auranofin

Action and Spectrum

Actions and Spectrum: 

auranofin is a gold-containing compound used as a disease-modifying antirheumatic drug (DMARD) for treating rheumatoid arthritis (RA).  

• Inhibition of T-cell activation: auranofin suppresses the activation and proliferation of T-cells, which play a vital role in the autoimmune response that causes RA. 
• Modulation of redox signaling: auranofin can modify the redox state of cells, affecting the activity of enzymes and transcription factors involved in inflammatory and immune responses. 
• Inhibition of metallothionein: auranofin binds to metallothionein, a protein regulating zinc and copper levels in the body. This binding can alter the function of metallothionein and affect the immune response. 

The spectrum of action of auranofin is primarily limited to the treatment of RA, as it is ineffective in treating other autoimmune or inflammatory conditions. auranofin is generally reserved for patients who have not responded adequately to other DMARDs or cannot tolerate other DMARDs due to adverse effects. auranofin is not recommended in patients with severe or uncontrolled RA, as it may not provide sufficient disease control.

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Diarrhea 

Pruritis 

Rash 

Stomatitis 

Abdominal Pain 

1-10% 

Nausea 

Conjunctivitis 

Anorexia 

Flatulence 

Dyspepsia 

Proteinuria 

Anemia 

Alopecia 

Eosinophilia 

Constipation 

Anemia 

Hematuria 

Glossitis 

Leukopenia 

Urticaria 

Thrombocytopenia 

Black Box Warning

Black Box Warning: 

The RMP should know the fatal and severe toxicities of chrysotherapy. 

It is essential to explain to the patients about the adverse reactions and their self-reporting by the patients. 

Check through the signs of toxicity of gold. 

The medication should be reserved for patients with active rheumatoid arthritis. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity: auranofin is contraindicated in patients with a history of hypersensitivity to the medication or its components. 
• Severe renal or hepatic impairment: auranofin is contraindicated in patients with severe hepatic or renal impairment, as the medication can worsen these conditions. 

Precautions: 

• Bone marrow suppression: auranofin can cause bone marrow suppression, increasing the risk of infection, bleeding, and anemia. The medication causes bone marrow suppression or hematologic abnormalities, hence should be used cautiously. 
• Gastrointestinal toxicity: auranofin can cause gastrointestinal toxicity, including diarrhea, nausea, vomiting, and abdominal pain. In patients with a gastrointestinal disease or dysfunction history, the medication should be used cautiously. 
• Dermatologic reactions: auranofin can cause dermatologic reactions, including rash, pruritus, and urticaria. Patients with a history of dermatologic disease or sensitivity to gold compounds should use the drug cautiously. 
• Immunodeficiency: auranofin can suppress the immune system, increasing the risk of infections.  
• Pregnancy and breastfeeding: auranofin should not be used during pregnancy or breastfeeding, as the medication can harm the fetus or infant. 
• Elderly patients: auranofin should be used cautiously in elderly patients, as they may be more susceptible to the medication’s toxicities. 

Pregnancy / Lactation

Pregnancy consideration:  

Category C 

Breastfeeding warnings:  

Lactation is not advised during the medication as it enters the breast milk. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

auranofin is an oral gold-containing medication that is used to treat rheumatoid arthritis. Its works by inhibiting the activity of certain enzymes involved in inflammation and immune response. 

auranofin is metabolized in the liver and excreted in the urine and feces. Its half-life is approximately 2 to 7 days, and its effects can take several weeks to manifest. 

auranofin is a relatively weak anti-inflammatory agent compared to other disease-modifying antirheumatic drugs (DMARDs). Still, it effectively reduces the signs and symptoms of rheumatoid arthritis in some patients. It is often combined with other DMARDs, such as methotrexate, to enhance its therapeutic effects. 

Pharmacodynamics: 

auranofin’s pharmacodynamics are not fully understood, but it is believed to work by inhibiting certain enzymes involved in inflammation and immune response, such as thioredoxin reductase and protein kinase C. 

Thioredoxin reductase is an enzyme that regulates cellular redox status and is essential in modulating the activity of transcription factors and other cellular processes. By inhibiting thioredoxin reductase, auranofin reduces the activity of these transcription factors and other cellular processes, leading to reduced inflammation and immune response. 

By inhibiting protein kinase C, auranofin reduces the activation of these immune cells, leading to reduced inflammation and immune response. 

auranofin has also been shown to increase the activity of natural killer cells, critical immune cells that play a role in the defense against viral infections and cancer. This immunomodulatory effect of auranofin may contribute to its therapeutic effects in rheumatoid arthritis. 

Pharmacokinetics: 

Absorption 

The peak plasma concentration is achieved in 2 hours 

Distribution 

The peak plasma concentration is 0.025 mcg/mL 

The onset of effects is 3-6 months 

Metabolism 

The half-life is 21-31 days 

The protein-bound is 60% 

Elimination and Excretion 

50% of the drug is excreted in urine and feces 

Adminstartion

Administration: 

auranofin is administered orally as tablets, usually taken once or twice daily with food or as directed by a healthcare provider. The dosage of auranofin varies depending on the patient’s age, weight, medical condition, and other factors, and it is typically started at a low dose and gradually increased as tolerated. 

auranofin is available in tablet form in strengths of 3 mg and 6 mg. The tablets should be swallowed whole and not crushed, chewed, or broken, which may affect the drug’s efficacy. 

It is essential to take auranofin exactly as a healthcare provider prescribes, even if symptoms improve or disappear. Missing a dose or taking a lower dose than prescribed may reduce the drug’s effectiveness. 

Patient Information Leaflet

Patient information leaflet 

Generic Name:  auranofin 

Pronounced: aw-RAN-oh-fin 

Why do we use auranofin? 

auranofin is used to treat rheumatoid arthritis, a chronic autoimmune disorder that causes joint inflammation and damage, as well as other systemic symptoms such as fatigue, fever, and weight loss.