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8/14/2019 Analgesic Anti Pyre Tic Agents Piatos
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ANALGESIC-ANTIPYRETICANALGESIC-ANTIPYRETICAGENTS;AGENTS;
PHARMACOTHERAPY OFPHARMACOTHERAPY OF
GOUTGOUTby:
Edgar Allan A. Piatos,Edgar Allan A. Piatos,
M.D.M.D.
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NSAIDSNon Steroidal Anti-Inflammatory DrugsMechanism of Action:
Inhibit cyclooxygenase enzymeCOX-1
COX-2
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Therapeutic Effects:
b. Pain- effective in pain of low to
moderate intensity
- do not change perception ofsensory modalities other than
pain
b. Fever
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Other Clinical Uses:
Systemic Mastocytosis
Bartters Syndrome
Cancer Chemoprevention
Niacin Tolerability
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Adverse Effects of NSAID Therapy:
Gastrointestinal
- Ulcers
Cardiovascular
- Myocardial Infarction; StrokeBlood Pressure, Renal, Renovascular
Adverse Events
- Retention of salt and waterAnalgesic Nephropathy
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Pregnancy and lactation
- Prolongation of gestation
- Increase risk of
postpartum hemorrhageHypersensitivity
Aspirin Resistance
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Drug Interactions
Concomitant NSAIDS and Low DoseAspirin
- increase likelihood of
gastrointestinal adverse events
ACE Inhibitors
- attenuate effectiveness of ACE
inhibitorsCorticosteroids/Warfarin
- increase incidence of bleeding
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SALICYLATES
Pharmacological Properties Analgesia
Antipyresis
Respiration Acid-Base and Electrolyte Balance and
Renal Effects
Cardiovascular Effects Gastrointestinal Effects
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Hepatic Effects
Uricosuric Effects
Effects on the Blood
Metabolic Effects
* Oxidative phosphorylation* Carbohydrate metabolism
Endocrine Effects
Salicylates and Pregnancy Local Irritant Effects
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Therapeutic Effects:
AntipyresisAnalgesia
Rheumatoid Arthritis
Inflammatory Bowel Disease
Salicylate Intoxication
Coma; ConvulsionsCardiovascular Collapse
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Salicylism:
Headache; dizziness; tinnitus; difficultyof hearing
Treatment of Salicylate Poisoning:
AirwayBreathing
Circulation
Decontamination
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DIFLUNISAL
Difluorophenyl derivative of salicylicacid
Devoid of antipyretic effects
Osteoarthritis, musculoskeletal strainsor sprains
No auditory side effects
Less gastrointestinal and platelet effects
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PARAAMINOPHENOL DERIVATIVES:
ACETAMINOPHEN
Active metabolite of phenacetin
Weak anti-inflammatory effects
No effect on CVS, respiratory systems,on platelets and coagulation
No acid-base changes or uricosuric
effects
Does not produce gastric irritation
Associated with hepatic necrosis
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ACETIC ACID DERIVATIVES
b. INDOMETHACIN
* more potent inhibitor of COX thanaspirin
* does not interfere with uricosuric
effects of probenecid* platelet inhibition; gastric irritation
* antagonizes the natriuretic and anti-
hypertensive effects of diuretics,betablockers, ACE inhibitors, AT1receptor antagonists
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* ankylosing spondylitis,
osteoarthritis, acute agout* closusre of persistent PDA
Adverse Effects
Gastrointestinal
Frontal headache
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c. ETODOLAC
- COX-2 selective- uricosuric
- osteoarthritis
-rheumatoid arthritis
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FENAMATES
(Mefenamic, Meclofenamic,Flufenamic Acid)
Pain in soft tissue injuries
Dysmenorrhea
Rheumatoid arthritis
osteoarthritis
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TOLMETIN
Osteoarthritis; Rheumatoid Arthritis
Juvenile Rheumatoid Arthritis
Ankylosing Spondylitis
KETOROLAC
Parenteral administration
Greater analgesic than anti-inflammatory activity
Short-term alternative to opoiodsUsed widely in post-operative patients
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DICLOFENAC
Most commonly used NSAID in EuropePotent against COX-2
Rheumatoid Arthritis; Osteoarthritis;
Ankylosing SpondylitisAcute musculoskeletal pain
Post-operative pain
Dysmenorrhea
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PROPIONIC ACID DERIVATIVES
IBUPROFEN NAPROXENFENOPROFEN KETOPROFEN
FLURBIPROFEN OXAPROZIN
- Rheumatoid Arthritis; Osteoarthritis- Ankylosing Spondylitis; Bursitis
- Acute Tendinitis
- Acute Gouty Arthritis
- Primary Dysmenorrhea
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ENOLIC ACIDS (OXICAMS)
PIROXICAMMELOXICAM
NABUMETONE
PYRAZOLON DERIVATIVESPHENYBUTAZONE OXYPHENBUTAZONE
ANTIPYRINE AMINOPYRINE DIPYRONE
- associated with agranulocytosis
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CYCLOOXYGENASE 2
SELECTIVE NSAIDSCELECOXIB VALDECOXIB
ROFECOXIB PARECOXIB
LUMIRACOXIB ETORICOXIB
OTHER NSAIDS APARAZONE NIMESULIDE
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PHARMACOTHERAPY OF GOUT
COLCHICINE
Acute Gout
Familial Mediterranean Fever
ALLOPURINOL
Most commonly used antihyperuricemicagent
Primary hyperuricemia of gout
Hyperuricemia secondary toPolycythemia Vera, MyeloidMetaplasia, Blood Dyscrasias
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RASBURICASE
Recombinant urate-oxidaseLowers urate levels more effectively
than allopurinol
Pediatric patients with leukemia,lymphoma, solid tumor
malignancies
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URICOSURIC AGENTS
PROBENECID
SULFINPYRAZONE
BENXBROMAZONE
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