1. DPP-IV Inhibitors, SGLT-2 Inhibitors, GLP-1 Receptor Agonists Flashcards
2016 RxPrep p550
MOA of dipeptidyl peptidase 4 inhibitors
prevent enzyme DPP-4 from breaking down incretin hormones, GLP-1 and glucose dependent
sitagliptin (brand, dosing, renal adjustments)
Januvia
100 mg daily
CrCl 30-49: 50 mg daily
CrCl
saxagliptin (brand, dosing, renal adjustments)
Onglyza
2.5-5 mg daily
CrCl
linagliptin (brand, dosing, renal adjustments)
Tradjenta
5 mg daily
No renal dose adjustment necessary
alogliptin (brand, dosing, renal adjustments)
Nesina
25 mg daily
CrCl 30-59: 12.5 mg daily
CrCl
DPP-4 warning: hypoglycemia when used with _____ or _____ ______; consider their dose reduction
insulin
insulin secretagogue
DPP-4 warning: acute _____ has been reported - d/c if suspected
pancreatitis (s/sx: severe, unresolving stomach pain ± vomiting; pain can radiate from abdomen to the back)
DPP-4 warning: severe and disabling _____ (____ pain) has been reported
arthralgia
joint
DPP-4 warning for aloglitpin
hepatotoxicity
DPP-4 SEs
nasopharyngitis, upper respiratory tract infections, UTIs, peripheral edema (especially if combined with a TZD), rash
DPP-4s are weight _____
neutral
DPP-4 monitoring (3)
BG, A1c, renal function
DPP-4s decrease A1c by ___%
0.5-0.8
DPP-4s target [pre/post]prandial BG
post
DPP-4s are pregnancy category __
B
DPP-4 note: possible risk of HF and death with _____ and _____
saxagliptin
alogliptin
DPP-4 DDI: with insulin or insulin secretagogue (management)
consider decreasing dose of insulin or insulin secretagogue; monitor BG closely after initiation of therapy
DPP-4 DDI: saxagliptin, a major ___ and ___ substrate (management)
3A4, Pgp
Limit dose to 2.5 with strong 3A4 inh. (atazanavir, clarithromycin, indinavir, triazole antifungals, telithromycin)
DPP-4 DDI: linagliptin, a major ___ and ___ substrate (management)
3A4, Pgp
linagliptin levels are decreased by strong inducers (carbamazepine, efavirenz, phenytoin, rifampin, St. John’s wort)
MOA of sodium glucose cotransporter-2 inhibitors
SGLT-2, expressed in the proximal renal tubules, is inhibited; this prevents the reabsorption of filtered glucose from the tubular lumen and lowers the renal threshold for glucose, increasing urinary glucose excretion
canagliflozin (brand, dosing, renal adjustments)
Invokana 100 mg daily prior to first meal of the day; max 300 mg daily CrCl 45-60: 100 mg daily max CrCl 30-44: not recommended CrCl
dapagliflozin (brand, dosing, renal adjustments)
Farxiga
5 mg daily in the morning; max 10 mg daily
CrCl 30-59: not recommended
CrCl
empagliflozin (brand, dosing, renal adjustments)
Jardiance
10 mg daily in the morning; max 25 mg daily
CrCl 30-44: not recommended
CrCl
SGLT-2 inh. CI
severe renal impairment (CrCl
SGLT-2 inh. warnings (all-6, cana-3, dapa-1)
all: genital mycotic infections, symptomatic hypotension 2/2 intravascular volume depletion, inc. LDL, UTIs, ketoacidosis, renal insufficiency
canagliflozin: increased risk of hyperkalemia, fractures and decreased bone mineral density
dapagliflozin: increased risk of bladder cancer
SGLT-2 inh. SEs
genital mycotic infections, serious UTIs, hypoglycemia, increased urination, hypotension, thirst
SGLT-2 inh. cause weight _____
loss
SGLT-2 inh. monitoring (5)
renal function, BG, A1c, LDL, BP
SGLT-2 inh. decrease A1c by ____%
0.7-1
SGLT-2 inh. are pregnancy category ___
C
_____ glucose tests are not recommended in patients taking SGLT-2 inh.
Urine
SGLT-2 inh. DDI: with insulin or insulin secretagogue (outcome, management)
risk of hypoglycemia, consider reducing their dose and monitor BG closely after initiation of therapy
SGLT-2 inh. DDI: with UGT inducers like rifampin (outcome, management)
decreases level of canagliflozin, consider 300 mg
SGLT-2 inh. DDI: digoxin with canagliflozin (outcome, management)
increases AUC of digoxin, monitor levels
SGLT-2 inh. DDI: diuretics (outcome)
worsen volume depletion, increasing risk of hypotension
SGLT-2 inh. DDI: canagliflozin and ACEi, ARBs.. (outcome, management)
canagliflozin and other K+ retaining/sparing drugs increase risk for hyperkalemia, monitor K+ closely