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Chapter 3 Anti-inflammatory Medications

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Title: Chapter 3 Anti-inflammatory Medications


1
Chapter 3 Anti-inflammatory Medications
2
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.

3
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

4
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.

5
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).

6
Figure 3-1 The Inflammatory Response
7
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.

8
Box 3-2 page 36
  • Major actions of the Eicosanoids
  • Prostaglandins
  • Thromboxane
  • Leukotrienes

9
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.

10
  • 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.

11
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

12
Effects of Aspirin
  • Analgesic
  • Antipyretic
  • Anticoagulant
  • Anti-inflammatory

13
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

14
Effects of Aspirin
  • The decrease in prostaglandin production leads to
    a corresponding reduction in inflammation and
    edema.

15
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.

16
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.

17
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.

18
Reyes Syndrome
  • Reyes 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.

19
Table 3-1 The Five Clinical Stages of Reyes
Syndrome
20
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.

21
Acetaminophen
  • Acetaminophen (Tylenol) is not an
    anti-inflammatory agent, it has antipyretic and
    analgesic properties.
  • Will be discussed with the analgesics (Chapter
    10).

22
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

23
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

24
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

25
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

26
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.

27
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.

28
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

29
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.

30
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).

31
Indomethacin
  • A half-life of about 2.5 hours.
  • Daily dosage ranges from 75 mg 100 mg taken in
    two to three doses.
  • Indomethacins use has declined as newer agents
    with a lower side-effect profile have emerged.

32
Nabumetone (Relafen)
  • Only nonacid NSAID currently available
  • Once-a-day treatment half-life is 24 hours

33
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.

34
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 drugs relatively recent
    introduction.

35
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 ?

36
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.

37
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.

38
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.

39
NSAID Indications
40
NSAID Adverse Effects
41
NSAID Use
42
Drug-Drug Interactions
43
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

44
Actions of Corticosteroids
45
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.

46
Box 3-7 Most Common Indications for Injectable
Corticosteroids
47
Box 3-8 Potential Complications of Injectable
Corticosteroids
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