NSAID Pharmacokinetics
From Proteopedia
(Difference between revisions)
| Line 93: | Line 93: | ||
! 4.77 | ! 4.77 | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| - | ! | + | ! 8-11 |
! 11.2 | ! 11.2 | ||
! 7.8 | ! 7.8 | ||
| Line 123: | Line 123: | ||
|- | |- | ||
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-1 (nM) | ! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] COX-1 (nM) | ||
| - | ! | + | ! 38000 |
| - | ! | + | ! 32000 |
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
| - | ! | + | ! ASPRIN |
| - | ! | + | ! 150000 |
| - | ! | + | ! 15000 |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
| - | ! | + | ! 680000 |
| - | ! | + | ! 82000 |
! Acetaminophen (Paracetamol) | ! Acetaminophen (Paracetamol) | ||
! Mefanamic Acid (Ponstel) | ! Mefanamic Acid (Ponstel) | ||
! Ketorolac (Toradol) | ! Ketorolac (Toradol) | ||
| - | ! | + | ! >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) | ||
| - | ! | + | ! 117000 |
| - | ! | + | ! 235000 |
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
| - | ! | + | ! ASPRIN |
| - | ! | + | ! 5 |
| - | ! | + | ! 40 |
! Sulindac (Clinoril) | ! Sulindac (Clinoril) | ||
! Oxaprozin (Daypro) | ! Oxaprozin (Daypro) | ||
| - | ! | + | ! 660000 |
| - | ! | + | ! >1000000 |
! Acetaminophen (Paracetamol) | ! Acetaminophen (Paracetamol) | ||
! Mefanamic Acid (Ponstel) | ! Mefanamic Acid (Ponstel) | ||
! Ketorolac (Toradol) | ! Ketorolac (Toradol) | ||
| - | ! | + | ! 500 |
| - | ! | + | ! 10 |
|- | |- | ||
! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h) | ! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h) | ||
| Line 161: | Line 161: | ||
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| - | ! | + | ! 6 |
! 27.7 | ! 27.7 | ||
! 4.1 | ! 4.1 | ||
Revision as of 19:55, 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 | 2.3 | Acetylsalicylic Acid (Aspirin) | 2.9 | 2.8 | 3.4 | 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 | 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) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| Protein Binding (%) | 99 | 99 | 99 | 99 | 98 | 97 | 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) | 8-11 | 11.2 | 7.8 | 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 | 6930 | Sulindac (Clinoril) | Oxaprozin (Daypro) | Piroxicam (Feldene) | Nabumetone (Relafen) | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
| IC50 COX-1 (nM) | 38000 | 32000 | Flurbiprofen (Ansaid) | ASPRIN | 150000 | 15000 | Sulindac (Clinoril) | Oxaprozin (Daypro) | 680000 | 82000 | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | >1000000 | 30 |
| IC50 COX-2 (nM) | 117000 | 235000 | Flurbiprofen (Ansaid) | ASPRIN | 5 | 40 | Sulindac (Clinoril) | Oxaprozin (Daypro) | 660000 | >1000000 | Acetaminophen (Paracetamol) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | 500 | 10 |
| 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) | Mefanamic Acid (Ponstel) | 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) | Mefanamic Acid (Ponstel) | 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) | Mefanamic Acid (Ponstel) | Ketorolac (Toradol) | Rofecoxib (Vioxx) | Diclofenac (Voltaren) |
For references, see: References
