NSAID Pharmacokinetics
From Proteopedia
| 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) | Mefanamic 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) | Mefanamic Acid (Ponstel) | 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) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| Protein Binding (%) | 99 | 99 | 99 | 99 | 98 | 97 | Sulindac (Clinoril) | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| T1/2 (hr) | 2.4 | 18.7 | 4.77 | Acetylsalicylic Acid (Aspirin) | 8-11 | 11.2 | 7.8 | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | 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) | 38000 | 32000 | Flurbiprofen (Ansaid) | ASPRIN | 150000 | 15000 | Sulindac (Clinoril) | Oxaprozin (Daypro) | 680000 | 82000 | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | >1000000 | 30 |
| IC50 COX-2 (nM) | 117000 | 235000 | Flurbiprofen (Ansaid) | ASPRIN | 5 | 40 | Sulindac (Clinoril) | Oxaprozin (Daypro) | 660000 | >1000000 | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | 500 | 10 |
| 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) | Mefanamic Acid (Ponstel) | 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) | Mefanamic Acid (Ponstel) | 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) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
For references, see: References
