Non-Steroidal Anti- Inflammatory Drugs (NSAIDs)
Mar 27, 2015
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
NSAIDs - Effects
Anti-inflammatroy - inhibit synthesis of prostaglandins by blocking the cyclooxygenase (COX) enzyme
Types– COX –1 – found in stomach– COX –2 – found at injury site
Pain-Spasm Cycle
Pain
Spasm
Hypoxia
Cell Death
Release of Chemical Mediators
Stimulus
(Prostaglandins)
Anti-inflammatory Effects
Inhibits chemical mediator –
prostaglandin Prostaglandin produces stomach
mucosa Inhibition of prostaglandin = less
stomach mucosa = GI effects
NSAIDs – Other Effects
Analgesic - decrease
pain
Antipyretic - decrease
fever
Anti-platelet - slows
blood clotting (increases clotting time)
Anti-platelet Effects
Binds to COX-1 enzyme preventing production of thromboxaneAspirin binds permanently
• ++ Decrease risk of heart attack & stroke• -- Discontinue before surgery• -- Bruising effects in athletes in contact sports
Aspirin (and other Salicylates)
acetylsalicylic acid In US since 1899 Cheaper than other NSAIDS Other uses
– Prevent heart attack & strokes– Decrease risk of colon & G.I. cancer
Usually orally administered Not banned …. but some combination products
may be No performance enhancing effect
Types of AspirinBuffered aspirin
Antacids added to neutralize stomach acid & GI effects
Delayed release aspirinSpecial coating delays dissolving action until in the small intestineWhat is also delayed?
Aspirin with caffeineActs faster – enhances effects
Other Salicylates Choline salicylate (Arthropan)
- liquid form- less potent – need more
Magnesium salicylate (Doan’s)- contains magnesium
Topical salicylates- methyl salicylate (Icy Hot, Ben-Gay)- trolamine salicylate (Aspercreme)
Bismus Subsalicylate (Pepto Bismal)Salsalate
- Disalcid is available only by Rx.
Dosing Recommendations
Normal dose 24 hr max How long before effect? Food 1st sign of OD Children’s Aspirin
– Reyes syndrome
10 days for pain / 3 days for fever
Dose Protocols
Every 4 hrs. 24 hr. max Acetylsalicytic acid 650 mg. 4000 mg.
Choline salicylate 870 mg. 5220 mg.
Magnesium salicylate 754 mg. 4640 mg.
Children’s doses 80 mg. Tablets / # determined by wt.
** initial loading dose of 975 mg. allowable but only one time!
** No more than 10 consecutive days!!
Aspirin Precautions
More side effects than other NSAIDs Bruising Not used w/ clotting disorders, etc GI side effects Nephrotoxicity Not w/ Gout Allergic Rxn OD Decreases effect of antacid
Avoid Aspirin if….
Child/Adolescent Pregnant Low back pain Bleeding disorders Hx of GI problems Long distance runners Asthma Kidney or liver problems
Avoid Aspirin in combo w/…
AnticoagulantsCorticosteroidsOther NSAIDSAlcohol
Aspirin Guidelines for the ATC
Short term Alcohol? Recognize allergy / OD
signs Appropriate for …? Reyes Syndrome Before exercise Runner’s bleed
Pros / Cons of Aspirin
Very effective for mild – moderate pain relief
Decreases risk of heart disease
Has anti-inflammatory and analgesic effects
Cheap and accessible
GI effects Very powerful anti-
platelet effects Nephrotoxicity Allergic reactions Reyes syndrome
Nonsalicylate NSAIDS
Definition
Table 4.1 and NSAID Handout– Differentiated by:
• Availability - OTC vs prescription
• Duration of action
• Potency
Indications and Uses
Anti-inflammatory, analgesic, antipyretic, and anti-platelet
1st analgesic then anti-inflammatory Mild to moderate pain, inflammation Anti-platelet effect less pronounced
Act similar to salicylates in body
Not necessarily better than aspirin - but less side effects (Gentler on stomach)
Arthritis, menstrual cramps, etc
Indications (con’t)…..
Administration
»Orally – pills vs liquid
»Ophthalmic
»Injection
»Topicals – not in US
Analgesic vs. anti-inflammatory regime Limit to 3 days for fever, 10 for pain
Dosing Protocols for OCT’s
***Stronger than aspirin so lower dose Ibuprofen (Advil)
– 2 tablets (400 mg) every 4-6 hrs
Naproxen Sodium (Aleve)– 1 tablet (220mg) every 8-12
Ketoprofen (Orudis KT)– 1 tablet (12.5mg) every 4-6 hrs
Side Effects / Adverse Reactions
Similar to aspirin Nephrotoxicity Anaphylatic reaction Overdose symptoms
• Tinnitis, headache, nausea, dizziness Toxicity
• Breathing, irregular HB, tarry stools, hematuria, jaundice
Contraindications
Aspirin intolerance Pregnancy Don’t take if allergic to aspirin In combination with
• Corticosteroids, anticoagulants, aspirin, alcohol
Considerations for ATCs
Long term use? Not on banned substances list Does not interfere with energy metabolism May have negative long term effect on
collagen formation Regular liver testing for…. Care with distance runners / alcohol Use w/ PRICE