NSAID Pharmacokinetics

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Line 57:		Line 57:
	! 49-73		! 49-73
	! 95		! 95
-	! Flurbiprofen (Ansaid)	+	! 96
	! Acetylsalicylic Acid (Aspirin)		! Acetylsalicylic Acid (Aspirin)
-	! Valdecoxib (Bextra)	+	! 83
	! Celecoxib (Celebrex)		! Celecoxib (Celebrex)
	! Sulindac (Clinoril)		! Sulindac (Clinoril)
Line 74:		Line 74:
	! 99		! 99
	! 99		! 99
-	! Flurbiprofen (Ansaid)	+	! 99
-	! Acetylsalicylic Acid (Aspirin)	+	! 99
-	! Valdecoxib (Bextra)	+	! 98
	! Celecoxib (Celebrex)		! Celecoxib (Celebrex)
	! Sulindac (Clinoril)		! Sulindac (Clinoril)
Line 192:		Line 192:
	! Metabolism		! Metabolism
	! Hepatic (CYP2C9)		! Hepatic (CYP2C9)
-	! Naproxen (Aleve)	+	! Naproxen
-	! Flurbiprofen (Ansaid)	+	! Hepatic (CYP2C9)
	! Acetylsalicylic Acid (Aspirin)		! Acetylsalicylic Acid (Aspirin)
-	! Valdecoxib (Bextra)	+	! Hepatic (CYP3A4 & CYP2C9)
	! Celecoxib (Celebrex)		! Celecoxib (Celebrex)
	! Sulindac (Clinoril)		! Sulindac (Clinoril)

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Revision as of 19:19, 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	2.29	Acetylsalicylic Acid (Aspirin)	2.94	Celecoxib (Celebrex)	Sulindac (Clinoril)	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	Celecoxib (Celebrex)	Sulindac (Clinoril)	Oxaprozin (Daypro)	Piroxicam (Feldene)	Nabumetone (Relafen)	Acetaminophen (Paracetamol)	Mefanamic Acid (Ponstel)	Ketorolac (Toradol)	Rofecoxib (Vioxx)	Diclofenac (Voltaren)
Bioavailability (%)	49-73	95	96	Acetylsalicylic Acid (Aspirin)	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	Celecoxib (Celebrex)	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)	Valdecoxib (Bextra)	Celecoxib (Celebrex)	Sulindac (Clinoril)	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	Celecoxib (Celebrex)	Sulindac (Clinoril)	Oxaprozin (Daypro)	Piroxicam (Feldene)	Nabumetone (Relafen)	Acetaminophen (Paracetamol)	Mefanamic Acid (Ponstel)	Ketorolac (Toradol)	Rofecoxib (Vioxx)	Diclofenac (Voltaren)
IC50 COX-1 (nM)	18	11	Flurbiprofen (Ansaid)	342	Valdecoxib (Bextra)	Celecoxib (Celebrex)	Sulindac (Clinoril)	Oxaprozin (Daypro)	Piroxicam (Feldene)	Nabumetone (Relafen)	Acetaminophen (Paracetamol)	Mefanamic Acid (Ponstel)	Ketorolac (Toradol)	Rofecoxib (Vioxx)	Diclofenac (Voltaren)
IC50 COX-2 (nM)	1030	1015	Flurbiprofen (Ansaid)	>5000	Valdecoxib (Bextra)	Celecoxib (Celebrex)	Sulindac (Clinoril)	Oxaprozin (Daypro)	Piroxicam (Feldene)	Nabumetone (Relafen)	Acetaminophen (Paracetamol)	Mefanamic Acid (Ponstel)	Ketorolac (Toradol)	Rofecoxib (Vioxx)	Diclofenac (Voltaren)
Clearance (L/h)	3.4	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)
Dosage (mg)	400	200	150	Acetylsalicylic Acid (Aspirin)	20	Celecoxib (Celebrex)	Sulindac (Clinoril)	Oxaprozin (Daypro)	Piroxicam (Feldene)	Nabumetone (Relafen)	Acetaminophen (Paracetamol)	Mefanamic Acid (Ponstel)	Ketorolac (Toradol)	Rofecoxib (Vioxx)	Diclofenac (Voltaren)
Metabolism	Hepatic (CYP2C9)	Naproxen	Hepatic (CYP2C9)	Acetylsalicylic Acid (Aspirin)	Hepatic (CYP3A4 & CYP2C9)	Celecoxib (Celebrex)	Sulindac (Clinoril)	Oxaprozin (Daypro)	Piroxicam (Feldene)	Nabumetone (Relafen)	Acetaminophen (Paracetamol)	Mefanamic Acid (Ponstel)	Ketorolac (Toradol)	Rofecoxib (Vioxx)	Diclofenac (Voltaren)

For references, see: References