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52 Cards in this Set
- Front
- Back
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What is the mechanism of action of sulfonylureas?
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Block ATP-Dependent potassium channels in B-cell membane --> leads to depolarization of B cell membrane --> Calcium channels open --> release of insulin
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Glut4 is present in what cell types?
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adipose and fat
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What conditions require INCREASE need for insulin?
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stress, pregnancy, thyrotoxicosis, grave's disease.
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What are the actions of insulin on the muscles?
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- Stimulates both glucogen synthesis and protein synthesis (anabolic and storage)
- stimulates glycogen synthase and inhibits glycogen phosphorylase -Protein Synthesis - enhances amino acid transport and ribosomal protein synthesis |
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What are the actions of insulin on adipose cells?
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- facilitates triglyceride storage and decreases free fatty acids in adipocytes
- activate plasma lipoprotein lipase -increase glucose transport into cells via Glut 4 - Reduce intracellular lipolysis |
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Can NPH be given IV?
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No! Because it's a suspension!
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What is the onset and duration of Insulin Glargine (Lantus, Lantus Solotar) and Insulin Detemir (Levemir, Levemir Flexpen)
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Slow onset and extended duration.
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what is the clinical use of Insulin Glargine (Lantus, Lantus Solotar) and Insulin Detemir (Levemir, Levemir Flexpen) ?
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Given ONCE a day to provide a PEAKLESS basal insulin level that lasts more than 24 hrs.
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what is the "4-shot method" of insulin delivery?
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Glargine or Determin given once a day PLUS a fast acting and short duration like Lisptro, Asprart, or Glulisine given 3 times a day.
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What is in the HumALOG Mix ?
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Isophane (NHP) Intulin Lispro + Insulin Lispro
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What is in Novolog Mix?
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Isophane (NHP) insulin Aspart and Insulin Aspart
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What is the clinical use of Humalog Mix and Novolog Mix?
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Covers both fasting AND postprandial glucose levels when injected TWICE a day - rapid absorption and prolonged duration.
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What is in Humulin and Novolin mix?
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Mixture of Isophane (NHP) insulin and regular insulin
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What are normal blood glucose levels?
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110 mg/dl
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What is the major advantage and disavantage of a tight glycemic control?
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Advantage: 60%decrease in lng-term diabetic complications
Disadvantage: Increased frequency of hypoglycemic episodes |
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What is the most common and severe side effect of insulin therapy?
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Hypoglycemia
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What are the sympathetic symptoms of hypoglycemia?
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Palpitations, tachycardia, sweating, tremulousness
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If a patient is sweating and has palpitations, tachycardia, convulsions, confusion they most likely have hypoglycemia. How is this managed?
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Reversed by prompt administration of glucose (orally or IV) or glucagon (IM or SC Injection)
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What drugs if administered with insulin can increase the risk of hypoglycemia by inhibiting the actions of catecholoamines on gluconeogenesis and glycogenolysis.
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B-adrenergic receptor antagonists (Beta Blockers - -OLOL)
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Which group of oral hypoglycemic agents require functional beta cells?
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Insulin Secretagogues - Sulfonylureas and Meglitinides
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Which Sulfonylurea is shortest acting and safe in geriatric treatment?
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Tolbutamide
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What is the clinical use of Glyburide (Diabeta), Glipizide (Glipizide XR) and Glimepiride (Amaryl) ?
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2nd generation sulfonylureas that manage both fasting and postprandial hyperglycemia.
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What Insulin Secretagogues are short acting so they must be used only as postprandial hyperglymic drugs and in combination with another drug?
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Meglitinides - Repaglinide (Prandin) and Nateglinide (Starlix)
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what are the adverse effects of insulin secretagogues?
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HYPOGLYCEMIA DUE TO OVERDOSE! (less likely with tolbutamide because its less potent) - rash, allergy, anemia, GI disturbance
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Which group of oral hypoglycemic agents require functional beta cells?
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Insulin Secretagogues - Sulfonylureas and Meglitinides
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Which Sulfonylurea is shortest acting and safe in geriatric treatment?
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Tolbutamide
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What is the clinical use of Glyburide (Diabeta), Glipizide (Glipizide XR) and Glimepiride (Amaryl) ?
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2nd generation sulfonylureas that manage both fasting and postprandial hyperglycemia.
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What Insulin Secretagogues are short acting so they must be used only as postprandial hyperglymic drugs and in combination with another drug?
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Meglitinides - Repaglinide (Prandin) and Nateglinide (Starlix)
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what are the adverse effects of insulin secretagogues?
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HYPOGLYCEMIA DUE TO OVERDOSE! (less likely with tolbutamide because its less potent) - rash, allergy, anemia, GI disturbance
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What drugs compete for binding protein and intensify the effects of first generation sulfonylureas?
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Clofibrate, phenylbutazone, sialcylates, sulfonamides.
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What is the mechanism of action of Biguanides (Metformin)?
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-reduces hepatic gluconeogenesis
-Reduces GI glucose absorption -Stimulates peripheral glycolysis -reduces glucagon concentrations - does NOT require funtional B cells! |
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What is the clinical use of Metformin ?
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management of both fasting and postprandial hyperglycemia for type 1 and 2 patients with significant insulin resistance.
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What oral hypoglycemic is the best choice for a patient with insulin resistant syndrome?
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Metformin
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What is the Black Box Warning for Biguanide - Metformin ?
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LACTIC ACIDOSIS! - decreases uptake of lactic acid by liver
CI - in patients with renal disease and hepatic disease |
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What is the mechanism of action of thazolidinediones (Rosiglitazone and Pioglizatone)?
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-Activates the peroxisome proliferator-activated receptor gamma nuvclear receptor
(PPAR-y) -Regulates gene transcription - stimulates glucose uptake in muscle and adipose tissue, decreases hepatic gluconeogenesis - Increased insulin sensitivity - reduced insulin resistance- enhanced insulin effect without increasing release |
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What is the clinical use of Rosiglizatone and Pioglitazone?
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-Used to manage both fasting and posprandial hyperglycemia.
- Used as monotherapy or in combination with insulin or other antidiabetic agents(For patients that are overweight and taking insulin) |
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What are adverse effects of Rosiglitazone (Avandia) ?
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Increased risk of heart failure and myocardial infarction due to increased cholesterol levels.
-also edema and mild anemia |
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What are the adverese effects of Pioglitazone (Actos)?
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Induces cytochrome P450 enzymes so increased metabolism of ORAL CONTRACEPTIVES and CYCLOSPORINE
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What is the mechanism of action of alpha-glucosidase inhibitors ?
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Inhibit intestinal alpha-glucosidase - enzyme required to convert starches and disacchirides into monosaccharides
- decreased carbohydrate absorption limits postprandial hyperglycemia -Insulin sparing actions - NO EFFECT ON FASTING BLOOD SUGAR |
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What is the clinical use of Acarbose (Precose) and Migitol (Glyset) ?
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Management of POSTPRANDIAL HYPERGLYCEMIA!
- employed as monotherapy or in combination with other antidiabetic agents. |
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What are the adverse side effects of alpha-glucosidase inhibitors?
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GI disturbances - Diarrhea, flatulence, abdominal pain due to increased fermentation of unabsorbed carbs
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Which hypoglycemic oral agents are given SubQ ?
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Amylin analog and Incretin Mimetics
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Which hypoglycemic oral agents MUST be given with Insulin and is given SQ ?
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Amylin analog - Pramlinitide (Symlin, symlinpen)
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What is the mechanism of action of Amylin analog - Pramlinitide (Symlin, symlinpen) ?
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-Slows gastric emptying
-Suppresses postprandial glucagon secretion - Centrally mediated reduction in appetite in hypothalamus - augments insulin in regulation of postprandial glucose concentrations |
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What is the mechanism of action of Incretin mimetics - Exenatide (Byetta) and Liraglutide (Victoza) ?
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Activate glucagon-like-polypeptide 1 (GPL-1) receptor in hypothalamus => Increases insulin secretion and decreases glucagon levels
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What is the clinical use of Incretin mimetics - Exenatide (Byetta) and Liraglutide (Victoza) ?
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Used to manage postprandial hyperglycemia. Given SQ as monotherapy ot in combination with other antidiabetic agents
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What is the machanism of action of DPP-4 inhibitors - Sitaliptin, Saxalipton, Linaliptin ?
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Potentiates effects of incretins (GLP-1) via inhibition of metabolism => increases insulin secretion and decreases
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Why does Sitaliptin (Jenuvia) doesn't have a risk to cause hypoglycemia even through the other DDP-4 inhibitors do?
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Sitaliptin is only active during hyperglycemic states!
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What adverse effect is specifically seen with Saxaliptin but not with the other DDP-4 inhibitors?
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LYMPHOPENIA!
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Which combination of Oral hypoglycemic agents are euglycemic?
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Avandamet (Rosiglitazone/Metformin)
Actoplus Met (Pioglitazone/Metformin) Janumet (Sitagliptin/metformin) |
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How is diabetes mellitus diagnosed?
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two or more fasting blood sugar levels above 126 mg/dL
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What can be administered to overcome effects of a patient that has overdosed on beta blockers?
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Glucagon
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