Quiz 8 (and Exam 4)

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leo25
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146695
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Quiz 8 (and Exam 4)
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2012-04-10 01:21:35
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MedChem
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diabetes drugs
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  1. How many disulfide linkages does insulin have?
    3
  2. How many amino acids does insulin contain?
    51
  3. Where is insulin synthesized?
    beta islet cells of the pancreas
  4. What ion regulates the two forming steps of insulin?
    calcium
  5. Stimulating what receptors will inhibit insulin release?
    alpha 2 adrenergic
  6. Stimulating what receptors will cause in a release of insulin?
    beta 2 adrenergic receptors and vagal nerves
  7. What is the primary stimulatory factor that releases insulin?
    glucose
  8. What neurotransmitter is found in beta cells in pancreas and is released along with insulin?
    serotonin
  9. What type of impairment has a more detrimental effect on insulin levels-- kidney or liver?
    kidney
  10. what is the most commonly used clinical marker utilized to screen for diabetes?
    Hemoglobin A1C
  11. This is a yellow fluorescent AGE that is formed when arginine groups in proteins react with methylglyoxal that has built up inside cells during hyperglycemia?
    Arg-pyrimidine
  12. ____ insulin differs from human by substitution of 1 different AA?
    porcine
  13. _____ insulin differs from human by substitution of 2 different AAs?
    bovine
  14. What is the normal range of glucose when fasted?
    70-130 mg/dl
  15. What drugs can cause hypoglycemia?
    • ethanol
    • beta adrenergic receptor antagonists
    • salicylates
  16. What drugs can cause hyperglycemia?
    • epinephrine
    • glucocorts
    • oral contraceptives
    • phenytoin
    • clonidine
    • calcium channel blockers
    • diuretics
  17. These drugs stimulate the release of insulin from beta cells by binding to and blocking an ATP-ase sensitive K+ channel, which causes depolarization and an increase in intracellular calcium which leads to release of insulin?
    sulfonylureas
  18. These drugs may also decrease the hepatic clearance of insulin?
    sulfonylureas
  19. Are first gen or second gen sulfonylureas 100 times more potent?
    second gen
  20. The dosage must be individualized for these oral hypoglycemic agents?
    sulfonylureas
  21. Name the four first gen sulfonylureas.
    • Tolazamide (Tolinase)
    • Chlorpropamide (Diabinese)
    • Tolbutamide (Orinase)
    • Acetohexamide (Dymelor)
  22. Which first gen sulfonylurea has no active metabolites?
    Tolbutamide
  23. Which first gen sulfonylurea has the longest serum half life of 36 hours and is therefore the longest acting?
    Chlorpropamide
  24. List first gen sulfonylureas in order of increasing half lives starting with the shortest half life.
    • Tolbutamide
    • Acetohexamide (6-8)
    • Tolazamide (7)
    • Chlorpropamide
  25. Name the two second gen sulfonylureas.
    • Glipizide
    • Glyburide
  26. Which second gen sulfonylurea has no active metabolites?
    glipizide
  27. Name the third gen sulfonylurea.
    glimepiride (Amaryl)
  28. What is the half life of glimepiride?
    9 hours
  29. What are the addtl MOAs of glimepiride?
    • appears to translocate GLUT4 to the cell surface -- insulin like activity
    • may bind to a different protein than the usual sulfonylurea receptor on the beta cell
  30. What is the indication for sulfonylureas?
    control glucose in Type 2 when diet and exercise do not work
  31. What is the pKa of sulfonylureas?
    5
  32. What is the most common side effect of the sulfonylureas?
    • hypoglycemia
    • lots of DIs
  33. What is the indication for the thiazolidinediones?
    • for Type 2
    • alone or in combo with sulfonylurea or insulin
  34. These drugs could cause hepatic failure?
    thiazolidinediones
  35. Monitor transaminase levels before and after starting therapy with these drugs?
    thiazolidinediones
  36. Name the two thiazolidinediones.
    • rosiglitazone (Avandia)
    • pioglitazone (Actos)
  37. Which thiazolid is metabolized by 2C8 (and to a lesser extent by 2C9)?
    rosiglitazone
  38. Which thiazolid is metabolized by 3A4?
    pioglitazone
  39. These drugs increase the activity of nuclear receptor PPAR gamma that regulates genes responsible for the control of glucose and insulin metabolism in adipose, liver and skeletal muscle tissues, which increases tissue sensitivity?
    thiazolids
  40. These drugs need to be taken with additional BC other than OCs?
    thiazolids (mainly pioglitazone)
  41. These drugs are contraindicated in patients at risk for heart failure?
    thiazolids
  42. What is a common side effect when taking thiazolids?
    edema
  43. This drug is a non-sulfonylurea analog of glyburide?
    repaglinide (Prandin)
  44. What enzyme metabolizes Prandin?
    3A4
  45. this drug is for Type 2 w/ diet and exercise and can be used in combo with a thiazolid?
    prandin
  46. This drug stimulates the release of insulin in beta cells by binding to and blocking an ATPase sensitive K+ channel, which causes depolarization and an increase in intracellular calcium, which leads to release of insulin? May also decrease hepatic clearance of insulin and is a miscellaneous non-sulf?
    Prandin
  47. This drug can decrease vit B12 and folate absorption?
    metformin
  48. This drug's half life is only 1.3-4.5 hours?
    metformin
  49. This drug has no protein binding and no metabolism with rapid renal excretion?
    metformin
  50. You should STOP taking this drug if you have an MI or septicemia?
    metformin
  51. Metformin
    Glucophage
  52. Nateglinide
    Starlix
  53. T/F: metformin causes insulin release in the pancreas.
    false
  54. This drug is for Type 2 with diet and exercise and can be used in combo with a sulfonylurea?
    metformin
  55. Acarbose
    Precose
  56. Repaglinide
    Prandin
  57. Pioglitazone
    Actos
  58. Rosiglitazone
    Avandia
  59. Glimepiride
    Amaryl
  60. Glyburide
    • DiaBeta
    • Micronase
    • Glynase PresTab
  61. Glipizide
    Glucotrol
  62. Tolazamide
    Tolinase
  63. Tolbutamide
    Orinase
  64. Chlorpropamide
    Diabinese
  65. Acetohexamide
    Dymelor
  66. This drug decreases hepatic gluconeogenesis and intestinal glucose absorption, increases peripheral tissue insulin sensititivity, and does NOT cause insulin release in the pancreas?
    metformin
  67. This drug is a D-phenylglycine and is unrelated to the sulfonylureas?
    Starlix
  68. Miglitol
    Glyset
  69. What enzymes metabolize Starlix?
    • 2C9 = 70%
    • 3A4 = 30%
  70. This drug is highly selective with low affinity for heart and skeletal muscle potassium channels and has 98% albumin binding?
    Starlix
  71. Which drug should you take w/ the first bite of every meal TID?
    Acarbose
  72. This drug decreases carb absorption by competitively inhibiting teh intestinal enzyme alpha glucosidase? Also prevents protonation of glycosidic bond in the saccharides.
    Acarbose
  73. Which one has minimal systemic absorption -- acarbose or miglitol?
    acarbose
  74. Which one has rapid and complete systemic absorption -- acarbose or miglitol?
    miglitol
  75. At what dose of acarbose can we see an elevated serum transaminase?
    >100mg
  76. Name two alpha-glucosidase inhibitors.
    • acarbose (Precose)
    • miglitol (Glyset)
  77. What is a common adverse side effect of using alpha glucosidase inhibitors to treat Type 2 diabetes?
    pneumatosis cystoides intestinalis
  78. Which drug could reduce Hemoglobin A1C that Sreejayan is studying?
    chromium picolinate
  79. Metaglip combo
    glipizide + metformin
  80. Avandamet combo
    rosiglitazone + metformin
  81. Glucovance combo
    glyburide + metformin
  82. Avandaryl combo
    rosiglitazone + glimepiride
  83. ACTOplus met combo
    pioglitazone + metformin
  84. PrandiMet combo
    Prandin (repag) + metformin
  85. Insulin glulisine
    Apidra
  86. Insulin Detemir
    Levemir
  87. Insulin Glargine
    Lantus
  88. Insulin aspart
    Novolog
  89. Insulin lispro
    Humalog
  90. What are the two long acting insulins?
    • lantus
    • levemir
  91. This insulin product is developed in saccharomyces cerevisiae and is followed by chemical modification with a fatty acid?
    levemir
  92. This long acting insulin forms microprecipitates in subQ tissue which prolongs its duration from 18 to 26 hours?
    lantus
  93. This insulin product is produced in E. coli?
    apidra
  94. Take this rapid acting insulin 5-10 min before a meal?
    novolog
  95. Take this rapid acting insulin 15 min before meals or immediately after eating?
    humalog
  96. What is the duration for both humalog and novolog?
    3-5 hours
  97. Name the recombinant/chemically modified insulins.
    • apidra- rapid
    • novolog- rapid
    • humalog- rapid
    • lantus- long
    • levemir- long
  98. Exenatide
    Byetta
  99. Pramlintide acetate
    Symlin
  100. This NME recombinant/synthetic insulin is an incretin mimetic or glucagon-like peptide -1 receptor agonist that binds the GLP1 receptor on beta cells causing insulin synthesis and excretion?
    Byetta
  101. This NME recombinant/synthetic insulin is a synthetic analog of human amylin (which is a neuroendocrine hormone made by beta cells that contribute to post prandial glucose control)?
    Symlin
  102. Duetact combo
    Pioglitazone + Glimepiride
  103. This is a rapid acting insulin product for inhalation that failed?
    Exubera
  104. What are incretins?
    peptide hormones released from the gut in response to ingestion of carbs
  105. What are the 2 MOAs of incretins?
    • regulate rate of nutrient transit in the GI tract (esp stomach emptying)
    • enhance glucose, stimulate insulin secretion from the pancreas when glucose levels are high
  106. T/F: IV insulin causes the release of incretins
    false
  107. This drug could cause acute pancreatitis and the FDA also warns of acute renal failure and insufficiency?
    Byetta
  108. This drug was originally identified in the Heloderm suspectum lizard (Gila monster) and has 39 amino acids?
    Byetta
  109. Why is the action of incretins so short (short half life)?
    because of rapid metabolism by DPP-IV
  110. This drug has a black box warning for risk of thyroid C-cell tumors?
    Victoza
  111. Inject this drug SubQ every day any time of the day independent of meals?
    victoza
  112. Victoza
    Iiraglutide
  113. What is the MOA of Victoza?
    mimics incretin or GLP-1 as an adjunct to diet and exercise
  114. Sitagliptin phosphate
    Januvia
  115. This drug is a DPP-IV inhibitor so it prolongs the biological levels of natural incretins GLP-1 and GIP, thereby increasing insulin release and decreasing glucagon release?
    Januvia
  116. Does Januvia inhibit any CYP enzymes?
    no
  117. T/F: Januvia is a substrate for PGP
    true
  118. You need to modify the dosage of this drug if patient has moderate to end-stage renal failure b/c it is excreted via active tubular secretion as unchanged drug via organic cation transporters (OCT)?
    Januvia
  119. Janumet Combo
    Januvia + metformin
  120. Juvisyns combo
    Januvia + simvastatin
  121. Saxagliptin
    Onglyza
  122. What is the MOA of Onglyza?
    DPP-IV inhibitor
  123. How is Onglyza metabolized?
    3A4 and 3A5 to an active metabolite
  124. What is an adverse effect of Januvia?
    cleaving other peptides like neuropeptides, cytokines, chemokines
  125. What is an adverse effect of Onglyza?
    • decreased Lymphocyte countsd = UTI and URI
    • hypoglycemia
    • urticaria
    • acute pancreatitis
    • headache
  126. Linagliptin
    Tradjenta
  127. What is the newest DPP-IV inhibitor (2011)?
    Tradjenta
  128. Do not use this new drug in Type 1 patients or patients with diabetic ketoacidosis or with insulin?
    Tradjenta
  129. This drug is a mild inducer and mild inhibitor of 3A4, and a substrate for PGP? (new)
    Tradjenta
  130. Old drug but new indication?
    Cycloset
  131. This drug is a dopamine receptor agonist, so it can increase dopamine levels early in the day and improve metabolism problems related to diabetes Type 2?
    Cycloset
  132. bromocriptine mesylate
    Cycloset
  133. This drug was also marketed as Parlodel for Parkinson's and hyperprolactinemia?
    Cycloset
  134. becaplermin
    Regranex
  135. colesevelam hcl
    Welchol
  136. this drug comes from human derived platelet growth factor?
    Regranex
  137. Use this drug with extreme caution in patients with any known malignancy?
    Regranex
  138. This is a 0.1% topical gel used to treat lower extremity diabetic neuropathic ulcers assuming that adequate blood supply is present?
    Regranex
  139. Who cannot use Regranex?
    anyone with a known neoplasm at the site of administration
  140. How do you calculate the dose for Regranex?
    length of gel in inches- (ulcer length) x (ulcer width) x 0.6
  141. This is a bile acid sequesterant used as an adjunct to diet and exercise to improve glycemic control in adults with Type 2 DM?
    Welchol

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