Anti-inflammatory Agents PDF

Antiinflammatory Agents  INFLAMMATION A response to tissue injury and infection A protective mechanism Fluid, elements of blood, leukocytes (WBCs), and chemical mediators accumulate at the injured tissue or infection site.  CARDINAL SIGNS OF INFLAMMATION REDNESS SWE...

Antiinflammatory Agents  INFLAMMATION A response to tissue injury and infection A protective mechanism Fluid, elements of blood, leukocytes (WBCs), and chemical mediators accumulate at the injured tissue or infection site.  CARDINAL SIGNS OF INFLAMMATION REDNESS SWELLING (EDEMA) HEAT PAIN LOSS OF FUNCTION  PROSTAGLANDINS CYCLOOXYGENASE (COX) Causes inflammation and pain at a tissue injury site  Antiinflammatory agents also relieve pain (analgesic), – Reduce elevated body temperature (antipyretic) – Inhibit platelet aggregation (anticoagulant) ASPIRIN is the oldest antiinflammatory drug Nonsteroidal Antiinflammatory Drugs (NSAIDs) NSAIDs are aspirin and aspirin-like drugs that inhibit the enzyme COX, which is needed for the biosynthesis of prostaglandins. Prostaglandin inhibitors Mild headaches and mildly elevated temp ASPIRIN IBUPROFEN (Advil, Motrin)  7 groups of NSAIDs 1. Salicylates 2. Para-chlorobenzoic Acid 3. Phenylacetic acid derivatives 4. Propionic acid derivatives 5. Fenamates 6. Oxicams 7. Selective COX-2 inhibitors  SALICYLATES ASPIRIN Acetylsalicylic acid (ASA) A prostaglandin inhibitor that decreases the inflammatory process Also an antiplatelet drug (for cardiac or cerebrovascular disorders) Common side effect: GASTRIC DISTRESS Take with food! EC – ENTERIC COATED ASPIRINS - doesn’t disintegrate in the stomach DO NOT CHEW OR CRUSH TABLET!  SALICYLATES DO NOT GIVE ASPIRIN TO CHILDREN WITH FLU SYMPTOMS (viral infection)! May cause the potentially fatal REYE SYNDROME (swelling in the liver and brain)  SALICYLATES Hypersensitivity to ASPIRIN: Tinnitus (ringing in the ears) Vertigo Bronchospasm (esp in asthma pts)  PARA-CHLOROBENZOIC ACID Used for rheumatoid arthritis, gouty arthritis, osteoarthritis Very irritating to the stomach, should be taken with food Indomethacin (Indocin) Sulindac (Clinoril) Tolmetin (Tolectin)  Phenylacetic acid derivatives Similar effects as aspirin, but it has minimal to no antipyretic effects. RA, osteoarthritis, ankylosing spondylitis Diclofenac Na (Voltaren, Voren) Ketorolac (Toradol) – first injectable NSAID – short-term mgmt of pain – For postsurgical pain  PROPIONIC ACID DERIVATIVES Aspirin-like but have stronger effects and create less GI irritation GI upset occurs, but not as severe as aspirin and indomethacin Ibuprofen (Advil, Motrin, Alaxan, Dolan) Naproxen (Naprosyn, Flanax, Skelan, Penles)  FENAMATES Used for acute and chronic arthritic conditions GI irritation CI: patients with Hx of peptic ulcer MEFENAMIC ACID (Ponstan, Dolfenal) Meclofenamate sodium monohydrate (Meclomen)  OXICAMS Long-term arthritic conditions, such as RA, osteoarthritis. Can also cause GI problems, but incidence is lower than other NSAIDs. Piroxicam (Feldene, Feldene Flash)  st General SE & AR for 1 Gen NSAIDs GASTRIC IRRITATION Na and water retention  nd 2 GEN: Selective COX-2 Inhibitors Protects the stomach lining Less GI upset Celecoxib (Celebrex) Parecoxib (Dynastat) CORTICOSTEROIDS  CORTICOSTEROIDS Prednisone Prednisolone Dexamethasone  DISEASE-MODIFYING ANTIRHEUMATIC DRUGS (DMARDS)  DMARDS When NSAIDs do not control immune-mediated arthritic disease sufficiently, although more toxic, can be prescribed to alter the disease process 1. Immunosuppressive agents 2. Immunomodulators 3. Antimalarials  Immunosuppressive Agents Used to treat refractory RA (arthritis that does not respond to antiinflammatory drugs) Azathioprine (Imuran) Cyclophosphamide (Cytoxan) Methotrexate (Mexate) Primarily used to suppress cancer growth and proliferation  Immunomodulators Treat to moderate to severe RA by disrupting the inflammatory process and delaying disease progression. Anakinra (Kineret) – administered subcutaneously Etanercept (Enbrel) - SQ Infliximab (Remicade) - IV Adalimumab (Humira) - SQ Leflunomide (Arava) - oral  ANTIGOUT DRUGS GOUT is an inflammatory condition that attacks joints, tendons, and other tissues. Gouty arthritis  Gouty arthritis The most common site of acute gouty inflammation is at the joint of the big toe Increase in urates (uric acid salts) and an accumulation of uric acid (hyperuricemia) or an ineffective clearance of uric acid by the kidneys Gout may appear as bumps or tophi, in the subcutaneous tissue of earlobes, elbows, hands, and the base of the large toe.  Gouty Arthritis Increase fluid intake while taking antigout drugs to promote uric acid excretion Causes: Foods high in purine (organ meats, sardines, salmon, gravy, herring, liver, meat soups) Alcohol (esp beer)  COLCHICINE Effective for acute gout attacks Not effective in decreasing inflammation occurring in other inflammatory disorders Causes GI irritation (taken with food) Stop giving if diarrhea occurs  Uric Acid Inhibitor Allopurinol (Zyloprim) – inhibits uric acid biosynthesis, lowers serum uric acid Used as prophylactic to prevent gout Increase fluids when taking this drug  Uricosurics Increase the rate of uric acid excretion Effective in chronic gout Probenecid (Benemid) May be taken with Colchicine NONOPIOID and OPIOID ANALGESICS  NONOPIOID ANALGESICS Less potent than opioid analgesics For mild to moderate pain ASPIRIN ACETAMINOPHEN IBUPROFEN NAPROXEN  Acetaminophen A nonopioid drug Not an NSAID Does not have the antiinflammatory properties of aspirin Tylenol Midol Vicodin Percocet  Acetaminophen Hepatotoxic – n/v, abd pain, diarrhea, elevated liver enzymes Nephrotoxic - oliguria ANTIDOTE: ACETYLCYSTEINE  OPIOID ANALGESICS Moderate to severe pain Obtained from the sap of seed pods of the opium poppy plant MORPHINE SULFATE – a potent opioid analgesic  Morphine SO4 Effective against acute pain from acute myocardial infarction (AMI), cancer, and dyspnea from pulmonary edema May be used as preoperative medication A/R: RESPIRATORY DEPRESSION! Orthostatic hypotension, urinary retention, constipation, miosis ANTIDOTE: ?  Morphine SO4 Monitor VS before and after, esp RR RR