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Glucagon
Identification
- Name
- Glucagon
- Accession Number
- DB00040
- 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.5,6,7,8,10 Glucagon raises blood sugar through activation of hepatic glucagon receptors, stimulating glycogenolysis and the release of glucose.7,8
Glucagon was granted FDA approval on 14 November 1960.4
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Structure
- Protein Chemical Formula
- C165H249N49O51S1
- Protein Average Weight
- 3767.1 Da
- Sequences
>Glucagon for Injection Sequence HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Download FASTA Format- Synonyms
- Glucagon
- Glucagon (recombinant dna origin)
- Glucagon recombinant
- Glucagon, human
- Glucagon, porcine
- Glucagone
- Glucagonum
Pharmacology
- Indication
Glucagon is indicated as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and to treat severe hypoglycemia.5,6,7,8,10
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Glucagon is indicated as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and severe hypoglycemia.1,5,6,7,8,10 Glucagon raises blood sugar through activation of hepatic glucagon receptors, stimulating glycogenolysis and the release of glucose.7,8 Glucagon has a short duration of action.5,6,7,8 Glucagon may cause hyperglycemia in diabetic patients.5,6,7,8
- Mechanism of action
Glucagon binds to the glucagon receptor activating Gsα and Gq.1 This activation activates adenylate cyclase, which increases intracellular cyclic AMP and activates protein kinase A.1 Activating Gq activates phospholipase C, increases production of inositol 1,4,5-triphosphate, and releases intracellular calcium.1 Protein kinase A phosphorylates glycogen phosphorylase kinase, which phosphorylates glycogen phosphorylase, which phosphorylates glycogen, causing its breakdown.1
Glucagon also relaxes smooth muscle of the stomach, duodenum, small bowel, and colon.5,8
Target Actions Organism AGlucagon receptor agonistHumans UGlucagon-like peptide 2 receptor agonistHumans UGlucagon-like peptide 1 receptor agonistHumans - Absorption
A 1mg intravenous dose of glucagon reaches a Cmax of 7.9ng/mL with a Tmax of 20 minutes.6 An intramuscular dose reaches a Cmax of 6.9ng/mL with a Tmax of 13 minutes.6 A 3mg dose of glucagon nasal powder reaches a Cmax of 6130pg/mL with a Tmax of 15 minutes.8
- Volume of distribution
The volume of distribution of glucagon is 0.25L/kg.6 The apparent volume of distribution is 885L.8
- Protein binding
Glucagon has not been described in the literature as bound to a protein in serum.2,3,5,6,7,8,9
- Metabolism
Glucagon is a protein and so it is metabolized into smaller polypeptides and amino acids in the liver, kidney, and plasma.5,8
- Route of elimination
Elimination of glucagon is not fully characterized in literature, however the kidney and liver appear to contribute significantly in animal models.2 The liver and kidney are responsible for approximately 30% of glucagon elimination each.9
- Half-life
The half life of glucagon is 26 minutes for an intramuscular dose.5 The half life of glucagon nasal powder is approximately 35 minutes.8 The half life of glucagon by a subcutaneous auto-injector or pre-filled syringe is 32 minutes.10
- Clearance
A 1mg intravenous dose of glucagon has a clearance of 13.5mL/min/kg.6
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- 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.5,6,7,8 Phentolamine may be given to control blood pressure.5,6,7,8 Treatment of glucagon overdose is largely symptomatic for nausea, vomiting, and hypokalemia.6
The LD50 for intravenous glucagon in mice is 300mg/kg and in rats is 38.6mg/kg.6
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAcebutolol The therapeutic efficacy of Acebutolol can be decreased when used in combination with Glucagon. Acenocoumarol The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Glucagon. Aclidinium Aclidinium may increase the gastrointestinal motility reducing activities of Glucagon. Amitriptyline Amitriptyline may increase the gastrointestinal motility reducing activities of Glucagon. Amoxapine Amoxapine may increase the gastrointestinal motility reducing activities of Glucagon. Anisotropine methylbromide Anisotropine methylbromide may increase the gastrointestinal motility reducing activities of Glucagon. Aripiprazole Aripiprazole may increase the gastrointestinal motility reducing activities of Glucagon. Atenolol The therapeutic efficacy of Atenolol can be decreased when used in combination with Glucagon. Atropine Atropine may increase the gastrointestinal motility reducing activities of Glucagon. Benzatropine Benzatropine may increase the gastrointestinal motility reducing activities of Glucagon. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- No interactions found.
Products
- Product Ingredients
Ingredient UNII CAS InChI Key Glucagon hydrochloride 1H87NVF4DB 19179-82-9 Not applicable - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBaqsimi Powder 3 mg Nasal Eli Lilly & Co. Ltd. 2019-11-20 Not applicable Canada 
Baqsimi Powder 3 mg/1 Nasal Eli Lilly and Company 2019-07-24 Not applicable US 
Glucag0n Kit 1 mg/1mL Intramuscular; Intravenous; Subcutaneous HF Acquisition Co LLC, DBA HealthFirst 2018-10-20 Not applicable US GlucaGen Injection, powder, for solution 1 mg/1mL Intramuscular; Intravenous; Subcutaneous Boehringer Ingelheim Pharmaceuticals, Inc. 2005-06-22 Not applicable US GlucaGen Kit 1 mg/1mL Intramuscular; Intravenous; Subcutaneous Boehringer Ingelheim Pharmaceuticals, Inc. 2005-06-22 Not applicable US GlucaGen Kit 1 mg/1mL Intramuscular; Intravenous; Subcutaneous Bedford Pharmaceuticals 2005-06-22 2016-11-30 US Glucagen Kit; Powder, for solution Intramuscular Novo Nordisk 2010-01-04 Not applicable Canada GlucaGen HypoKit Kit 1 mg/1mL Intramuscular; Intravenous; Subcutaneous Novo Nordisk 2005-06-22 Not applicable US Glucagen Hypokit Kit; Powder, for solution Intramuscular Novo Nordisk 2009-12-23 Not applicable Canada Glucagon Kit 1 mg/1mL Intramuscular; Intravenous; Subcutaneous TYA Pharmaceuticals 1999-03-01 Not applicable US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Glucagon Glucagon hydrochloride (1 mg/1mL) + Water (1 mL/1mL) Kit Intramuscular; Intravenous HF Acquisition Co LLC, DBA HealthFirst 2020-03-10 Not applicable US Glucagon Glucagon hydrochloride (1 mg/1mL) + Water (1 mL/1mL) Kit Intramuscular; Intravenous Fresenius Kabi USA, LLC 2015-12-01 Not applicable US Glucagon Glucagon hydrochloride (1 mg/1mL) + Water (1 mL/1mL) Intramuscular; Intravenous Fresenius Kabi USA, LLC 2019-09-09 Not applicable US Glucagon Glucagon hydrochloride (1 mg/1mL) + Water (1 mL/1mL) Kit Intramuscular; Intravenous Fresenius Kabi USA, LLC 2015-05-08 Not applicable US
Categories
- ATC Codes
- H04AA01 — Glucagon
- Drug 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
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
Chemical Identifiers
- UNII
- 76LA80IG2G
- CAS number
- 16941-32-5
References
- General References
- Jiang G, Zhang BB: Glucagon and regulation of glucose metabolism. Am J Physiol Endocrinol Metab. 2003 Apr;284(4):E671-8. [PubMed:12626323]
- Zhou A, Pacini G, Ahren B, D'Argenio DZ: Glucagon clearance is regulated by nutritional state: evidence from experimental studies in mice. Diabetologia. 2014 Apr;57(4):801-8. doi: 10.1007/s00125-013-3148-x. Epub 2013 Dec 28. [PubMed:24370975]
- Holst JJ, Galbo H, Richter EA: Neutralization of glucagon by antiserum as a tool in glucagon physiology. Lack of depression of basal blood glucose after antiserum treatment in rats. J Clin Invest. 1978 Jul;62(1):182-90. doi: 10.1172/JCI109104. [PubMed:659632]
- FDA Approved Drug Products: Glucagon Hydrochloride Injection (Discontinued) [Link]
- FDA Approved Drug Products: Glucagon Intravenous or Intramuscular Injection [Link]
- FDA Approved Drug Products: Glucagon for Injection [Link]
- FDA Approved Drug Products: Glucagon Subcutaneous, Intramuscular, or Intravenous Injection [Link]
- FDA Approved Drug Products: Glucagon Nasal Powder [Link]
- Medsafe New Zealand: Glucagon Data Sheet [Link]
- FDA Approved Drug Products: Glucagon Subcutaneous Auto-Injector and Pre-Filled Syringe [Link]
- External Links
- UniProt
- Q8MJ25
- Genbank
- AF529185
- KEGG Drug
- D00116
- KEGG Compound
- C01501
- PubChem Substance
- 46504732
- 261716
- ChEMBL
- CHEMBL266481
- Therapeutic Targets Database
- DAP001037
- PharmGKB
- PA164779052
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Glucagon
- AHFS Codes
- 68:22.12 — Glycogenolytic Agents
- FDA label
- Download (43.7 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Basic Science Type 1 Diabetes Mellitus 1 4 Completed Basic Science Overdose of Beta-adrenergic Blocking Drug / Overdose, Drug 1 4 Completed Diagnostic Diabetes 1 4 Completed Diagnostic Malignant Neoplasm of Colon 1 4 Not Yet Recruiting Basic Science BMI >30 kg/m2 / Type2 Diabetes 1 4 Recruiting Treatment Hypoglycemia / Type 1 Diabetes Mellitus 1 4 Unknown Status Diagnostic Liver Diseases 1 4 Withdrawn Treatment Women With Fertility Disorder 1 3 Completed Other Diabetes Mellitus / Drug Specific Antibodies / Drug-Specific Antibodies / Hypoglycemia 1 3 Completed Treatment Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Eli lilly and co
- Novo nordisk pharmaceuticals inc
- Packagers
- Bedford Labs
- Eli Lilly & Co.
- Novo Nordisk Inc.
- Physicians Total Care Inc.
- Dosage Forms
Form Route Strength Powder Nasal 3 mg/1 Powder Nasal 3 MG Injection, powder, for solution Intramuscular; Intravenous; Subcutaneous 1 mg/1mL Injection, powder, for solution Parenteral 1 MG Kit; powder, for solution Intramuscular Injection Injection 1 mg Injection, powder, lyophilized, for solution Intramuscular; Intravenous; Subcutaneous 1 mg Injection, powder, lyophilized, for solution Intramuscular; Intravenous 1 mg/1mL Kit Intramuscular; Intravenous Kit Intramuscular; Intravenous; Subcutaneous 1 mg/1mL Kit; powder, for solution Intramuscular; Intravenous; Subcutaneous Powder, for solution Intramuscular; Intravenous; Subcutaneous Injection, solution Subcutaneous 0.5 mg/0.1mL Injection, solution Subcutaneous 1 mg/0.2mL - Prices
Unit description Cost Unit Glucagon 1 mg kit 128.34USD kit Glucagon Emergency 1 mg Kit Box 124.05USD box GlucaGen HypoKit 1 mg Solution Box 123.72USD box Glucagen 1 mg hypokit 120.36USD kit Glucagon 1 mg emergency kit 119.28USD kit Glucagon 1 mg/vial 94.98USD vial Glucagen 1 mg vial 84.0USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS10213487 No 2019-02-26 2036-02-16 US US6938798 No 2005-09-06 2022-01-03 US US9649364 No 2017-05-16 2036-04-22 US Additional Data Available- Filed On
Properties
- State
- Liquid
- Experimental Properties
Property Value Source isoelectric point 7.1 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005042/
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Peptide hormone binding
- Specific Function
- G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting gl...
- Gene Name
- GCGR
- Uniprot ID
- P47871
- Uniprot Name
- Glucagon receptor
- Molecular Weight
- 54008.44 Da
References
- Katayama T, Shimamoto S, Oda H, Nakahara K, Kangawa K, Murakami N: Glucagon receptor expression and glucagon stimulation of ghrelin secretion in rat stomach. Biochem Biophys Res Commun. 2007 Jun 15;357(4):865-70. Epub 2007 Apr 9. [PubMed:17462598]
- Li P, Rogers T, Smiley D, DiMarchi RD, Zhang F: Design, synthesis and crystallization of a novel glucagon analog as a therapeutic agent. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2007 Jul 1;63(Pt 7):599-601. Epub 2007 Jun 15. [PubMed:17620721]
- Li XC, Zhuo JL: Targeting glucagon receptor signalling in treating metabolic syndrome and renal injury in Type 2 diabetes: theory versus promise. Clin Sci (Lond). 2007 Aug;113(4):183-93. [PubMed:17623014]
- Fischer AJ, Stanke JJ, Ghai K, Scott M, Omar G: Development of bullwhip neurons in the embryonic chicken retina. J Comp Neurol. 2007 Aug 1;503(4):538-49. [PubMed:17534934]
- Winzell MS, Brand CL, Wierup N, Sidelmann UG, Sundler F, Nishimura E, Ahren B: Glucagon receptor antagonism improves islet function in mice with insulin resistance induced by a high-fat diet. Diabetologia. 2007 Jul;50(7):1453-62. Epub 2007 May 4. [PubMed:17479245]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Menzel S, Stoffel M, Espinosa R 3rd, Fernald AA, Le Beau MM, Bell GI: Localization of the glucagon receptor gene to human chromosome band 17q25. Genomics. 1994 Mar 15;20(2):327-8. [PubMed:8020989]
- Brubaker PL, Drucker DJ: Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels. 2002;8(3-4):179-88. [PubMed:12529935]
- Lok S, Kuijper JL, Jelinek LJ, Kramer JM, Whitmore TE, Sprecher CA, Mathewes S, Grant FJ, Biggs SH, Rosenberg GB, et al.: The human glucagon receptor encoding gene: structure, cDNA sequence and chromosomal localization. Gene. 1994 Mar 25;140(2):203-9. [PubMed:8144028]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Glucagon receptor activity
- Specific Function
- This is a receptor for glucagon-like peptide 2. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- GLP2R
- Uniprot ID
- O95838
- Uniprot Name
- Glucagon-like peptide 2 receptor
- Molecular Weight
- 63000.84 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
- Boushey RP, Yusta B, Drucker DJ: Glucagon-like peptide (GLP)-2 reduces chemotherapy-associated mortality and enhances cell survival in cells expressing a transfected GLP-2 receptor. Cancer Res. 2001 Jan 15;61(2):687-93. [PubMed:11212269]
- Munroe DG, Gupta AK, Kooshesh F, Vyas TB, Rizkalla G, Wang H, Demchyshyn L, Yang ZJ, Kamboj RK, Chen H, McCallum K, Sumner-Smith M, Drucker DJ, Crivici A: Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2. Proc Natl Acad Sci U S A. 1999 Feb 16;96(4):1569-73. [PubMed:9990065]
- Estall JL, Koehler JA, Yusta B, Drucker DJ: The glucagon-like peptide-2 receptor C terminus modulates beta-arrestin-2 association but is dispensable for ligand-induced desensitization, endocytosis, and G-protein-dependent effector activation. J Biol Chem. 2005 Jun 10;280(23):22124-34. Epub 2005 Apr 6. [PubMed:15817468]
- Brubaker PL, Drucker DJ: Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels. 2002;8(3-4):179-88. [PubMed:12529935]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Transmembrane signaling receptor activity
- Specific Function
- This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- GLP1R
- Uniprot ID
- P43220
- Uniprot Name
- Glucagon-like peptide 1 receptor
- Molecular Weight
- 53025.22 Da
References
- Korner M, Stockli M, Waser B, Reubi JC: GLP-1 receptor expression in human tumors and human normal tissues: potential for in vivo targeting. J Nucl Med. 2007 May;48(5):736-43. [PubMed:17475961]
- Baggio LL, Drucker DJ: Biology of incretins: GLP-1 and GIP. Gastroenterology. 2007 May;132(6):2131-57. [PubMed:17498508]
- Fischer AJ, Stanke JJ, Ghai K, Scott M, Omar G: Development of bullwhip neurons in the embryonic chicken retina. J Comp Neurol. 2007 Aug 1;503(4):538-49. [PubMed:17534934]
- Brubaker PL, Drucker DJ: Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels. 2002;8(3-4):179-88. [PubMed:12529935]
Drug created on June 13, 2005 07:24 / Updated on September 25, 2020 15:13
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