Table 2.
Secondary Outcome: Dose, Substrates, Steady-State
| Classification per FDA Table of Inhibitors |
Inhibitor Name | Observed inhibitor classification, n (%) |
Doses of Inhibitor studied, n (concordance %) |
Substrates studied, n (concordance %) |
Inhibitor Steady State Status, n (concordance %) |
|---|---|---|---|---|---|
| Moderate | Cinacalcet n = 4 |
Moderate, 3 (75) Insignificant, 1 (25) |
“25 or 100 mg”, 1 (0) 50 mg, 1 (100) 90 mg, 2 (100) |
Amitriptyline, 1 (100) Desipramine, 2 (100) Dextromethorphan, 1 (0) |
SS: 3, (100) Pre-SS: 1,(0) |
| Duloxetine, n = 9 |
Moderate, 4 (44) Weak, 4 (44) Insignificant, 1 (11) |
30 mg, 1 (0) 60 mg, 5 (40) 80 mg, 1 (0) 120 mg, 2 (100) |
Desipramine, 3 (100) Dextromethorphan, 2 (50) Metoprolol, 1 (0) Tolterodine, 1 (0) Tramadol, 2 (0) |
SS: 4 (50) Pre-SS: 4(25) Unknown: 1 (100) |
|
| Fluvoxamine, n = 7 |
Strong, 1 (14) Moderate, 2 (29) Weak, 3 (43) Insignificant, 1 (14) |
50 mg, 1 (0) 50-100 mga, 2 (0) 100 mg, 3 (67) 150 mg, 1 (0) |
Amitriptyline, 1 (0) Atomoxetine, 1 (0) Desipramine, 1 (0) Dextromethorphan, 1 (0) Imipramine, 2 (100) Nebivolol, 1 (0) |
SS: 6 (33) Pre-SS: 1 (0) |
|
| Mirabegron, n = 7 |
Moderate 5 (71) Weak, 1 (14) Insignificant, 1 (14) |
50 mg, 3 (33) 100 mg, 2 (100) 160 mg, 2 (100) |
Desipramine, 2 (100) Metoprolol, 2 (100) Tolterodine, 3 (33) |
SS: 2 (100) Pre-SS: 5 (40) |
|
| Weak | Abiraterone, n = 2 |
Moderate, 1 (50) Weak, 1 (50) |
1,000 mg, 2 (50) | Dextromethorphan, 2 (50) | SS: 1 (100) Unknown: 1 (0) |
| Celecoxib, n = 3 |
Weak, 1 (33) Insignificant, 2 (67) |
100 mg, 1 (0) 200 mg, 1 (0) 400 mg, 1 (100) |
Metoprolol, 1 (100) Tramadol, 2 (0) |
SS: 2 (50) Pre-SS: 1 (0) |
|
| Cimetidineb, n = 26 |
Moderate, 2 (8) Weak, 20 (77) Insignificant, 4 (15) |
400 mg, 2 (50) 600 mg, 1 (100) 800 mg, 8 (100) 1,000 mg, 6 (67) 1,200 mg, 9 (67) |
Amitriptyline, 1 (100) Desipramine, 2 (50) Imipramine, 3 (67) Metoprolol, 6 (83) Nebivolol, 1 (100) Nortriptyline, 1 (0) Propafenone, 2 (50) Propranolol, 9 (89) Venlafaxine, 1 (100) |
SS: 23, (78) Pre-SS: 3, (67) |
|
| Clobazam, n = 2 |
Weak, 2 (100) | 40 mg, 2 (100) | Dextromethorphan, 2 (100) | SS: 1 (100) Unknown: 1 (100) |
|
| Desvenlafaxine, n = 6 |
Weak, 3 (50) Insignificant, 3 (50) |
100 mg, 4 (50) 400 mg, 2 (100) |
Desipramine, 6 (50) | SS: 4 (50) Unknown: 2 (50) |
|
| Escitalopram, n = 3 |
Moderate, 1 (33) Weak, 2 (67) |
10 mg, 1 (100) 20 mg, 2 (50) |
Desipramine, 1 (0) Metoprolol, 1 (100) Tramadol, 1 (100) |
SS: 3 (67) | |
| Ritonavir, n = 5 |
Moderate, 3 (60) Weak, 2 (40) |
200 mg, 2 (100) 400 mg, 2 (0) 1,000 mg, 1 (0) |
Desipramine, 2 (50) Dextromethorphan, 3 (33) |
SS: 4 (50) Pre-SS: 1 (0) |
|
| Sertraline, n = 10 |
Moderate, 1 (10) Weak, 6 (60) Insignificant, 3 (30) |
50 mg, 5 (80) 100 mg, 1 (100) 150 mg, 4 (25) |
Desipramine, 6 (66) Imipramine, 2 (0) Metoprolol, 2 (100) |
SS: 6 (83) Pre-SS: 4 (25) |
a,
50 mg daily for 3 days and 100 mg daily for 3 days
b,
Cimetidine is also listed as a moderate inhibitor in the FDA Table of inhibitors, we only treated it as a weak inhibitor as the overall concordance with weak inhibitor was 77%, while it was 8% if treated as a moderate inhibitor.
The bolded classification within the column “observed inhibitor classification” represents the concordance with the classifications listed in FDA Table of Inhibitors.
SS: Steady state; Pre-SS: Pre steady-state