Glucagon

Identification

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Name
Glucagon
Accession Number
DB00040  (BTD00057, BIOD00057)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Hormones
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 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

Protein structure
Db00040
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
Product Ingredients
IngredientUNIICASInChI Key
Glucagon hydrochloride1H87NVF4DB19179-82-9Not applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BaqsimiPowder3 mg/1NasalEli Lilly and Company2019-07-24Not applicableUs
Glucag0nKit1 mg/1mLIntramuscular; Intravenous; SubcutaneousHF Acquisition Co LLC, DBA HealthFirst2018-10-20Not applicableUs
GlucaGenKit1 mg/1mLIntramuscular; Intravenous; SubcutaneousBedford Pharmaceuticals2005-06-222016-11-30Us
GlucaGenKit; Powder, for solution1 mgIntramuscularNovo Nordisk2010-01-04Not applicableCanada
GlucaGenInjection, powder, for solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousBoehringer Ingelheim Pharmaceuticals, Inc.2005-06-22Not applicableUs
GlucaGenKit1 mg/1mLIntramuscular; Intravenous; SubcutaneousBoehringer Ingelheim Pharmaceuticals, Inc.2005-06-22Not applicableUs
GlucaGen HypoKitKit; Powder, for solution1 mgIntramuscularNovo Nordisk2009-12-23Not applicableCanada
GlucaGen HypoKitKit1 mg/1mLIntramuscular; Intravenous; SubcutaneousNovo Nordisk2005-06-22Not applicableUs
GlucagonKit1 mg/1mLIntramuscular; Intravenous; SubcutaneousEli Lilly and Company1999-03-01Not applicableUs
GlucagonKit1 mg/1mLIntramuscular; Intravenous; SubcutaneousA-S Medication Solutions1999-03-01Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
GlucagonGlucagon hydrochloride (1 mg/1mL) + Water (1 mg/1mL)KitIntramuscular; IntravenousFresenius Kabi USA, LLC2015-12-01Not applicableUs
Categories
UNII
76LA80IG2G
CAS number
16941-32-5

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

Associated Conditions
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 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

TargetActionsOrganism
AGlucagon receptor
agonist
Humans
UGlucagon-like peptide 2 receptor
agonist
Humans
UGlucagon-like peptide 1 receptor
agonist
Humans
Additional Data Available
Adverse Effects

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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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

Clearance

A 1mg intravenous dose of glucagon has a clearance of 13.5mL/min/kg.6

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
DrugInteraction
(R)-warfarinThe therapeutic efficacy of (R)-warfarin can be increased when used in combination with Glucagon.
(S)-WarfarinThe therapeutic efficacy of (S)-Warfarin can be increased when used in combination with Glucagon.
4-hydroxycoumarinThe therapeutic efficacy of 4-hydroxycoumarin can be increased when used in combination with Glucagon.
AcebutololThe therapeutic efficacy of Acebutolol can be decreased when used in combination with Glucagon.
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be increased when used in combination with Glucagon.
AclidiniumAclidinium may increase the gastrointestinal motility reducing activities of Glucagon.
AlprenololThe therapeutic efficacy of Alprenolol can be decreased when used in combination with Glucagon.
AmitriptylineAmitriptyline may increase the gastrointestinal motility reducing activities of Glucagon.
AmoxapineAmoxapine may increase the gastrointestinal motility reducing activities of Glucagon.
AnisodamineThe therapeutic efficacy of Anisodamine can be decreased when used in combination with Glucagon.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

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  • Action
    Action

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Food Interactions
Not Available

References

General References
  1. Jiang G, Zhang BB: Glucagon and regulation of glucose metabolism. Am J Physiol Endocrinol Metab. 2003 Apr;284(4):E671-8. [PubMed:12626323]
  2. 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]
  3. 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]
  4. FDA Approved Drug Products: Glucagon Hydrochloride Injection (Discontinued) [Link]
  5. FDA Approved Drug Products: Glucagon Intravenous or Intramuscular Injection [Link]
  6. FDA Approved Drug Products: Glucagon for Injection [Link]
  7. FDA Approved Drug Products: Glucagon Subcutaneous, Intramuscular, or Intravenous Injection [Link]
  8. FDA Approved Drug Products: Glucagon Nasal Powder [Link]
  9. Medsafe New Zealand: Glucagon Data Sheet [Link]
External Links
UniProt
Q8MJ25
Genbank
AF529185
KEGG Drug
D00116
KEGG Compound
C01501
PubChem Substance
46504732
ChEMBL
CHEMBL266481
Therapeutic Targets Database
DAP001037
PharmGKB
PA164779052
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Glucagon_recombinant
ATC Codes
H04AA01 — Glucagon
AHFS Codes
  • 68:22.12 — Glycogenolytic Agents
FDA label
Download (43.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingBasic ScienceHealthy Participants1
1Active Not RecruitingBasic ScienceBMI >30 kg/m22
1CompletedBasic ScienceBMI >30 kg/m2 / Hyperglucagonaemia1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceHypoglycemia / Type 1 Insulin-Dependent Diabetes Mellitus1
1CompletedBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentDiabetes Mellitus (DM)1
1CompletedTreatmentDiabetes Mellitus (DM) / Type 1 Insulin-Dependent Diabetes Mellitus / Type 2 Diabetes Mellitus1
1CompletedTreatmentHealthy Volunteers / Type 2 Diabetes Mellitus1
1CompletedTreatmentHypoglycemia4
1CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus2
1CompletedTreatmentType 2 Diabetes Mellitus3
1RecruitingTreatmentType1 Diabetes Mellitus1
1WithdrawnBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
1, 2CompletedPreventionPost-bariatric Hypoglycemia1
2CompletedPreventionCongenital Hyperinsulinism1
2CompletedPreventionType 1 Insulin-Dependent Diabetes Mellitus1
2CompletedTreatmentComplications of Bariatric Procedures / Hypoglycemia1
2CompletedTreatmentHypoglycemia6
2CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus7
2RecruitingPreventionHypoglycemia1
2RecruitingTreatmentHyperinsulinemic Hypoglycemia1
2RecruitingTreatmentHypoglycemia Unawareness / Type 1 Insulin-Dependent Diabetes Mellitus1
2WithdrawnTreatmentType 1 Insulin-Dependent Diabetes Mellitus3
2, 3CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
2, 3RecruitingBasic ScienceBMI >30 kg/m21
3CompletedNot AvailableDiabetes Mellitus (DM) / Drug-Specific Antibodies / Hypoglycemia1
3CompletedTreatmentDiabetes Mellitus (DM)1
3CompletedTreatmentDiabetes Mellitus (DM) / Drug-Specific Antibodies / Hypoglycemia1
3CompletedTreatmentDiabetes Mellitus (DM) / Hypoglycemia1
3CompletedTreatmentHypoglycemia1
3CompletedTreatmentHypoglycemia / Type 1 Insulin-Dependent Diabetes Mellitus3
3CompletedTreatmentInsulin Hypoglycemia / Severe Hypoglycemia / Type 1 Insulin-Dependent Diabetes Mellitus2
3CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus2
3CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus / Type 2 Diabetes Mellitus1
3Unknown StatusBasic ScienceBMI >30 kg/m2 / Healthy Volunteers / Type 1 Insulin-Dependent Diabetes Mellitus1
4Active Not RecruitingBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
4CompletedDiagnosticDiabetes Mellitus (DM)1
4CompletedDiagnosticMalignant Neoplasm of Colon1
4RecruitingBasic ScienceDrug Overdose / Overdose of Beta-adrenergic Blocking Drug1
4RecruitingTreatmentHypoglycemia / Type 1 Insulin-Dependent Diabetes Mellitus1
4Unknown StatusDiagnosticLiver Diseases1
4WithdrawnTreatmentWomen With Fertility Disorder1
Not AvailableActive Not RecruitingBasic ScienceDiabetes Mellitus (DM) / Metabolic Syndromes1
Not AvailableActive Not RecruitingBasic ScienceMetabolic Diseases1
Not AvailableActive Not RecruitingBasic ScienceNormal Cellular Metabolism1
Not AvailableActive Not RecruitingTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableCompletedBasic ScienceDiabetes Mellitus (DM)1
Not AvailableCompletedBasic ScienceDiabetes Mellitus (DM) / Non-Alcoholic Fatty Liver Disease (NAFLD) / Total Pancreatectomy1
Not AvailableCompletedBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus2
Not AvailableCompletedSupportive CareType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableRecruitingBasic ScienceCardiovascular Disease (CVD)1
Not AvailableRecruitingTreatmentFasting Hypoglycemia / Type 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableSuspendedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableTerminatedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableUnknown StatusBasic ScienceHealthy Volunteers1
Not AvailableUnknown StatusTreatmentHyperglycemias / Infant, Low Birth Weight1

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
FormRouteStrength
PowderNasal3 mg/1
Injection, powder, for solutionIntramuscular; Intravenous; Subcutaneous1 mg/1mL
Kit; powder, for solutionIntramuscular1 mg
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous1 mg/1mL
KitIntramuscular; Intravenous1 mg/1mL
KitIntramuscular; Intravenous1 mg/1mL
KitIntramuscular; Intravenous; Subcutaneous1 mg/1mL
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.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
isoelectric point7.1https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005042/

Taxonomy

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

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
  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
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
  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
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
  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]

Drug created on June 13, 2005 07:24 / Updated on August 24, 2019 06:25