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Pronunciation |
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(au
RANE oh
fin) |
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U.S. Brand
Names |
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Ridaura® |
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Generic
Available |
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No |
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Pharmacological Index |
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Gold Compound |
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Use |
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Management of active stage of classic or definite rheumatoid arthritis in
patients that do not respond to or tolerate other agents; psoriatic arthritis;
adjunctive or alternative therapy for pemphigus |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Renal disease, history of blood dyscrasias, congestive heart failure,
exfoliative dermatitis, necrotizing enterocolitis, history of anaphylactic
reactions |
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Warnings/Precautions |
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NSAIDs and corticosteroids may be discontinued after starting gold therapy;
therapy should be discontinued if platelet count falls to
<100,000/mm3; WBC <4000, granulocytes <1500/mm3,
explain possibility of adverse effects and their manifestations; use with
caution in patients with renal or hepatic impairment |
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Adverse
Reactions |
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>10%:
Dermatologic: Itching, rash
Gastrointestinal: Stomatitis
Ocular: Conjunctivitis
Renal: Proteinuria
1% to 10%:
Dermatologic: Urticaria, alopecia
Gastrointestinal: Glossitis
Hematologic: Eosinophilia, leukopenia, thrombocytopenia
Renal: Hematuria
<1%: Angioedema, ulcerative enterocolitis, GI hemorrhage, gingivitis,
dysphagia, metallic taste, agranulocytosis, anemia, aplastic anemia,
hepatotoxicity, peripheral neuropathy, interstitial pneumonitis
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Overdosage/Toxicology |
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Symptoms of overdose include hematuria, proteinuria, fever, nausea, vomiting,
diarrhea; signs of gold toxicity include decrease in hemoglobin, leukopenia,
granulocytes and platelets, proteinuria, hematuria, pruritus, stomatitis or
persistent diarrhea; advise patients to report any symptoms of toxicity;
metallic taste may indicate stomatitis
Mild gold poisoning: Dimercaprol 2.5 mg/kg 4 times/day for 2 days or for more
severe forms of gold intoxication, dimercaprol 3 mg/kg every 4 hours for 2 days,
should be initiated; after 2 days the initial dose should be repeated twice
daily on the third day and once daily thereafter for 10 days; other chelating
agents have been used with some success |
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Drug
Interactions |
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Increased toxicity: Penicillamine, antimalarials, hydroxychloroquine,
cytotoxic agents, immunosuppressants |
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Stability |
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Store in tight, light-resistant containers at 15°C to
30°C |
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Mechanism of
Action |
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The exact mechanism of action of gold is unknown; gold is taken up by
macrophages which results in inhibition of phagocytosis and lysosomal membrane
stabilization; other actions observed are decreased serum rheumatoid factor and
alterations in immunoglobulins. Additionally, complement activation is
decreased, prostaglandin synthesis is inhibited, and lysosomal enzyme activity
is decreased. |
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Pharmacodynamics/Kinetics |
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Onset of action: Delayed; may require as long as 3 months
Duration: Prolonged
Therapeutic response may not be seen for 3-4 months after start of therapy
Absorption: Oral: ~20% gold in dose is absorbed
Protein binding: 60%
Half-life: 21-31 days (half-life dependent upon single or multiple dosing)
Time to peak serum concentration: Peak blood gold concentrations seen within
2 hours
Elimination: 60% of absorbed gold is eliminated in urine; remainder
eliminated in feces |
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Usual Dosage |
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Oral:
Adults: 6 mg/day in 1-2 divided doses; after 3 months may be increased to 9
mg/day in 3 divided doses; if still no response after 3 months at 9 mg/day,
discontinue drug
Dosing adjustment in renal impairment:
Clcr 50-80 mL/minute: Reduce dose to 50%
Clcr <50 mL/minute: Avoid use |
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Monitoring
Parameters |
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Monitor urine for protein; CBC and platelets; monitor for mouth ulcers and
skin reactions; may monitor auranofin serum levels |
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Reference Range |
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Gold: Normal: 0-0.1 mg/mL (SI: 0-0.0064
mmol/L); Therapeutic: 1-3
mg/mL (SI:
0.06-0.18 mmol/L); Urine: <0.1
mg/24 hours |
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Test
Interactions |
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May enhance the response to a tuberculin skin test |
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Mental Health: Effects
on Mental Status |
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None reported |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely produce agranulocytosis; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take exactly as directed. Drug effects may not be seen for as long as 3 weeks
to 3 months. You may experience metallic taste or mouth sores (frequent mouth
care and sucking lozenges may help); gray-blue color or irritation and reddening
of skin (avoid excessive exposure to sunlight; use sunscreen, sunglasses, and
protective clothing); nausea, bloating, or loss of appetite (small frequent
meals, chewing gum, or sucking on lozenges may help); or loss of hair
(reversible). Report unusual bruising; blood in mouth, urine, stool, vomitus;
persistent fatigue; persistent metallic taste; abdominal cramping, vomiting,
diarrhea; sores in mouth; skin rash or itching; or irritated or painful eyes.
Pregnancy/breast-feeding precautions: Inform prescriber if you are or
intend to be pregnant. Do not breast-feed. |
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Nursing
Implications |
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Discontinue therapy if platelet count falls
<100,000/mm3 |
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Dosage Forms |
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Capsule: 3 mg [29% gold] |
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References |
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Bell RA and Dale IM, "Gold Secretion in Maternal Milk," Arthritis
Rheum, 1976, 19(6):1374.
Bunch TW, "Gold Overdose Treated With BAL," Arthritis Rheum, 1974,
19(1):123-5.
Cook NJ, Owen ET, and Donlon JB,
"A Further Possible Cause of Diarrhoea Caused by Oral Gold," Br J
Rheumatol, 1995, 34(4):395-6.
Davis CM, "D-Penicillamine for the Treatment of Gold Dermatitis," Am J
Med, 1969, 46(3):472-6.
Fernandez-Herlihy L, "Requiem for Gold?" Ann Intern Med, 1991,
114(11):993-4.
Godfrey NF, Peter A, Simon TM, et al,
"I.V. N-acetylcysteine Treatment of Hematologic Reactions to Chrysotherapy,"
J Rheumatol, 1982, 9(4):519-26.
Kozloff M, Votaw M, and Penner JA,
"Gold-Induced Thrombocytopenia Responsive to Cyclophosphamide," South Med
J, 1979, 72(11):1490-2.
Parez MC, Gomez C, Mataix R, et al,
"Bone Marrow Splasia and Gold Salts. Report of Two Cases and Review of the Literature,"
Rev Clin Esp, 1995, 194:540-2.
Ulmeanu V, Toma M, Eugah B, et al,
"Severe Thrombocytopenia Following Treatment With Gold Salts," Clin Exp
Rheumatol, 12(Suppl 11):112. |
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