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NSAID Pharmacokinetics
From Proteopedia
(Difference between revisions)
| Line 57: | Line 57: | ||
! 49-73 | ! 49-73 | ||
! 95 | ! 95 | ||
| - | ! | + | ! 96 |
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| - | ! | + | ! 83 |
! Celecoxib (Celebrex) | ! Celecoxib (Celebrex) | ||
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
| Line 74: | Line 74: | ||
! 99 | ! 99 | ||
! 99 | ! 99 | ||
| - | ! | + | ! 99 |
| - | ! | + | ! 99 |
| - | ! | + | ! 98 |
! Celecoxib (Celebrex) | ! Celecoxib (Celebrex) | ||
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
| Line 192: | Line 192: | ||
! Metabolism | ! Metabolism | ||
! Hepatic (CYP2C9) | ! Hepatic (CYP2C9) | ||
| - | ! Naproxen | + | ! Naproxen |
| - | ! | + | ! Hepatic (CYP2C9) |
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| - | ! | + | ! Hepatic (CYP3A4 & CYP2C9) |
! Celecoxib (Celebrex) | ! Celecoxib (Celebrex) | ||
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
Revision as of 19:19, 9 December 2010
| 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 | 2.29 | Acetylsalicylic Acid (Aspirin) | 2.94 | Celecoxib (Celebrex) | Sulindac (Clinoril) | 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 | Celecoxib (Celebrex) | Sulindac (Clinoril) | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| Bioavailability (%) | 49-73 | 95 | 96 | Acetylsalicylic Acid (Aspirin) | 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 | Celecoxib (Celebrex) | 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) | Valdecoxib (Bextra) | Celecoxib (Celebrex) | Sulindac (Clinoril) | 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 | Celecoxib (Celebrex) | Sulindac (Clinoril) | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| IC50 COX-1 (nM) | 18 | 11 | Flurbiprofen (Ansaid) | 342 | Valdecoxib (Bextra) | Celecoxib (Celebrex) | Sulindac (Clinoril) | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| IC50 COX-2 (nM) | 1030 | 1015 | Flurbiprofen (Ansaid) | >5000 | Valdecoxib (Bextra) | Celecoxib (Celebrex) | Sulindac (Clinoril) | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| Clearance (L/h) | 3.4 | 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) |
| Dosage (mg) | 400 | 200 | 150 | Acetylsalicylic Acid (Aspirin) | 20 | Celecoxib (Celebrex) | Sulindac (Clinoril) | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| Metabolism | Hepatic (CYP2C9) | Naproxen | Hepatic (CYP2C9) | Acetylsalicylic Acid (Aspirin) | Hepatic (CYP3A4 & CYP2C9) | Celecoxib (Celebrex) | Sulindac (Clinoril) | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
For references, see: References
