NSAID Pharmacokinetics

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Current revision (16:39, 11 December 2010) (edit) (undo)
 
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Line 15: Line 15:
! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! Mefenamic Acid (Ponstel)
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
Line 23: Line 23:
! 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)
! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! 22
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
Line 43: Line 43:
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
! 340
! 340
-
! 614)
+
! 705
! Sulindac (Clinoril)
! Sulindac (Clinoril)
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
Line 66: Line 66:
! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! 90
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
Line 83: Line 83:
! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! 90
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
Line 92: Line 92:
! 18.7
! 18.7
! 4.77
! 4.77
-
! Acetylsalicylic Acid (Aspirin)
+
! .25
-
! Valdecoxib (Bextra)
+
! 8-11
! 11.2
! 11.2
-
! Sulindac (Clinoril)
+
! 7.8
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
! Piroxicam (Feldene)
! Piroxicam (Feldene)
! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! 2-4
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
Line 122: Line 122:
! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-1 (nM)
+
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-1 (nM) in Whole Blood
-
! 18
+
! Ibuprofen (Advil)
-
! 11
+
! Naproxen (Aleve)
-
! Flurbiprofen (Ansaid)
+
! 440
-
! 342
+
! 4400
-
! Valdecoxib (Bextra)
+
! 25400
-
! Celecoxib (Celebrex)
+
! 140
-
! Sulindac (Clinoril)
+
! 1900
-
! Oxaprozin (Daypro)
+
! 15000
-
! Piroxicam (Feldene)
+
! 2900
-
! Nabumetone (Relafen)
+
! 278000
-
! Acetaminophen (Paracetamol)
+
! 42000
-
! Mefanamic Acid (Ponstel)
+
! 1900
-
! Ketorolac (Toradol)
+
! 110
-
! Rofecoxib (Vioxx)
+
! 63000
-
! Diclofenac (Voltaren)
+
! 140
|-
|-
-
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-2 (nM)
+
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-2 (nM) in Whole Blood
-
! 1030
+
! Ibuprofen (Advil)
-
! 1015
+
! Naproxen (Aleve)
-
! Flurbiprofen (Ansaid)
+
! 6420
-
! >5000
+
! 13900
-
! Valdecoxib (Bextra)
+
! 329
-
! Celecoxib (Celebrex)
+
! 50
-
! Sulindac (Clinoril)
+
! 55000
-
! Oxaprozin (Daypro)
+
! 37000
-
! Piroxicam (Feldene)
+
! 930
-
! Nabumetone (Relafen)
+
! 187000
-
! Acetaminophen (Paracetamol)
+
! 11000
-
! Mefanamic Acid (Ponstel)
+
! 160
-
! Ketorolac (Toradol)
+
! 60
-
! Rofecoxib (Vioxx)
+
! 840
-
! Diclofenac (Voltaren)
+
! 50
|-
|-
! [[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
-
! Sulindac (Clinoril)
+
! 4.1
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
! Piroxicam (Feldene)
! Piroxicam (Feldene)
! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! 21.23
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
Line 180: Line 180:
! 20
! 20
! 200
! 200
-
! Sulindac (Clinoril)
+
! 200
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
! Piroxicam (Feldene)
! Piroxicam (Feldene)
! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! 500
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
Line 202: Line 202:
! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! Hepatic (CYP2C9)
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|}
|}
-
For references, see: [[Treatments:NSAID References|References]]
+
For references for NSAID Pharmacokinetics, see: [[Treatments:NSAID References|References]]

Current revision

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) Mefenamic 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) 22 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) 90 Ketorolac (Toradol) Rofecoxib (Vioxx) Diclofenac (Voltaren)
Protein Binding (%) 99 99 99 99 98 97 Sulindac (Clinoril) Oxaprozin (Daypro) Piroxicam (Feldene) Nabumetone (Relafen) Acetaminophen (Paracetamol) 90 Ketorolac (Toradol) Rofecoxib (Vioxx) Diclofenac (Voltaren)
T1/2 (hr) 2.4 18.7 4.77 .25 8-11 11.2 7.8 Oxaprozin (Daypro) Piroxicam (Feldene) Nabumetone (Relafen) Acetaminophen (Paracetamol) 2-4 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) in Whole Blood Ibuprofen (Advil) Naproxen (Aleve) 440 4400 25400 140 1900 15000 2900 278000 42000 1900 110 63000 140
IC50 COX-2 (nM) in Whole Blood Ibuprofen (Advil) Naproxen (Aleve) 6420 13900 329 50 55000 37000 930 187000 11000 160 60 840 50
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) 21.23 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) 500 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) Hepatic (CYP2C9) Ketorolac (Toradol) Rofecoxib (Vioxx) Diclofenac (Voltaren)

For references for NSAID Pharmacokinetics, see: References

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David Canner

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