Lecture 14 Flashcards
DPP-4 inhibitors
MOA:
- increases activity of endogenous incretin hormones, ___ and ___
GLP-1, GIP
DPP-4 inhibitors
Efficacy:
A1C: decrease ___ - ___ %
FBG: decrease ___ mg/dL
PPG: decrease ___ - ___ mg/dL
Weight: decrease ___ - ___ kg (weight ___ )
- 0.5-1%
- 20 mg/dL
- 20-40 mg/dL
- 0-0.5 kg, neutral
DPP-4 inhibitors
PK
- excreted unchanged in the ___
- adjust dose for ___ function (exception: ___ )
- urine
- renal, linagliptin
DPP-4 inhibitors
adverse effects
- ___ pharyngitis
- ___ infections
- headache
- some reports of acute ___
- nasopharyngitis
- upper respiratory tract
- pancreatitis
DPP-4 inhibitors
FDA warning for ___ pain
- symptoms usually resolved in 1 month after drug ___
- joint
- discontinuation
DPP-4 inhibitors
FDA warning for ___ risk
with ___ and ___
- if you have to use a DPP-4, use ___
HF, saxagliptin, alogliptin
- sitagliptin
DPP-V inhibitors - sitagliptin dosing
- CrCl > 50 mg/min: ___ mg daily
- CrCl 30-50 mg/min: ___ mg daily
- CrCl < 30 mL/min or ESRD on dialysis: ___ mg daily
- 100 mg
- 50 mg
- 25 mg
DPP-4 inhibitors - saxagliptin dosing
- ___ mg daily
- CrCl < 50 mg/min: ___ mg daily
- 2.5-5 mg
- 2.5 mg
DPP-4 inhibitors - linagliptin dosing
___ mg once daily
5 mg
DPP-V inhibitors - alogliptin dosing
- __ mg daily
- CrCl 30-60: ___ mg
- CrCl < 30 or ESRD and dialysis: ___ mg
- 25 mg
- 12.5 mg
- 6.25 mg
SUs
MOA:
- stimulate ___ release from ___ cells
- may increase binding between insulin and receptors or increase the number of ___
- insulin, beta
- receptors
SUs
Clinical Application
- adjunct to diet and exercise in type ___ pts
- used in combination therapy with insulin and other non-insulin agents
2
SUs
Efficacy
- A1C: decrease ___ - ___%
- FBG: decrease ___ - ___ mg/dL
- 1-2%
- 60-70 mg/dL
SUs
PK of 2nd gens:
- glyburide and glipizide, more effective when taken ___ min AC (before ___ would be ideal)
- metabolized by ___
- some excreted in the ___
- glipizide metabolized without the formation of ___ metabolites, therefore it is preferred in ___ disease
- 30 min, breakfast
- liver
- urine
- active, renal
SUs
What is the preferred SUs in general?
Especially in:
- elderly/malnourished pts
- renal/heptain insfficiency
- concurrent use of hypoglycemic drugs like insulin
glipizide
SUs
adverse effects
- ____glycemia
- weight ___ (up to ___ kg)
- ____ upset
- ___ logic: leukopeniam thrombocytopenia, aplastic anemia
- allergic skin reactions/ ____ sensitivity
- Hypoglycemia
- gain, 3 kg
- GI
- hematologic
- photosensitivity
SUs
Dosing
- start at ___ end of the dosing range, especially in the ____
- increase dose every ___ weeks until maximum dosage
- exceeding the max dosage increases ___, but does not decrease ___
- current max doses now being questioned; estimated to be 60-75% of package insert max dose
- low, elderly
- 1-2 weeks
- side effect, BG
SUs - glipizide (Glucotrol) dosing
starting dose: ___ - ___ mg daily
Max daily dose: ___ mg
Max daily dose (XL): ___ mg
- 2.5-5 mg
- 40 mg
- 20 mg
SUs - glyburide (Micronase/Diabeta)
starting dose: ___ - ___ mg daily
Max daily dose: ___ mg
- 1.25-5 mg
- 20 mg
SUs - glyburide micronized (Glynase)
starting dose: ___ - ___ mg daily
Max daily dose: ___ mg
- 1.5-3 mg
- 12 mg
SUs
use cautiously in the following pts due to increased risk of hypoglycemia
- ___ pts
- pts with ___ / ___ disease
- ___ dietary intake
- alcoholics
- pts taking concomitant ___ agents
- elderly
- renal/hepatic
- irregular
- hypoglycemic
SUs
best candidates:
- no type ___ pts
- short duration of ___
- FBG < ___ mg/dL
- high fasting ___ peptide levels (means that the pt can still make ___. )
- 1
- diabetes
- 250 mg/dL
- C, insulin
SUs
Treatment Failure
- ___ % will have primary failure
- after 5 years ___ - ___ % may experience secondary failure
- commons for these meds to fail after ___ months
- 25%
- 50-75%
- 6-12 months
TzDs
MOA:
- bind to PPAR-gamma on ___ and ___ cells
- improved cellular response to insulin without increasing ___
- decreases insulin ___
- decreases ___ glucose production
- fat, vascular
- secretion
- resistance
- hepatic
TzDs
Other benefits
- pioglitazone can decrease ___ by 10-20%
- ___ remains unchanged; rosiglitazone may increase
- both meds increased ___ by 3-9 mg/dL
- endothelial function has improved and ___ may decrease slightly
- TG
- LDL
- HDL
- blood pressure
TzDs
Efficay
- A1C: decrease ___ - ___ %
- FBG: decrease ___ - ___ mg/dL
- 0.5-1.5%
- 60-70 mg/dL
TzDs
Adverse Effects: ___ toxicity
- do not start therapy in pts with baseline LFTs > ___ x normal
- check LFTs ___ months after starting, if stable, check in ___ months
- D/C med if LFTs are > ___ x normal
Hepatotoxicity
- 2.5x
- 3 months, 6 months
- 3x
TzDs
Other Adverse Effects
- N/V
- abdominal pain
- fatigue
- anorexia
- dark urine
- resumption of ___
- exacerbations of ___ : use in caution with NYHA class III and IV
- increased ___ , greater than 10 lb weight gain in some pts
- ___ edema
- increased ___ risk
- ovulation
- HF
- edema
- macular
- fracture
T or F: TzD studies on CV benefit are controversial
True; not a lot of great evidence to use for CV. pioglitazone might have some anti-atherogenic potential
TzDs - pioglitazone dosing
initial dose: ___ - ___ mg daily
Max dose: ___ - ___ mg daily
titrate dose every ___ weeks
- 15-30
- 30-45
- 12
in pts with high risk ASCVD, HF, and/or CKD;
___ and ___ are recommended independent of A1C
SGLT2s and GLP-1s
start dual therapy if
ADA: A1C > ___ %
AACE: A1C > ___ - ___ %
- 9%
- 7.5-9%
in pts with T2DM, a ___ is preferred to insulin when possible
GLP-1
___ should be used if there is evidence of ongoing catabolism ( weight ___ ), if symptoms of ___ are present, or if A1C > ___ %, or blood glucose readings are > ___ mg/dL
insulin
loss
hyperglycemia
10%
300 mg/dL
if insulin is used, combination therapy with a ___ is recommended for efficacy and durability of treatment
GLP-1
if pt isnt controlled on basal + GLP-1, switch to basal + bolus
Be aware of overbasalization with insulin. If the basal dose is about ___ units/kg/day or there is high variability in BG readings, evaluate basal level and consider basal-bolus initiation
0.5 units/kg/day
