Diabetes drugs Flashcards
TZDs
PioGlitazone (Actos) and RosiGlitazone (Avandia) / sensitizer: decreases insulin resistance and ins-sparing: decr ins requirements
- may worsen CHF!!!!!!!!! Don’t use in stage 3 or 4
- take 3-8 wks to see result, WGT GAIN, LIVER TOX (LFTs)
- Rosi: Black Box increased MI/angina and stroke?
- SE: LIVER TOXICITY (need freq LFT monitoring)
WGT GAIN
Metformin
(BiGuanides) / insuline sensitizer
DOC DM2 initial Tx for all types: under-over wgt and normal wgt
-reduces BS only (no effect on Insulin levels):
reduces hepatic glucose production and increases glucose uptake by cells
-NO HYPOglycemia, NO WGT GAIN
SE:
1) GI (bloat, gas) so TITRATE SLOWLY: start with 500mg before largest meal for 1 week, then increase to 500 BID for 1 wk, then to 1000 BID
2) LACTIC ACIDOSIS: cleared by kidney so avoid if cr >1.5 (men) cr > 1.4(women)
3) Iodine CONTRAST DYE: stop 2 days BF contrast and resume only after check cr and kidney fx is normal
SulfonuUreas
Ins Secretagogue
- Blocks K channels on B cells -> increase Ins secretion
- SE: HYPO and WGT GAIN (C/I: sulfa allergy)
- Glipizide and Glimepiride are once daily
Meglitinides
Insulin secretagogues: increase ins secretion
- RepaGlinide and NateGlinide
- RAPID onset and 1/2 life: take 30 min BF meal
- good for ppl with irratic eating schl, kinda like short-acting (“regular”) insulin
Which drug is not used in overwgt bc can cause wgt gain?
Sulfonylureas and TZD
Alpha-Glucosidase Inhibitors
"carb blockers": delay absorption, - helps with PostP hyperglycemia - aCARBose, MigLitol - SE: GAS, safe, work in all who can tolerate farting (no wgt changes)
DM pathogenesis
- increasing insulin resistance of liver, muscle receptors (type 2)
- Decreasing insulin secretion by panctiatic B cells
- excessive GLUCAGON section by alpha cells of pancreas
- impaired INCRETIN hormones (incretin mimetics: boyetta, victoria, trucitia)
- When DM appears, 80% of beta cells are gone
Incretin hormones
GLP-1 acts like insuline (looks like glucagon)
GIP: glucose-dependent Insulinotropic Polypeptide
- Both are stimulate insulin secretion in response to food consumption
- eat -> GIP and GLP1 secreted _> bind to b cells -> increase insulin section
(Resist GPP4 degradation)
Byetta/Exenatide
Incretin mimetic (synthetic version of GLP1)
GLP1 receptor Anogist -> binds to Beta cells -> increase insulin secreted
- MAY INCREASE BETA CELL # AND MASS!!!!!!!!!!!
- beta cell release insuline ONLY IF BS is high
decrease glucagon
- decreases hepatic glucose production (reducing insulin demand)
- increases SATIETY = eat less
- slows emptying - good for overwgt
When is Byetta/Exenatide indicate
- in DM2, when failedt to respond to metformin, sulfonyreas or combo
- SE: N/D, WGT LOSS (good!), hypoglycemia
- BID subQ injection (has a once weekly injections Bydureion)
Necrotizing Pancreatitis is a SE of
Byetta/Edenatide
PrAMlintide
synthetic Amylin
- in COMBO with insulin lowers BS
- use in both type 1 and 2, control PP sugar
- must inject separately before a meal
- control PP sugar
- less commonly used
- comes in a pen
DPP4 inhibitors
“gliptins” (Sita, Saxa)
- DPP4 degrades incretins
- prevent GLP1 degradation by DPP4 -> GLP1 binds to b cell - > increase insulin secretion and glucose uptake by tissues, decreasing BS
SGLT2 inhibitors
Pee!out
CanAgliFLOzin 100-300 mg PO daily bf 1st meal!!!
dapagliFLOzin (farxiga) 5-10 mg PO qAM
- MOA: inhibit Na-Glucose contrasporter (SGLT2) in kidney -> reduces glucose reabsorption from nephron -> pee out
Which med to use if you have pancreatic failure (decreased insulin production) - type 1
Sulfonylueras Incretin mimetic (byetta, victoria, trucilia)
Which med to use if you have glucose overproduction by liver (When would that happen except early AM?)
metformin - DOC for type 2
DPP4 inhibitor -> increase incretin binding to Beta cells -> increase insulin section -> decrease BS
which drug to use for overeating (high PP glucose)
Byetta (exenatide) (INCRETIN mimetic)
aCARBose (migLitol) (alpha gluconodase inh)
DPP4 inhibitor (“glipins”) – why?
Why not metformin - no wgt changes in pharm and wgt loss Clin med
which drug to use in insulin resistance (type 2)
metformin
TZD (Pio, Rosi) - prophylactic
which to use in combo glucotherapy
when single drug not enough
Metformin is DOC for type 2
bc wgt loss and reduces insulin resistace (and good for heart: decrease MI, Strokes)
Tx of type 2
- start with metformin (decreases insulin resistance)
- if taget HgA1c ( hunger -> wgt gain -> increase resistance
Insulin injection
Must give to DM1, may need in DM2
- normally don’t add oral agents in DM1