Insulin Regular Drugbank ID : DB00030 Protein chemical formula : C257H383N65O77S6 Protein average weight : 5808 Daltons

Description : Indication : Pharmacodynamics : Insulin regular is a 51 residue peptide hormone, composed of two amino acid chains covalently linked by disulfide bonds. The structure is identical to native human insulin. Recombinant insulin is synthesized by recombinant DNA techncology. Inserting the human insulin gene into the Escherichia coli bacteria or Saccharomyces cerevisiae produces insulin for human use. Indication : Indicated as an adjunct to diet and exercise to improve glycemic control in adults and children with type 1 and type 2 diabetes mellitus. Pharmacodynamics : Insulin regular is a short-acting insulin. When subcutaneously administered, the onset of action (as evidenced by a decrease in glucose level) occurs 30 minutes post-dose. Maximal effect occurs between 1.5 and 3.5 hours post-dose. The glucose-lowering effect occurs 8 hours post-dose. Compared to other rapid-acting insulin analogs, insulin regular has a slower onset of action and longer duration of action.

Mechanism of action : The primary activity of insulin is the regulation of glucose metabolism. Insulin promotes glucose and amino acid uptake into muscle and adipose tissues, and other tissues except brain and liver. It also has an anabolic role in stimulating glycogen, fatty acid, and protein synthesis. Insulin inhibits gluconeogenesis in the liver. Insulin 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 is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead 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) which play a critical role in metabolism and catabolism. Metabolism : Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process. Absorption : Insulin is generally well absorbed.

Volume of distribution : 0.15 L/kg Toxicity : Hypoglycemia is one of the most frequent adverse events experienced by insulin users. Drug Interaction: Liraglutide : Coadministration may increase the risk of hypoglycemia. A lower dose of the antidiabetic agent may be needed.

Categories : Sequence : Targets : Insulin receptor,Insulin-like growth factor 1 receptor,Retinoblastoma-associated protein,Cathepsin D,Insulin-degrading enzyme,Neuroendocrine convertase 2,Carboxypeptidase E,Neuroendocrine convertase 1,Protein NOV homolog,Low-density lipoprotein receptor-related protein 2,Insulin-like growth factor-binding protein 7,Synaptotagmin-like protein 4 Affected organisms : Humans and other mammals . Categories : Antidiabetic Agents Sequence : A chainGIVEQCCTSICSLYQLENYCN B chainFVNQHLCGSHLVEALYLVCGERGFFYTPKT

Brands : Humulin R Company : Eli Lilly and Company Description : Humulin® R U-100 is a polypeptide hormone structurally identical to human insulin synthesized through rDNA technology in a special non-disease-producing laboratory strain of Escherichia coli bacteria. Humulin R (insulin human recombinant) U-100 has the empirical formula C257H383N65O77S6 and a molecular weight of 5808. Used for/Prescribed for : Treating diabetes mellitus. Formulation : It contains human insulin (rDNA origin) 100 units/mL, glycerin 16 mg/mL and metacresol 2.5 mg/mL, endogenous zinc (approximately 0.015 mg/100 units) and water for injection. The pH is 7.0 to 7.8. Sodiumhydroxide and/or hydrochloric acid may be added during manufacture to adjust the pH. Form : sterile, clear, aqueous, and colorless solution Route of administration : subcutaneous injection in the abdominal wall, the thigh, the gluteal region or in the upper arm AND Also Intravenous administration of Humulin R (insulin (human recombinant)) U-100 is possible under medical supervision.

Dosage : Humulin R (insulin (human recombinant)) U-100, when used subcutaneously, is usually given three or more times daily before meals. The average range of total daily insulin requirement for maintenance therapy in insulin-treated patients without severe insulin resistance lies between 0.5 and 1 unit/kg/day. However, in prepubertal children it usually varies from 0.7 to 1 unit/kg/day, but can be much lower during the period of partial remission. Initial dosages for patients with diabetes are often lower, e.g., 0.2 to 0.4 units/kg/day. Contraindication : contraindicated during episodes of hypoglycemia and in patients hypersensitive to humulin R. Side effects : Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; wheezing; muscle pain); changes in vision; chills; confusion; dizziness; drowsiness; fainting; fast or irregular heartbeat; headache; loss of consciousness; mood changes; muscle weakness or cramping; painful burning, numbness, or tingling; seizures; shortness of breath; slurred speech; swelling of the hands, ankles, or feet; tremor; trouble breathing; trouble concentrating; unusual hunger; unusual sweating; unusual or persistent weight gain; weakness Drug interaction : A total of 799 drugs (5322 brand and generic names) are known to interact with Humulin R (insulin regular). 1 major drug interactions (3 brand and generic names), 709 moderate drug interactions (4725 brand and generic names), 89 minor drug interactions (594 brand and generic names)

General references : # Herrmann BL, Kasser C, Keuthage W, Huptas M, Dette H, Klute A: Comparison of insulin aspart vs. regular human insulin with or without insulin detemir concerning adipozytokines and metabolic effects in patients with type 2 diabetes mellitus. Exp Clin Endocrinol Diabetes. 2013 Apr;121(4):210-3. doi: 10.1055/s-0033-1334905. Epub 2013 Mar 19. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23512415.

References : http://www. rxlist. com/humulin-r-drug. htm http://www