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Non-Opioids
NSAIDs
| Question | Answer |
|---|---|
| What is COX? | Cyclooxygenase (COX) is the key enzyme required for the conversion of arachidonic acid to prostaglandins |
| What is COX-1? | The constitutive isoform, it has clear physiological functions and makes PGs that protect the stomach and kidney from damage |
| What is COX-2? | The inducible isoform, it is induced by pro-inflammatory stimuli such as cytokines, and produces PGs that contribute to the pain and swelling of inflammation. |
| Is there a COX-1 inducer? | misoprostol (cytotec); approved for the treatment and prevention of stomach ulcers. It is also available in combination with diclofenac (Voltaren), an NSAID, as Arthrotec. It is also used to induce labor and as an abortifacient |
| Name some non-selective COX (block 1 & 2) inhibitors? | ibuprofen (Motrin, Advil) naproxen (Aleve, Naprosyn), diclofenac (Voltaren), ASA, nabumetone (Relafen), indomethacin (Indocin), meloxicam (Mobic), sulindac (Clinoril) |
| Name some selective COX-2 inhibitors? | celecoxib (Celebrex), rofecoxib (Vioxx), valdecoxib (Bextra) Vioxx and Bextra are no longer on the market d/t increased incidence of MIs |
| What is an NSAID with efficacy similar to morphine that can be used IV for acute pain? | ketorolac (Toradol) |
| Why can't ketorolac be used for more than 5 days or long term? | kidney damage |
| If you inhibit COX-1, what are the effects? | decreased gastric mucus production, therefore there is an increased incidence of irritation from gastric acid which can lead to peptic ulceration |
| If you inhibit COX-2, what are the effects | decrease in inflammation & pain and antipyretic & antiplatelet activity |
| From a renal prospective, what is the down side to COX-1 inhibition? | PGs produced by COX-1 primarily affect renal homeostasis by promoting vasodilation in the renal vascular bed → ↓renal vascular resistance therefore↑renal perfusion. SO...inhibition would result in renal vasoconstriction → ↑resistance and ↓perfusion |
| From a renal perspective, what is the down side to COX-2 inhibition? | COX-2 has a diuretic and natriuretic effect, inhibition would therefore result in ↑sodium retention, ↑fluid retention (peripheral edema) and ↑arterial pressure → ↑BP |
| What is the advantage of using NSAIDS in combination with opioids? | the opioid-sparing effect of NSAID therapy allows the clinician to decrease the opioid dose thereby diminishing the side effects associated with opioid therapy without sacrificing pain control |
Created by:
psfisher50
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