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NSAID Pharmacokinetics

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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 22: Line 22:
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
! 1.3
! 1.3
-
! Naproxen (Aleve)
+
! .92
-
! Flurbiprofen (Ansaid)
+
! 2.3
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! Valdecoxib (Bextra)
+
! 2.9
-
! Celecoxib (Celebrex)
+
! 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 38: Line 38:
|-
|-
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
-
! 16.2
+
! 16200
-
! Naproxen (Aleve)
+
! 47100
-
! Flurbiprofen (Ansaid)
+
! 19670
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! Valdecoxib (Bextra)
+
! 340
-
! Celecoxib (Celebrex)
+
! 705
! Sulindac (Clinoril)
! Sulindac (Clinoril)
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
Line 55: Line 55:
|-
|-
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
-
! Ibuprofen (Advil)
+
! 49-73
-
! Naproxen (Aleve)
+
! 95
-
! Flurbiprofen (Ansaid)
+
! 96
-
! Acetylsalicylic Acid (Aspirin)
+
! 99
-
! Valdecoxib (Bextra)
+
! 83
! Celecoxib (Celebrex)
! Celecoxib (Celebrex)
! Sulindac (Clinoril)
! Sulindac (Clinoril)
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 72: Line 72:
|-
|-
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
-
! Ibuprofen (Advil)
+
! 99
-
! Naproxen (Aleve)
+
! 99
-
! Flurbiprofen (Ansaid)
+
! 99
-
! Acetylsalicylic Acid (Aspirin)
+
! 99
-
! Valdecoxib (Bextra)
+
! 98
-
! Celecoxib (Celebrex)
+
! 97
! Sulindac (Clinoril)
! Sulindac (Clinoril)
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
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 90: Line 90:
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! 2.4
! 2.4
-
! Naproxen (Aleve)
+
! 18.7
-
! Flurbiprofen (Ansaid)
+
! 4.77
-
! Acetylsalicylic Acid (Aspirin)
+
! .25
-
! Valdecoxib (Bextra)
+
! 8-11
-
! Celecoxib (Celebrex)
+
! 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 106: Line 106:
|-
|-
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
-
! 67.4
+
! 67400
-
! Naproxen (Aleve)
+
! 777400
-
! Flurbiprofen (Ansaid)
+
! 124320
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! Valdecoxib (Bextra)
+
! 7548
-
! Celecoxib (Celebrex)
+
! 6930
! Sulindac (Clinoril)
! Sulindac (Clinoril)
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
Line 122: Line 122:
! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
+
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-1 (nM) in Whole Blood
! Ibuprofen (Advil)
! Ibuprofen (Advil)
! Naproxen (Aleve)
! Naproxen (Aleve)
-
! Flurbiprofen (Ansaid)
+
! 440
-
! Acetylsalicylic Acid (Aspirin)
+
! 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) in Whole Blood
 +
! Ibuprofen (Advil)
 +
! Naproxen (Aleve)
 +
! 6420
 +
! 13900
 +
! 329
 +
! 50
 +
! 55000
 +
! 37000
 +
! 930
 +
! 187000
 +
! 11000
 +
! 160
 +
! 60
 +
! 840
 +
! 50
|-
|-
! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
Line 144: Line 161:
! Flurbiprofen (Ansaid)
! Flurbiprofen (Ansaid)
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! Valdecoxib (Bextra)
+
! 6
-
! Celecoxib (Celebrex)
+
! 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 158: Line 175:
! Dosage (mg)
! Dosage (mg)
! 400
! 400
-
! Naproxen (Aleve)
+
! 200
-
! Flurbiprofen (Ansaid)
+
! 150
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! Valdecoxib (Bextra)
+
! 20
-
! Celecoxib (Celebrex)
+
! 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 174: Line 191:
|-
|-
! Metabolism
! Metabolism
-
! Ibuprofen (Advil)
+
! Hepatic (CYP2C9)
-
! Naproxen (Aleve)
+
! Hepatic (CYP2C9)
-
! Flurbiprofen (Ansaid)
+
! Hepatic (CYP2C9)
! Acetylsalicylic Acid (Aspirin)
! Acetylsalicylic Acid (Aspirin)
-
! Valdecoxib (Bextra)
+
! Hepatic (CYP3A4 & CYP2C9)
-
! Celecoxib (Celebrex)
+
! Hepatic (CYP2C9)
! Sulindac (Clinoril)
! Sulindac (Clinoril)
! Oxaprozin (Daypro)
! Oxaprozin (Daypro)
Line 185: 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

Proteopedia Page Contributors and Editors (what is this?)

David Canner

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