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Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

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. Stimulus. Release of Chemical Mediators.

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Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

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  1. Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

  2. 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

  3. Pain-Spasm Cycle Stimulus Release of Chemical Mediators (Prostaglandins) Pain Cell Death Spasm Hypoxia

  4. Anti-inflammatory Effects • Inhibits chemical mediator – prostaglandin • Prostaglandin produces stomach mucosa • Inhibition of prostaglandin = less stomach mucosa = GI effects

  5. NSAIDs – Other Effects • Analgesic - decrease pain • Antipyretic - decrease fever • Anti-platelet - slows blood clotting (increases clotting time)

  6. Anti-platelet Effects • Binds to COX-1 enzyme preventing production of thromboxane • Aspirin binds permanently • ++ Decrease risk of heart attack & stroke • -- Discontinue before surgery • -- Bruising effects in athletes in contact sports

  7. 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

  8. Types of Aspirin • Buffered aspirin • Antacids added to neutralize stomach acid & GI effects • Delayed release aspirin • Special coating delays dissolving action until in the small intestine • What is also delayed? • Aspirin with caffeine • Acts faster – enhances effects

  9. 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.

  10. 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

  11. 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!!

  12. 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

  13. Avoid Aspirin if…. • Child/Adolescent • Pregnant • Low back pain • Bleeding disorders • Hx of GI problems • Long distance runners • Asthma • Kidney or liver problems

  14. Avoid Aspirin in combo w/… • Anticoagulants • Corticosteroids • Other NSAIDS • Alcohol

  15. Aspirin Guidelines for the ATC • Short term • Alcohol? • Recognize allergy / OD signs • Appropriate for …? • Reyes Syndrome • Before exercise • Runner’s bleed

  16. 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 Pros / Cons of Aspirin

  17. Nonsalicylate NSAIDS • Definition • Table 4.1 and NSAID Handout • Differentiated by: • Availability - OTC vs prescription • Duration of action • Potency

  18. 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

  19. Indications (con’t)….. • Act similar to salicylates in body • Not necessarily better than aspirin - but less side effects (Gentler on stomach) • Arthritis, menstrual cramps, etc

  20. 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

  21. 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

  22. Side Effects / Adverse Reactions • Similar to aspirin • Nephrotoxicity • Anaphylatic reaction • Overdose symptoms • Tinnitis, headache, nausea, dizziness • Toxicity • Breathing, irregular HB, tarry stools, hematuria, jaundice

  23. Contraindications • Aspirin intolerance • Pregnancy • Don’t take if allergic to aspirin • In combination with • Corticosteroids, anticoagulants, aspirin, alcohol

  24. 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

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