NSAIDs PPT Flashcards
(13 cards)
What is the role of the enzyme COX 1?
COX 1 isoform is believed to be homeostatic, meaning it is continually being synthesized in the body for cell maintenance, “house keeping”
What is the role of the enzyme COX 2?
COX 2 isoform is an inducible enzyme that is normally synthesized only in response to inflammation. COX 2 may also stimulate cell proliferation which is important in tumor development.
Which NSAID does not have high bioavailability?
Diclofenac
How is the PK of NSAIDs effected by age?
pharmacokinetics parameters can change with aging since the elderly have low body water fraction compared with adults
What drugs are the selective Cox 2 inhibitors?
Celecoxib (Celebrex)
Meloxicam (Mobic)- only selective at lowest doses, 7.5 mg/day
What drugs are the non-selective Cox inhibitors?
ASA
Ibuprofen (Motrin)
Ketoprofen
Naproxen
Diclofenac (Voltaren)
Ketorolac (Toradol)
Etodolac (Lodine)
Indomethacin (Indocin)
Piroxicam (Feldene)
Meloxicam (Mobic)
Mefenamic Acid (Ponstel)
Nabumetone (Relafen)
What drug is considered a “other analgesic” and why?
Acetaminophen, as it’s analgesic mechanism of action is not well understood
What are the therapeutic uses of NSAIDs?
Mild to moderate pain
Acute nociceptive pain
Chronic pain due to inflammation
Arthritis
Autoimmune disorder-related pain
If suboptimal response, try another NSAID
What are the beneficial effects of non-selective Cox inhibitors?
Inhibit Cox 1 & 2
Decrease effect bradykinin and histamine
Reverse vasodilation
Inhibit platelet aggregation
Antipyretic, anti-inflammatory, analgesic
What are the adverse effects of non-selective Cox inhibitors?
Gastric erosion & ulceration
Bleeding tendencies
Renal Impairment
Asthma
Cardiovascular: edema, hypertension, HF
CNS: HA, tinnitus, dizziness
What is the additional possible benefit of Celebrex?
protection against the development of colon cancer
When should Celebrex be avoided?
in patients with established CVD and elevated risk of CVD due to increased risk of cardio events
What is the benefit of prescribing Celebrex?
comparable analgesia and anti-inflammatory effects to the nonselective NSAIDs, but with fewer symptomatic gastric and duodenal ulcers and a decrease in gastrointestinal symptoms