Transcript 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
(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
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
 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 antiinflammatory 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