This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
NSAID Pharmacokinetics
From Proteopedia
(Difference between revisions)
| Line 22: | Line 22: | ||
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr) | ! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr) | ||
! 1.3 | ! 1.3 | ||
| - | ! | + | ! .92 |
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| Line 38: | Line 38: | ||
|- | |- | ||
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ||
| - | ! | + | ! 16200 |
| - | ! | + | ! 47100 |
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| Line 90: | Line 90: | ||
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ||
! 2.4 | ! 2.4 | ||
| - | ! | + | ! 18.7 |
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
| Line 106: | Line 106: | ||
|- | |- | ||
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
| - | ! | + | ! 67400 |
| - | ! | + | ! 777400 |
! Flurbiprofen (Ansaid) | ! Flurbiprofen (Ansaid) | ||
! Acetylsalicylic Acid (Aspirin) | ! Acetylsalicylic Acid (Aspirin) | ||
Revision as of 18:44, 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 | 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) |
| Cmax (ng/ml) | 16200 | 47100 | 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) |
| Bioavailability (%) | 49-73 | 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) |
| Protein Binding (%) | 99 | 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) |
| T1/2 (hr) | 2.4 | 18.7 | 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) |
| AUC (ng/ml/hr) | 67400 | 777400 | 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) |
| 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 | 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) |
| 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
