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 (Prostaglandins) Pain Cell Death Spasm Hypoxia

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 thromboxane Aspirin 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 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

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 Acetylsalicytic acid 650 mg. 4000 mg. 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/… Anticoagulants Corticosteroids Other NSAIDS Alcohol

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

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

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