| 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
