Aurothioglucose
Aurothioglucose Uses, Dosage, Side Effects, Food Interaction and all others data.
Aurothioglucose, also known as gold thioglucose, was formerly used to treat rheumatoid arthritis.
Contemporary research on the effect of gold salts treatment began in 1935, primarily to reduce inflammation and to slow disease progression in patients with rheumatoid arthritis . The use of gold compounds has decreased since the 1980s owing to numerous side effects, limited efficacy, and slow onset of action. Many if not most gold compounds that were indicated for rheumatoid arthritis therapy have since been replaced with the use of various current disease modifying anti-rheumatic drugs (DMARDs) like methotrexate and others, which are far more effective.
After administration, patient serum levels of gold rise sharply but decline over the following week . Peak levels with aqueous preparations are higher and decline faster than those with oily preparations . Regular weekly administration produces a continuous rise in the basal value for several months, after which the serum level becomes relatively stable . After a standard weekly dose, considerable individual variation in the levels of gold can be observed . A steady decline in gold levels occurs when the interval between injections is lengthened, and small amounts may be found in the serum for months after discontinuation of therapy . The incidence of toxic reactions is seemingly unrelated to the plasma level of gold, but may perhaps be more associated with the total cumulative content of gold in the body .
| Trade Name | Aurothioglucose |
| Availability | Discontinued |
| Generic | Aurothioglucose |
| Aurothioglucose Other Names | Auromyose, Aurothioglucose, Gold thioglucose |
| Related Drugs | Humira, hydroxychloroquine, Enbrel, Remicade, Rituxan, Orencia |
| Type | |
| Formula | C6H11AuO5S |
| Weight | Average: 392.18 Monoisotopic: 391.999289 |
| Protein binding | In plasma, 95-99% of the drug is bound to albumin fraction . |
| Groups | Approved, Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Aurothioglucose is a gold compound used in the treatment of rheumatoid arthritis.
Aurothioglucose is indicated for the adjunctive treatment of early active adult and juvenile type rheumatoid arthritis that is not adequately controlled by other anti-inflammatory agents and conservative measures like salicylate, glucocorticoids, etc. . In chronic, advanced cases of rheumatoid arthritis, such gold therapy is not demonstrated to be as valuable .
Antirheumatic measures such as salicylate and other anti-inflammatory drugs (both steroidal and non steroidal) may be continued after initiation of gold therapy . After improvement commences, these measures may be discontinued slowly as symptoms permit .
How Aurothioglucose works
Rheumatoid arthritis is an autoimmune disease in which the body's immune system mistakenly attacks the lining of various skeletal bone joints of the body . These attacks are facilitated by various pro-inflammatory immune cells and agents like cytokines, histamines, mast cells, macrophages, monocytes, lymphocytes, leukocytes, and many others . The longterm result of this unwanted immune response is chronic inflammation and painful tissue damage . The cause of the malfunctioning immune system in rheumatoid arthritis is unknown and there is no definitive cure for the condition .
Similarly, the mechanism of action of aurothioglucose is also not well elucidated. Nevertheless, some studies have suggested that the combination of both the sulfhydryl ligand and aureus cation present in aurothioglucose elicits an inhibitory effect on adenylyl cyclase activity in human lymphocyte membranes and in membranes of T and B lymphocyte subsets . In particular, such inhibition of the activity of adenylyl cyclase and its various isoforms would theoretically also limit the cyclases' ability to induce mast cell degranulation and histamine release, to enhance respiratory burst effects, to stimulate the action of resting macrophages, to induce and activate phagocytes, to induce neutrophil chemotaxis, etc. - all of which are pro-inflammatory actions .
Toxicity
Overdose as a result of too rapid increases in dosing with aurothioglucose will be manifested by rapid appearance of toxic reactions, including those that are particular to renal damage, like hematuria and proteinuria, while hematologic effects include thrombocytopenia and granulocytopenia .
Other toxic effects, including fever, nausea, vomiting, diarrhea, and various skin disorders like papulovesicular lesions, urticaria, and exfoliative dermatitis, each of which are typically combined with severe pruritus can also develop .
The intramuscular TDLo for males is reported to be approximately 3.357 mg/kg when considering sense organs and special senses like eye vision and about 5.5 mg/kg for affects on the lungs, thorax, or respiration . For women, the intramuscular TDLo for effects on the liver, gastrointestinal tract, and cholestatic jaundice is between 2.6-2.7 mg/kg while the value for effects on the kidney, ureter, bladder, and acute renal failure, acute tubular necrosis, and other changes in urine composition is about 14.402 mg/kg .
Aurothioglucose Hypertension interaction
[Major] The use of gold compounds is contraindicated in patients with severe hypertension.
Prior to initiation of gold compounds medical problems that might affect the signs and symptoms used to detect gold compounds toxicity should be under control.
Aurothioglucose Disease Interaction
Major: bone marrow aplasia, congestive heart failure, diabetes mellitus, liver disease, rash, renal dysfunction, severe hypertension, systemic lupus erythematosus
Volume of Distribution
Readily accessible data regarding the volume of distribution of aurothioglucose is not available.
Elimination Route
In general, aurothioglucose is administered via intramuscular injection - preferably intragluteally - after which the resultant absorption is typically slow and erratic .
Gold is absorbed from injection sites, reaching peak concentration in blood in about 4 to 6 hours . After a single intramuscular injection of 50 mg of aurothioglucose suspension in two subjects, peak serum levels were observed at approximately 235 g/dL and 450 g/dL .
Storage of gold in human tissues depends upon organ mass as well as the concentration of gold .Subsequently, tissues having the highest gold levels (w/w) may not necessarily have the largest total amounts of gold . The highest concentrations of gold are generally found in the lymph nodes, adrenal glands, liver, kidneys, bone marrow, and spleen . Relatively small concentrations are actually found in the articular structures . In particular, following the administration of aurothioglucose doses, about 85% of the resultant plasma gold will be stored in the major bodily gold depots, which in decreasing order of total gold content are, the lymph nodes, bone marrow, liver, skin, and bone .
Half Life
The biological half-life of gold salts (like aurothioglucose) following a single 50 mg dose demonstrates a biological half-life of about 3-27 days, where the half-life seemingly increases with increased number of doses . Following successive weekly doses, the half-life increases and may become 14-40 days after the third dose and up to 168 days after the eleventh weekly dose .
Clearance
When a standard weekly treatment schedule of aurothioglucose administrations is followed, about 40% of the given dose is excreted each week, while the remainder is excreted over a longer period .
Elimination Route
Following a single intramuscular injection of 50 mg aurothioglucose in each of two patients, one study determined that approximately 70% of the agent is eliminated in the urine and 30% in the faeces . In general, excretion is primarily in the urine .
Innovators Monograph
You find simplified version here Aurothioglucose
