Table 1.
Receptor selectivity and pharmacokinetics parameter of alfuzosin compared with tamsulosin and silodosin.
| Receptor selectivity | Tamsulosin | Alfuzosin | Silodosin |
|---|---|---|---|
| A1 blocker selectivity profile a,b,c | α1A = α1D > α1B | α1A = α1D = α1B | α1A > α1D > α1B |
| A1 blocker selective affinity (α1A:α1B) | 10:1 | 1:1 | 162:1 |
| Pharmacokinetics parameters | Tamsulosin | Alfuzosin | Silodosin |
| Cmax (ng/mL) | 10.1 ± 4.8 | 13.6 ± 5.6 | 27.9 ± 9.6 |
| Bioavailability (%) | 100 | 49 | 32 |
| Protein binding (%) | 94–99 | 82–90 | 97 |
| Excretion in urine (%) | 76 | 24 | 33.5 |
| Excretion in bile/feces (%) | 21 | 69 | 54.9 |
| AUC∞ (ng/h/mL) | 151–199 | 194 ± 75 | 133.7 ± 58 |
| Tmax (h) | 6.67 | 6.69 | 1.36 ± 1.12 |
| T1/2 (h) | 16.13 | 10 | 4.714 ± 3.710 |
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AUC∞, area under the plasma concentration-time curve from time zero to infinity; Cmax, maximum plasma concentration; t1/2, elimination half-life; tmax, time to reach the Cmax; uroselective receptors, α1A and α1D; vascular epithelium, α1b.