Over-the-counter management of inflammation

Lon Kilgore, Ph.D.
USA Weightlifting Regional Development Center Wichita Falls Weightlifting, Inc. Wichita Falls, Texas

Inflammation Defined
A localized protective response elicited by injury or destruction of tissues, which serves to destroy, dilute, or wall off both the injurious agent and the injured tissue. It is characterized in the acute form by the classical signs of pain, heat, redness, swelling and loss of function. Histologically, it involves a complex series of events, including dilatation of arterioles, capillaries, and venules, with increased permeability and blood flow, exudation of fluids, including plasma proteins, and leukocytic migration into the inflammatory site.

00 Moderate Work Moderate Work Maximal Work Light Work High Pain 1 4 10 Time in Weeks 13 7 16 S1 .00 5.50 7.00 7.50 5.Reduction in work capacity American Academy of Orthopedic Surgeon epidemiological study reported 79% of recreational weight-trainers listed inflammation as their most common injury Frequency of occurrence in athletes … Low Pain P A I N 10.50 8.00 6.Symptoms of Inflammation Pain – Swelling .50 6.00 9.00 8.50 9.

bradykinin. TNF. serotonin. PDGF Acute: Injury Pain Repair Clean-up Chronic: Tissue destruction Pain Disability .Sequence of Inflammatory Events Stage 1 – Acute inflammation Initial response to injury Release of histamine. leukotrienes Stage 2 – Immune response Activation of immune cells (leukocytes) Can be directed at pathogen or self Stage 3 – Chronic inflammation Release of interleukins. GMCSF. interferons. prostaglandins.

More intense training may be more stressful. 2004 .. From Sun et al.Inflammatory Events Findings: Increased force of shock increases transcription of collagenase and gelatinase genes in synovial cells Interpretation: Training may disrupt joint homeostasis.

Diagnosis of Inflammation Pain Swelling Reduction in work capacity Reduced mobility ESR CRP CK AST ALT Myoglobinurua .

.Inflammatory Cells and Competition Leukocytes 12 10 9 Lymphocytes Neutrophills /L Cell counts x 10 8 6 4 2 0 Pre Post 2 24 48 72 WBC numbers followed pattern of work induced leukocytosis described as early as 1901.

100 1.500 1 Pre 2 Post 3 2h Time 4 24h 5 48h 6 72h FINDINGS: CRP concentrations are significantly elevated at 72 hours after competition (p=0.900 2.900 1.300 2.C-Reactive Protein Response to Competition 2.04) INTERPRETATION: Inflammation occurs following competition .500 [CRP] 2.700 2.700 1.

Inflammatory Cell Response to Training FINDINGS: Although not statistically significant. monocyte numbers went down INTERPRETATION: May indicate that training was stressful enough to cause exodus of monocytes from the blood in order to clean up and repair damaged tissue (inflammation) .

5 3 2.47) INTERPRETATION: Lots of training is potentially more inflammatory than very hard training .5 5 4.5 1 1 Pre 2 Week1 3 Week 2 4 Week 3 5 Week 4 6 Week 5 FINDINGS: CRP was strongly correlated to training volume (r=0.5 4 [CRP] 3.74) and mildly correlated to intensity (r=0.C-Reactive Protein Response to Training 5.5 2 1.

Inflammation in Power Athletes Since these athletes work and play very hard … high volumes … high intensity … lots of compressive forces … it’s a sure bet inflammation occurs .

Countermeasures to inflammation Typical Recommendations: Rest Ice Compression Elevation .

Countermeasures to inflammation Non-steroidal anti-inflammatory drugs Aspirin Acetominophen Ibuprofen Naproxen Ketoprofen .

LTD4. LTE4 Thromboxane TXA2 Hydroxyeicosa tetranoic acid (HETE) Leukotrienes Different NSAIDs block COX by different mechanisms (Tylenol vs.Non-steroidal anti-inflammatory drug action Phospholipid PhospholipaseA2 Glucocorticoids Arachidonic Acid NSAID Cyclooxygenase Lipooxygenase COX-1. PGE2. LTB4. PGF2α. Aspirin) Different NSAIDs structure and action contribute to differing effectiveness (Ibuprofen 20-30 times more effective than simple aspirin) . LTC4. COX-2 Cyclic Endoperoxides Hydroperoxy Eicosatetranoic Acid Prostaglandins PGD2. PGI2 LTA4.

increased risk of Reye's disease (serious liver & neurological disease) Signs of Taking Too Much Aspirin Tinnitus.Effectiveness of NSAIDs Aspirin (acetylsalicylic acid) Most common "salicylate" analgesic 1. impaired hearing. flu or chicken pox. In those <16 yr with virus. thirst. anti-pyretic (anti-fever) 3. confusion Recommended Dosage: 325-650 mg 4-6 times per day Lethal Dosage: 20 g/day . anti-skin cancer effects Adverse Effects of Aspirin 1. Anticoagulant effect may be undesirable 4. analgesic for mild to moderate pain 2. has anti-colon cancer. Causes stomach irritation & bleeding 3. anti-inflammatory Also: anticoagulant action (used to prevent heart attack or stroke due to clots). rapid breathing. nausea & vomiting.

Effectiveness of NSAIDs Acetaminophen (Tylenol. "non-aspirin pain reliever") • • • • • • Same potency as aspirin Equal analgesic & antipyretic action Not anti-inflammatory or anticoagulant Less gastric distress & tinnitus. but more damaging to liver with heavy use Can be used by those with aspirin allergy. No risk of Reye’s syndrome in kids Recommended Dosage: 325-650 mg 4-6 times per day Lethal Dosage: 15-20 g/day .

Advil) 1. More effective for certain conditions (inflammation.Effectiveness of NSAIDs Ibuprofen (e. dental pain) 3. Weaker anticoagulant effect than aspirin 4. More potent than aspirin or acetominophen (take less) 2. dysmenorrhea. sports injuries. joint problems.g. Motrin. GI irritant 5. 5000 count observation – increased likelihood of death from end-stage renal failure Boots 7268 Weed killer turned Pain killer Recommended Dosage: 200 mg 4-6 times per day Toxicity: 8 g/day results in hospitalization .

Naproxen sodium is absorbed faster. Absorbed more slowly (peaks in 2-4 hrs) & stays longer (binds to proteins in the blood). Recommended Dosage: 3.Effectiveness of NSAIDs Naproxen (OTC Aleve. If taken regularly.5 g/day caused hospitalization LD50 in dogs 100 mg/kg . PDR states that pain relief lasts UP TO 7. blood levels will be maintained by taking just 2 doses a day.8 hrs BUT FDA pushed 12 hr OTC dosing to limit risks. 2. Stronger stomach irritation compared to other NSAIDs & should be avoided by those with kidney disease. 200 mg 2 times per day Toxicity: 27. Uses lower dosage Naproxen’s Time course 7. 3. Very similar to ibuprofen but somewhat different time course 2. Naprosyn or Anaprox) 1.

Effectiveness of NSAIDs Ketoprofen (e. Same analgesic/anti-inflammatory family More potent. Actron) 2. 3. Orudis.5 mg 2 times per day Toxicity: 5000 mg/day may induce GI symptoms . but otherwise not different in its effects/risks from other NSAIDs (about 1% incidence of some side effect) Recommended Dosage: 12.g.

Other considerations for NSAID useage Increased appetite Reduced hypertrophy Additives Caffeine Diuretics Ephedra (*) .

Alternative therapeutic measures Lesson from Chinese herbal medicine • Prepared cartilage • Collagen OK … as long as the active agent is “unknown” some dork is still gonna be poppin’ chicken beaks so he can freakin’ squat! • Glucosamine • Chondroitan Sulfate .

Mechanism of Effect Glucosamine Sulfate and Chondroitan Sulfate Component of Glycosaminoglycans Extra-cellular matrix Growth factor mediation Shock absorption Stabilization of cell membrane .

5 g/day and 400-800 mg/day respectively .Effectiveness of Glucosamine & Chondroitan • Incorporated into cartilage in about 4 hours • Stimulates proteoglycan synthesis • Virtually no data on athletes BUT • Arthritics has a 72% pain reduction by 7 days of supplementation • Has proven to be more effective than Ibuprofen with chronic use • Residual effect for up to 30 days after cessation • Potentially may slow joint erosion or augment repair Recommended Dosage: 1.

An Apple a Day … Flavonoids – Anti-oxidant neutraceuticals Apples (120 mg) Onions (35 mg) Chocolate (510 mg) Potato (8 mg) Tea (69 mg) Wine (40-150 mg) Beer (10-50 mg) Elderberry Juice (570 mg) Content per 100g or 100ml .

LTE4 Thromboxane TXA2 Hydroxyeicosa tetranoic acid (HETE) Leukotrienes . LTD4. PGI2 LTA4. PGF2α. PGE2.Summary and Recommendations Phospholipid PhospholipaseA2 Glucocorticoids Arachidonic Acid NSAID Cyclooxygenase Lipooxygenase COX-1. COX-2 Cyclic Endoperoxides Hydroperoxy Eicosatetranoic Acid Prostaglandins PGD2. LTC4. LTB4.

consult a physician before using “prescription” doses OR get them to prescribe COX2 inhibitors to maximize relief to risk (Celebrex. etc. .) Satellite cell activity suppression – As only about 5% of muscular hypertrophy is derived from SC activity. it is likely more important to manage pain and train than to reduce loading and not use NSAIDs.Summary and Recommendations All OTC NSAIDs are effective at reducing pain and or inflammation All OTC NSAIDS are COX inhibitors and carry with them a variety of side effects Tylenol has the lowest effect on inflammation Naproxen and Ketoprofen reduce the chance for side effects and are least toxic of the OTC drugs If maximal doses of OTC NSAIDs are ineffective.

Summary and Recommendations Consider using glucosamine or chondroitan sulfate as an adjunct to NSAID therapy Not appropriate for acute inflammation Not appropriate for intermittent use Action is long lasting and as effective at reducing pain as NSAIDs May actually assist in tissue repair May reduce the amount of NSAIDs consumed .

Consumption has both risk and benefit 2 – 12 oz servings for males 1 – 12 oz serving for females .Summary and Recommendations Pay attention to fruit and vegetable consumption Consider decaffeinated tea Consider wine and beer consumption carefully.