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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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