Version May 2024
Auranofin contains gold and, like other gold-containing drugs, can cause gold toxicity, signs of which include: Fall in hemoglobin, leukopenia <4,000 WBC/mm3, granulocytes <1,500/mm3, decrease in platelets <150,000/mm3, proteinuria, hematuria, pruritus, rash, stomatitis or persistent diarrhea.
Like other gold preparations, auranofin is only indicated for use in selected patients with active rheumatoid arthritis.
Physicians planning to use auranofin should be experienced with chrysotherapy and should thoroughly familiarize themselves with the toxicity and benefits of auranofin.
The results of recommended laboratory work should be reviewed before writing each auranofin prescription. In addition, the following precautions should be routinely employed: The possibility of adverse reactions should be explained to patients before starting therapy and patients should be advised to report promptly any symptoms suggesting toxicity.
Rheumatoid arthritis: Oral: Initial: 6 mg/day in 1 or 2 divided doses; after 6 months may be increased to 9 mg/day in 3 divided doses; discontinue therapy if no response after 3 months at 9 mg/day
Note: Signs of clinical improvement may not be evident until after 3 months of therapy.
There are no dosage adjustments provided in the manufacturer’s labeling. The following guidelines have been used by some clinicians (Ref):
GFR 51 to 80 mL/minute: Administer 50% of dose.
GFR ≤50 mL/minute: Avoid use.
There are no dosage adjustments provided in the manufacturer’s labeling.
Refer to adult dosing.
(For additional information see "Auranofin: Pediatric drug information")
Juvenile idiopathic arthritis: Limited data available: Note: Due to lack of favorable prospective data, auranofin is no longer recommended as a preferred choice for treatment of juvenile idiopathic arthritis and no longer appears as a treatment option in the US guidelines (Ref). Reserve for patients intolerant to or unresponsive to other therapies.
Children ≥18 months and Adolescents ≤17 years: Oral: Initial: 0.1 to 0.15 mg/kg/day in 1 to 2 divided doses; usual maintenance: 0.15 mg/kg/day in 1 to 2 divided doses; maximum daily dose: 0.2 mg/kg/day or 9 mg/day. Note: With current market availability, may not be able to replicate the exact dosing used in trials; in trials, doses were rounded to nearest whole mg using 1 mg tablet (no longer available) (Ref).
There are no pediatric-specific recommendations; based on experience in adult patients, dosing adjustment suggested.
There are no dosage adjustments provided in the manufacturer's labeling. Use with caution; may increase risk of and/or symptoms of gold toxicity.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Dermatologic: Skin rash (24%), pruritus (17%)
Gastrointestinal: Diarrhea (≤47%), loose stools (≤47%), abdominal pain (14%), stomatitis (13%)
1% to 10%:
Dermatologic: Alopecia (1% to 3%), urticaria (1% to 3%)
Gastrointestinal: Nausea (10%), vomiting (10%), anorexia (3% to 9%), dyspepsia (3% to 9%), flatulence (3% to 9%), constipation (1% to 3%), dysgeusia (1% to 3%), glossitis (1% to 3%)
Genitourinary: Proteinuria (3% to 9%), hematuria (1% to 3%)
Hematologic and Oncologic: Anemia (1% to 3%), eosinophilia (1% to 3%), leukopenia (1% to 3%), thrombocytopenia (1% to 3%)
Hepatic: Increased serum transaminases (1% to 3%)
Ophthalmic: Conjunctivitis (3% to 9%)
<1%, postmarketing, and/or case reports: Agranulocytosis, aplastic anemia, angioedema, bronchitis (gold), corneal deposits, dysphagia, exfoliative dermatitis (other gold compounds), fever, gastrointestinal hemorrhage, gingivitis, hepatotoxicity, interstitial pneumonitis, jaundice, metallic taste, melena, neutropenia, pancytopenia, peripheral neuropathy, pure red cell aplasia, ulcerative enterocolitis
History of gold-induced disorders, including anaphylactic reactions, bone marrow aplasia, severe hematologic disorders, exfoliative dermatitis, necrotizing enterocolitis, or pulmonary fibrosis.
Concerns related to adverse effects:
• Dermatologic reactions: [US Boxed Warning]: Signs of gold toxicity include pruritus, rash, and stomatitis. Stomatitis and dermatitis are common reactions and may be serious (including exfoliative dermatitis). Pruritus and metallic taste may occur before dermatitis and oral mucous membrane reactions, respectively, and should be considered warning signs. Stomatitis may be manifested by shallow ulcers on the buccal membranes, on border of tongue, and on palate or in the pharynx; sometimes diffuse glossitis or gingivitis develops. Gold dermatitis may be aggravated by sunlight exposure, or an actinic rash may develop. Use with caution in patients with skin rash; may increase risk and/or symptoms of gold toxicity and toxicity may be more difficult to detect.
• Gastrointestinal effects: [US Boxed Warning]: Signs of gold toxicity include persistent diarrhea/loose stools, as well as nausea, vomiting, anorexia, abdominal cramps, and ulcerative enterocolitis (rare). Diarrhea may be managed with a dose reduction. Use with caution in patients with inflammatory bowel disease; may increase risk and/or symptoms of gold toxicity and toxicity may be more difficult to detect. In pediatric trials evaluating off-label use, diarrhea was the most common adverse effect (Giannini 1990). Monitor patients for GI bleeding.
• Hematologic effects: [US Boxed Warning]: Signs of gold toxicity include hematologic depression (decreased hemoglobin, leukocytes (WBC <4000/mm3), granulocytes (<1500/mm3), or decreased platelets (<150,000/mm3). Use with caution in patients with bone marrow depression; may increase risk and/or symptoms of gold toxicity and toxicity may be more difficult to detect. Therapy should be discontinued if signs and symptoms (eg, purpura, ecchymoses, petechiae) of thrombocytopenia develop or if platelet count falls to <100,000/mm3; therapy should not be reinitiated until thrombocytopenia resolves and if thrombocytopenia was not caused by the gold therapy.
• Hepatic effects: May be associated with the development of cholestatic jaundice (rare). Use with caution in patients with hepatic impairment; may increase risk and/or symptoms of gold toxicity and toxicity may be more difficult to detect.
• Pulmonary toxicity: May be associated with rare reactions, including gold bronchitis, interstitial pneumonitis and fibrosis; monitor closely.
• Renal effects: [US Boxed Warning]: Signs of gold toxicity include proteinuria and hematuria. Renal toxicity ranges from mild proteinuria to nephrotic syndrome or glomerulitis with proteinuria and hematuria. Use with caution in patients with renal impairment; may increase risk and/or symptoms of gold toxicity and toxicity may be more difficult to detect. Therapy should be discontinued promptly if proteinuria or microscopic hematuria develops.
Dosage form specific issues:
• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.
Other warnings/precautions:
• Appropriate use: [US Boxed Warning]: Use is only indicated in select patients with active rheumatoid arthritis.
• Experienced physician: [US Boxed Warning]: Physicians should be experienced with chrysotherapy and should be familiar with the toxicity and benefits of therapy.
• Monitoring: [US Boxed Warning]: Laboratory monitoring should be reviewed prior to each new prescription. The possibility of adverse reactions should be discussed with patients prior to starting therapy and patients should be advised to promptly report any symptoms suggesting toxicity. Disease states should be stable prior to initiating therapy.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Ridaura: 3 mg [contains fd&c blue #1 (brilliant blue), fd&c red #40 (allura red ac dye), fd&c yellow #6 (sunset yellow)]
No
Capsules (Ridaura Oral)
3 mg (per each): $31.32
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Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Ridaura: 3 mg
Oral: Take with or without food; some centers have recommended to administer with food if it causes GI upset.
Rheumatoid arthritis: Management of adult patients with active stage classic or definite rheumatoid arthritis who do not respond to or tolerate an adequate trial of full doses of one or more nonsteroidal anti-inflammatory drugs.
Ridaura may be confused with Cardura
None known.
There are no known significant interactions.
Adverse events were observed in animal reproduction studies.
Injectable gold salts have been detected in breast milk. Breastfeeding is not recommended by the manufacturer.
Patients should have baseline CBC with differential, platelet count, renal function tests, liver function tests, and urinalysis; CBC with differential, platelet count and urinalysis should also be monitored monthly during therapy. Monitor for GI bleeding. Skin and oral mucosa should be inspected for skin rash, bruising or oral ulceration/stomatitis. Specific questioning for symptoms such as pruritus, rash, stomatitis or metallic taste should be included.
The exact mechanism of action of gold is unknown; gold salts decrease cellular proliferation, reduce antibody and cytokine release, and inhibit collagenase action (Doan 2005).
Note: Due to rapid metabolism, the pharmacokinetics of auranofin are based on gold concentrations, not auranofin.
Onset of action: Delayed; therapeutic response may not be seen for 3-4 months after start of therapy, as long as 6 months in some patients
Duration: Prolonged
Absorption: Oral: ~25% gold in dose is absorbed
Protein binding: 60%
Metabolism: Rapid; intact auranofin not detectable in the blood
Half-life elimination (single or multiple dose dependent): 21 to 31 days
Time to peak, serum: ~2 hours (Blocka 1986)
Excretion: Urine (~60% of absorbed gold); remainder in feces
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