Glucagon

Identification

Summary

Glucagon is a form of recombinant glucagon used to treat hypoglycemia in diabetes mellitus and as a part of gastrointestinal imaging procedures.

Brand Names

Baqsimi, Glucagen, Gvoke

Generic Name

Glucagon

DrugBank Accession Number

DB00040

Background

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

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Associated Conditions

Severe Hypoglycemia

Contraindications & Blackbox Warnings

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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 G_sα and G_q.¹ This activation activates adenylate cyclase, which increases intracellular cyclic AMP and activates protein kinase A.¹ Activating G_q 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	agonist	Humans
UGlucagon-like peptide 2 receptor	agonist	Humans
UGlucagon-like peptide 1 receptor	agonist	Humans

Absorption

A 1mg intravenous dose of glucagon reaches a C_max of 7.9ng/mL with a T_max of 20 minutes.⁶ An intramuscular dose reaches a C_max of 6.9ng/mL with a T_max of 13 minutes.⁶ A 3mg dose of glucagon nasal powder reaches a C_max of 6130pg/mL with a T_max 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

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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

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
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Acebutolol	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.
Belladonna	Belladonna may increase the gastrointestinal motility reducing activities of Glucagon.

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Food Interactions

No interactions found.

Products

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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
Baqsimi		3 mg		Eli Lilly Nederland B.V.	2020-12-16	Not applicable
Baqsimi	Powder	3 mg / container	Nasal	Eli Lilly & Co. Ltd.	2019-11-20	Not applicable
Baqsimi		3 mg		Eli Lilly Nederland B.V.	2020-12-16	Not applicable
Baqsimi	Powder	3 mg/1	Nasal	Eli Lilly and Company	2019-07-24	Not applicable
Glucag0n	Kit	1 mg/1mL	Intramuscular; Intravenous; Subcutaneous	HF Acquisition Co LLC, DBA HealthFirst	2018-10-20	Not applicable
GlucaGen	Injection, powder, for solution	1 mg/1mL	Intramuscular; Intravenous; Subcutaneous	Boehringer Ingelheim Pharmaceuticals, Inc.	2005-06-22	Not applicable
GlucaGen	Kit; Powder, for solution	1 mg / vial	Intramuscular	Novo Nordisk	2010-01-04	Not applicable
GlucaGen	Kit	1 mg/1mL	Intramuscular; Intravenous; Subcutaneous	Bedford Pharmaceuticals	2005-06-22	2016-11-30
GlucaGen	Kit	1 mg/1mL	Intramuscular; Intravenous; Subcutaneous	Boehringer Ingelheim Pharmaceuticals, Inc.	2005-06-22	Not applicable
GlucaGen HypoKit	Kit; Powder, for solution	1 mg / vial	Intramuscular	Novo Nordisk	2009-12-23	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Glucagon		1 mg/1mL	Intramuscular; Intravenous; Subcutaneous	Amphastar Pharmaceuticals, Inc.	2021-02-10	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Glucagon	Glucagon hydrochloride (1 mg/1mL) + Water (1 mL/1mL)	Kit	Intramuscular; Intravenous	Fresenius Kabi USA, LLC	2015-12-01	Not applicable
Glucagon	Glucagon hydrochloride (1 mg/1mL) + Water (1 mL/1mL)	Kit	Intramuscular; Intravenous	Fresenius Kabi USA, LLC	2019-09-09	Not applicable
Glucagon	Glucagon hydrochloride (1 mg/1mL) + Water (1 mL/1mL)	Kit	Intramuscular; Intravenous	Fresenius Kabi USA, LLC	2015-05-08	Not applicable
Glucagon	Glucagon hydrochloride (1 mg/1mL) + Water (1 mL/1mL)	Kit	Intramuscular; Intravenous	HF Acquisition Co LLC, DBA HealthFirst	2020-03-10	Not applicable

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. [Article]
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. [Article]
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. [Article]
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
RxNav: 261716
ChEMBL: CHEMBL266481
Therapeutic Targets Database: DAP001037
PharmGKB: PA164779052
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Glucagon

FDA label

Download (43.7 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
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	Completed	Treatment	Type 1 Diabetes Mellitus	1
4	Not Yet Recruiting	Basic Science	Obesity (Disorder) / Type 2 Diabetes Mellitus	1
4	Recruiting	Treatment	Hypoglycemic reaction / Type 1 Diabetes Mellitus	1
4	Recruiting	Treatment	Type 1 Diabetes Mellitus	1
4	Unknown Status	Basic Science	Type 1 Diabetes Mellitus	1
4	Unknown Status	Diagnostic	Liver Diseases	1
4	Withdrawn	Treatment	Women With Fertility Disorder	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 / container
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	1 mg / vial
Injection, powder, for solution	Parenteral
Injection, powder, for solution	Intramuscular; Subcutaneous
Injection, powder, for solution	Intramuscular; Intravenous; Subcutaneous	1 mg/ml
Injection, solution	Subcutaneous	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	1 mg / vial
Powder, for solution	Intramuscular; Intravenous; Subcutaneous	1 mg / mL
Injection, solution	Subcutaneous	0.5 mg/0.1mL
Injection, solution	Subcutaneous	1 mg/0.2mL
Injection, solution	Subcutaneous	0.5 mg
Solution		1 mg/1ml

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)
US10213487	No	2019-02-26	2036-02-16
US6938798	No	2005-09-06	2022-01-03
US9649364	No	2017-05-16	2036-04-22
US10765602	No	2020-09-08	2039-09-23
US10894133	No	2021-01-19	2038-01-03

Properties

State

Liquid

Experimental Properties

Property	Value	Source
isoelectric point	7.1	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005042/

Targets

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insights and accelerate drug research.

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Details1. Glucagon receptor

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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
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. [Article]
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. [Article]
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. [Article]

Details2. Glucagon-like peptide 2 receptor

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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]

Details3. Glucagon-like peptide 1 receptor

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. [Article]
Baggio LL, Drucker DJ: Biology of incretins: GLP-1 and GIP. Gastroenterology. 2007 May;132(6):2131-57. [Article]
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. [Article]
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. [Article]

Drug created at June 13, 2005 13:24 / Updated at December 08, 2021 01:57

Glucagon

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

References

References