rifampin.
Effects of Saxagliptin on Other Drugs
Table 8: Effect of Saxagliptin on Systemic Exposures of Coadministered Drugs
Coadministered
Drug
Dosage of
Coadministered
Drug*
Dosage of
Saxagliptin*
Coadministered Drug
Change†
in AUC‡
Change†
in Cmax
Metformin 1000 mg 100 mg metformin ↑20% ↑9%
Glyburide 5 mg 10 mg glyburide ↑6% ↑16%
Pioglitazone§ 45 mg QD for 10
days
10 mg QD
for 5 days
pioglitazone
hydroxy-pioglitaz
one
↑8%
ND
↑14%
ND
Digoxin 0.25 mg q6h first
day followed by
q12h second day
followed by QD
for 5 days
10 mg QD
for 7 days
digoxin ↑6% ↑9%
Simvastatin 40 mg QD for 8
days
10 mg QD
for 4 days
simvastatin
simvastatin acid
↑4%
↑16%
↓12%
0%
Diltiazem 360 mg LA QD
for 9 days
10 mg diltiazem ↑10% ↑16%
Ketoconazole 200 mg BID for 9
days
100 mg ketoconazole ↓13% ↓16%
Ethinyl estradiol
and Norgestimate
ethinyl estradiol
0.035 mg and
norgestimate
5 mg QD for
21 days
ethinyl estradiol
norelgestromin
norgestrel
↑7%
↑10%
↑13%
↓2%
↑9%
↑17%
Table 8: Effect of Saxagliptin on Systemic Exposures of Coadministered Drugs
Coadministered
Drug
Dosage of
Coadministered
Drug*
Dosage of
Saxagliptin*
Coadministered Drug
Change†
in AUC‡
Change†
in Cmax
0.250 mg for 21
days
ND=not determined; QD=once daily; q6h=every 6 hours; q12h=every 12 hours; BID=twice daily; LA=long acting.
* Single dose unless otherwise noted.
† Percent change (with/without coadministered drug and no change=0%); ↑ and ↓ indicate the exposure increase
and decrease, respectively.
‡ AUC=AUC(INF) for drugs given as single dose and AUC=AUC(TAU) for drugs given in multiple doses.
§ Results include all subjects.
Metformin
Effects of Other Drugs on Metformin
Table 9: Effect of Coadministered Drug on Plasma Metformin Systemic Exposure
Coadministered
Drug
Dose of
Coadministered
Drug*
Dose of
Metformin*
Metformin
Change† in
AUC‡
Change† in
Cmax
Glyburide 5 mg 850 mg ↓9%§ ↓7%§
Furosemide 40 mg 850 mg ↑15%§ ↑22%§
Nifedipine 10 mg 850 mg ↑9% ↑20%
Propranolol 40 mg 850 mg ↓10% ↓6%
Ibuprofen 400 mg 850 mg ↑5%§