1.0
|
3.5 mg h/l
|
|
Imatinib
|
8–14 l/h
|
0.72–1.26 l/h
|
0.05–0.13
|
400
|
0.98
|
36 mg h/l
|
|
Mesna/dimesna
|
1.23 l/h/kg
|
0.41 l/h/kg
|
0.33
|
5,000
|
0.89
|
3,618 mg h/l/kg
|
|
Cardiovascular
|
Procainamide
|
705
|
391
|
0.3–0.6
|
500
|
1.0
|
709 μg min/ml
|
|
Amiodarone
|
87.5
|
0
|
<1%
|
400
|
0.5
|
2.3 mg min/ml
|
|
Quinidine
|
2.8
|
0.7
|
0.05–0.20
|
200
|
0.7
|
50 mg min/ml
|
|
Depression
|
Imipramine
|
1 l/h/kg
|
0.001 l/h/kg
|
0.001
|
100 mg
|
0.95
|
95 mg h/l/kg
|
|
Diabetes
|
Metformin
|
542–642
|
542–642
|
1
|
850
|
0.55
|
779 μg min/ml
|
|
Hypertension
|
Captopril
|
0.8 l/h/kg
|
0.4 l/kg/h
|
0.95
|
25
|
0.75
|
23.4 mg h/l/kg
|
|
Diltiazem
|
11.8 ml/min/kg
|
4.13 ml/min/kg
|
0.35
|
120
|
0.95
|
9.7 mg min/ml/kg
|
|
Verapamil
|
10.4–12.4 ml/h/kg
|
7.3–8.7 ml/h/kg
|
0.70
|
120
|
0.20–0.35
|
2.9 mg h/l/kg
|
|
Clonidine
|
180–390
|
133
|
0.40–0.60
|
0.1
|
0.90
|
0.3 μg min/ml
|
|
Atenolol
|
100–176
|
95–168
|
0.40–0.50
|
50
|
0.50
|
17.8 μg min/ml
|
|
Nadolol
|
2.78–3.22 ml/min/kg
|
0.9–1.92 ml/min/kg
|
0.25
|
40
|
0.30
|
4.0 mg min/ml/kg
|
|
Leg cramps
|
Quinine
|
0.17 l/h/kg
|
0.034 l/h/kg
|
0.20
|
650
|
0.76–0.88
|
3,058 mg h/l/kg
|
|
Reflux disease
|
Cimetidine
|
30–48 l/h
|
13.8–30 l/h
|
0.48
|
400
|
0.73
|
7.3 mg h/l
|
a Units reported other than ml/min are delineated.
b Units reported other than mg are delineated.
TABLE 3.4 MATE1 and MATE2‐K inhibitors identified in human studies
|
Indication
|
Druga
|
Dose
|
|
Asthma
|
Zafirlukast
|
20 mg
|
|
Cancer
|
Imatinib
|
400 mg
|
|
Cardiovascular
|
Ranolazine
|
1,000 mg
|
|
Emesis
|
Ondansetron
|
8 mg
|
|
Infections
|
Pyrimethamine
|
50 mg
|
|
Trimethoprim
|
200 mg
|
|
Dolutegravir
|
50 mg
|
|
Isavuconazole
|
200 mg
|
|
Levofloxacin
|
750 mg
|
|
Ciprofloxacin
|
500 mg
|
|
Cetirizine
|
10 mg
|
|
Cephalexin
|
500 mg
|
|
Cephradine
|
500 mg
|
|
Cobicistat
|
150 mg
|
|
Indinavir
|
800 mg
|
|
Ritonavir
|
100 mg
|
|
Reflux disease
|
Cimetidine
|
400 mg
|
|
Ranitidine
|
300 mg
|
|
Famotidine
|
200 mg
|
