NSAID Pharmacokinetics

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Revision as of 16:36, 11 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)	Mefenamic Acid (Ponstel)	Ketorolac (Toradol)	Rofecoxib (Vioxx)	Diclofenac (Voltaren)
T_max (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)
C_max (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)
T_1/2 (hr)	2.4	18.7	4.77	Acetylsalicylic Acid (Aspirin)	8-11	11.2	7.8	Oxaprozin (Daypro)	Piroxicam (Feldene)	Nabumetone (Relafen)	Acetaminophen (Paracetamol)	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, see: References

Proteopedia Page Contributors and Editors (what is this?)

David Canner

Retrieved from "http://52.214.119.220/wiki/index.php/NSAID_Pharmacokinetics"

@@ Line 32: / Line 32: @@
 ! Nabumetone (Relafen)
 ! Acetaminophen (Paracetamol)
-! Mefanamic Acid (Ponstel)
+! 22
 ! Ketorolac (Toradol)
 ! Rofecoxib (Vioxx)
@@ Line 66: / Line 66: @@
 ! Nabumetone (Relafen)
 ! Acetaminophen (Paracetamol)
-! Mefanamic Acid (Ponstel)
+! 90
 ! Ketorolac (Toradol)
 ! Rofecoxib (Vioxx)
@@ Line 83: / Line 83: @@
 ! Nabumetone (Relafen)
 ! Acetaminophen (Paracetamol)
-! Mefanamic Acid (Ponstel)
+! 90
 ! Ketorolac (Toradol)
 ! Rofecoxib (Vioxx)
@@ Line 100: / Line 100: @@
 ! Nabumetone (Relafen)
 ! Acetaminophen (Paracetamol)
-! Mefanamic Acid (Ponstel)
+! 2-4
 ! Ketorolac (Toradol)
 ! Rofecoxib (Vioxx)
@@ Line 122: / Line 122: @@
 ! 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
-! 38000
+! Ibuprofen (Advil)
-! 32000
+! Naproxen (Aleve)
-! Flurbiprofen (Ansaid)
+! 440
-! ASPRIN
+! 4400
-! 150000
+! 25400
+! 140
+! 1900
 ! 15000
-! Sulindac (Clinoril)
+! 2900
-! Oxaprozin (Daypro)
+! 278000
-! 680000
+! 42000
-! 82000
+! 1900
-! Acetaminophen (Paracetamol)
+! 110
-! Mefanamic Acid (Ponstel)
+! 63000
-! Ketorolac (Toradol)
+! 140
-! >1000000
-! 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) in Whole Blood
-! 117000
+! Ibuprofen (Advil)
-! 235000
+! Naproxen (Aleve)
-! Flurbiprofen (Ansaid)
+! 6420
-! ASPRIN
+! 13900
-! 5
+! 329
-! 40
+! 50
-! Sulindac (Clinoril)
+! 55000
-! Oxaprozin (Daypro)
+! 37000
-! 660000
+! 930
-! >1000000
+! 187000
-! Acetaminophen (Paracetamol)
+! 11000
-! Mefanamic Acid (Ponstel)
+! 160
-! Ketorolac (Toradol)
+! 60
-! 500
+! 840
-! 10
+! 50
 |-
 ! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
@@ Line 168: / Line 168: @@
 ! Nabumetone (Relafen)
 ! Acetaminophen (Paracetamol)
-! Mefanamic Acid (Ponstel)
+! 21.23
 ! Ketorolac (Toradol)
 ! Rofecoxib (Vioxx)
@@ Line 185: / Line 185: @@
 ! Nabumetone (Relafen)
 ! Acetaminophen (Paracetamol)
-! Mefanamic Acid (Ponstel)
+! 500
 ! Ketorolac (Toradol)
 ! Rofecoxib (Vioxx)
@@ Line 202: / Line 202: @@
 ! Nabumetone (Relafen)
 ! Acetaminophen (Paracetamol)
-! Mefanamic Acid (Ponstel)
+! Hepatic (CYP2C9)
 ! Ketorolac (Toradol)
 ! Rofecoxib (Vioxx)

NSAID Pharmacokinetics

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Revision as of 16:36, 11 December 2010

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