bile acid sequestrant used adjuntly to diet and exercise to improve glycemic control in adults with type 2 DM
colesevelam - welchol
recombinant biotechnology product
treatment of lower extremity diabetic neuropathic ulcers
becaplermin - regranex
adjunct to diet and exercise to improve glycemic control in type 2 diabetes only
dopamine receptor agonist
taken orally (low doses) within 2 hours of awakening with food
bromocriptine mesylate - cycloset
DPP-IV inhibitor
new in 2011
taken with or without food
not used in patients with type 1 diabetes or treatment of diabetic ketoacidosis
90% excreted unchanged
linagliptin - tradjenta
found in beta-islet cells in pancreas
acts within a cell in contrast to a receptor
released along with insulin
binds directly to a series of GTPase enzymes
seratonin
sulfonylureas - first gen.
serum half life - 7 hours
active metabolites
tolazamide - tolinase
sulfonylureas - first gen.
half life - 4.5-6.5 hours
NO active metablolites
tolbutamide - orinase
sulfonylureas - first gen.
half life - 36 hours
active metabolites
chlorproppamide - diabinese
sulfonylureas - first gen.
half life - 6-8 hours
acitve metabolites
acetohexamide - dymelor
sulfonylureas - second gen
half life - 2-4 hours
NO active metabolites
glipizide - glucotrol
sulfonylureas - second gen.
nonmicronized half life - 10 hours
weakly active metabolites
micronized half life - 4 hours
weakly active metabolites
sulfonylureas - third gen.
half life 9 hours
active metabolites
causes tranlocation of GLUT-4 to cell surface
may bind to a different protein than beta-islet cell
glimepiride - amaryl
thiazolidinediones
type 2 diabetes alone or with sulfonylurea or insulin
only work in the presence of insulin
increase the activity of PPAR -gamma
metabolized by CYP2C8 and some CYP2C9
rosiglitazone maleate - avandia
thiazolidinedionestype 2 diabetes alone or with sulfonylurea or insulinonly work in the presence of insulinincrease the activity of PPAR -gamma
metabolized by CYP3A4
decreases the efficacy of OC's
monitor ALT for hepatotoxicity
pioglitazone HCL - actos
non-sulfonylurea analog of glyburide
binds, and blocks an ATP-ase sensitve K+ channel.
metabolized by CYP3A4
take preprandially
repaglinide - prandlin
decrease hepatic gluconeogenesis and intestinal glucose absorption
increase peripheral tisssue insulin sensitivity
does not cause insulin release in the pancrease
half life - 1.3-4.5 hours
metformin HCL - glucophage
unrelated to sulfonylureas
stimulates insulin release in the pancreas
98% albumin binding
CYP2C9 metabolism (70%)
CYP3A4 metabloism (30%)
nateglinide - starlix
alpha-glucosidase inhibitor
decrease carbohydrate absorption
amino group prevents protonation of glycosidic bonds in the saccharides
tell patients take drug with the first bite of meals tid
minimal systemic absorption
acarbose - precose
alpha-glucosidase inhibitordecrease carbohydrate absorptionamino group prevents protonation of glycosidic bonds in the saccharidestell patients take drug with the first bite of meals tid
rapid and complete systemic absorption
miglitol - glyset
combination products for type 2 diabetes (6)
glipizide and metformin HCL - metaglip
rosiglitazone maleate and metformin - avandamet
glyburide and metformin HCL - glucovnace
rosiglitazone maleate and glimepiride - avandaryl
repaglinide and metformin - prandimet
rapid acting product recombinant site directed mutation human insulin produced in E. Coli
lysine replaces asparagine at position 3 and glutamic acid replaces lysine at postion 29
insulin glulisine - apidra
long acting 24 hour product reconbinant site directed mutation human insulin produced in saccharoyces cerevisiae followed by chemical modification with a fatty acid
98% bound to plasma albumin
threonine at B30 deleted and a C14 fatty acid chain has been attached to the B29 amino acid lysine
insulin detemir - levemir
forms microprecipitates in subcutaneous tissue prolinging diration from 18-26 hours
recombinant/chemically modified insulins
insulin glargine - lantus
rapid acting 3-5 hour duration
take 5-10 minutes before meals
recombinant/chemically modified insulin
insulin aspart - novolog
rapid acting 3-5 hour durationt
take 15 minutes before meals or immediately after eating
insulin lispro - humalog
incretin memetic or glucagon-like peptide-1 receptor agonist that binds the GLP-1 receptor on beta islet cells causing insulin synthesis and excretion
exenatide - byetta
synthetic analog of human amylin
pramlintide acetate-symlin
combination product for type 2 diabetes
two modes of action - directly targets insulin resistance and acts primarily to increase the amount of insulin produced by the pancreas
pioglitazone HCL and glimepiride - duetact
inhaled insulin for diabetes mellitus
rapid acting insulin
patient variability on correct use and dose left in blister packages = not marketed
exubera
peptide hormones released from the gut in response to the ingestion of carbohydrates
incretins
incretin memetic or glucagon like peptide-1 receptor agonist as an adjunct to diet and excercise
inject sub Q qd any time of the day independent of meals
black box warning - risk of thyroid C-cell tumors
victoza - liraglutide
monotherapy for type 2 diabetes, NOT for 1
combination therapy with metformin and thiazolidines
with or without food
substrate of p-glycoprotein
sitagliptin - januvia
DPP-4 inhibitor
metabolism - CYP3A4/5 to active metabolite
AR - decreased lymphocyte count, hypoglycemia, uticaria, acute pancreatitis, and headaches