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Identification
NameGlucagon recombinant
Accession NumberDB00040  (BTD00057, BIOD00057)
TypeBiotech
GroupsApproved
Description29 residue peptide hormone. Glucagon is 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
Protein structureDb00040
Related Articles
Protein chemical formulaC165H249N49O51S1
Protein average weight3767.1 Da
Sequences
>Glucagon for Injection Sequence 
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Download FASTA Format
Synonyms
Glucagon
Glucagon (recombinant dna origin)
Glucagon, human
Glucagon, porcine
Glucagone
Glucagonum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Glucagenkit; powder for solution1 mgintramuscularNovo Nordisk Canada Inc2010-01-04Not applicableCanada
GlucagenkitBedford Laboratories2005-06-22Not applicableUs
Glucageninjection, powder, for solution1 mg/mLintramuscular; intravenous; subcutaneousBoehringer Ingelheim Pharmaceuticals, Inc.2005-06-22Not applicableUs
GlucagenkitBoehringer Ingelheim Pharmaceuticals, Inc.2005-06-22Not applicableUs
Glucagen HypokitkitNovo Nordisk2005-06-22Not applicableUs
Glucagen Hypokitkit; powder for solution1 mgintramuscularNovo Nordisk Canada Inc2009-12-23Not applicableCanada
GlucagonkitTYA Pharmaceuticals1999-03-01Not applicableUs
GlucagonkitEli Lilly and Company1999-03-01Not applicableUs
GlucagonkitPhysicians Total Care, Inc.2004-05-24Not applicableUs
GlucagonkitFresenius Kabi USA, LLC2015-12-01Not applicableUs
Glucagonkit; powder for solution1 mgintramuscular; intravenous; subcutaneousEli Lilly Canada Inc2002-05-27Not applicableCanada
Glucagoninjection, powder, lyophilized, for solution1 mg/mLintramuscular; intravenousFresenius Kabi USA, LLC2015-05-08Not applicableUs
Glucagon Ampoule 666 1mgpowder for solution1 mgintramuscular; intravenous; subcutaneousEli Lilly And Company Limited1961-12-312002-05-27Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Glucagon hydrochloride
19179-82-9
ThumbNot applicableDBSALT001413
Categories
UNII76LA80IG2G
CAS number16941-32-5
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor treatment of severe hypoglycemia, also used in gastrointestinal imaging
PharmacodynamicsUsed 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 actionGlucagon binds the glucagon receptor, a 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
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AbsorptionNot Available
Volume of distribution
  • 0.25 L/kg
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
Clearance
  • 13.5  mL/min/kg [Adults with IV 1 mg]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Eli lilly and co
  • Novo nordisk pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionintramuscular; intravenous; subcutaneous1 mg/mL
Kit; powder for solutionintramuscular1 mg
Injection, powder, lyophilized, for solutionintramuscular; intravenous1 mg/mL
Kit
Kit; powder for solutionintramuscular; intravenous; subcutaneous1 mg
Powder for solutionintramuscular; intravenous; subcutaneous1 mg
Prices
Unit descriptionCostUnit
Glucagon 1 mg kit128.34USD kit
Glucagon Emergency 1 mg Kit Box124.05USD box
GlucaGen HypoKit 1 mg Solution Box123.72USD box
Glucagen 1 mg hypokit120.36USD kit
Glucagon 1 mg emergency kit119.28USD kit
Glucagon 1 mg/vial94.98USD vial
Glucagen 1 mg vial84.0USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
hydrophobicity-1.197Not Available
isoelectric point9.52Not Available
References
Synthesis ReferenceNot Available
General References
  1. White CM: A review of potential cardiovascular uses of intravenous glucagon administration. J Clin Pharmacol. 1999 May;39(5):442-7. [PubMed:10234590 ]
External Links
ATC CodesH04AA01
AHFS Codes
  • 68:22.12
PDB Entries
FDA labelDownload (43.7 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcenocoumarolGlucagon recombinant may increase the anticoagulant activities of Acenocoumarol.
AclidiniumThe risk or severity of adverse effects can be increased when Aclidinium is combined with Glucagon recombinant.
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Anisotropine Methylbromide is combined with Glucagon recombinant.
Atracurium besylateThe risk or severity of adverse effects can be increased when Atracurium besylate is combined with Glucagon recombinant.
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Glucagon recombinant.
BenactyzineThe risk or severity of adverse effects can be increased when Benactyzine is combined with Glucagon recombinant.
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Glucagon recombinant.
BiperidenThe risk or severity of adverse effects can be increased when Biperiden is combined with Glucagon recombinant.
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Chlorphenoxamine is combined with Glucagon recombinant.
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Glucagon recombinant.
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Glucagon recombinant.
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Glucagon recombinant.
DexetimideThe risk or severity of adverse effects can be increased when Dexetimide is combined with Glucagon recombinant.
DicoumarolGlucagon recombinant may increase the anticoagulant activities of Dicoumarol.
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Glucagon recombinant.
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Glucagon recombinant.
Ethyl biscoumacetateGlucagon recombinant may increase the anticoagulant activities of Ethyl biscoumacetate.
FesoterodineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Glucagon recombinant.
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Glucagon recombinant.
GlycopyrroniumThe risk or severity of adverse effects can be increased when Glycopyrronium is combined with Glucagon recombinant.
HexamethoniumThe risk or severity of adverse effects can be increased when Hexamethonium is combined with Glucagon recombinant.
HomatropineThe risk or severity of adverse effects can be increased when Homatropine is combined with Glucagon recombinant.
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Glucagon recombinant.
IndomethacinThe therapeutic efficacy of Glucagon recombinant can be decreased when used in combination with Indomethacin.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Glucagon recombinant.
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Glucagon recombinant.
MethanthelineThe risk or severity of adverse effects can be increased when Methantheline is combined with Glucagon recombinant.
MetixeneThe risk or severity of adverse effects can be increased when Metixene is combined with Glucagon recombinant.
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when N-butylscopolammonium bromide is combined with Glucagon recombinant.
NVA237The risk or severity of adverse effects can be increased when NVA237 is combined with Glucagon recombinant.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Glucagon recombinant.
OxybutyninThe risk or severity of adverse effects can be increased when Oxybutynin is combined with Glucagon recombinant.
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Glucagon recombinant.
PancuroniumThe risk or severity of adverse effects can be increased when Pancuronium is combined with Glucagon recombinant.
PentoliniumThe risk or severity of adverse effects can be increased when Pentolinium is combined with Glucagon recombinant.
PhenindioneGlucagon recombinant may increase the anticoagulant activities of Phenindione.
PhenprocoumonGlucagon recombinant may increase the anticoagulant activities of Phenprocoumon.
PipecuroniumThe risk or severity of adverse effects can be increased when Pipecuronium is combined with Glucagon recombinant.
PirenzepineThe risk or severity of adverse effects can be increased when Pirenzepine is combined with Glucagon recombinant.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Glucagon recombinant.
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Glucagon recombinant.
QuinidineThe risk or severity of adverse effects can be increased when Quinidine is combined with Glucagon recombinant.
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Glucagon recombinant.
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Scopolamine butylbromide is combined with Glucagon recombinant.
SolifenacinThe risk or severity of adverse effects can be increased when Solifenacin is combined with Glucagon recombinant.
TiotropiumThe risk or severity of adverse effects can be increased when Tiotropium is combined with Glucagon recombinant.
TolterodineThe risk or severity of adverse effects can be increased when Tolterodine is combined with Glucagon recombinant.
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Glucagon recombinant.
TrimethaphanThe risk or severity of adverse effects can be increased when Trimethaphan is combined with Glucagon recombinant.
TropicamideThe risk or severity of adverse effects can be increased when Tropicamide is combined with Glucagon recombinant.
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Glucagon recombinant.
TubocurarineThe risk or severity of adverse effects can be increased when Tubocurarine is combined with Glucagon recombinant.
UmeclidiniumThe risk or severity of adverse effects can be increased when Umeclidinium is combined with Glucagon recombinant.
VecuroniumThe risk or severity of adverse effects can be increased when Vecuronium is combined with Glucagon recombinant.
WarfarinGlucagon recombinant may increase the anticoagulant activities of Warfarin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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 glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding...
Gene Name:
GCGR
Uniprot ID:
P47871
Molecular Weight:
54008.44 Da
References
  1. 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 ]
  2. 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 ]
  3. 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 ]
  4. 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 ]
  5. 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 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. 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 ]
  8. 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 ]
  9. 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
Human
Pharmacological action
unknown
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
Molecular Weight:
63000.84 Da
References
  1. 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 ]
  2. 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 ]
  3. 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 ]
  4. 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 ]
  5. 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 ]
  6. 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
Human
Pharmacological action
unknown
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
Molecular Weight:
53025.22 Da
References
  1. 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 ]
  2. Baggio LL, Drucker DJ: Biology of incretins: GLP-1 and GIP. Gastroenterology. 2007 May;132(6):2131-57. [PubMed:17498508 ]
  3. 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 ]
  4. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23