auranofin

Absorption: 20–25% absorbed from the GI tract.

Distribution: Widely distributed; appears to concentrate in arthritic joints more than in uninvolved joints. Enters breast milk.

Metabolism/Excretion: 60% of absorbed dose slowly excreted by the kidneys; 40% of absorbed dose excreted in the feces.

Half-Life: 26 days in blood, 40–128 days in tissue.

Time/Action Profile ⬆ ⬇

(anti-inflammatory activity)

ROUTE	ONSET	PEAK	DURATION
PO	3–6 mo	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Previous gold toxicity (e.g. anaphylaxis, necrotizing enterocolitis, pulmonary fibrosis, exfoliative dermatitis, bone marrow aplasia, hematologic disorders);
OB: Potential for congenital anomalies;
Lactation: Appears in breast milk. Use formula or discontinue auranofin.

Use Cautiously in:

History of blood dyscrasias;
Rashes;
Severe hepatic or renal dysfunction;
Inflammatory bowel disease;
Patients taking other immunosuppressant drugs;
Pedi: Efficacy and safety not established.

Adv. Reactions/Side Effects ⬆ ⬇

CV: bradycardia

Derm: dermatitis, pruritus, rash, alopecia, photosensitivity reactions, urticaria

EENT: conjunctivitis, corneal gold deposition

GI: abdominal pain, cramping, diarrhea, stomatitis, ↑liver enzymes, flatulence, anorexia, difficulty swallowing, dyspepsia, GI BLEEDING, gingivitis, glossitis, metallic taste, nausea, vomiting

GU: hematuria, proteinuria,

Hemat: AGRANULOCYTOSIS, anemia, APLASTIC ANEMIA, eosinophilia, leukopenia, thrombocytopenia

Neuro: peripheral neuropathy

Resp: bronchitis, pneumonitis, pulmonary fibrosis

Misc: ANGIOEDEMA, ANAPHYLAXIS ALLERGIC REACTIONS, INCLUDING

Interactions ⬆ ⬇

Drug-drug:

Bone marrow toxicity may be additive with other myelosuppressive agents (antineoplastics, radiation therapy, azathioprine) or high doses of corticosteroids.
Concurrent use with penicillamine↑ the risk of adverse hematologic or renal reactions.
May ↑ blood levels of phenytoin.

Route/Dosage ⬆ ⬇

PO (Adults ): 6 mg/day in 1–2 doses; may ↑ to 9 mg/day in 3 divided doses if no improvement after 6 mo.

Availability ⬆ ⬇

Assessment ⬆ ⬇

Assess range of motion and degree of swelling and pain in affected joints before and periodically throughout therapy.

Lab Test Considerations:

Monitor renal, hepatic, and hematologic function and urinalysis before and monthly during therapy. May cause thrombocytopenia, leukopenia, and anemia. May also cause ↑ liver enzymes, proteinuria, and hematuria.

Toxicity and Overdose:

Rapid decrease in hemoglobin, WBC <4000/mm³, granulocytes <1500/mm³, or platelets <150,000/mm³, albuminuria, hematuria, rash, dermatitis, pruritus, skin eruption, stomatitis, persistent diarrhea, jaundice, or petechiae may indicate gold toxicity. Withhold therapy until toxicity has been ruled out. If signs of overdose occur, corticosteroids are usually used to reverse effects.

Implementation ⬆ ⬇

PO: Administer with meals to minimize gastric irritation.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication exactly as directed; do not skip or double doses. Take missed dose as soon as possible except if next dose is almost due.
Concurrent therapy with salicylates or other NSAIDs or corticosteroids is usually necessary, especially during the first few mo of gold therapy. Patients should continue physical therapy and ensure adequate rest. Explain that joint damage will not be reversed; the goal is to slow or stop the disease process.
Emphasize the importance of good oral hygiene to reduce stomatitis.
Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Instruct patient to report symptoms of leukopenia (fever, sore throat, signs of infection); thrombocytopenia (bleeding gums; bruising; petechiae; blood in stools, urine, or emesis); or gold toxicity immediately. Diarrhea may be resolved by decreasing the dose.
Emphasize the importance of regular visits to health care professional to monitor progress and evaluate blood and urine tests for side effects.
Discuss the need for contraception while receiving this medication. Advise female patients to notify health care professional promptly if pregnancy is suspected.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇