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36 Cards in this Set
- Front
- Back
Cleavage of proinsulin produces insulin and what other product?
The absence of this indicates what? |
C-peptide
exogenous administration of insulin |
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What is insulin's mechanism of signal transduction?
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Insulin + tyrosine kinase receptor --> autophosphorylation --> IRS-1 binds receptor and is phosphorylated --> SH2-proteins bind IRS-1 --> translocation of GLUT-4 (PI-3 kinase activity), gene expression in nucleus (PI-3 kinase and p21ras G-protein activity)
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Rapid-acting insulins?
Clinical Use? |
Lispro, Aspart, Glulisine
control of postprandial glucose levels, emergency tx of diabetic ketoacidosis |
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Short acting insulin?
Clinical use? |
Regular insulin
IV in emergencies, SQ in normal maintenance regimens (must be taken 1h before meal) |
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Intermediate-acting insulins?
Characteristics? |
NPH
Combination regular insulin and protamine, delayed onset and peak of action |
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Long-acting insulins?
Characteristics? |
Glargine, detemir
peakless basal insulin level lasting more than 20h w/o causing hypoglycemia |
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Tx for hypoglycemia d/t excessive insulin effect?
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Prompt admin of glucose or glucagon
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What are the classes of non-insulin antidiabetic drugs?
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Sulfonylureas
Biguanides Thiazolidinediones α-glucosidase inhibitors |
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MOA of sulfonylureas?
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Close K channels in B cell membrane --> cell depolarization --> increase Ca --> insulin release
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2G sulfonylureas?
Characteristics? |
glyburide, glipizide, glimepiride
more potent than 1G |
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1G sulfonylureas?
characteristics? |
tolbutamide, chlorpropamide
Chlorpropamide has long duration Extensively bound to serum proteins (drugs that compete for protein binding may enhance hypoglycemic effects) |
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Newest class of insulin secretagogues?
Characteristics? |
Repaglinide (meglitinide), nateglinide
rapid onset, short duration |
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Most common side effects of all insulin secretagogues?
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hypoglycemia, weight gain
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Actions of metformin?
Significance? |
inhibit hepatic gluconeogenesis, stimulate glucose uptake and glycolysis in peripheral tissue, slow glucose absorption in GI, reduce plasma glucagon levels.
Does not cause hypoglycemia or weight gain |
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Which of the treatments for Type II diabetes cause weight gain?
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insulin, insulin secretagogues, and thiazolidinediones
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Toxic effects of metformin?
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GI distress (nausea, diarrhea), lactic acidosis
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Thiazolidinediones?
MOA? |
Rosiglitazone, pioglitazone
1. Increase insulin sensitivity by activating PPAR-γ receptor (which regulates txn of proteins for CHO and lipid metabolism) 2. Increase glucose uptake in adipose and muscle 3. Inhibit hepatic gluconeogenesis |
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Toxic effects of thiazolidinediones?
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Fluid retention (anemia, edema, may increase risk for CHF)
Liver toxicity (induce CYP450) |
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α-glucosidase inhibitors?
MOA? |
Acarbose, miglitol
CHO analogs that inhibit α-glucosidase (converts CHOs in intestines to saccharides that can be absorbed - do not affect fasting blood glucose) |
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Toxic effects of α-glucosidase inhibitors?
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flatulence, diarrhea, abd pain from increased fermentation of unabsorbed CHO
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How would you treat a pt experiencing hypoglycemia from taking an α-glucosidase inhibitor?
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Oral dextrose (glucose), NOT sucrose (will not be absorbed)
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MOA of pramlintide?
Clinical use? |
analog of amylin (pancreatic hormone), suppresses glucagon release, slows gastric emptying, CNS anorexogenic
Used w/ insulin for postprandial glucose control |
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Toxic effects of pramlintide?
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hypoglycemia, GI upset
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Which antidiabetic drug is a synthetic analog of glucagon-like peptide-1?
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Exenatide
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MOA of Exenatide?
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Augment glucose-stimulated insulin release from beta cells, retard gastric emptying, inhibit glucagon secretion, and produce a feeling of satiety
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Clinical use of Exenatide?
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Combination with metformin or sulfonylurea for type 2 DM
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Toxic effects of Exenatide?
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GI upset (esp nausea)
hypoglycemia when combined with sulfonylurea |
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MOA of Sitagliptin?
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inhibits dipeptidyl peptidase-4 (DPP4) which degrades GLP-1 and other incretins, thus, has same effects as Exenatide
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Toxic effects of Stagliptin?
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HA, nasopharyngitis, URI
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Treatment regimen for type 2 DM?
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Insulin-action-augmenting drug (metformin, thiazolidinedione, or α-glucosidase inhibitor)
+ insulin-supply-augmenting drug (insulin secretagogue or insulin) |
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Actions of glucagon?
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Acts through G protein-coupled receptors in heart, sm. muscle and liver to increase HR and contractility, increase hepatic glycogenolysis and gluconeogenesis, relaxes sm. muscle (esp in gut)
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What drug is used to treat severe hypoglycemia in diabetics, but requires intact hepatic glycogen stores?
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Glucagon
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Which antidiabetic drugs promote the release of endogenous insulin?
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Sulfonylureas (tolbutamide, chlorpropamide, glyburide, glipizide, glimepiride)
Repaglinide Nateglinide |
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Why should pts with renal or liver dz, or alcoholism not receive metformin?
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Increased risk of lactic acidosis
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Which antidiabetic drugs are taken at the beginning of a meal to delay the absorption of CHOs?
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α-glucosidase inhibitors
(Acarbose, Miglitol) |
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What non-diabetic condition is also treated using glucagon?
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Beta-blocker-induced cardiac depression
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