TABLE 4.
Comparison of the physiochemical properties and human pharmacokinetic parameters for atenolol and metformin
| Parameters | Atenolola | Metformina |
|---|---|---|
| MW | 266 | 129 |
| Log D7.4 | −2.0 | −5.5 |
| pKa | 9.6 | 12.4 |
| F (%) | 52–63 | 40–60 |
| fu (%) | > 95 | 100 |
| Vd (l) | 95 | 63–276 |
| CL (ml/min) | 178 | 459 |
| CLR (ml/min) | 168 | 454 |
| fe (%) | > 95 | 99.9 |
| t1/2 (hours) | 6 | 8–20 |
CL, total plasma clearance; CLR, renal clearance; F, oral bioavailability; fe, fraction excreted unchanged in urine after i.v. dosing; fu, plasma unbound fraction; Log D7.4, distribution coefficient at pH 7.4; MW, molecular weight; Vd, volume of distribution; t1/2, terminal elimination half-life.
a
The human pharmacokinetic parameters were compiled from Mason et al. (1979), Goodman et al. (2011), Brown et al. (1976), Wadworth et al. (1991), Pentikäinen et al. (1979), and Scheen (1996).