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Aspart
insulin and analogs
rapid acting
modified aAA sequence (B28 --pro-->asp)
promotes absorbtion by preventing self association
Detemir
insulin and analogs
long acting
increases self aggragation and binding to albumin
Glargine
insulin and analogs
modified AA sequence
makes insulin soluble at lower pH, but precipitates at neutral pH thus slowing absorbtion
Glulisine
insulin and analogs
rapid acting
modified AA sequence
promotes absorbtion by preventing self association
Lispro
insulin and analogs
rapid acting
modifiication of AA sequence
promotes absorbtion by preventing self association
NPH
insulin and analogs
intermediate acting
wild-type AA sequence with protamine added to give 1:6 molar ratio to insulin
all protamine and insulin are in complex
Regular crystalline insulin
insulin and analogs
short acting
wild type AA sequence
Exenatide
incretin-like drugs
incretin agonist
sub Q injections
useful only in type-2 diabetes
Sitagliptin
incretin-like drugs
inhibitor or incretin degradation
orally active
Pramlintide
amylin analogs
sub Q injection
useful for type - 2 diabetics
also type 1 if given with insulin
Chlorpropamide
sulfonylureas
1st generation (not as readily available)
60 hour duration
Glipizide
sulfonylureas
2nd generation (more potent)
10-24 hour duration
Glyburide
sulfonylureas
2nd generation (more potent)
10-24 hours
Glimepiride
sulfonylureas
2nd generation (more potent)
12-24 hours
Tolbutamide
sulfonylureas
1st generation (not as readily available)
6-12 hours duration
Repaglinide
meglitinide
bind to receptors associated with ATP-senstitive K+ channels in B-cells, stimulate their closing, ultimately leading to increase insulin secretion
chemically unrelated to sulfonylureas
binding affinity of meglitinides for the K+ channel is higher than sulfonylureas
more potent than 2nd generation sulfonylureas but of shorter duration (4-5 hours)
SE: hypoglycemia, weight gain, use cautiously in pts with renal or hepatic insufficiency
Nateglinide
phenylalanine analogs
same mech as meglitinidies but chemically unrelated
faster but less sustained than meglitinides
SE: hypoglycemia
safe for ppl with renal sysfunction
Metformin
biguanides
activate AMP-activated protein kinase, serves sensor of energy changes
activation of this kinase reduces hepatic glucose output
first line tx for type 2 diabetics
SE: GI discomfort, lactic acidosis (dont use for ppl predisposed)
doesnt induce hypoglycemia
Rosiglitazone
thiazolidiediones
agonist for PPARy
increase insulin sensitivity in target tissue (liver, fat, muscle)
SE: liver toxicity, CV side effects, weight gain
Pioglitazone
thiazolidinediones
agonist for PPARy
increase insulin sensitivity in target tissue (liver, fat, muscle)
SE: liver toxicity, weight gain
Acarbose
a-glucosidase inhibitors
reduce intestinal absorbtion of carbohydrates
SE: flatulence, diarrhea, abdominal pain, hepatic toxicity
Miglitol
a-glcosidase inhibitors
reduce intestinal absorbtion of carbohydrates
SE: flatulence, diarrhea, abdominal pain, hepatic toxicity
incretin
made after a meal by neuroendocrine cells in the gut
cause increase of insulin by pancreatic b-cells
cause decreased glucagon by pancreatic alpha cells
overall decrease in postprandial glucose
amylin
hormone made in alpha cells of the pancrease
inhibits glucagon secretion and has CNS-mediated anorectic effect
sulfonylureas
increase insulin secretion by decreasing K+ efflux
reduce glucagon levels
bind to receptor associated with K+ channels
SE: hypoglycemia
sulfonylurea resistance - tachyphylaxis
weight gain
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