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