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Chapter 3 Anti-inflammatory Medications. NSAIDs. The use of NSAIDs for the treatment of sports-related injuries, as well as other maladies, (namely osteoarthritis) continues to rise. In 2001, sales of NSAID prescriptions accounted for $10.9 billion in the United States. . NSAIDs ( cont. ).

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nsaids
NSAIDs
  • The use of NSAIDs for the treatment of sports-related injuries, as well as other maladies, (namely osteoarthritis) continues to rise.
  • In 2001, sales of NSAID prescriptions accounted for $10.9 billion in the United States.
nsaids cont
NSAIDs (cont.)
  • A thorough understanding of drug actions, interactions, and effects allows the athletic trainer to educate athletes on treatment plans and symptoms resulting from NSAIDs
nsaids cont4
NSAIDs (cont.)
  • A recent study of high school football players revealed that 75% of those surveyed had used NSAIDs in the previous 3 months and 15% of the respondents were daily NSAID users. The daily users often used the drugs prophylactically prior to practices and games.
the inflammatory response
The Inflammatory Response
  • The acute inflammatory cascade is set into motion by the initial tissue insult.
  • Grossly, acute inflammation is recognized by the classic and familiar signs of pain (dolor), heat (calor), erythema (rubor), swelling (tumor), and loss of function (functio laesa).
inflammatory response cont
Inflammatory Response (cont.)
  • Following a short period of vasoconstriction - cellular injury signals the release of chemical mediators, such as histamine, serotonin, anaphylatoxins, bradykinin, thromboxane, leukotrienes, and prostaglandins.
box 3 2 page 36
Box 3-2 page 36
  • Major actions of the Eicosanoids
    • Prostaglandins
    • Thromboxane
    • Leukotrienes
anti inflammatory medications
Anti-inflammatory Medications
  • Aspirin (acetylsalicylic acid) - a derivative of salicylic acid.
    • Salicylic acid, in turn, was created from salicin, which is found in the bark of willow trees.
    • Aspirin was first synthesized by a Bayer Company chemist in the late 19th century.
    • It proved to be far less of a gastric irritant than salicylic acid and was introduced to the marketplace in the spring of 1899.
slide10
In 1971, Sir John Vane discovered that the aspirin molecule transfers a functional group onto the cyclooxygenase enzyme. Until this time the actual mechanism of action for aspirin was unknown.
cyclooxygenase enzyme cox
Cyclooxygenase Enzyme (COX)
  • This enzyme is irreversibly inhibited and unable to bind arachidonic acid, therefore, the enzyme can no longer convert arachidonic acid to prostaglandins and thromboxane.
  • The Leukotriene pathway, however, is unaffected
effects of aspirin
Effects of Aspirin
  • Analgesic
  • Antipyretic
  • Anticoagulant
  • Anti-inflammatory
effects of aspirin13
Effects of Aspirin
  • 3000 – 6000 mg per day for anti-inflammatory action; a series of chemical events results from the blockage of cyclooxygenase
  • 325 mg aspirin = 12 to 18 aspirin per day to reach an anti-inflammatory effect
effects of aspirin14
Effects of Aspirin
  • The decrease in prostaglandin production leads to a corresponding reduction in inflammation and edema.
effects of aspirin15
Effects of Aspirin
  • Blocks prostaglandin production, even the “cytoprotection.”
  • In the GI tract, aspirin can cause gastric upset, bleeding, and even ulcers.
    • Various studies have shown GI disturbance incidence of anywhere from 2 percent to 40 percent.
effects of aspirin16
Effects of Aspirin
  • The mechanism of gastric irritation appears related to the direct effect of aspirin upon the lining of the stomach.
  • Mild gastrointestinal upset can often be avoided if aspirin is taken with a meal, due to the "buffering" action of the food.
effects of aspirin17
Effects of Aspirin
  • Aspirin use may also result in complications, such as prolonged bleeding and tinnitus.
    • Decreased platelet function lasts from 4 to 6 days (used for blood thinning in heart patients).
    • Tinnitus may be an indication of aspirin toxicity.
reye s syndrome
Reye’s Syndrome
  • Reye’s syndrome is a rare and potentially devastating, acute illness that usually strikes children following a viral infection when they are given aspirin to lower fever.
  • This syndrome is now suspected in teens and young adults with viral infections who take aspirin.
aspirin sensitive asthma
Aspirin Sensitive Asthma
  • Upon exposure to even small quantities of aspirin, those affected may develop nasal congestion and acute, often severe bronchospasm.
  • There is an almost universal cross-reactivity with other NSAIDs.
  • Patients can be desensitized over time with daily administration of aspirin and cross-tolerance to other NSAIDs usually occurs.
acetaminophen
Acetaminophen
  • Acetaminophen (Tylenol) is not an anti-inflammatory agent, it has antipyretic and analgesic properties.
  • Will be discussed with the analgesics (Chapter 10).
nsaids22
NSAIDs
  • COX-2 Inhibitors
    • Primarily induced at sites of inflammation
    • COX-2 inhibitor could block the production of proinflammatory prostaglandins without interfering with gastric protection or platelet activity
    • Research is controversial and the drugs are expensive
overview of selected nsaids
Overview of Selected NSAIDs
  • Box 3-4 Page 42 – Factors to Consider in Choosing an NSAID
    • Age of Patient
    • Duration of Treatment
    • Time of Onset
    • Compliance
    • Other Medications
    • General Health of Patient
    • Cost of Treatment
ibuprofen
Ibuprofen
  • Advil, Motrin, Nuprin
  • Most frequently used NSAID
  • Introduced to the OTC market in 1985, it is available in 200 to 800 mg tablets by prescription, and 200 mg tablets OTC
  • Frequently used as an antipyretic in adults and children, as its longer duration of action makes it a popular alternative to acetaminophen
ibuprofen25
Ibuprofen
  • Peak plasma levels are achieved within 15 to 30 minutes of ingestion
  • Rapid onset of action can be quite beneficial for quick relief of pain
  • Half-life of about 2 hours, it must be taken every 6 to 8 hours to maintain effect
  • An anti-inflammatory regimen requires 2400 – 3200 mg daily
ibuprofen26
Ibuprofen
  • Taken in three separate doses, allowing it to be taken at meal times, lessening the likelihood of gastric irritation.
  • Sufficient analgesia should be achieved by daily dosages of less than 2400 mg per day.
  • Approximately 10 percent to 15 percent of individuals must discontinue use secondary to gastrointestinal symptoms.
naproxen
Naproxen
  • Naprosyn, Aleve.
  • Chemically similar to ibuprofen.
  • Naproxen is available as the OTC preparation Aleve, and as Anaprox by prescription.
  • Due to naproxen's long half-life (approximately 12 hours), the daily recommended dosage of 750 – 1000 mg can be taken on a twice daily schedule, reducing gastric upset due to only two exposures and improving compliance.
naproxen28
Naproxen
  • Peak plasma levels are achieved within 2 to 4 hours
  • Incidence of upper gastrointestinal bleeding in OTC use is double that of OTC ibuprofen
indomethacin
Indomethacin
  • Indocin.
  • Although particularly effective in maladies such as rheumatoid arthritis, ankylosing spondylitis, and gout, indomethacin is typically not recommended for use as a simple analgesic or antipyretic due to potentially severe side-effects.
  • Up to half of those using indomethacin may experience some side-effects and almost one-third will discontinue use.
indomethacin30
Indomethacin
  • Common side-effects include gastrointestinal symptoms (ulceration, nausea, abdominal pain) and headaches (15 percent to 25 percent of patients).
  • Peak concentrations can be achieved in 1 to 2 hours (in fasting subjects, onset is delayed by food intake).
indomethacin31
Indomethacin
  • A half-life of about 2.5 hours.
  • Daily dosage ranges from 75 mg – 100 mg taken in two to three doses.
  • Indomethacin’s use has declined as newer agents with a lower side-effect profile have emerged.
nabumetone relafen
Nabumetone (Relafen)
  • Only nonacid NSAID currently available
  • Once-a-day treatment; half-life is 24 hours
rofecoxib
Rofecoxib
  • Vioxx
  • One of only three potent and highly selective COX-2 inhibitors available.
  • It does not inhibit COX-1 and has no effect on platelet function.
  • It is FDA approved for the treatment of osteoarthritis, dysmenorrhea, and acute pain.
rofecoxib34
Rofecoxib
  • Dosages range from 12.5 mg – 50 mg. It is administered once daily given its nearly 17-hour half-life.
  • Long-term toxic effects, including gastrointestinal and renal effects, are not yet known given the drug’s relatively recent introduction.
celecoxib
Celecoxib
  • Celebrex
  • COX-2 inhibitor
    • 200 mg tablets
    • Peak Plasma levels = 3 hours
    • Half-life (approximate-effective) = 11 hours
    • Problems include:
      • Liver and kidneys
      • Heart ?
ketorolac
Ketorolac
  • Toradol.
  • Not typically employed for its anti-inflammatory properties.
  • It is the only NSAID available for intramuscular or intravenous injection as well as oral administration.
ketorolac37
Ketorolac
  • Although it also has anti-inflammatory and antipyretic properties, it is most commonly marketed and used as an analgesic, particularly in postoperative patients.
  • As an analgesic, ketorolac offers great promise as it avoids the most common shortcomings of opioids, i.e., tolerance, withdrawal effects, and respiratory depression.
ketorolac38
Ketorolac
  • Interestingly, Tokish et al (1992) recently reported that 28 of 30 National Football League team medical staffs commonly use ketorolac intramuscular injections on game days for pain relief.
  • Due to high risk of renal effects, duration of ketorolac treatment is typically held to less than 5 days.
glucocorticosteroids
Glucocorticosteroids
  • Animal studies demonstrate:
    • Potent anti-inflammatory actions of glucocorticosteroids and their subsequent effects upon healing
    • Glucocorticosteroids induced an early, transient recovery of the force-generating capacity of the effected muscle
    • Long-term findings revealed irreversible damage to the healing muscle, including atrophy and diminished force-generating capacity
corticosteroids in sports medicine
Corticosteroids in Sports Medicine
  • Stanley and Weaver (1989) state that “inconsistency in the studies on glucocorticosteroid use does not lend adequate support or direction to the sports medicine clinician in their use.”
  • Extremely powerful anti-inflammatory medications but no good research to demonstrate their effectiveness in activity-related injury.