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Auranofin

Pronunciation

(au RANE oh fin)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Ridaura: 3 mg [contains benzyl alcohol]

Brand Names: U.S.

  • Ridaura

Pharmacologic Category

  • Gold Compound

Pharmacology

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.

Absorption

Oral: ~25% gold in dose is absorbed

Metabolism

Rapid; intact auranofin not detectable in the blood

Excretion

Urine (~60% of absorbed gold); remainder in feces

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

Time to Peak

Serum: ~2 hours

Duration of Action

Prolonged

Half-Life Elimination

Single or multiple dosing dependent: 21-31 days

Protein Binding

60%

Use: Labeled Indications

Management of active stage classic or definite rheumatoid arthritis in patients who do not respond to or tolerate other agents

Contraindications

History of severe toxicity to gold compounds including anaphylaxis, bone marrow aplasia, severe hematologic disorders, exfoliative dermatitis, necrotizing enterocolitis, or pulmonary fibrosis.

Dosage

Oral: Adults: 6 mg/day in 1-2 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.

Dosage adjustment in renal impairment: There are no dosage adjustments provided in the manufacturer’s labeling. The following guidelines have been used by some clinicians (Aronoff, 2007):

CrCl 50-80 mL/minute: Reduce dose to 50%

CrCl <50 mL/minute: Avoid use

Dosage adjustment in hepatic impairment: No dosage adjustment provided in manufacturer’s labeling.

Storage

Store at 15°C to 30°C (59°F to 86°F). Protect from light.

Drug Interactions

There are no known significant interactions.

Test Interactions

May enhance the response to a tuberculin skin test

Adverse Reactions

>10%:

Dermatologic: Rash (24%), pruritus (17%)

Gastrointestinal: Diarrhea/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%)

Hematologic: Anemia (1% to 3%), eosinophilia (1% to 3%), leukopenia (1% to 3%), thrombocytopenia (1% to 3%)

Hepatic: Transaminases increased (1% to 3%)

Ocular: Conjunctivitis (3% to 9%)

Renal: Proteinuria (3% to 9%), hematuria (1% to 3%)

<1% (Limited to important or life-threatening): Agranulocytosis, aplastic anemia, angioedema, corneal deposits, dysphagia, enterocolitis (ulcerative), fever, GI hemorrhage, gingivitis, gold bronchitis, hepatotoxicity, interstitial pneumonitis, jaundice, metallic taste, melena, neutropenia, pancytopenia, peripheral neuropathy, pure red cell aplasia. Note: Exfoliative dermatitis has been reported with other gold compounds.

ALERT: U.S. Boxed Warning

Gold toxicities:

Auranofin contains gold and, like other gold-containing drugs, can cause gold toxicity, signs of which include: Fall in hemoglobin, leukopenia <4000 WBC/mm3, granulocytes <1500/mm3, decrease in platelets <150,000/mm3, proteinuria, hematuria, pruritus, rash, stomatitis or persistent diarrhea.

Appropriate use:

Like other gold preparations, auranofin is only indicated for use in selected patients with active rheumatoid arthritis.

Experienced physician:

Physicians planning to use auranofin should be experienced with chrysotherapy and should thoroughly familiarize themselves with the toxicity and benefits of auranofin.

Monitoring:

Therefore, 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. Patients should be advised to report promptly any symptoms suggesting toxicity.

Warnings/Precautions

Concerns related to adverse effects:

• Dermatologic reactions: [US Boxed Warning]: Signs of gold toxicity include pruritus, rash, and stomatitis. Dermatitis and lesions of the mucous membranes are common and may be serious; pruritus may precede the early development of a skin reaction and a metallic taste may precede oral mucous membrane reactions. Dermatitis may be aggravated by sun exposure. 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 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.

• Hematologic effects: [US Boxed Warning]: Signs of gold toxicity include hematologic depression (decreased hemoglobin, leukocytes (WBC <4000/mm3), granulocytes (<1500/mm3), or platelets (<150,000/mm3). Symptoms of gold toxicity may be difficult to detect in patients with prior abnormalities. 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. 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 interstitial 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. 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 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 risks 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 initiation and patients should be advised to report any symptoms indicating toxicity. Disease states should be stable prior to initiating therapy.

Monitoring Parameters

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. 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. Dosing should be withheld in patients with significant gastrointestinal, renal, dermatologic, or hematologic effects (platelet count falls to <100,000/mm3, WBC <4000, granulocytes <1500/mm3

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience abdominal pain, lack of appetite, nausea, vomiting, flatulence, or mouth sores. Have patient report immediately to prescriber loss of strength and energy; bruising; bleeding; blood in the urine; itching; rash; severe diarrhea; signs of infection; black, tarry, or bloody stools; vomiting blood or vomit that looks like coffee grounds; urine discoloration; jaundice; shortness of breath; vision changes; eye pain; or eye irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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