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PHARMACOLOGICAL ASPECT OF ANTI-HYPERURICEMIC DRUGS Department of Pharmacology

K - FARMAKOLOGI OBAT ANTI HIPERURICEMIA.pptx

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PHARMACOLOGICAL ASPECT OF ANTI-

HYPERURICEMIC DRUGSDepartment of Pharmacology

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Learning objectives

To Explain Classification of the anti hyperuricemic

drugs.Pharmacological Aspect of anti

hyperuricemic drugsPrinciples of clinical Use of anti

hyperuricemic drugs

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Uric acidProblems

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↑uric acid

level

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DRUGS USED IN TEATMENT OF HYPERURICEMIA

Target : lowering the uric acid level below the saturation point (<6 mg/dL), interfering with uric acid synthesis

allopurinol increasing uric acid excretion

Probenecid Sulfinpyrazone Large doses of aspirin

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Inhibition of uric acid synthesis

ALLOPURINOL

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Mechanism of action

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80%-completely absorbed after oral administration.

Metabolized to active metabolite alloxanthine (oxypurinol).

Plasma Half-life allopurinol 2 hour, while oxypurinol 15 hour

Given once daily.Drug & its metabolite are excreted in the feces & urine.

Pharmacokinetics

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Gout arthritisChronic tophaceous deposits (reabsorption

is more rapid)High serum uric acid in patients with

impaired renal functionsuric acid stones or nephropathyused to prevent increased uric acid levels

in patients receiving cancer chemotherapy

Clinical Uses

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exacerbation of an acute attack of goutHypersensitivity:

Maculopopular skin rashnausea, diarrheaBody : fever, headacheCVS : vasculitisThrombocytopeniaEpistaxis

SIDE EFFECT

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With oral anticoagulant: ◦ Potentiates warfarin and dicumarol inhibits their metabolism in

liver With anticancer :

◦ 6-mercaptopurine and azathioprine inhibits their metabolism (doses are reduced up to 75%

With ampicillin : ◦ Increases frequency of skin rash

Prolongs half life of Chlorpropamide• both compete for excretion in renal tubule

DRUG INTERACTION

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DRUG INCREASE URIC ACID EXCRETION : Uricosuric

Probenecid SulfinpyrazoneLarge doses of aspirin

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 Probenesid increases uric acid excretion in the urine

Sulfinpyrazone metabolite of phenylbutazone Metabolized into an active

metabolite in the liver.

URICOSURIC DRUGS

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Uricosuric drugs ( probenecid, sulfinpyrazone, large dose of aspirin) block the active transport sites of the proximal tubules(middle segment ) the re-absorption of uric acid is decreased.

Mechanism of action

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Should not be started until 2-3 weeks after an acute attack of gout.

In chronic gout when :◦Evidence of tophi appears◦Plasma levels of uric acid are so high that may cause tissue damage

Clinical uses

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Urine volume should be maintained at a high level, and urinary pH kept alkaline .

Probenecid is a general inhibitor of the tubular secretion of organic acids , so it is used to prolong action of other weak organic acids as some antibiotics ◦e.g. penicillin.

Clinical uses ( continue)

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Probenecid prolong the action of some antibiotics as: penicillin and cephalosporins (result from block tubular secretion)

Probenecid also inhibit excretion of Naproxen, ketoprofen and Indomethacine

DRUG INTERACTIONS

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Acute attack of gout Risk of uric acid stone GIT upset Allergic rash Nephrotic syndrome ( probenecid) Aplastic anemia ( not common )

Side effects

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History of urinary tract stone

Impaired renal functionRecent acute gouty attackAdministration of low doses of aspirin

Contra-indications

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TERIMA KASIH