Veterinary Drug Handbook (VDH) is the reference veterinarians turn to when they want an independent source of information on the drugs that are used in veterinary medicine today.

AURANOFIN

Chemistry - An orally administered gold compound, auranofin occurs as a white, odorless, crystalline powder. It is very slightly soluble in water and soluble in alcohol. Auranofin contains 29% gold.

Storage, Stability, Compatibility

Store capsules in tight, light resistant containers at room temperature. After manufacture, expiration dates of 4 years are assigned to the capsules.

Pharmacology - AURANOFIN

Auranofin is an orally available gold salt. Gold has anti-inflammatory, antirheumatic, immunomodulating, and antimicrobial (in vitro) effects. The exact mechanisms for these actions are not well understood. Gold is taken up by macrophages where it inhibits phagocytosis and may inhibit lysosomal enzyme activity. Gold also inhibits the release of histamine, andthe production of prostaglandins. While gold does have antimicrobial effects in vitro, it is notclinically useful for this purpose. Auranofin suppresses helper T-cells, without affecting suppressor
T-cell populations.

Uses, Indications

Auranofin has been used to treat idiopathic polyarthritis and pemphigus foliaceus in dogs. Several clinicians report that while auranofin may be less toxic, it also less efficacious than injectable gold (aurothioglucose).

Pharmacokinetics - AURANOFIN

Unlike other available gold salts, auranofin is absorbed when given by mouth(20-25% of the gold) primarily in the small and large intestines. In contrast to the other gold salts, auranofin is only moderately bound to plasma proteins (the others are highly bound). Auranofincrosses the placenta and is distributed into maternal milk. Tissues with the highest levels of gold arekidneys, spleen, lungs, adrenals and liver. Accumulation of gold does not appear to occur, unlike theparenteral gold salts. About 15% of an administered dose (60% of the absorbed dose) is excretedby the kidneys and remainder in the feces.

Contraindications, Precautions, Reproductive Safety

Auranofin should only be administeredto dogs where other less expensive and toxic therapies are ineffective and the veterinarian and ownerare aware of the potential pitfalls of auranofin therapy and are willing to accept the associated risksand expenses. Auranofin has been demonstrated to be teratogenic and maternotoxic in laboratoryanimals; it should not be used during pregnancy unless the owner accepts the potential risks of use.

Adverse Effects, Warnings

A dose dependent immune-mediated thrombocytopenia, hemolyticanemia or leukopenias have been noted in dogs. Discontinuation of the drug and administration ofsteroids have been recommended. Auranofin has a higher incidence of dose dependent GIdisturbances (particularly diarrhea) in dogs than with the injectable products. Discontinuation of thedrug or a lowered dose will generally resolve the problem. Renal toxicity manifested by proteinuriais possible as is hepatotoxicity (increased liver enzymes). These effects are less likely than eitherthe GI or hematologic effects.

Overdosage, Acute Toxicity

Very limited data is available. The minimum lethal oral dose in ratsis 30 mg/kg It is recommended that gut emptying protocols be employed after an acute overdosewhen applicable. Use of chelating agents (e.g., penicillamine, dimercaprol) for severe toxicities havebeen used, but are controversial. One human patient who took an overdose over 10 days developedvarious neurologic sequelae, but eventually (after 3 months) recovered completely afterdiscontinuation of the drug and chelation therapy.

Drug Interactions

There is one report of a human patient who had increased blood phenytoinlevels after receiving auranofin. The veterinary significance of this potential interaction is minimal.
Use of penicillamine or antimalarial drugs with gold salts is not recommended due to theincreased potential for hematologic or renal toxicity. Auranofin's safety when used with othercytotoxic agents, including high dose steroids, has not been established; use with caution.
Laboratory Considerations - In humans, response to tuberculin skin tests may be enhanced;veterinary significance is unclear.
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