Ref. | Glucocorticoid | Administration protocol | MF | Results in urine samples | ||||||
Reference | GC | Route | Dose, administration | Volunteers | Marker | Cmean±sd (ng/ml) | Cmax (ng/ml) | Detection time | ||
Budesonide (BUD) | ||||||||||
2 | Matabosch et al 2 | BUD | Inhaled | 400 ug × 3 days | 8 M | F+G | 6β-OHBUD | 3.0±2.1 | 10.6 | none |
3 | Coll et al 3 | BUD | Inhaled | 800 ug × 3 days | 4 M + 4 F | F+G | 6β-OHBUD | 5.8±6.5 | 35.4 | none |
3 | Coll et al 3 | BUD | Inhaled | 1600 ug × 3 days | 4 M | F+G | 6β-OHBUD | 9.0±8.7 | 31.0 | none |
3 | Coll et al 3 | BUD | Intranasal | 256 ug × 3 days | 4 M + 4 F | F+G | 6β-OHBUD | 1.3±1.9 | 7.1 | none |
2.3 | Matabosch et al; Coll et al 2 3 | BUD | Oral | 3 mg | 10 M + 8 F | F+G | 6β-OHBUD | 24 hours | ||
4 | Athanasiadou et al 4 | BUD | Oral | 9 mg (different hydration protocols) | 7 M × 3 | F+G | 6β-OHBUD | 48 hours | ||
Triamcinolone acetonide (TA) and hexacetonide (THA) | ||||||||||
5.6 | Matabosch et al; Coll et al 5 6 | TA | Intranasal | 220 ug × 3 days | 8 M + 6 F | F+G | TA | 0.8±0.9 | 3.6 | none |
11 | Avois et al | TA | Intranasal | 220 ug | 5 | F+G | TA | na* | 7.0 | none |
11 | Avois et al | TA | Intranasal | 220 ug × 5 days | 6 | F+G | TA | na | 7.0 | none |
5 | Matabosch et al 5 | TA | Dermatological | 10 mg × 5 days | 8 M | F+G | TA | 0.4±0.4 | 1.8 | none |
12 | Wicka et al 12 | TA | Dermatological | 4.4 mg once a day × 3 days + 4.4 mg twice a day × 3 days | 4 M | F+G | TA | na | 0.8 | none |
5 | Matabosch et al 5 | TA | Intramuscular | 20 mg | 10 M | F+G | TA | 8 days | ||
6 | Coll et al 6 | TA | Intramuscular | 40 mg | 4 M + 4 F | F+G | TA | 11 days | ||
6 | Coll et al 6 | TA | Intramuscular | 80 mg | 4 M | F+G | TA | 23 days ** | ||
11 | Avois et al | TA | Intramuscular | 80 mg | 6 | F+G | TA | 28 days *** | ||
7 | Coll et al 6 | THA | Intra-articular | 40 mg | 4 M + 4 F | F+G | TA | 8 days | ||
13 | Ventura et al13 | TA | Intra-articular | 40–80 mg | 1 M + 3 F | F+G | TA | 3 days | ||
1.11 | Avois and Saugy; Avois et al | TA | Intra-articular | 40 mg | 6 | F+G | TA | 4 days | ||
13 | Ventura et al 13 | TA | Periarticular | 40–80 mg | 4 F | F+G | TA | 8 days | ||
Triamcinolone (T) | ||||||||||
18 | Chen et al 18 | T | Oral | 4 mg | 4 M+8 F | F+G | T | >24 hours | ||
1 | Avois and Saugy | T | Oral | 16 mg | 6 | F+G | T | 48 hours | ||
1 | Avois and Saugy | T | Oral | 16+16, 16+8, 16+0, 8+0, 8+0 (mg) | 6 | F+G | T | 48 hours **** | ||
Betamethasone (BET) | ||||||||||
14 | Bakkene et al 14 | BET | Dermatological | 3 mg | 8 | F | BET | na | 1.3 | none |
15 | Coll et al 15 | BET | Dermatological | 10 mg once a day × 5 days | 6 M | F+G | BET | 1.0±1.4 | 6.6 | none |
15 | Coll et al 15 | BET | Intranasal | 320 ug × 3 days | 4 M+4 F | F+G | BET | 11.6±6.7 | 32.0 | none |
15 | Coll et al 15 | BET | Oral | 0.5 mg | 8 M | F+G | BET | 36 hours | ||
1 | Avois and Saugy | BET | Oral | 2 mg | 6 | F+G | BET | 40 hours | ||
1 | Avois and Saugy | BET | Oral | 2+2+2, 2+2+1, 2+2+0, 2+0+0, 1+0+0 (mg) | 5 | F+G | BET | 48 hours **** | ||
14 | Bakkene et al 14 | BET | Intramuscular | 5.7 mg | 8 | F | BET | 48 hours | ||
15 | Coll et al 15 | BET | Intramuscular | 6 mg | 6 M | F+G | BET | 72 hours | ||
1 | Avois and Saugy | BET | Intramuscular | 7 mg | 6 | F+G | BET | 50 hours | ||
15 | Coll et al 15 | BET | Intramuscular | 12 mg | 4 M+4F | F+G | BET | 96 hours | ||
13 | Ventura et al 13 | BET | Intra-articular | 3–12 mg | 10 F | F+G | BET | 48 hours | ||
1 | Avois and Saugy | BET | Intra-articular | 7 mg | 3 | F+G | BET | 45 hours | ||
13 | Ventura et al 13 | BET | Periarticular | 6–12 mg | 3 M+11 F | F+G | BET | 72 hours | ||
Dexamethasone (DEX) | ||||||||||
1 | Avois and Saugy | DEX | Intramuscular | 7 mg | 6 | F+G | DEX | 57 hours | ||
Prednisolone (PRED) and prednisone (PSONE) | ||||||||||
8 | Mazzarino et al 8 | PRED | Intranasal | 2 mg (two sprays three times a day) | 1 M+1 F | F+G | PRED, PSONE | na | 40, 120 | none, none |
14 | Bakkene et al 14 | PRED | Intraocular | 0.9 mg | 8 | F | PRED ***** | na | 19, na | none, na |
8 | Mazzarino et al 8 | PRED | Intraocular | 1 mg (four drops twice per day) | 1 M+1 F | F+G | PRED, PSONE | na | 50, 45 | none, none |
17 | Coll et al 17 | PRED | Dermatological | 5 mg × 5 days | 6 M | F+G | PRED, PSONE | 3.5±3.5; 3.7±3.9 | 12,1; 18, 0 | none, none |
8 | Mazzarino et al 8 | PSONE | Oral | 1 mg | 2 F | F+G | PRED, PSONE | 12 hours, 12 hours | ||
8 | Mazzarino et al 8 | PRED | Oral | 5 mg | 2 M | F+G | PRED, PSONE | 24 hours, 12 hours | ||
17 | Coll et al 17 | PRED | Oral | 5 mg | 6 M | F+G | PRED, PSONE | 8 hours, 8 hours | ||
8 | Mazzarino et al 8 | PSONE | Oral | 5 mg | 2 M | F+G | PRED, PSONE | 24 hours, 12 hours | ||
17 | Coll et al 17 | PSONE | Oral | 5 mg | 2 M | F+G | PRED, PSONE | 8 hours, 8 hours | ||
14 | Bakkene et al 14 | PRED | Oral | 10 mg | 8 | F | PRED ***** | 24 hours, na | ||
17 | Coll et al 17 | PRED | Oral | 10 mg | 2 M | F+G | PRED, PSONE | 24 hours, 24 hours | ||
9 | Ahí et al 9 | PRED | Oral | 20 mg | 1 M | F+G | PRED, PSONE | 9 hours, none | ||
17 | Coll et al 17 | PSONE | Oral | 30 mg | 2 M | F+G | PRED, PSONE | 8 hours, 24 hours | ||
9 | Ahí et al 9 | PRED | Oral | 40 mg | 1 M | F+G | PRED, PSONE | 14 hours, 20 hours | ||
1 | Avois and Saugy1 | PRED | Intramuscular | 25 mg | 6 | F+G | PRED, PSONE | 10 days, 7 days | ||
Methylprednisolone (MP) | ||||||||||
10 | Matabosch et al 10 | MP | Dermatological | 10 mg × 5 days | 2 M | F+G | MP | 0.5±0.3 | 2.0 | none |
10 | Matabosch et al 10 | MP | Oral | 4 mg | 2 M | F+G | MP | 12 hours | ||
16 | Simoes et al | MP | Oral | 4 mg | 1 M | F+G | MP | 10 hours | ||
10 | Matabosch et al 10 | MP | Oral | 40 mg | 2 M | F+G | MP | 24 hours | ||
1 | Avois and Saugy | MP | Intra-articular | 80 mg | 4 | F+G | MP | 48 hours |
*, data not available.
**, last sample collected at 23 days.
***, concentrations between 10 and 15 ng/ml up to 56 days.
****, after the last dose.
*****, only concentrations of PRED reported.
F, female; F, free fraction; G, glucurono conjugated fraction; GC, glucocorticoid; M, male; MF, metabolic fraction; 6β-OHBUD, 6β-hydroxy-budesonide.