NSAID Pharmacokinetics
From Proteopedia
(Difference between revisions)
Line 26: | Line 26: | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! 2.94 | ! 2.94 | ||
- | ! | + | ! 2.8 |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
Line 43: | Line 43: | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! 340 | ! 340 | ||
- | ! | + | ! 614) |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
Line 77: | Line 77: | ||
! 99 | ! 99 | ||
! 98 | ! 98 | ||
- | ! | + | ! 97 |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
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! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! Valdecoxib (Bextra) | ! Valdecoxib (Bextra) | ||
- | ! | + | ! 11.2 |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
Line 111: | Line 111: | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! 7548 | ! 7548 | ||
- | ! | + | ! 6930 |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
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! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! Valdecoxib (Bextra) | ! Valdecoxib (Bextra) | ||
- | ! | + | ! 27.7 |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
Line 179: | Line 179: | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! 20 | ! 20 | ||
- | ! | + | ! 200 |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
Line 196: | Line 196: | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! Hepatic (CYP3A4 & CYP2C9) | ! Hepatic (CYP3A4 & CYP2C9) | ||
- | ! | + | ! Hepatic (CYP2C9) |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) |
Revision as of 19:27, 9 December 2010
Cyclooxygenase Inhibitor Pharmacokinetics | |||||||||||||||
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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 | 2.8 | 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 | 614) | 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 | 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) | Valdecoxib (Bextra) | 11.2 | 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 | 6930 | 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) | 27.7 | 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 | 200 | 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) | 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