Property Name |
Property Value |
Unit |
Raw Value |
Raw Unit |
Annotation |
Factor |
Reference |
Absorption |
90.0 |
% |
>90 |
% |
PO, oral; |
|
DRUGBANK |
AUC |
1037.0 |
ng.h/ml |
1037.0 |
ng.h/ml |
PO, oral; Optical rotation R; |
|
DRUGBANK |
AUC |
195.0 |
ng.h/ml |
195.0 |
ng.h/ml |
PO, oral; Optical rotation S; |
|
DRUGBANK |
Bioavailability |
25.0 |
% |
20-30 |
% |
PO, oral; |
|
DRUGBANK |
Bioavailability |
22.0 |
% |
22±8 |
% |
PO, oral; |
|
The Pharmacological Basis of Therapeutics |
Bioavailability |
35.0 |
% |
35±13 |
% |
sublingual; |
|
The Pharmacological Basis of Therapeutics |
C Max |
262.5 |
ng/ml |
125-400 |
ng/ml |
PO, oral; immediate release formulation; |
|
DRUGBANK |
C Max |
77.8 |
ng/ml |
77.8 |
ng/ml |
PO, oral; Optical rotation R; |
|
DRUGBANK |
C Max |
16.8 |
ng/ml |
16.8 |
ng/ml |
PO, oral; Optical rotation S; |
|
DRUGBANK |
C Max |
272.0 |
ng/ml |
272.0 |
ng/ml |
Tablet, PO, oral; immediate release formulation; adults; normal,healthy; |
|
The Pharmacological Basis of Therapeutics |
C Max |
141.5 |
ng/ml |
118-165 |
ng/ml |
Tablet, PO, oral; extended release formulation; adults; normal,healthy; |
|
The Pharmacological Basis of Therapeutics |
T Max |
1.5 |
h |
1-2 |
h |
PO, oral; immediate release formulation; |
|
DRUGBANK |
T Max |
8.5 |
h |
6-11 |
h |
PO, oral; extended release formulation; |
|
DRUGBANK |
T Max |
1.1 |
h |
1.1 |
h |
Tablet, PO, oral; immediate release formulation; adults; normal,healthy; |
|
The Pharmacological Basis of Therapeutics |
T Max |
6.7 |
h |
5.6-7.7 |
h |
Tablet, PO, oral; extended release formulation; adults; normal,healthy; |
|
The Pharmacological Basis of Therapeutics |
Metabolic |
80.0 |
% |
80 |
% |
Liver metabolism; |
|
DRUGBANK |
Clearance |
20.4 |
L/h |
~340 |
ml/min |
Total clearance; Oral multiple dose; |
|
DRUGBANK |
Clearance |
39.8 |
L/h |
~664 |
ml/min |
Total clearance; Oral multiple dose; |
|
DRUGBANK |
Clearance |
60.4 |
L/h |
~1007 |
ml/min |
Total clearance; Oral single dose; |
|
DRUGBANK |
Clearance |
328.9 |
L/h |
~5481 |
ml/min |
Total clearance; Oral single dose; |
|
DRUGBANK |
Clearance |
39.1 |
L/h |
~651 |
ml/min |
Total clearance; Oral multiple dose; |
|
DRUGBANK |
Clearance |
171.3 |
L/h |
~2855 |
ml/min |
Total clearance; Oral multiple dose; |
|
DRUGBANK |
Clearance |
0.90 |
L/h/kg |
15±6 |
ml/min/kg |
hydrolysis; hydrolysis; |
Children → ;Elderly ↑ ;Hepatic cirrhosis, cirr ↑ ;Obesity ↑ ;RD, renal impairment, Renal disease,including uremia → ;Attenuated Total Reflectance ↑ ;Attenuated Total Reflectance → ; |
The Pharmacological Basis of Therapeutics |
Clearance |
1.1 |
L/h/kg |
18 |
ml/min/kg |
intravenous injection, IV; human, homo sapiens; |
|
Human Intravenous Pharmacokinetic Dataset |
Volume of Distribution |
300.0 |
L |
~300 |
L |
|
|
DRUGBANK |
Volume of Distribution |
500.0 |
L |
500.0 |
L |
|
|
DRUGBANK |
Volume of Distribution |
5.0 |
L/kg |
5.0±2.1 |
L/kg |
|
Elderly → ;Hepatic cirrhosis, cirr ↑ ;RD, renal impairment, Renal disease,including uremia → ;Obesity → ; |
The Pharmacological Basis of Therapeutics |
Volume of Distribution |
3.7 |
L/kg |
3.7 |
L/kg |
intravenous injection, IV; human, homo sapiens; |
|
Human Intravenous Pharmacokinetic Dataset |
Half-life |
5.1 |
h |
2.8-7.4 |
h |
elimination half-life; immediate release formulation; Single dose; |
|
DRUGBANK |
Half-life |
8.3 |
h |
4.5-12.0 |
h |
Multiple dose; |
|
DRUGBANK |
Half-life |
15.0 |
h |
14-16 |
h |
elimination half-life; hepatic insufficiency; |
|
DRUGBANK |
Half-life |
20.0 |
h |
~20 |
h |
Elderly; |
|
DRUGBANK |
Half-life |
0.0667 |
h |
~4 |
min |
rapid distribution half-life; intravenous injection, IV; |
|
DRUGBANK |
Half-life |
3.5 |
h |
2-5 |
h |
elimination half-life; |
|
DRUGBANK |
Half-life |
4.0 |
h |
4.0±1.5 |
h |
|
Children → ;Hepatic cirrhosis, cirr ↑ ;Obesity ↑ ;atrial fibrillation ↑ ;RD, renal impairment, Renal disease,including uremia → ;Age ↑ ; |
The Pharmacological Basis of Therapeutics |
Half-life |
2.8 |
h |
2.8 |
h |
intravenous injection, IV; human, homo sapiens; |
|
Human Intravenous Pharmacokinetic Dataset |
Toxicity LD50 |
150.0 |
mg/kg |
150.0 |
mg/kg |
PO, oral; Rattus, Rat; |
|
DRUGBANK |
Toxicity LD50 |
163.0 |
mg/kg |
163.0 |
mg/kg |
PO, oral; mouse; |
|
DRUGBANK |
Toxicity LD50 |
8.0 |
mg/kg |
8.0 |
mg/kg |
intravenous injection, IV; mouse; |
|
T3DB |
Toxicity TDLo |
14.4 |
mg/kg |
14.4 |
mg/kg |
PO, oral; Female, women; |
|
DRUGBANK |
Toxicity TDLo |
3.4 |
mg/kg |
3.429 |
mg/kg |
PO, oral; Male, men; |
|
DRUGBANK |
Eliminate Route |
3.5 |
% |
~3-4 |
% |
Urinary excretion; Unchanged drug; |
|
DRUGBANK |
Eliminate Route |
3.0 |
% |
<3 |
% |
Urinary excretion; Unchanged drug; |
|
The Pharmacological Basis of Therapeutics |
Protein Binding |
94.0 |
% |
94 |
% |
Optical rotation R; |
|
DRUGBANK |
Protein Binding |
88.0 |
% |
88 |
% |
Optical rotation S; |
|
DRUGBANK |
Protein Binding |
92.0 |
% |
92 |
% |
Optical rotation R; |
|
DRUGBANK |
Protein Binding |
86.0 |
% |
86 |
% |
Optical rotation S; |
|
DRUGBANK |
Protein Binding |
90.0 |
% |
90±2 |
% |
|
Elderly → ;Hepatic cirrhosis, cirr ↑ ;RD, renal impairment, Renal disease,including uremia → ;atrial fibrillation → ; |
The Pharmacological Basis of Therapeutics |