| Cyclooxygenase Inhibitor Pharmacokinetics
|
| Parameter
|
Ibuprofen (Advil)
|
Naproxen (Aleve)
|
Flurbiprofen (Ansaid)
|
Acetylsalicylic Acid (Aspirin)
|
Valdecoxib (Bextra)
|
Celecoxib (Celebrex)
|
Sulindac (Clinoril)
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
Mefenamic Acid (Ponstel)
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| Tmax (hr)
|
1.3
|
.92
|
2.3
|
Acetylsalicylic Acid (Aspirin)
|
2.9
|
2.8
|
3.4
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
22
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| Cmax (ng/ml)
|
16200
|
47100
|
19670
|
Acetylsalicylic Acid (Aspirin)
|
340
|
705
|
Sulindac (Clinoril)
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
Mefanamic Acid (Ponstel)
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| Bioavailability (%)
|
49-73
|
95
|
96
|
99
|
83
|
Celecoxib (Celebrex)
|
Sulindac (Clinoril)
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
90
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| Protein Binding (%)
|
99
|
99
|
99
|
99
|
98
|
97
|
Sulindac (Clinoril)
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
90
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| T1/2 (hr)
|
2.4
|
18.7
|
4.77
|
.25
|
8-11
|
11.2
|
7.8
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
2-4
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| AUC (ng/ml/hr)
|
67400
|
777400
|
124320
|
Acetylsalicylic Acid (Aspirin)
|
7548
|
6930
|
Sulindac (Clinoril)
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
Mefanamic Acid (Ponstel)
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| IC50 COX-1 (nM) in Whole Blood
|
Ibuprofen (Advil)
|
Naproxen (Aleve)
|
440
|
4400
|
25400
|
140
|
1900
|
15000
|
2900
|
278000
|
42000
|
1900
|
110
|
63000
|
140
|
| IC50 COX-2 (nM) in Whole Blood
|
Ibuprofen (Advil)
|
Naproxen (Aleve)
|
6420
|
13900
|
329
|
50
|
55000
|
37000
|
930
|
187000
|
11000
|
160
|
60
|
840
|
50
|
| Clearance (L/h)
|
3.4
|
Naproxen (Aleve)
|
Flurbiprofen (Ansaid)
|
Acetylsalicylic Acid (Aspirin)
|
6
|
27.7
|
4.1
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
21.23
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| Dosage (mg)
|
400
|
200
|
150
|
Acetylsalicylic Acid (Aspirin)
|
20
|
200
|
200
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
500
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
| Metabolism
|
Hepatic (CYP2C9)
|
Hepatic (CYP2C9)
|
Hepatic (CYP2C9)
|
Acetylsalicylic Acid (Aspirin)
|
Hepatic (CYP3A4 & CYP2C9)
|
Hepatic (CYP2C9)
|
Sulindac (Clinoril)
|
Oxaprozin (Daypro)
|
Piroxicam (Feldene)
|
Nabumetone (Relafen)
|
Acetaminophen (Paracetamol)
|
Hepatic (CYP2C9)
|
Ketorolac (Toradol)
|
Rofecoxib (Vioxx)
|
Diclofenac (Voltaren)
|
For references for NSAID Pharmacokinetics, see: References
