Anti-Anti-Inflammatory Inflammatory
AgentsAgentsESAT 4001ESAT 4001
Pharmacology in Athletic Pharmacology in Athletic TrainingTraining
Effects of NSAIDSEffects of NSAIDS
AnalgesiaAnalgesia AntipyresisAntipyresis AnticoagulationAnticoagulation Control inflammationControl inflammation
Action of NSAIDsAction of NSAIDs
Hinder cyclooxygenase pathwayHinder cyclooxygenase pathway Block synthesis of prostaglandins and Block synthesis of prostaglandins and
thromboxanesthromboxanes prostaglandins and thromboxanes involved prostaglandins and thromboxanes involved
in production of pain, inflammation, fever in production of pain, inflammation, fever and excessive blood clottingand excessive blood clotting
NSAIDs inhibit platelet formation = NSAIDs inhibit platelet formation = decreased thrombus formationdecreased thrombus formation 2 reasons this may be counterproductive2 reasons this may be counterproductive
Tissue trauma while taking for tendinitisTissue trauma while taking for tendinitis If started immediately following trauma platelet If started immediately following trauma platelet
aggregation may be affectedaggregation may be affected
Side Effects of NSAIDsSide Effects of NSAIDs
GI irritation/damageGI irritation/damage Irritation of gastric mucosaIrritation of gastric mucosa Inhibition of prostaglandinsInhibition of prostaglandins
Hepatic and renal disordersHepatic and renal disorders Some studies indicate aspirin and Some studies indicate aspirin and
other NSAIDs inhibit synthesis of other NSAIDs inhibit synthesis of some components of connective some components of connective tissuetissue
Side Effects Specific to Side Effects Specific to AspirinAspirin
OverdoseOverdose S&S – headache, tinnitus, hearing difficulties, S&S – headache, tinnitus, hearing difficulties,
confusion, & GI irritationconfusion, & GI irritation Reye’s syndromeReye’s syndrome
S&S – high fever, vomiting, liver dysfunction, S&S – high fever, vomiting, liver dysfunction, & decreasing level of alertness& decreasing level of alertness
HypersensitivityHypersensitivity Allergic reactions – bronchospasms, hives, Allergic reactions – bronchospasms, hives,
sever rhinitissever rhinitis Possibility of CV shock in these peoplePossibility of CV shock in these people
Classes of NSAIDsClasses of NSAIDs
Acetic Acids ProductsAcetic Acids Products
IndomethacinIndomethacin IndocineIndocine One of the strongest cyclooxygenase One of the strongest cyclooxygenase
inhibitorsinhibitors Typically fully excreted w/in 48 hoursTypically fully excreted w/in 48 hours
DiclofenacDiclofenac Voltaren & cataflamVoltaren & cataflam Absorbed rapidly, short half-lifeAbsorbed rapidly, short half-life
Acetic Acids ProductsAcetic Acids Products
SulindacSulindac ClinorilClinoril Structurally/pharmacologically related Structurally/pharmacologically related
to indomethacinto indomethacin ProdrugProdrug
Converted to active sulfide metaboliteConverted to active sulfide metabolite Sulfide metabolite is 500 times more potent Sulfide metabolite is 500 times more potent
as a cyclooxygenase inhibitors than parent as a cyclooxygenase inhibitors than parent drugdrug
Acetic Acids ProductsAcetic Acids Products
TolmetinTolmetin TolectinTolectin ArthritisArthritis Rapid absorption and eliminationRapid absorption and elimination
Complete excretion w/in 24 hoursComplete excretion w/in 24 hours Common side effects – nausea and Common side effects – nausea and
vomitingvomiting
Acetic Acids ProductsAcetic Acids Products
KetorolacKetorolac ToradolToradol Excellent analgesic effects w/o side Excellent analgesic effects w/o side
affects of morphineaffects of morphine Loading dose (IM or IV)Loading dose (IM or IV) Rapid absorptionRapid absorption
Common side effects associated with Common side effects associated with acetic acid productsacetic acid products Abdominal pain, headache, dizziness, Abdominal pain, headache, dizziness,
and tinnitusand tinnitus
Enolic AcidsEnolic Acids
PhenylbutazonePhenylbutazone ButazolidinButazolidin Originally, was first NSAID alternative Originally, was first NSAID alternative
to aspirinto aspirin Has been found to be potentially fatalHas been found to be potentially fatal
Used only in short-term treatment (gout)Used only in short-term treatment (gout) Side effects – bone marrow depression, Side effects – bone marrow depression,
decreased production of platelets and decreased production of platelets and RBCsRBCs
Not often used in athletic medicineNot often used in athletic medicine
Enolic AcidsEnolic Acids
PiroxicamPiroxicam FeldeneFeldene Long half-life ~ one-a-day dosageLong half-life ~ one-a-day dosage Rapid absorption, long actionRapid absorption, long action Side effects – GI symptoms, dizziness, Side effects – GI symptoms, dizziness,
tinnitus, and headache most commonly tinnitus, and headache most commonly reportedreported
Taking w/ food does not effect Taking w/ food does not effect absorption, but does decrease gastric absorption, but does decrease gastric symptomssymptoms
Fenamic Acid DerivativesFenamic Acid Derivatives
MeclofenamateMeclofenamate MeclomenMeclomen
Rapid absorptionRapid absorption Peak effect of drug w/in .5-2 hoursPeak effect of drug w/in .5-2 hours
Common side effects of all NSAIDsCommon side effects of all NSAIDs Side effects tend to be more commonSide effects tend to be more common
Propionic AcidsPropionic Acids
IbuprofenIbuprofen Advil, Motrin, NuprinAdvil, Motrin, Nuprin Used more often for analgesic effect than for Used more often for analgesic effect than for
anti-inflammatory effectanti-inflammatory effect Analgesic effects in 2-4 hoursAnalgesic effects in 2-4 hours Anti-inflammatory effects require days to weeksAnti-inflammatory effects require days to weeks Absorption slowed when taking w/ food, Absorption slowed when taking w/ food,
however total absorption is unaffectedhowever total absorption is unaffected Maximum dose = 3200 mg/dayMaximum dose = 3200 mg/day Self-medication is commonSelf-medication is common
Propionic AcidsPropionic Acids
KetoprofenKetoprofen OrudisOrudis Absorbed rapidly and completelyAbsorbed rapidly and completely Analgesia w/in 1 hr ~ last 3-4 hrsAnalgesia w/in 1 hr ~ last 3-4 hrs Upset stomach (dyspepsia) most Upset stomach (dyspepsia) most
common side effectcommon side effect
Propionic AcidsPropionic Acids
NaproxenNaproxen Aleve, Naprosyn, AnaproxAleve, Naprosyn, Anaprox Better patient tolerance than aspirin Better patient tolerance than aspirin
and indomethacinand indomethacin Aleve – loading dose of 440 mg followed Aleve – loading dose of 440 mg followed
by 220 mg 12 hr laterby 220 mg 12 hr later 660 mg daily max or 10 days of treatment660 mg daily max or 10 days of treatment
Half-life of 10-20 hr.Half-life of 10-20 hr.
Propionic AcidsPropionic Acids
FenoprofenFenoprofen NalfonNalfon GI irritation is commonGI irritation is common Taken w/ food decreases GI side effectTaken w/ food decreases GI side effect
Delays absorption, decreased peak plasma Delays absorption, decreased peak plasma concentrationconcentration
Analgesic effects w/in 15-30 m., lasts 4-Analgesic effects w/in 15-30 m., lasts 4-6 hr.6 hr.
Half-life = 2.5-3.0 hr, q 4-6 hr. Half-life = 2.5-3.0 hr, q 4-6 hr.
Carboxylic AcidsCarboxylic Acids
AspirinAspirin 11stst NSAID introduced NSAID introduced Prodrug – inactive until metabolized Prodrug – inactive until metabolized
into constituent partsinto constituent parts LiverLiver
Permanently binds to platelets ~ Permanently binds to platelets ~ producing anticoagulant effect up to 10 producing anticoagulant effect up to 10 daysdays
Each tablet = 325 mgEach tablet = 325 mg
Carboxylic AcidsCarboxylic Acids
DiflunisalDiflunisal DolobidDolobid Good anti-inflammatory and analgesic Good anti-inflammatory and analgesic
effectseffects Poor antipyreticPoor antipyretic Loading does of 1 g, followed by 500 mg Loading does of 1 g, followed by 500 mg
every 8-12 hours as neededevery 8-12 hours as needed
Adrenal Steroid Adrenal Steroid CompoundsCompounds
GlucocorticoidsGlucocorticoids Most frequently used Most frequently used
in athleticsin athletics Excellent anti-Excellent anti-
inflammatory responseinflammatory response Effects include: Effects include:
reduction of tissue reduction of tissue heat, reduction of heat, reduction of erythema, control of erythema, control of swelling, & swelling, & decreased local decreased local temperaturetemperature
GlucocorticoidGlucocorticoid
ActionAction Works by inhibiting prostaglandin and Works by inhibiting prostaglandin and
leukotriene productionleukotriene production Also impair function of macrophages and Also impair function of macrophages and
leukocytesleukocytes Side effects/precautionsSide effects/precautions
Catabolic effect not limited to target structuresCatabolic effect not limited to target structures Injection directly into ligament or tendon will Injection directly into ligament or tendon will
weaken structure for 2-6 weeksweaken structure for 2-6 weeks Repeated injections into a joint can lead to intra-Repeated injections into a joint can lead to intra-
articular degeneration and arthritis.articular degeneration and arthritis.
Types of GlucocorticoidsTypes of Glucocorticoids
CortisoneCortisone Short-acting (8-12 hr)Short-acting (8-12 hr) Often provided in pill form in a dose Often provided in pill form in a dose
packpack Long term use can be harmfulLong term use can be harmful Can be used to prevent/suppress Can be used to prevent/suppress
inflammation, and suppress immune inflammation, and suppress immune reactionsreactions
Types of GlucocorticoidsTypes of Glucocorticoids
HydrocortisoneHydrocortisone Administered orally, topically, or by Administered orally, topically, or by
injectioninjection Peak effect w/in 1-2 hrPeak effect w/in 1-2 hr Duration dependant on injection siteDuration dependant on injection site Average duration is 8-12 hrAverage duration is 8-12 hr
Types of GlucocorticoidsTypes of Glucocorticoids
PrednisonePrednisone Most commonly prescribed oral Most commonly prescribed oral
corticosteroidcorticosteroid 4x more potent than Hydrocortisone4x more potent than Hydrocortisone Intermediate actingIntermediate acting
Duration of action is 18-36 hr.Duration of action is 18-36 hr. Metabolized in liver to active form Metabolized in liver to active form
prednisoloneprednisolone
Types of GlucocorticoidsTypes of Glucocorticoids
DexamethasoneDexamethasone DecadronDecadron Anti-inflammatory and Anti-inflammatory and
immunosuppressive usesimmunosuppressive uses Administered enterally and parenterallyAdministered enterally and parenterally
Injection or iontophoresisInjection or iontophoresis Longest acting glucocorticoidLongest acting glucocorticoid
Duration of action from 1-3 daysDuration of action from 1-3 days