The elimination half-life, bioavailability, protein binding, the blood concentration Cmax at time tmax, and other pharmacokinetic parameters of various medications of this class are present in table 2. These medications are excreted in the urine as inactive metabolites. + TABLE 2: PHARMACOKINETIC PARAMETERS OF VARIOUS<unk> S Name of drug Bioavailability Protein binding tmax (hours) t1/2 (hours) Cmax<unk>  selectivity over<unk>  Canagliflozin 65% (300 mg dose) 99% 1–2 10.6 (100 mg dose); 13.1 (300 mg dose) 1096 ng/mL (100 mg dose); 3480 ng/mL (300 mg dose) 250 fold Dapagliflozin 78% 91% 1–1.5 12.9 79.6 ng/mL (5 mg dose); 165.0 ng/mL (10 mg dose) 1200 fold Empagliflozin 90–97% (mice); 89% (dogs); 31% (rats) 86.20% 1.5 13.2 (10 mg dose); 13.3h (25 mg dose) 259nmol/L (10 mg dose); 687nmol/L (25 mg dose) 2500 fold Ertugliflozin 70-90% 95% 0.5-1.5 11-17 268 ng/mL (15 mg dose) 2000 fold Ipragliflozin (50 mg) 90% 96.30% 1 15–16 (50 mg dose) 975 ng/mL 360 fold Luseogliflozin 35.3% (male rats); 58.2% (female rats); 92.7% (male dogs) 96.0–96.3% 0.625±0.354 9.24±0.928 119±27.0 ng/mL 1650 fold Tofogliflozin (10 mg) 97.50% 83% 0.75 6.8 489 ng/mL 2900 fold *Cmax: Maximum serum concentration that drug achieves in body after the drug has been and administrated *tmax: Time to achieve maximum plasma concentration *t1/2: Biological half-life In studies that were made on healthy people and people with type II diabetes mellitus, who were given dapagliflozin in either single ascending dose (SAD) or multiple ascending dose (MAD) showed results that confirmed a pharmacokinetic profile of the medication. With dose-dependent concentrations the half-life is about 12–13 hours, Tmax 1–2 hours and it is protein-bound, so the medication has a rapid absorption and minimal excretion by the kidney. Dapagliflozin disposition is not evidently affected by BMI or body weight, therefore the pharmacokinetic findings are expected to be applicable to patients with a higher BMI. Dapagliflozin resulted in dose-dependent increases excretions in urinary glucose, up to 47g/d following single-dose administration, which can be expected from its mechanism of action, dapagliflozin. In some long term clinical studies that have been made on dapagliflozin, dapagliflozin was associated with a decrease in body weight which was statistically superior compared to placebo or other active comparators. It is primarily associated with caloric rather than fluid loss. In contrast with other anti-hyperglycemic diabetes medications,<unk> s enhance, rather than suppress, gluconeogenesis and ketogenesis. Because<unk> s activate sirtuin 1 (and thus PGC-1α and FGF21), they are more cardioprotective than the other medications used to treat diabetes.
SGLT2 inhibitor
Chloride channel opener
COX-2 inhibitor
CYP17A1 inhibitor
Norepinephrine–dopamine disinhibitor
Beta-adrenergic agonist
Reuptake inhibitor
Protein kinase inhibitor