TABLE 1.
PHARMACODYNAMIC/PHARMACOKINETIC PROPERTIES OF CURRENTLY AVAILABLE INHALED CORTICOSTEROIDS*
| Determinants of Efficacy |
Determinants of Therapeutic Index |
|||||
|---|---|---|---|---|---|---|
| ICS/Dosage | Binding Affinity† | Lung Delivery‡ (%) | Relative Equivalency (μg)§ | Oral Bioavailability (%) | Systemic Clearance (L/h) | Volumes of Distribution (L) |
| BDP MDI/40 and 80 μg | 0.4 | 50–60 | 80 | 20 | 150 | 424‖ |
| BUD DPI/90 and 180 μg nebules/250, 500, and 1,000 μg | 9.4 | 15–30 | 180 | 11 | 84 | 280 |
| 5–8 | 500 | |||||
| CIC MDI/80 or 160 μg | 0.12 | 50 | 80 | <1 | 152 | 897‖ |
| FLU/80 μg | 1.8 | 68 | 160 | 20 | 58 | 96 |
| FP MDI/44, 110, and 220 μg DPI/ 50, 100, and 250 μg | 18 | 20 | 88 | ≤1 | 66 | 602 |
| 15 | 100 | |||||
| MF/110 and 220 μg | 23 | 11 | 110 | <1 | 53 | 332 |
Definition of abbreviations: BDP = beclomethasone dipropionate; BUD = budesonide; CIC = ciclesonide; DPI = dry-powder inhaler; FLU = flunisolide; FP = fluticasone propionate; ICS = inhaled corticosteroid; MDI = metered-dose inhaler; MF = mometasone furoate.
*
Data from References 9–11.
†
Receptor binding affinities of ICSs relative to dexamethasone equal to 1.
‡
Assuming appropriate inhalation technique.
§
The relative potency is based on clinical efficacy rather than systemic activity.
‖
Distribution volumes are for the active metabolites of BDP and CIC.