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Chapter 48
Integrative Inflammation Pharmacology: Gout
11
Pharmacology
Professional
03/30/2012

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Term
Colchicine
Definition
Mech: Inhibits microtubule formation by binding to tubulin, inhibiting cell movement and division; Inhibits neutrophil activation
APP: Acute Gout, Prevention of recurrent Gout
AE: Myelosuppression and neuropathy
CI: Severe cardiac, GI (due to decreased epithelial turnover), or Renal Disease
CI: Hepatic Failure and Blood dyscrasias
TC: DOSE SHOULD BE LOWERED WHEN ADMINISTERED WITH CYCLOSPORINE, TACROLIMUS, and /or VERAPAMIL
Term
Prednisone
Definition
Mech: Mimic cortisol function by acting as glucocorticoid receptor
APP: Acute polyarticular Gout
AE: Immunosupression, cataracts, anything that excess cortisol causes
CI: Systemic fungal infection
Term
Methylprednisolone
Definition
Mech: Mimic cortisol function by acting as glucocorticoid receptor
APP: Acute polyarticular Gout
AE: Immunosupression, cataracts, anything that excess cortisol causes
CI: Systemic fungal infection
TC: MAY BE INJECTED INTO AN INFLAMED JOINT FOR TREATMENT OF ACUTE GOUT
Term
Allopurinol and Oxypurinol (product of Allopurinol degradation)
Definition
Mech:Inhibit Xanthine Oxidase (structural analog of Xanthine)
APP: Chronic Gout, Cancer related hyperurecemia, Calcium and uric acid renal calculus
AE: Agranulocytosis, Aplastic Anemia, Renal Failure, Hepatic Necrosis, SJ Syndrome, and Toxic epidermal necolysis
CI: Idiopathic hemochromatosis
TC: Increase levels of Azathiopine and 6-mercaptupurine
TC: AMOXICILLIN, AMPICILLIN, AND THIAZIDE DIURETICS MAY CAUSE SEVER RASH
TC: NEVER ADMINISTER DURING AN ACUTE ATTACK!!!
TC: SHOULD BE ADMINISTERED WITH NSAID OR COLCHICINE FOR FIRST 4-6 MONTHS
Term
Febuxostat
Definition
Mech: Inhibit Xanthine Oxidase
APP: Prevention of recurrent Gout
AE: Myocardial infarction, stroke, Abnormal liver enzymes
CI: Cannot use with MERCAPTOPURINE THEOPHYLLINE, OR AZATHIOPRINE
TC: SHOULD BE USED WITH COLCHICINE
Term
Sulfinpyrazone
Definition
Mech: Inhibits renal tubule URAT1 and other transporters, increasing Uric acid secretion
APP: Prevention of recurrent Gout
AE: Leukopenia, Thrombocytopenia, Bronchoconstriction in patients with Gout
CI: Acute Gout Attack, Uric acid kidney stones
TC: Increase levels of penicillin and other organic anions
TC: HAS ANTI-PLATELET EFFECTS
Term
Probenecid
Definition
Mech: Inhibits renal tubule URAT1 and other transporters, increasing Uric acid secretion
APP: Prevention of recurrent gout and chronic hyperurecemia
AE: Thrombocytopenia, bronchoconstriction, APLASTIC ANEMIA, HEPATIC NECROSIS, ANAPHYLAXIS AND KIDNEY STONES
CI: Acute gout attack, uric acid kidney stones
TC: INCREASES levels of PENICILLIN and serum levels of METHOTREXATE
Term
Losartan
Definition
Mech: Angiotension II receptor antagonist
APP: Hypertension and prevention of recurrent gout
AE: Angioedema, rhabdomyolysis
CI: Pregnancy
Term
Rasburicase
Definition
Mech: converts soluble urate to more solluble allantoin
APP: TUMOR LYSIS SYNDROME
AE: Hemolysis, methemoglobinemia, neutropenia, respiratory distress, sepsis, fever
CI: G6PD déficience or aspergillus sensitivity
TC: RECOMBINANT FORM OF ASPERGILLUS URICASE
Term
Pegloticase
Definition
Mech: converts soluble urate to more solluble allantoin
APP: TREATMENT OF GOUT UNRESPONSIVE TO STANDARD TREATMENTS
AE: Hemolysis, methemoglobinemia, neutropenia, respiratory distress, sepsis, fever
CI: G6PD déficience or aspergillus sensitivity
TC: MANUFACTURED URICASE WITH A LONGER HALF LIFE
Term
Indomethacin
Definition
Mech: Inhibit COX, preventing prostaglandin and thromboxane synthesis
APP: Acute Gout attacks
AE: Bleeding, salt and water retention, and renal insufficiency
TC: HAVE TO DECIDE BETWEEN THIS DRUG AND COLCHICINE
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