med chem

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  1. bile acid sequestrant used adjuntly to diet and exercise to improve glycemic control in adults with type 2 DM
    colesevelam - welchol
  2. recombinant biotechnology product
    treatment of lower extremity diabetic neuropathic ulcers
    becaplermin - regranex
  3. adjunct to diet and exercise to improve glycemic control in type 2 diabetes only
    dopamine receptor agonist
    taken orally (low doses) within 2 hours of awakening with food
    bromocriptine mesylate - cycloset
  4. DPP-IV inhibitor
    new in 2011
    taken with or without food
    not used in patients with type 1 diabetes or treatment of diabetic ketoacidosis
    90% excreted unchanged
    linagliptin - tradjenta
  5. found in beta-islet cells in pancreas
    acts within a cell in contrast to a receptor
    released along with insulin
    binds directly to a series of GTPase enzymes
  6. sulfonylureas - first gen.
    serum half life - 7 hours
    active metabolites
    tolazamide - tolinase
  7. sulfonylureas - first gen.
    half life - 4.5-6.5 hours
    NO active metablolites
    tolbutamide - orinase
  8. sulfonylureas - first gen.
    half life - 36 hours
    active metabolites
    chlorproppamide - diabinese
  9. sulfonylureas - first gen.
    half life - 6-8 hours
    acitve metabolites
    acetohexamide - dymelor
  10. sulfonylureas - second gen
    half life - 2-4 hours
    NO active metabolites
    glipizide - glucotrol
  11. sulfonylureas - second gen.
    nonmicronized half life - 10 hours
    weakly active metabolites
    micronized half life - 4 hours
    weakly active metabolites
    glyburide (glibenclamide) - DiaBeta, micronase, glynase prestab
  12. sulfonylureas - third gen.
    half life 9 hours
    active metabolites
    causes tranlocation of GLUT-4 to cell surface
    may bind to a different protein than beta-islet cell
    glimepiride - amaryl
  13. thiazolidinediones
    type 2 diabetes alone or with sulfonylurea or insulin
    only work in the presence of insulin
    increase the activity of PPAR -gamma
    metabolized by CYP2C8 and some CYP2C9
    rosiglitazone maleate - avandia
  14. thiazolidinedionestype 2 diabetes alone or with sulfonylurea or insulinonly work in the presence of insulinincrease the activity of PPAR -gamma
    metabolized by CYP3A4
    decreases the efficacy of OC's
    monitor ALT for hepatotoxicity
    pioglitazone HCL - actos
  15. non-sulfonylurea analog of glyburide
    binds, and blocks an ATP-ase sensitve K+ channel.
    metabolized by CYP3A4
    take preprandially
    repaglinide - prandlin
  16. decrease hepatic gluconeogenesis and intestinal glucose absorption
    increase peripheral tisssue insulin sensitivity
    does not cause insulin release in the pancrease
    half life - 1.3-4.5 hours
    metformin HCL - glucophage
  17. unrelated to sulfonylureas
    stimulates insulin release in the pancreas
    98% albumin binding
    CYP2C9 metabolism (70%)
    CYP3A4 metabloism (30%)
    nateglinide - starlix
  18. alpha-glucosidase inhibitor
    decrease carbohydrate absorption
    amino group prevents protonation of glycosidic bonds in the saccharides
    tell patients take drug with the first bite of meals tid
    minimal systemic absorption
    acarbose - precose
  19. alpha-glucosidase inhibitordecrease carbohydrate absorptionamino group prevents protonation of glycosidic bonds in the saccharidestell patients take drug with the first bite of meals tid
    rapid and complete systemic absorption
    miglitol - glyset
  20. combination products for type 2 diabetes (6)
    • glipizide and metformin HCL - metaglip
    • rosiglitazone maleate and metformin - avandamet
    • glyburide and metformin HCL - glucovnace
    • rosiglitazone maleate and glimepiride - avandaryl
    • repaglinide and metformin - prandimet
  21. rapid acting product recombinant site directed mutation human insulin produced in E. Coli
    lysine replaces asparagine at position 3 and glutamic acid replaces lysine at postion 29
    insulin glulisine - apidra
  22. long acting 24 hour product reconbinant site directed mutation human insulin produced in saccharoyces cerevisiae followed by chemical modification with a fatty acid
    98% bound to plasma albumin
    threonine at B30 deleted and a C14 fatty acid chain has been attached to the B29 amino acid lysine
    insulin detemir - levemir
  23. forms microprecipitates in subcutaneous tissue prolinging diration from 18-26 hours
    recombinant/chemically modified insulins
    insulin glargine - lantus
  24. rapid acting 3-5 hour duration
    take 5-10 minutes before meals
    recombinant/chemically modified insulin
    insulin aspart - novolog
  25. rapid acting 3-5 hour durationt
    take 15 minutes before meals or immediately after eating
    insulin lispro - humalog
  26. incretin memetic or glucagon-like peptide-1 receptor agonist that binds the GLP-1 receptor on beta islet cells causing insulin synthesis and excretion
    exenatide - byetta
  27. synthetic analog of human amylin
    pramlintide acetate-symlin
  28. combination product for type 2 diabetes
    two modes of action - directly targets insulin resistance and acts primarily to increase the amount of insulin produced by the pancreas
    pioglitazone HCL and glimepiride - duetact
  29. inhaled insulin for diabetes mellitus
    rapid acting insulin
    patient variability on correct use and dose left in blister packages = not marketed
  30. peptide hormones released from the gut in response to the ingestion of carbohydrates
  31. incretin memetic or glucagon like peptide-1 receptor agonist as an adjunct to diet and excercise
    inject sub Q qd any time of the day independent of meals
    black box warning - risk of thyroid C-cell tumors
    victoza - liraglutide
  32. monotherapy for type 2 diabetes, NOT for 1
    combination therapy with metformin and thiazolidines
    with or without food
    substrate of p-glycoprotein
    sitagliptin - januvia
  33. DPP-4 inhibitor
    metabolism - CYP3A4/5 to active metabolite
    AR - decreased lymphocyte count, hypoglycemia, uticaria, acute pancreatitis, and headaches
    saxagliptin - onglyza
  34. combo products with sitagliptin (2)
    • with metformin - janumet
    • with simvastatin - juvisyns
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med chem
med chem quiz 8
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