Auranofin

Indications
 Oral
Active progressive rheumatoid arthritis
Adult: Initially, 6 mg/day in 2 divided doses, if tolerated, may be given as single dose subsequently. May increase dose to 9 mg/day in 3 divided doses if response is inadequate after 6 mth; assess response 3 mth later, discontinue if there is still no response.
CrCl (ml/min)Dosage Recommendation
50-80Half the normal dose.
<50Avoid use.


Special Populations: Dose in renal impairment: Crcl 50-80 mL/min: Reduce dose to 50%; Crcl <50 mL/min: Avoid use.
Contraindications
 Congestive heart failure, SLE, renal dysfunction; history of blood dyscrasias, history of gold-induced anaphylactic reactions (e.g. necrotising enterocolitis, pulmonary fibrosis, exfoliative dermatitis, bone marrow aplasia). Lactation; porphyria.
Warnings / Precautions
 Chronic cardiac failure, history of allergies; elderly. Monitor urine and blood tests before starting therapy and mthly thereafter. Withdraw treatment when platelets drop <100 000/mm3 or if there are signs and symptoms of thrombocytopenia. Consider alternative treatment in patients with dermatitis, history of inflammatory bowel disease, hepatic impairment. Pregnancy.
Adverse Reactions
 GI disturbances (nausea, vomiting, abdominal pain, diarrhoea), pruritus, rash; dermatitis, lesions of mucous membranes, ulcerative enterocolitis, haemotological disorders (including aplastic anaemia), proteinuria, nephrotic syndrome, alopoecia, conjunctivitis, metallic taste, blood dyscrasias, pulmonary fibrosis, psychosis; stomatitis, haematuria.
Potentially Fatal: Agranulocytosis, thrombocytopenia, toxic hepatitis, encephalitis.
Overdose Reactions
 Induction of emesis or gastric lavage and supportive therapy are recommended.
Drug Interactions
 Possible increased risk of nitritoid reactions when used with ACE inhibitors. Increased risk of toxicity with other nephrotoxic, hepatotoxic or myelosuppressive drugs. Possible increase in phenytoin level in blood.
See Below for More auranofin Drug Interactions
Mechanism of Actions
 Auranofin is a gold compound that exhibits anti-inflammatory and antiarthritic effects. It is taken up by macrophages, resulting in inhibition of phagocytosis and lysosomal membrane stabilisation. It also reduces serum rheumatoid factor, lysosomal enzyme activity and complement activation; and inhibits prostaglandin synthesis.
Absorption: Only about 25% absorbed from the GI tract (oral); steady-state conc in blood is 0.7 mcg/mL.
Distribution: Penetrates into synovial fluid; bound to plasma proteins and RBCs.
Excretion: Majority of a dose is removed in faeces. 60% of absorbed dose is removed in urine and the remainder in faeces; about 26 days (elimination half-life).
Administration
 Should be taken with food. (Take after meals or a light snack.)
Storage Conditions
 Oral: Store at 15-30°C.
ATC Classification
 M01CB03 - auranofin ; Belongs to the class of gold preparations of antirheumatic agents.
Storage
 Oral: Store at 15-30°C.
Available As
  • Auranofin 3 mg

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