 0.25L/kg.[L7637] The apparent volume of distribution is 885L.[L7643] |
| Clearance | A 1mg intravenous dose of glucagon has a clearance of 13.5mL/min/kg.[L7637] |
| Categories | NA |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Glucagon receptor,Glucagon-like peptide 2 receptor,Glucagon-like peptide 1 receptor |
| Brand Name | Gvoke PFS 0.5 mg Pre-filled Syringe |
| Company | Xeris Pharmaceuticals, Inc. |
| Brand Description | Xeris Pharmaceuticals, Inc. |
| Prescribed For | Subcutaneous |
| Chemical Name | 0.5 mg/0.1mL |
| Formulation | GVOKE is contraindicated in patients with: Pheochromocytoma Insulinoma [ see WARNINGS AND PRECAUTIONS] because of the risk of hypoglycemia Known hypersensitivity to glucagon or to any of the excipients in GVOKE. Allergic reactions have been reported with glucagon and include anaphylactic shock with breathing difficulties and hypotension. |
| Physical Appearance | nausea vomiting hives injection site swelling or redness headache fast heartbeat |
| Route of Administration | Glucagon comes as a solution (liquid) in a prefilled syringe and an auto-injector device to inject subcutaneously (just under the skin). It also comes as a powder to be mixed with a provided liquid to be injected subcutaneously, intramuscularly (into the muscle), or intravenously (into a vein). It is usually injected as needed at the first sign of severe hypoglycemia. |
| Recommended Dosage | Glucagon is used along with emergency medical treatment to treat very low blood sugar. Glucagon is also used in diagnostic testing of the stomach and other digestive organs. Glucagon is in a class of medications called glycogenolytic agents. It works by causing the liver to release stored sugar to the blood. It also works by relaxing smooth muscles of the stomach and other digestive organs for diagnostic testing. |
| Contraindication | (3S)-3-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid |
| Side Effects | NA |
| Useful Link 1 | Link |
| Useful Link 2 | Link |
| Remarks | NA |