NSAID Pharmacokinetics

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{| class="wikitable" border="1" width="40%" style="text-align:center"
{| class="wikitable" border="1" width="40%" style="text-align:center"
|-
|-
-
! colspan="16" align="center"| Cyclooxygenase Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]]
+
! colspan="16" align="center"| Cyclooxygenase Inhibitor [[Pharmacokinetics]]
|-
|-
! Parameter
! Parameter
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)
! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
+
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
-
! Ibuprofen (Advil)
+
! 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)
! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
+
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
-
! Ibuprofen (Advil)
+
! 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)
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! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmaceutical_Drugs#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)
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! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! 90
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmaceutical_Drugs#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)
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! Nabumetone (Relafen)
! Nabumetone (Relafen)
! Acetaminophen (Paracetamol)
! Acetaminophen (Paracetamol)
-
! Mefanamic Acid (Ponstel)
+
! 90
! Ketorolac (Toradol)
! Ketorolac (Toradol)
! Rofecoxib (Vioxx)
! Rofecoxib (Vioxx)
! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
+
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
-
! Ibuprofen (Advil)
+
! 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)
! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
+
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
-
! Ibuprofen (Advil)
+
! 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)
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! Diclofenac (Voltaren)
! Diclofenac (Voltaren)
|-
|-
-
! [[Pharmaceutical_Drugs#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
|-
|-
-
! [[Pharmaceutical_Drugs#Clearance_.28Cl.29|Clearance]] (L/h)
+
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-2 (nM) in Whole Blood
! Ibuprofen (Advil)
! Ibuprofen (Advil)
 +
! Naproxen (Aleve)
 +
! 6420
 +
! 13900
 +
! 329
 +
! 50
 +
! 55000
 +
! 37000
 +
! 930
 +
! 187000
 +
! 11000
 +
! 160
 +
! 60
 +
! 840
 +
! 50
 +
|-
 +
! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
 +
! 3.4
! Naproxen (Aleve)
! Naproxen (Aleve)
! 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)
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|-
|-
! Dosage (mg)
! Dosage (mg)
-
! Ibuprofen (Advil)
+
! 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)
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|-
|-
! 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)
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! 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 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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