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Table 3 Metabolic parameters of some drugs generated from Vmax and Km using modified Michaelis-Menten equations

From: Application of modified Michaelis – Menten equations for determination of enzyme inducing and inhibiting drugs

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]

  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