|
Drug
|
Binding Site
|
Metabolites
|
Dose (mg)
|
Vmax
|
Km
|
Cs
|
R
|
CMR
|
Vo
|
Clint
|
% saturation
|
S/Km
|
Status
|
pH
|
References
|
|---|
|
Theophylline (mg)
|
Adenosine receptor/RNA
|
1, 3 – DMU
|
300
|
34.2
|
14.2
|
1.08
|
0.18
|
14.85
|
2.60
|
2.41
|
7.07
|
0.08
|
Inducer
|
Weak base
|
[25]
|
|
1 – MU
|
300
|
13.1
|
9.3
|
1.12
|
0.17
|
5.69
|
1.58
|
1.41
|
10.74
|
0.12
|
Inducer
|
Week base
|
[24]
|
|
3 - MX
|
300
|
4.9
|
2.0
|
2.0
|
2.45
|
2.13
|
4.90
|
2.45
|
50.00
|
1.00
|
Inducer
|
Weak base
|
[25]
|
|
Mibefradil (mg)
|
Globulin
|
Dealkylated
|
100
|
6.79
|
70.2
|
1.02
|
0.003
|
2.95
|
0.10
|
0.097
|
1.43
|
0.01
|
Inhibitor
|
Base
|
[57]
|
|
Voriconazole (ng)
|
Albumin/globulin
|
Hydroxylated
|
400
|
114
|
1.15
|
7.67
|
661.2
|
49.51
|
160.33
|
99.13
|
86.96
|
6.67
|
Inducer
|
Acidic
|
[6]
|
|
Metronidazole (μm)
|
Plasma protein
|
2-hydroxy
|
300
|
0.366
|
0.911
|
1.00
|
0.00
|
0.16
|
4.02
|
4.02
|
52.32
|
1.10
|
Inhibitor
|
Acidic
|
[23]
|
|
metronidazole
|
300
|
0.527
|
0.235
|
0.31
|
−2.10
|
0.23
|
0.14
|
2.24
|
56.88
|
1.32
|
Inhibitor
|
Acidic
|
[1]
|
|
Isoniazid (mg)
|
Protein
|
Isonicotinic acid
|
250
|
30.87
|
1.669
|
2.50
|
27.75
|
13.41
|
46.25
|
18.50
|
59.97
|
1.50
|
Inhibitor
|
Base
|
[35]
|
|
Puromicin(mg)
|
Ribosome
|
5′-monophosphate
|
100
|
193.9
|
0.0435
|
0.00
|
0.00
|
84.21
|
0.00
|
0.875
|
0.00
|
0.00
|
Inhibitor
|
Acidic-basic
|
[15]
|
|
Phenytoin (mg)
|
Na + receptor
|
Phenylhydantoin
|
300
|
8.25
|
9.43
|
0.049
|
0.00
|
3.58
|
0.00
|
0.043
|
0.52
|
0.01
|
Inducer
|
Base
|
[7]
|
|
R – Thiopental(mg)
|
GABAA
|
–
|
120
|
0.86
|
20.0
|
1.03
|
−0.002
|
0.37
|
0.04
|
0.042
|
4.90
|
0.05
|
Inducer
|
Base
|
[10]
|
|
Phenytoin (mg)
|
Na + receptor
|
Hydroxyphenytoin
|
300
|
28.0
|
91.0
|
1.01
|
0.23
|
12.16
|
0.31
|
0.308
|
1.10
|
0.01
|
Inducer
|
Base
|
[37]
|
|
S – Thiopental (mg)
|
GABAA
|
–
|
300
|
1.01
|
24.0
|
1.04
|
0.002
|
0.44
|
0.04
|
0.042
|
4.15
|
0.04
|
Inducer
|
Base
|
[33]
|
|
Thymidine(mg)
|
Nucleoside
|
Baminoisobutyric acid
|
–
|
2.45
|
45.5
|
1.00
|
0.00
|
1.06
|
0.053
|
0.053
|
2.15
|
0.02
|
Inducer
|
Acidic
|
[11]
|
|
Thymine(mg)
|
DNA
|
–
|
–
|
2.55
|
82.5
|
0.98
|
0.00
|
1.11
|
0.03
|
0.030
|
1.17
|
0.01
|
Inducer
|
Base
|
[12]
|
|
Fluorouracil(mg)
|
Albumin
|
Dihydrofluorouracil
|
–
|
2.16
|
39.8
|
1.02
|
0.006
|
0.94
|
0.06
|
0.054
|
2.50
|
0.03
|
Inducer
|
Base
|
[13]
|
|
Tylosin(mg)
|
Ribosome
|
Relomycin
|
110
|
0.018
|
0.37
|
0.58
|
−0.021
|
0.01
|
0.028
|
0.049
|
61.05
|
1.57
|
Inducer
|
Acid-basic
|
[1]
|
- Keys: Vmax Maximal velocity (mg/h), Km Metabolism constant (mg/L), Cs Concentration of substrate (μg; ng; μm; mg), R Rate of endogenous substrate production (h), CMR Cellular metabolic rate (/h), Vo Initial velocity (mg/h), Clint Proportionality constant between rate of metabolism and the drug substrate concentration at the enzyme site Cs, % saturation Extent of enzyme saturation; 3-MX: 3-methylxanthine; 1,3-DMU:1,3 dimethyluric acid;1-MU:1-methyluric acid
