NSAID Pharmacokinetics

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! 1.3
! 1.3
! .92
! .92
-
! 2.29
+
! 2.3
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! 2.94
+
! 2.9
! 2.8
! 2.8
-
! Sulindac (Clinoril)
+
! 3.4
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
! Piroxicam (Feldene)
! Piroxicam (Feldene)
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! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
! 340
! 340
-
! 614)
+
! 705
! Sulindac (Clinoril)
! Sulindac (Clinoril)
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
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! Valdecoxib (Bextra)
! Valdecoxib (Bextra)
! 11.2
! 11.2
-
! Sulindac (Clinoril)
+
! 7.8
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
! Piroxicam (Feldene)
! Piroxicam (Feldene)
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! Valdecoxib (Bextra)
! Valdecoxib (Bextra)
! 27.7
! 27.7
-
! Sulindac (Clinoril)
+
! 4.1
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
! Piroxicam (Feldene)
! Piroxicam (Feldene)
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! 20
! 20
! 200
! 200
-
! Sulindac (Clinoril)
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! 200
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
! Piroxicam (Feldene)
! Piroxicam (Feldene)

Revision as of 19:41, 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 2.3 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) Valdecoxib (Bextra) 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) 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 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

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