Aurothioglucose

Aurothioglucose is a gold-containing compound used in the treatment of rheumatoid arthritis. It belongs to a class of drugs known as disease-modifying antirheumatic drugs (DMARDs). Aurothioglucose is administered via intramuscular injection and has been used historically to reduce inflammation and slow the progression of joint damage in patients with rheumatoid arthritis.

Chemical Structure and Properties

Aurothioglucose is a coordination complex of gold with the chemical formula C₆H₁₁AuO₅S. It consists of a gold atom bound to a thioglucose ligand. The presence of gold is crucial for its therapeutic effects, although the exact mechanism by which gold compounds exert their effects in rheumatoid arthritis is not fully understood.

Mechanism of Action

The precise mechanism of action of aurothioglucose in rheumatoid arthritis is not completely elucidated. However, it is believed to involve the inhibition of macrophage activity and the suppression of inflammatory cytokines. Gold compounds may also interfere with the function of lysosomes and inhibit the release of lysosomal enzymes, which are involved in the inflammatory process.

Pharmacokinetics

Aurothioglucose is administered intramuscularly, allowing for slow release and absorption into the bloodstream. It is highly protein-bound, primarily to albumin, and is distributed throughout the body. The elimination half-life of gold compounds can be quite long, often extending to several weeks, which contributes to their prolonged effects.

Clinical Use

Aurothioglucose is used primarily in the management of rheumatoid arthritis, particularly in patients who have not responded adequately to other treatments. It is considered a second-line therapy due to its potential side effects and the availability of newer DMARDs with more favorable safety profiles.

Adverse Effects

The use of aurothioglucose can be associated with a range of adverse effects. Common side effects include dermatitis, stomatitis, and proteinuria. More serious adverse effects can include bone marrow suppression, leading to anemia, leukopenia, and thrombocytopenia. Patients receiving aurothioglucose require regular monitoring of blood counts and renal function.

Contraindications

Aurothioglucose is contraindicated in patients with a history of gold allergy, severe renal impairment, or hepatic dysfunction. It should be used with caution in patients with a history of blood dyscrasias.

History

Aurothioglucose was first introduced in the 1930s as a treatment for rheumatoid arthritis. It was one of the first gold compounds used for this purpose, along with gold sodium thiomalate and auranofin. Although its use has declined with the advent of newer therapies, it remains a part of the historical treatment landscape for rheumatoid arthritis.

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  Aurothioglucose

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  Aurothioglucose 3D Model