NonSteroidal AntiInflammatory Drugs NSAIDs NSAIDs Effects 4 Antiinflammatroy

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Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

NSAIDs - Effects 4 Anti-inflammatroy - inhibit synthesis of prostaglandins by blocking the cyclooxygenase

NSAIDs - Effects 4 Anti-inflammatroy - inhibit synthesis of prostaglandins by blocking the cyclooxygenase (COX) enzyme 4 Types – COX – 1 – found in stomach – COX – 2 – found at injury site

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

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

Anti-inflammatory Effects 4 Inhibits chemical mediator – prostaglandin 4 Prostaglandin produces stomach mucosa 4

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

NSAIDs – Other Effects 4 Analgesic - decrease pain 4 Antipyretic - decrease fever

NSAIDs – Other Effects 4 Analgesic - decrease pain 4 Antipyretic - decrease fever 4 Anti-platelet - slows blood clotting (increases clotting time)

Anti-platelet Effects q Binds to COX-1 enzyme preventing production of thromboxane q. Aspirin binds

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

Aspirin (and other Salicylates) 4 acetylsalicylic acid 4 In US since 1899 4 Cheaper

Aspirin (and other Salicylates) 4 acetylsalicylic acid 4 In US since 1899 4 Cheaper than other NSAIDS 4 Other uses – Prevent heart attack & strokes – Decrease risk of colon & G. I. cancer 4 Usually orally administered 4 Not banned …. but some combination products may be 4 No performance enhancing effect

Types of Aspirin q. Buffered aspirin q. Antacids added to neutralize stomach acid &

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

Other Salicylates q Choline salicylate (Arthropan) - liquid form - less potent – need

Other Salicylates q Choline salicylate (Arthropan) - liquid form - less potent – need more q Magnesium salicylate (Doan’s) - contains magnesium q Topical salicylates - methyl salicylate (Icy Hot, Ben-Gay) - trolamine salicylate (Aspercreme) q. Bismus Subsalicylate (Pepto Bismal) q. Salsalate - Disalcid is available only by Rx.

Dosing Recommendations 4 Normal dose 4 24 hr max 4 How long before effect?

Dosing Recommendations 4 Normal dose 4 24 hr max 4 How long before effect? 4 Food 4 1 st sign of OD 4 Children’s Aspirin – Reyes syndrome 4 10 days for pain / 3 days for fever

Dose Protocols Every 4 hrs. 24 hr. max Acetylsalicytic acid 650 mg. 4000 mg.

Dose Protocols Every 4 hrs. 24 hr. max Acetylsalicytic acid 650 mg. 4000 mg. Choline salicylate 870 mg. 5220 mg. Magnesium salicylate Children’s doses 754 mg. 4640 mg. 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 4 More side effects than other NSAIDs 4 Bruising 4 Not used

Aspirin Precautions 4 More side effects than other NSAIDs 4 Bruising 4 Not used w/ clotting disorders, etc 4 GI side effects 4 Nephrotoxicity 4 Not w/ Gout 4 Allergic Rxn 4 OD 4 Decreases effect of antacid

Avoid Aspirin if…. 4 Child/Adolescent 4 Pregnant 4 Low back pain 4 Bleeding disorders

Avoid Aspirin if…. 4 Child/Adolescent 4 Pregnant 4 Low back pain 4 Bleeding disorders 4 Hx of GI problems 4 Long distance runners 4 Asthma 4 Kidney or liver problems

Avoid Aspirin in combo w/… 4 Anticoagulants 4 Corticosteroids 4 Other NSAIDS 4 Alcohol

Avoid Aspirin in combo w/… 4 Anticoagulants 4 Corticosteroids 4 Other NSAIDS 4 Alcohol

Aspirin Guidelines for the ATC 4 Short term 4 Alcohol? 4 Recognize allergy /

Aspirin Guidelines for the ATC 4 Short term 4 Alcohol? 4 Recognize allergy / OD signs 4 Appropriate for …? 4 Reyes Syndrome 4 Before exercise 4 Runner’s bleed

Pros / Cons of Aspirin 4 Very effective for mild – moderate pain relief

Pros / Cons of Aspirin 4 Very effective for mild – moderate pain relief 4 Decreases risk of heart disease 4 Has antiinflammatory and analgesic effects 4 Cheap and accessible 4 GI effects 4 Very powerful anti- platelet effects 4 Nephrotoxicity 4 Allergic reactions 4 Reyes syndrome

Nonsalicylate NSAIDS 4 Definition 4 Table 4. 1 and NSAID Handout – Differentiated by:

Nonsalicylate NSAIDS 4 Definition 4 Table 4. 1 and NSAID Handout – Differentiated by: • Availability - OTC vs prescription • Duration of action • Potency

Indications and Uses 4 Anti-inflammatory, analgesic, antipyretic, and anti-platelet 4 1 st analgesic then

Indications and Uses 4 Anti-inflammatory, analgesic, antipyretic, and anti-platelet 4 1 st analgesic then anti-inflammatory 4 Mild to moderate pain, inflammation 4 Anti-platelet effect less pronounced

Indications (con’t)…. . q. Act similar to salicylates in body q. Not necessarily better

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

Administration » Orally – pills vs liquid » Ophthalmic » Injection » Topicals –

Administration » Orally – pills vs liquid » Ophthalmic » Injection » Topicals – not in US 4 Analgesic vs. anti-inflammatory regime 4 Limit to 3 days for fever, 10 for pain

Dosing Protocols for OCT’s ***Stronger than aspirin so lower dose 4 Ibuprofen (Advil) –

Dosing Protocols for OCT’s ***Stronger than aspirin so lower dose 4 Ibuprofen (Advil) – 2 tablets (400 mg) every 4 -6 hrs 4 Naproxen Sodium (Aleve) – 1 tablet (220 mg) every 8 -12 4 Ketoprofen (Orudis KT) – 1 tablet (12. 5 mg) every 4 -6 hrs

Side Effects / Adverse Reactions 4 Similar to aspirin 4 Nephrotoxicity 4 Anaphylatic reaction

Side Effects / Adverse Reactions 4 Similar to aspirin 4 Nephrotoxicity 4 Anaphylatic reaction 4 Overdose symptoms • Tinnitis, headache, nausea, dizziness 4 Toxicity • Breathing, irregular HB, tarry stools, hematuria, jaundice

Contraindications 4 Aspirin intolerance 4 Pregnancy 4 Don’t take if allergic to aspirin 4

Contraindications 4 Aspirin intolerance 4 Pregnancy 4 Don’t take if allergic to aspirin 4 In combination with • Corticosteroids, anticoagulants, aspirin, alcohol

Considerations for ATCs 4 Long term use? 4 Not on banned substances list 4

Considerations for ATCs 4 Long term use? 4 Not on banned substances list 4 Does not interfere with energy metabolism 4 May have negative long term effect on collagen formation 4 Regular liver testing for…. 4 Care with distance runners / alcohol 4 Use w/ PRICE