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.

AUROTHIOGLUCOSE

Chemistry - A water soluble gold salt, aurothioglucose contains approximately 50% gold. It ispractically insoluble in alcohol and insoluble in vegetable oils. The commercial product is a 5% (50mg/ml) suspension in sesame oil, 2% aluminum monostearate, and propylparaben is added as apreservative.

Storage, Stability, Compatibility

Protect from light and store between 15-30° C; avoid freezing.
A five year expiration date is assigned after manufacture. Do not mix with any other compound when injecting.

Pharmacology - AUROTHIOGLUCOSE

Aurothioglucose has anti-inflammatory, antirheumatic, immunomodulating, andantimicrobial (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 enzymeactivity. Gold also inhibits the release of histamine, and the production of prostaglandins. Whilegold does have antimicrobial effects in vitro, it is not clinically useful for this purpose.

Uses, Indications

In human medicine, gold compounds are used primarily as a treatment forrheumatoid arthritis that has not adequately responded to less toxic treatment modalities. In veterinary medicine (primarily small animal medicine), it use has been generally used for treatingimmune-mediated serious skin disorders such as pemphigus complex.

Pharmacokinetics - AUROTHIOGLUCOSE

After IM injection, aurothioglucose is quite rapidly absorbed and peak serumconcentrations are reached in 4-6 hours. It is distributed to several tissues (liver, kidney, spleen, bone marrow, adrenals, and lymph nodes), but highest levels are found in the synovium. In theplasma, 95% is bound to plasma proteins. Gold salts may be found in the epithelial cells in the renaltubules years after dosing has ended. Plasma half-lives increase in length after multiple doses havebeen given. These values have ranged from 21 - 168 hours in humans. Approximately 70% of adose is excreted by the kidneys, while the remaining 30% is excreted in the feces.
There appears to be no correlation with serum levels and efficacy. It usually takes from 6-12weeks for a beneficial effect to be noted after beginning therapy.
Contraindications/Precautions - Contraindications for chrysotherapy (gold therapy) includepatients with renal or hepatic disease, SLE (lupus erythematosus, diabetes mellitus (uncontrolled), severe debilitation, and preexisting hematologic disorders.
The safety of aurothioglucose has not been established during pregnancy, it should only be usedwhen the potential benefits outweigh the risks involved. Gold salts are distributed into milk andthere have been reports of human infants developing rashes after nursing from mothers taking gold.

Adverse Effects, Warnings

Veterinary experience with aurothioglucose is limited. Pain at theinjection site is common and some animals may develop thrombocytopenia with petechia andechymoses. One author (Kummel 1995) reports that four pemphigus canine cases treated withaurothioglucose that was given immediately after cessation of azathioprine, developed a fatal toxicepidermal necrolysis.
Adverse reactions seen in people include, mucocutaneous reactions which are fairly common (15-20%) and are characterized by rashes, (with or preceded by pruritis), and mucosal lesions (usuallyseen as a stomatitis). Hematologic reactions (thrombocytopenia, leukopenia, aplastic anemias), although rare in humans, can be life-threatening. Renal effects are generally mild and reversible withcessation of therapy if noted early. Proteinuria is an early sign associated with the proximal tubuledamage that gold can cause. Reversible pulmonary infiltrates have been noted, but are reversiblewhen therapy is discontinued. Enterocolitis, which may be fatal, has been reported in rare instances.
Because of the serious nature of these adverse reactions, adequate patient monitoring is essential.
Overdosage - Overdosages resulting from a too rapid increase in dosages are exhibited by rapiddevelopment of toxic signs, primarily renal (hematuria, proteinuria) and hematologic(thrombocytopenia, granulocytopenia) effects. Other symptoms include: nausea, vomiting, diarrhea, skin lesions, and fever.
Treat with dimercaprol (BAL) to chelate the gold and treat the hematologic and renal effectssupportively.

Drug Interactions

Patients receiving aurothioglucose should generally not receive penicillamine, antimalarials, hydroxychloroquin, immunosuppresive or cytotoxic drugs (e.g., cyclophosphamide, methotrexate, azathioprine) other than corticosteroids, because of similartoxicity profiles.
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