Table 1.
Corticosteroid physicochemical, pharmacokinetic and pharmacological characteristics
| Corticosteroid/dose form | Relative glucocorticoid receptor binding affinity | Lipophilicity (log P) | Aqueous solubility (µg ml–1) | PPB (%) | Vss l | CL l h–1 | F (%) | Sources |
|---|---|---|---|---|---|---|---|---|
| Fluticasone furoate DPI | 2989 | 4.17 | 0.03 | 99.7 | 608 | 65 | 15DPI 1oral | [7, 21, 23, 33, 35] |
| Mometasone furoate DPI | 2100 | 4.73 | <0.1 | 99.5 | 332 | 54 | 11DPI 1oral | [7, 21, 23, 31, 32, 39–42] |
| Fluticasone propionate DPI | 1775 | 3.89 | 0.14 | 99.3 | 318 | 69 | 16DPI 1oral | [7, 21, 23, 31, 32, 43–45, 40, 46, 47, 42] |
| Beclomethasone dipropionate (BMP) MDI | 53 (1345) | 4.59 (3.27) | 0.13 (15.5) | 95.9 | 424 | 120 | 62CFC 82HFA 41oral | [7, 21, 22, 43, 39] |
| Ciclesonide (des-CIC) MDI | 12 (1200) | 3.2 (3.0) | <0.1 (7) | 98.7 | 396 | 228 | 63HFA 1oral | [7, 21, 23, 39, 44, 42] |
| Budesonide DPI | 935 | 2.32 | 16 | 91.4 | 180 | 84 | 39DPI 11oral | [7, 21, 23, 43, 39, 45, 46, 48, 49, 42] |
| Triamcinolone acetonide MDI | 233 | 1.85 | 21 | 73.2 | 103 | 37 | 25CFC 23oral | [7, 21, 22, 43, 39, 45, 50, 51, 42] |
| Flunisolide MDI | 190 | 1.36 | 140 | 61.2 | 96 | 58 | 33CFC 70HFA 20oral | [7, 21, 23, 43, 39, 45] |
| Prednisolone oral | 12 | 1.65 | 223 | 57.6 | 93 | 37 | 82oral | [7, 21, 23, 45, 52, 42] |
For beclomethasone dipropionate (BDP) and ciclesonide (CIC), values in parenthesis are for the active metabolites – beclomethasone 17-monopropionate (BMP) and desisobutyryl ciclesonide (des-CIC). Glucocorticoid receptor binding affinity is relative to dexamethasone where dexamethasone affinity = 100. Log P values are defined as the log10 of the octanol/water partition coefficient. CFC, chlorofluorocarbon propellant MDI; CL, plasma clearance; DPI, dry-powder inhaler; F, absolute bioavailability determined in healthy subjects; HFA, hydrofluoroalkane propellant MDI; MDI; metered-dose inhaler; PPB, plasma protein binding; Vss, volume of distribution at steady state.