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Identification
NameGlucagon recombinant
Accession NumberDB00040  (BTD00057, BIOD00057)
TypeBiotech
GroupsApproved
Description

29 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
GlucagenkitBedford Laboratories2005-06-22Not applicableUs
Glucagenkit; powder for solution1 mgintramuscularNovo Nordisk Canada Inc2010-01-04Not applicableCanada
GlucagenkitBoehringer Ingelheim Pharmaceuticals, Inc.2005-06-22Not applicableUs
Glucageninjection, powder, for solution1 mg/mLintramuscular; intravenous; subcutaneousBoehringer Ingelheim Pharmaceuticals, Inc.2005-06-22Not applicableUs
Glucagen Hypokitkit; powder for solution1 mgintramuscularNovo Nordisk Canada Inc2009-12-23Not applicableCanada
Glucagen HypokitkitNovo Nordisk2005-06-22Not applicableUs
GlucagonkitEli Lilly and Company1999-03-01Not applicableUs
Glucagoninjection, powder, lyophilized, for solution1 mg/mLintramuscular; intravenousFresenius Kabi USA, LLC2015-05-08Not applicableUs
GlucagonkitPhysicians Total Care, Inc.2004-05-24Not applicableUs
Glucagonkit; powder for solution1 mgintramuscular; intravenous; subcutaneousEli Lilly Canada Inc2002-05-27Not applicableCanada
GlucagonkitFresenius Kabi USA, LLC2015-12-01Not applicableUs
GlucagonkitTYA Pharmaceuticals1999-03-01Not 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
Related Articles
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.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Glucagon recombinant.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Glucagon recombinant.
AtropineThe risk or severity of adverse effects can be increased when Atropine is combined with Glucagon recombinant.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Glucagon recombinant.
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Glucagon recombinant.
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Glucagon recombinant.
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Glucagon recombinant.
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Glucagon recombinant.
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Glucagon recombinant.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Glucagon recombinant.
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Glucagon recombinant.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Glucagon recombinant.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Glucagon recombinant.
CyclizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Glucagon recombinant.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Glucagon recombinant.
CyclopentolateThe risk or severity of adverse effects can be increased when Cyclopentolate is combined with Glucagon recombinant.
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Glucagon recombinant.
DarifenacinThe risk or severity of adverse effects can be increased when Darifenacin is combined with Glucagon recombinant.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Glucagon recombinant.
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Glucagon recombinant.
Dexchlorpheniramine maleateThe risk or severity of adverse effects can be increased when Dexchlorpheniramine maleate is combined with Glucagon recombinant.
DicyclomineThe risk or severity of adverse effects can be increased when Dicyclomine is combined with Glucagon recombinant.
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Glucagon recombinant.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Glucagon recombinant.
DisopyramideThe risk or severity of adverse effects can be increased when Disopyramide is combined with Glucagon recombinant.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Glucagon recombinant.
DoxylamineThe risk or severity of adverse effects can be increased when Doxylamine is combined with Glucagon recombinant.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with Glucagon recombinant.
FesoterodineThe risk or severity of adverse effects can be increased when Fesoterodine is combined with Glucagon recombinant.
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Glucagon recombinant.
FlavoxateThe risk or severity of adverse effects can be increased when Flavoxate is combined with Glucagon recombinant.
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Glucagon recombinant.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Glucagon recombinant.
GlycopyrroniumThe risk or severity of adverse effects can be increased when Glycopyrrolate is combined with Glucagon recombinant.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Glucagon recombinant.
HomatropineThe risk or severity of adverse effects can be increased when Homatropine is combined with Glucagon recombinant.
HydroxyzineThe risk or severity of adverse effects can be increased when Hydroxyzine is combined with Glucagon recombinant.
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Glucagon recombinant.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine 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.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Glucagon recombinant.
LevocabastineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Glucagon recombinant.
LevocetirizineThe risk or severity of adverse effects can be increased when Levocetirizine is combined with Glucagon recombinant.
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Glucagon recombinant.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Glucagon recombinant.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Glucagon recombinant.
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Glucagon recombinant.
MepenzolateThe risk or severity of adverse effects can be increased when Mepenzolate is combined with Glucagon recombinant.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Glucagon recombinant.
MethscopolamineThe risk or severity of adverse effects can be increased when Methscopolamine is combined with Glucagon recombinant.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Glucagon recombinant.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Glucagon recombinant.
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Glucagon recombinant.
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine 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.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Glucagon recombinant.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Glucagon recombinant.
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Glucagon recombinant.
PizotifenThe risk or severity of adverse effects can be increased when Pizotifen is combined with Glucagon recombinant.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Glucagon recombinant.
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Glucagon recombinant.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Glucagon recombinant.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Glucagon recombinant.
PropanthelineThe risk or severity of adverse effects can be increased when Propantheline is combined with Glucagon recombinant.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Glucagon recombinant.
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Glucagon recombinant.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone 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.
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Glucagon recombinant.
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene 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.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Glucagon recombinant.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Glucagon recombinant.
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Glucagon recombinant.
TrimethobenzamideThe risk or severity of adverse effects can be increased when Trimethobenzamide is combined with Glucagon recombinant.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Glucagon recombinant.
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Glucagon recombinant.
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Glucagon recombinant.
UmeclidiniumThe risk or severity of adverse effects can be increased when Umeclidinium is combined with Glucagon recombinant.
WarfarinGlucagon recombinant may increase the anticoagulant activities of Warfarin.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Glucagon recombinant.
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 May 01, 2016 15:42