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NSAID Pharmacokinetics

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Line 93: Line 93:
! 4.77
! 4.77
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! Valdecoxib (Bextra)
+
! 8-11
! 11.2
! 11.2
! 7.8
! 7.8
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|-
|-
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-1 (nM)
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-1 (nM)
-
! 18
+
! 38000
-
! 11
+
! 32000
! Flurbiprofen (Ansaid)
! Flurbiprofen (Ansaid)
-
! 342
+
! ASPRIN
-
! Valdecoxib (Bextra)
+
! 150000
-
! Celecoxib (Celebrex)
+
! 15000
! Sulindac (Clinoril)
! Sulindac (Clinoril)
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
-
! Piroxicam (Feldene)
+
! 680000
-
! Nabumetone (Relafen)
+
! 82000
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
! Mefanamic Acid (Ponstel)
! Mefanamic Acid (Ponstel)
! Ketorolac (Toradol)
! Ketorolac (Toradol)
-
! Rofecoxib (Vioxx)
+
! >1000000
-
! Diclofenac (Voltaren)
+
! 30
|-
|-
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-2 (nM)
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-2 (nM)
-
! 1030
+
! 117000
-
! 1015
+
! 235000
! Flurbiprofen (Ansaid)
! Flurbiprofen (Ansaid)
-
! >5000
+
! ASPRIN
-
! Valdecoxib (Bextra)
+
! 5
-
! Celecoxib (Celebrex)
+
! 40
! Sulindac (Clinoril)
! Sulindac (Clinoril)
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
-
! Piroxicam (Feldene)
+
! 660000
-
! Nabumetone (Relafen)
+
! >1000000
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
! Mefanamic Acid (Ponstel)
! Mefanamic Acid (Ponstel)
! Ketorolac (Toradol)
! Ketorolac (Toradol)
-
! Rofecoxib (Vioxx)
+
! 500
-
! Diclofenac (Voltaren)
+
! 10
|-
|-
! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
Line 161: Line 161:
! Flurbiprofen (Ansaid)
! Flurbiprofen (Ansaid)
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! Valdecoxib (Bextra)
+
! 6
! 27.7
! 27.7
! 4.1
! 4.1

Revision as of 19:55, 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) 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

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David Canner

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