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NSAID Pharmacokinetics
From Proteopedia
(Difference between revisions)
| Line 23: | Line 23: | ||
! 1.3 | ! 1.3 | ||
! .92 | ! .92 | ||
| - | ! | + | ! 2.29 |
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! Valdecoxib (Bextra) | ! Valdecoxib (Bextra) | ||
| Line 40: | Line 40: | ||
! 16200 | ! 16200 | ||
! 47100 | ! 47100 | ||
| - | ! | + | ! 19670 |
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! Valdecoxib (Bextra) | ! Valdecoxib (Bextra) | ||
| Line 56: | Line 56: | ||
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ||
! 49-73 | ! 49-73 | ||
| - | ! | + | ! 95 |
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| Line 73: | Line 73: | ||
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ||
! 99 | ! 99 | ||
| - | ! | + | ! 99 |
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| Line 91: | Line 91: | ||
! 2.4 | ! 2.4 | ||
! 18.7 | ! 18.7 | ||
| - | ! | + | ! 4.77 |
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! Valdecoxib (Bextra) | ! Valdecoxib (Bextra) | ||
| Line 108: | Line 108: | ||
! 67400 | ! 67400 | ||
! 777400 | ! 777400 | ||
| - | ! | + | ! 124320 |
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! Valdecoxib (Bextra) | ! Valdecoxib (Bextra) | ||
| Line 175: | Line 175: | ||
! Dosage (mg) | ! Dosage (mg) | ||
! 400 | ! 400 | ||
| - | ! | + | ! 200 |
| - | ! | + | ! 150 |
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
! Valdecoxib (Bextra) | ! Valdecoxib (Bextra) | ||
Revision as of 18:53, 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) | Valdecoxib (Bextra) | 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) | Valdecoxib (Bextra) | 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 | 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) |
| Protein Binding (%) | 99 | 99 | 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) |
| 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) | 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-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) | Valdecoxib (Bextra) | 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 (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) |
For references, see: References
