Insulin/Oral Anti-diabetic Agents Flashcards
rosiglitazone
thiazolidinedione
- Agonist of PPAR gamma leading to an increase in in insulin sensitivity (liver, fat, and muscle).
- Adverse Rxn: cardiac disturbances, edema, fluid retention, wt gain, liver toxicity, and increased risk for bladder CA
pioglitazone
thiazolidinedione
- Agonist of PPAR gamma leading to an increase in in insulin sensitivity (liver, fat, and muscle).
- Adverse Rxn: cardiac disturbances, edema, fluid retention, wt gain, liver toxicity, and increased risk for bladder CA
acarbose
alpha-glucosidase inhibitor
- decrease intestinal absorption of carbs
- Adverse Rxn: flatulence, diarrhea, and abd pain.
miglitol
alpha-glucosidase inhibitor
- decrease intestinal absorption of carbs
- Adverse Rxn: flatulence, diarrhea, and abd pain.
canagliflozin
glucose reabsorption inhibitor
- prevents reabsorption of glucose in the kidneys, thus increasing the body’s excretion of glucose.
- S/E: UTI’s and increased urinary frequencies
empagliflozin
glucose reabsorption inhibitor
- prevents reabsorption of glucose in the kidneys, thus increasing the body’s excretion of glucose.
- S/E: UTI’s and increased urinary frequencies
insulin aspart
rapid acting
modification of the amino acid sequence (B28 changed from Pro to Asp) that promotes absorption by preventing self association
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance
insulin detemir
long acting
modification of amino acid sequence (c-terminal Thr B chain was deleted & myristic acid attached to new c-terminal Lys) that increases self aggregation and binding to albumin
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance
insulin glargine
long acting
modification of the amino acid sequence (A21 changed from Asn to Gly and two Arg added to positions B31 & B32) that makes insulin soluble at acidic pH but precipitates at neutral pH thus slowing down absorption
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance
insulin glulisine
rapid acting
modification of the amino acid sequence (B3 & B29 changed from Asn to Lys & Lys to Glu) that promote absorption by preventing self association
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance
insulin lispro
rapid acting
modification of the amino acid sequence (residues B28 & B29 changed from Pro-Lys to Lys-Pro) that promotes absorption by preventing self association
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance
NPH
Intermediate acting
wild-type amino acid sequence
cloudy suspension with protamine added to give 1:6 molar ratio to insulin– all protamine and insulin are in a complex
-clinical use now waning in favor of long-acting insulins
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance
regular crystalline insulin
short acting
wild-type amino acid sequence
-adverse effects: hypoglycemia, lipodystrophy at injection site, allergy/resistance
exenatide
incretin agonist
increases insulin and decreases glucagon
SQ injection
side effects: nasuea, anorexia, headaches, diarrhea, pancreatitis
liraglutide
incretin agonist
increases insulin and decreases glucagon
SQ injection
side effects: nasuea, anorexia, headaches, diarrhea, pancreatitis
saxagliptin
inhibitor of incretin degradation
increases insulin and decrease glucagon
oral
side effects: headache, increased rate of infections and pnacreatitis
sitaglitpin
inhibitor of incretin degradation
increases insulin and decrease glucagon
oral
side effects: headache, increased rate of infections and pnacreatitis
pramlintide
amylin analog (hormone made in the beta cells, it acts on the alpha cells to inhibit glucagon secretion, also has CNS mediated anorectic effect)
- can increase the effectiveness of insulin therapy in type 1 DM
- SQ
- useful in type 2 when given alone
- side effects: hypoglycemia, nausea, vomiting, anorexia
chlorpropamide (Drabinese)
Sulfonylurea- First generation
- oral anti-diabetic, ~60 hr half-life
- inc. insulin secretion by decreasing K+ efflux from beta cells in the pancreas
- S/Fx: hypoglycemia, tachyphylaxis
- no longer readily available and rarely used
glipizide (Glucotrol)
Sulfonylurea- Second generation
- oral anti-diabetic, 10-24 h duration
- generally more potent, more readily available, and commonly used
- S/fx: hypoglycemia, tachyphylaxis
glyburide (Micronase)
Sulfonylurea- Second generation
- oral anti-diabetic, 10-24 h duration
- generally more potent, more readily available, and commonly used
- S/fx: hypoglycemia, tachyphylaxis
glimepiride (Amaryl)
Sulfonylurea- Second generation
- oral anti-diabetic, 10-24 h duration
- generally more potent, more readily available, and commonly used
- S/fx: hypoglycemia, tachyphylaxis
tolbutamide (Orinase)
Sulfonylurea- First generation
- oral anti-diabetic, ~60 hr half-life
- inc. insulin secretion by decreasing K+ efflux from beta cells in the pancreas
- S/Fx: hypoglycemia, tachyphylaxis
- no longer readily available and rarely used
repaglinide (Prandin)
Meglitinide- oral anti-diabetic
- like sulfonylureas, prevent K+ efflux from beta cells, ultimately leading to inc. insulin secretion
- chemically unrelated to and have greater binding affinity to K+ channels then sulfonylureas
- more potent then second gen. sulfonylureas but shorter DOA
- used to control postpandrial glucose levels
- S/Fx: hypoglycemia, need to use cautiously in patients with renal or hepatic insufficiency
nateglinide (Starlix)
Pheylalanine analog- oral anti-diabetic
- chemically unrelated to sulfonylureas and meglitinides but stimulate insulin secretion by same mechanism
- effect is faster but less sustained then with meglitinides
- S/Fx: hypoglycemia
- safer in those with reduced renal function
metformin (Glucophage)
Biguanide- oral anti-diabetic
- inactivate mitochondrial glycerophosphate dehydrogenase, antagonize the action of glucagon and/or activate the AMP-activated protein kinase
- actions occur in liver and lead to reduction in gluconeogenesis and thus hepatic glucose output
- commonly used as first line therapy in DM type II
- S/Fx: GI discomfort, lactic acidosis, Vitamin B12 deficiency
