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ANTIINFLAMATORY

DRUG
PUTU PADMIDEWI WK., S.FARM,
APT.

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PROSTAGLANDIN .

OBAT-OBAT ANTIINFLAMASI NONSTEROID • BEKERJA DGN MENGHAMBAT ENZIM SIKLO-OKSIGENASE • YG PLG SERING DIGUNAKAN ADLH ASPIRIN .

ANTI INLAMATORY DRUGS ACETAMINOPHEN ACETAMINOPHEN ANTI INLAMATORY DRUGS ASPIRIN OTHER NON SELECTIVE NSAID COX-2 SELECTIVE INHIBITOR .

ANALGESIK ANTIINLAMASI KUAT ANTIINFLAMASI (-) ANTIINFLAMASI SEDANG/RINGAN SALICYLATE (aspirin) PYRAZOLONE (dipyrone) INDOL (indomethacine) ANILINE (Paracetamol) PROPIONIC ACID (Ibuprofen) ANTHRANICIL ACID (Mefenamic acid) ARYLACETIC ACID (Diclofenac) .

MECHANISM OF ACTON DISTURBANCE OF CELL MEMBRANES PHOSPOLIPIDS ARACHIDONIC ACID ASPIRIN CYCLOOXIGENASE ENDOPEROXIDASE PROSTAGLANDIN .

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EFFECTS • ANALGESIC • REDUCE THE MANIFESTATIONS OF INFLAMATION • ANTIPYRETIC • HOMEOSTATIC FUNCTION • REDUCE PROSTAGLANDIN-MEDIATED CYTOPROTECTION IN THE GASTROINTESTINAL TRACT .

yielding a peak plasma level with 1-2 hours .The salicylates Rapidly absorbed from the stomach and upper small intestine .Rapidly hydrolyzed to acetic acid and salicylat by esterases .excreted unchanged .PHARMACOKINETICS AND CLINICAL USE Aspirin • Pharmacokinetics .

stabilizing lysosome.Inhibiting the granulocytes adherence to damaged vasculature. inhibits platelet aggregation .Mechanisms of Action 1.Aspirin is nonselective inhibitor of both COX isoform .High doses (2400-4000 mg/d) . Anti-inflammatory Effects .Irreversibly. and inhibiting the chemotaxis of leucocytes and macrophages .

Probably mediated by both COX inhibition and inhibition of IL-1 4.Most effective in reducing pain of mild to moderate intensity . Antipyretic Effects . Antiplatelet Effects .Reduces elevated temperature .Single low doses (81 mg daily) .2.Intermediate (300-2400 mg/d) have antipyretic dan analgesic 3. Analgesic Effects .

High-dose for treatment of rheumatic fever. Antipyresis.Clincal Uses Analgesia. rheumatoid arthritis and other inflammatory join conditions . and Antiinflammatory Effects .Combined with opioid analgesics for treatment of cancer pain .For mild to moderate pain .

hyperpnea. gastric and duodenal uncers. tinnitus.Adverse Effects Usual dosage Gastric upset (intolerance). hepatotoxicity. rashes. decreased hearing and vertigo (rever). and renal toxicity Higher doses Salicylism. asthma. metabolic acidosis .

a second-generation COX-2 .120 mg for acute gouty arthritis .As effective as other NSAID . Celecoxib .Fewer endoscopic ulcer than NSAID .COX-2 SELECTIVE INHIBITOR 1.60 mg once daily for acute osteoarthritis . Etoricoxib .No more edema or renal effects 2.

3. osteoarthritis. Meloxicam .For treatment of rheumatic diseases. osteoarthritis.Therapeutic dose 7.5 mg/d . rheumatoid arthritis. rheumatoid arthritis 4. Rofecoxib For treatment of rheumatic diseases. analgesic and antipyretic 5. Valdecoxib A new highly selective cox-2 inhibitor Dosage is 20 mg twice daily No effect on platelet aggregation or bleeding time .

. Diclofenac Phenylacetic acid derivate A preparation diclofenac combining and misoprostol decreases gastrointestinal ulceration. Another combination of diclofenac and omeperazol for prevention of recurrent bleeding.NON SELECTIVE COX INHIBITORS 1.

0.1 % diclofenac for prevention of postoperative ophthalmic inflammation A topical gel containing 3 % diclofenac for solar keratoses Suppository form for preemptive analgesis and postoperative nausea .

Etodolac Acetic acid derivate More Cox-2 selective than most other NSAID. Diflunisial Diflunisial is derived from salicylat acid It undergoes an enterohepatic cycle Effective for cancer pain A 2 % diflunisial for pianful oral lession 3. with a cox-2:cox1 about 10 For post operative pain Less gastric toxicity .2.

Flurbibiprofen Propionic acid derivate Oral : 200-400 mg/d for gout. rheumatoid arthritis. Ibuprofen Phenylpropionat acid derivate Doses: < 240 mg daily for analgesic but antiinflammatory efficacy 400 mg efficacy in postsurgical dental pain Used to treat patent ductus arteriosus Anti-inflammatory effect = aspirin GI irritation and bleeding< aspirin . ankylosing spondylitis. neeck and nose surgery Topical: intraoperative miosis 5.4. osteoarthritis IV: for perioprative analgesia in minor ear.

Indomethacin Potent cox inhibitor. nephrotic syndrom. gingival inflammatory Adverse Effects abdominal pain. confusion. conjunctival inflammatory. ankylosing.6. reduce neutrophil migration. patent ductus arteriosus. decrease T cell and B cell proliferation Clinical use Gout. postepisiotomy pain. aplastic anemia . diabetes insipidus. inhibit phospholipase A and C. headache. trombocytopenia. dizziness. juvenile rheumatoid.

Ketoprofen Propionic acid derivate With probenecid elevates ketoprofen level and prolongs its plasma half-life The effectiveness at dosages 100300 mg/d .7.

Nabumetone Acetic acid derivate Prodrug. Mefenamic acid less effective than aspirin Not be used for longer than 1 week Should not be given to children 10. SE mirror of other NSAID .8. half-life more than 24 hours It may be less damaging to the stomach. Ketorolac For systemic use mainly as an analgesic Used to replace morphine Mild to moderate pain 9.

leukocytoclastic vasculitis and pseudoporphyria 12. Oxaprozin Propionic acid derivate Very long half-life (50-60 hours) Can be given once a day .11. Naproxen Naphthylpropionic acid derivate effective for the usual rheumatologic indications Gastrointestinal bleeding is low Rare case of allergic pneumonitis.

13. particularly the hematologic effect (aplastic anemia) Rarely used today 14. Phenylbutazone Pyrazolone derivate Its toxicities. decrease oxygen radical production and inhibits lymphocyte funtion Dosages higher than 20 mg/d. an increased incidence of peptic ulcer and bleeding . Piroxicam Oral: dosages 20 mg/d Used for the usual rheumatic indication High concentration also inhibits polymorphonuclear leukocyte migration.

15. agranulocytosis . trombocytopenia. Sulindac Sulfoxide prodrug Indication Rheumatic disease Suppresses familial intestinal polyposis Adverse effects Reversible renal failure and nephrotic syndrome.

Indomethacin is potent NSAID .2. Other NSAID .Naproxen and piroxicam half-life 1224 hours .Ibuprofen a half-life of about 2 hour .Are well absorbed after oral administration .

NONSELECTIVE COX INHIBITOR Used for the treatment of mild to moderate pain COX-2 inhibitors are primarily used in anflammatory disorders Selected NSAID are also used to treat other conditions (dysmenorrhea) .

TOXICITY 1. vertigo 2. COX-2-selective inhibitor Have reduce risk of gastrointestinal. hypersensitivity . nepritis. Aspirin Hypersensitivity. tinitus.Gastrointestinal disturbance.

Jelaskan sintesa prostaglandin dan dimana obat NSAID bekerja ! Jelaskan farmakokinetik. farmakodinamik dan toksisitas dari aspirin ! Jelaskan farmakokinetik. 5. farmakodinamik dan toksisitas dari non selective NSAID ! Jelaskan farmakokinetik. 3. 2. farmakodinamik. dan toksisitas dari COX-2 selective inhibitors ! Jelaskan mekanisme kerja dan toksisitas dari acetaminophen ! .LEARNING TASK 1. 4.