About: Insulin Glulisine     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Insulin glulisine is a biosynthetic, rapid-acting human insulin analogue produced in a non-pathogenic laboratory strain of _Escherichia coli_ (K12). This recombinant hormone differs from native human insulin in that the amino acid arginine at position B3 is replaced by lysine and the lysine at position B29 is replaced by glutamic acid. These structural modifications decrease hexamer formation, stabilize insulin glulisine monomers and increase the rate of absorption and onset of action compared to human insulin. (en)
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http://linked.open...generalReferences
  • # Arnolds S, Rave K, Hovelmann U, Fischer A, Sert-Langeron C, Heise T: Insulin Glulisine Has a Faster Onset of Action Compared with Insulin Aspart in Healthy Volunteers. Exp Clin Endocrinol Diabetes. 2010 Apr 28. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20429049 # Becker RH: Insulin glulisine complementing basal insulins: a review of structure and activity. Diabetes Technol Ther. 2007 Feb;9(1):109-21. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17316105 # Becker RH, Frick AD: Clinical pharmacokinetics and pharmacodynamics of insulin glulisine. Clin Pharmacokinet. 2008;47(1):7-20. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18076215 # Cox SL: Insulin glulisine. Drugs Today (Barc). 2005 Jul;41(7):433-40. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16193096 # Garnock-Jones KP, Plosker GL: Insulin glulisine: a review of its use in the management of diabetes mellitus. Drugs. 2009 May 29;69(8):1035-57. doi: 10.2165/00003495-200969080-00006. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19496630 # Horvath K, Bock G, Regittnig W, Bodenlenz M, Wutte A, Plank J, Magnes C, Sinner F, Furst-Recktenwald S, Theobald K, Pieber TR: Insulin glulisine, insulin lispro and regular human insulin show comparable end-organ metabolic effects: an exploratory study. Diabetes Obes Metab. 2008 Jun;10(6):484-91. Epub 2007 Aug 30. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17764465 # Insuline glusine (Apidra): a new rapid-acting insulin. Med Lett Drugs Ther. 2006 Apr 24;48(1233):33-4. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16625142 # Robinson DM, Wellington K: Insulin glulisine. Drugs. 2006;66(6):861-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16706558 # Ulrich H, Snyder B, Garg SK: Combining insulins for optimal blood glucose control in type I and 2 diabetes: focus on insulin glulisine. Vasc Health Risk Manag. 2007;3(3):245-54. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17703632 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Elimination half life= 42 minutes (following subcutaneous injection) (en)
http://linked.open...ugbank/indication
  • For the treatment of Type 1 and 2 diabetes mellitus. Should be used in regimens including a long-acting or basal insulin analogue unless it is used in a continuous infusion pump. May be used with oral antidiabetic agents. (en)
sameAs
Title
  • Insulin Glulisine (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Insulin glulisine binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor autophosphorylates and phosphorylates numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. Activation of these proteins leads to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC), both of which play critical roles in metabolism and catabolism. In humans, insulin is stored in the form of hexamers; however, only insulin monomers are able to interact with IR. Substitution of the arginine at position B3 for lysine and replacement of the B29 lysine with glutamic acid decreases the propensity to form hexamers, stabilizes the hormone in monomeric form and results in a rapid rate of absorption and short duration of action. (en)
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http://linked.open...drugbank/toxicity
  • Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs and symptoms of hypoglycemia include difficulty concentrating, lethargy/weakness, confusion, drowsiness, vision changes, difficulty speaking, headache, and dizziness. Mild hypoglycemia is characterized by the presence of autonomic symptoms. Moderate hypoglycemia is characterized by the presence of autonomic and neuroglycopenic symptoms. Individuals may become unconscious in severe cases of hypoglycemia. (en)
http://linked.open...umeOfDistribution
  • 13 L (en)
http://linked.open.../drug/hasAHFSCode
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http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...l/drug/hasATCCode
http://linked.open...ugbank/absorption
  • Compared to regular human insulin, insulin glulisine is faster absorbed. When 0.15 units/kg was subcutaneously administered to type 1 diabetes patients, the pharmacokinetic parameters are as follows: Tmax = 60 minutes (range of 40 - 120 minutes); Cmax = 83 microUnits/mL (range of 40 - 131 microUnits/mL). Absolute bioavailability following subcutaneous administration is approximately 70%, regardless of site of injection. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 207748-29-6 (en)
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  • (en)
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