Non-Insulin Anti-Diabetics Flashcards
Name the 4 groups of ORAL hypoglycemics
Insulin secretagogues (sulfonylurea and meglitinides)
Biguanides
Thiazolidinediones (TZDs)
Alpha- glucosidase inhibitors
Which non-insulin anti-diabetic drugs (2) produce the biggest drop in fasting plasma glucose AND HbA1c? MOAs?
Sulfonylureas: Stimulate insulin release via SUR1 subunit and reduce serum glucagon levels
metformin: inhibits gluconeogenesis
Name the two first generation sulfonylureas
Tolbutamide
Chlorpropamide
Which first generation sulfonylurea has a short half life and rarely causes hypoglycemia?
Tolbutamide
Which first generation sulfonylurea has a long half life and is contraindicated in patients with hepatic or renal insufficiency?
Chlorpropamide
Which sulfonylurea causes jaundice in doses over 500mg?
Chlorpropamide
Which sulfonylurea is contraindicated in the elderly? Why?
Chlorpropamide
Higher risk of prolonged hypoglycemia
Which sulfonylurea causes a hyperemic flush if taken with alcohol?
Chlorpropamide
Which non-insulin anti-diabetic drugs can be used to treat central diabetes insipidus? How?
Sulfonylureas esp Chlorpropamide
Can cause SIADH -> hyponatremia
Name the three second generation sulfonylureas
Glyburide
Glipizide
Glimepiride
Which sulfonylurea results in hypoglycemia in 20-30% of pts?
Glyburide
How do second generation sulfonylureas differ from first?
100x more potent and fewer adverse effects
Which sulfonylurea has the shortest half life? Why is this important?
Glipizide
Less likely to cause serious hypoglycemia
Which sulfonylurea is approved for once-daily monotherapy or in combo with metformin or insulin?
Glimepiride
How are sulfonylureas delivered?
Orally
Which oral anti-diabetic agents are associated with wt gain?
Sulfonylureas
Meglitinides
Thiazolidinediones (TZDs)
Which group of oral anti-diabetic drugs can lead to tachyphylaxis? (where they initially respond to treatment then regress)
Sulfonylureas
Name the two meglitinides. Which is more effective? MOA?
Repaglinide - more effective
Nateglinide
Like sulfonylureas, stimulate insulin secretion by binding SUR1 (at different place though)
Which group of oral anti-diabetic drugs have rapid onset, short duration and are used for postprandial glucose regulation? When are they taken?
Meglitinides
Taken before each meal
Which class of oral anti-diabetic drugs can safely be given to patients with a sulfa allergy?
Meglitinides
Which insulin secretagogue produces fewer incidences of hypoglycemia?
Nateglinide
Secretagogues are sulfonylureas and meglitinides
Name the only biguanide. MOA?
Metformin
Inhibits gluconeogenesis by reducing gene expression of necessary enzymes
Which oral anti-diabetic drug doesn’t cause hypoglycemia even at large doses?
Metformin
Which oral anti-diabetic drug is associated with a LOSS of weight?
Metformin
What is the only hypoglycemic drug shown to reduce macro vascular events in type II DM?
Metformin
What is the first line therapy in type II DM?
Metformin + diet and exercise
Which oral anti-diabetic drug is not metabolized and excreted in urine?
Metformin
Which oral anti-diabetic drug used long term can interfere with B12 absorption?
Metformin
What is metformin’s major adverse effect in 20% of pts?
GIT: anorexia, nausea, vomiting, diarrhea
Which oral anti-diabetic drug is contraindicated in pts with renal or hepatic disease due to increased risk of lactic acidosis?
Metformin
What is a major off label use for metformin?
It lowers insulin resistance and can lead to ovulation in PCOD and possibly pregnancy
Name the two thiazolidinediones (TZDs)
Pioglitazone
Rosiglitazone
Which oral anti-diabetic drugs act by agonism of PPAR-gamma? How does this decrease insulin resistance?
TZDs (-glitazones)
PPAR-gamma is involved in lipid and glucose metabolism and TZDs promote glucose uptake and use in adipose tissue
Which class of oral anti-diabetic drugs has a slow onset that can take weeks to months to act? Why?
TZDs because they act through gene expression
Which TZD increases HDL and decreases TAGs? How does the other affect lipids?
Pioglitazone
Rosiglitazone also inc HDL but has no effects on TAGs and also increases LDL
Which class of oral anti-diabetic drugs is contraindicated in class III and class IV heart failure?
TZDs
Which class of oral anti-diabetic drugs requires periodic monitoring of liver function?
TZDs (and Acarbose - alpha-glucosidase inhibitor)
Name the two alpha-glucosidase inhibitors. MOA?
Acarbose
Miglitol
Reduce postprandial digestion and absorption of starch and disaccharides
Which class of oral anti-diabetic drugs are associated with increased flatulence and contraindicated in IBD?
Alpha-glucosidase inhibitors
Pt is using Acarbose and a sulfonylurea and develops hypoglycemia. How should he be treated and why
With glucose because breakdown of sucrose is inhibited by Acarbose
What must be monitored in patients taking Acarbose?
Liver function
Which drug is a GLP-1 analog derived from the salivary gland of the Gila monster? MOA?
Exenatide
Incretin resistant to DPP-IV (enzyme that degrades incretins) so it enhances glucose-dependent insulin secretion, suppresses glucagon release, slows gastric emptying, and decreases appetite
How is exenatide administered? Type of drug?
SC injection 2x/day
Incretin analog
Which drug is given orally and is a selective inhibitor of DPP-IV? What is DPP-IV?
Sitagliptin
DPP-IV degrades incretins
Which drug is a synthetic analog of amylin? MOA?
Pramlintide
They both inhibit food intake, gastric emptying, and glucagon secretion
Amylin is cosecreted with insulin
Which anti-diabetic drug lowers LDL, slightly reduces HbA1c, and can cause constipation, dyspepsia and increase TAGs?
Colesevelam
Bile-acid sequestrant
What is the only drug approved for use in conjunction with insulin for type II diabetes?
Metformin
If initial treatment with metformin does not work, what is the next step? How do you choose which drug to give?
Either insulin or a sulfonylurea
Give insulin if HbA1c is >8.5%
If hypoglycemia is particularly undesirable and weight loss is a major goal, what drug would you prescribe, assuming HbA1c is <8%?
Exenatide
What is the most effective diabetes medication at lowering glycemia?
Insulin
When is insulin considered as a first line treatment?
When HbA1c is >10%
Name two effects glucagon can have on cancers.
Causes release of insulin from pancreas, catecholamines from pheochromocytoma, and calcitonin from medullary carcinoma
Which anti-diabetic drug is used in radiology of the bowel due to its ability to relax intestine?
Glucagon
Which type of insulin is used in an insulin pump?
Rapid acting