Detailed description page of ThPDB2
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11405 details |
| Primary information | |
|---|---|
| ID | 11405 |
| 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 | Amino Acids, Peptides, and Proteins |
| Patents Number | 10213487 |
| Date of Issue | 26-02-2019 |
| Date of Expiry | 16-02-2036 |
| Drug Interaction | Tramadol,Trospium,Oxyphenonium,Benzatropine,Ziprasidone,Disopyramide,Amitriptyline,Ipratropium,Olanzapine,Metixene,Terfenadine,Buclizine,Clozapine,Doxylamine,Trihexyphenidyl,Oxyphencyclimine,Procyclidine,Profenamine,Promazine,Hyoscyamine,Cyproheptadine,Imipramine,Methscopolamine bromide,Chlorpromazine,Gallamine triethiodide,Darifenacin,Tridihexethyl,Triflupromazine,Anisotropine methylbromide,Nortriptyline,Amoxapine,Lamotrigine,Atropine,Nicardipine,Pirenzepine,Paroxetine,Homatropine methylbromide,Rocuronium,Scopolamine,Benzquinamide,Clidinium,Propiomazine,Propantheline,Dicyclomine,Biperiden,Brompheniramine,Flupentixol,Cocaine,Quinidine,Maprotiline,Methantheline,Cycrimine,Glycopyrronium,Tolterodine,Oxybutynin,Promethazine,Diphenhydramine,Doxacurium,Doxepin,Flavoxate,Desipramine,Orphenadrine,Escitalopram,Quetiapine,Mivacurium,Diphenidol,Aripiprazole,Chlorprothixene,Metocurine,Pancuronium,Pipecuronium,Methotrimeprazine,Tiotropium,Solifenacin,Isopropamide,Rapacuronium,Mepenzolate,Pizotifen,Fesoterodine,Hexocyclium,Dimetindene,Aclidinium,Dexetimide,Benactyzine,Umeclidinium,Trimebutine,Dosulepin,Imidafenacin,Butylscopolamine,Thonzylamine,Methscopolamine,Revefenacin,Oxitropium,Propiverine,Batefenterol,Mebeverine,Tropatepine,Prifinium,Piperidolate,Benzilone,Difemerine,Phenglutarimide,Mazaticol,Etybenzatropine,Otilonium,Emepronium,Poldine,Bevonium,Rociverine,Bornaprine,Etanautine,Tiemonium iodide,Dihexyverine,Penthienate,Diphemanil,Camylofin,Fenpiverinium,Emetonium iodide,Pipenzolate,Timepidium,Chlorphenoxamine,Indomethacin,Dicoumarol,Phenindione,Warfarin,Phenprocoumon,Acenocoumarol,4-hydroxycoumarin,Coumarin,(R)-warfarin,Ethyl biscoumacetate,Fluindione,Clorindione,Diphenadione,Tioclomarol,(S)-Warfarin,Esmolol,Betaxolol,Metoprolol,Atenolol,Timolol,Sotalol,Propranolol,Labetalol,Bisoprolol,Alprenolol,Pindolol,Carvedilol,Propafenone,Acebutolol,Nadolol,Bevantolol,Practolol,Penbutolol,Oxprenolol,Dexpropranolol,Celiprolol,Nebivolol,Bufuralol,Bopindolol,Bupranolol,Indenolol,Arotinolol,Levobetaxolol,Talinolol,Anisodamine,Bucindolol,Esatenolol,Cloranolol,Mepindolol,Epanolol,Tertatolol,Landiolol,Insulin human,Insulin lispro,Insulin glargine,Insulin pork,Insulin aspart,Insulin detemir,Insulin glulisine,NN344,Insulin beef,Insulin degludec,Insulin peglispro,Insulin tregopil,Insulin argine,Magnesium,Belladonna |
| Target | Glucagon receptor,Glucagon-like peptide 2 receptor,Glucagon-like peptide 1 receptor |
| Brand Name | Baqsimi |
| Company | Eli Lilly and Company |
| Brand Description | Eli Lilly and Company |
| Prescribed For | Nasal |
| Chemical Name | 3 mg/1 |
| Formulation | BAQSIMI is contraindicated in patients with:Pheochromocytoma because of the risk of substantial increase in blood pressure [see WARNINGS AND PRECAUTIONS]Insulinoma because of the risk of hypoglycemia [see WARNINGS AND PRECAUTIONS]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 [see WARNINGS AND PRECAUTIONS] |
| Physical Appearance | nausea, vomiting, headache, upper respiratory tract irritation (i.e., runny nose, nasal discomfort, nasal congestion, cough, and nosebleed), watery eyes, eye redness, sneezing, and itchy nose, throat, and eyes |
| Route of Administration | Baqsimi is a hormone that increases blood sugar levels. It also slows involuntary muscle movements of the stomach and intestines that aid in digestion. Baqsimi Nasal Powder is a prescription medicine used to treat severe hypoglycemia (low blood sugar) in adult and children at least 4 years old. Baqsimi... |
| Recommended Dosage | BAQSIMI⢠is indicated for the treatment of severe hypoglycemia in adult and pediatric patients with diabetes ages 4 years and above. |
| 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 | Its molecular formula is C153H225N43O49S, with the following molecular structure: |
| Useful Link 1 | Link |
| Useful Link 2 | Link |
| Remarks | NA |