Gold Sodium Thiomalate is a sterile aqueous solution. It contains 0.5 percent BENZYL alcohol added as a preservative. The pH of the product is 5.8 to 6.5.

Gold Sodium Thiomalate is a mixture of the mono- and di-sodium salts of gold thiomalic acid. The structural formula is:

mercaptobutanedioic acid, monogold (1+) sodium salt

The molecular weight for C₄H₃AuNa₂O₄S (the disodium salt) is 390.07 and for C₄H₄AuNaO₄S (the mono-sodium salt) is 368.09.

Gold Sodium Thiomalate is supplied as a solution for intramuscular injection containing 50 mg of Gold Sodium Thiomalate per mL.

Last updated on RxList: 11/25/2008

Gold Sodium Thiomalate is indicated in the treatment of selected cases of active rheumatoid arthritis—both adult and juvenile type. The greatest benefit occurs in the early active stage. In late stages of the illness when cartilage and bone damage have occurred, gold can only check the progression of rheumatoid arthritis and prevent further structural damage to joints. It cannot repair damage caused by previously active disease.

Gold Sodium Thiomalate should be used only as one part of a complete program of therapy; alone it is not a complete treatment.

Gold Sodium Thiomalate should be administered only by intramuscular injection, preferably intragluteally. It should be given with the patient lying down. He should remain recumbent for approximately 10 minutes after the injection.

Therapeutic effects from Gold Sodium Thiomalate occur slowly. Early improvement, often limited to a reduction in morning stiffness, may begin after six to eight weeks of treatment, but beneficial effects may not be observed until after months of therapy.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration. Do not use if material has darkened. Color should not exceed pale yellow.

For the adult of average size the following dosage schedule is suggested:

Weekly Injections:

1st injection............................................................. 10 mg

2nd injection........................................................... 25 mg

3rd and subsequent injections, 25 to 50 mg until there is toxicity or major clinical improvement, or, in the absence of either of these, the cumulative dose of Gold Sodium Thiomalate reaches one gram.

Gold Sodium Thiomalate is continued until the cumulative dose reaches one gram unless toxicity or major clinical improvement occurs. If significant clinical improvement occurs before a cumulative dose of one gram has been administered, the dose may be decreased or the interval between injections increased as with maintenance therapy. Maintenance doses of 25 to 50 mg every other week for two to 20 weeks are recommended. If the clinical course remains stable, injections of 25 to 50 mg may be given every third and subsequently every fourth week indefinitely. Some patients may require maintenance treatment at intervals of one to three weeks. Should the arthritis exacerbate during maintenance therapy, weekly injections may be resumed temporarily until disease activity is suppressed. Should a patient fail to improve during initial therapy (cumulative dose of one gram), several options are available.

1. the patient may be considered to be unresponsive and Gold Sodium Thiomalate is discontinued.
2. the same dose (25 to 50 mg) of Gold Sodium Thiomalate may be continued for approximately ten additional weeks.
3. the dose of Gold Sodium Thiomalate may be increased by increments of 10 mg every one to four weeks, not to exceed 100 mg in single injection.

If significant clinical improvement occurs using option 2 or 3, the maintenance schedule described above should be initiated. If there is no significant improvement or if toxicity occurs, therapy with Gold Sodium Thiomalate should be stopped. The higher the individual dose of Gold Sodium Thiomalate, the greater the risk of gold toxicity. Selection of one of these options for chrysotherapy should be based upon a number of factors, including the physician's experience with gold salt therapy, the course of the patient's condition, the choice of alternative treatments, and the availability of the patient for the close supervision required.

Juvenile Rheumatoid Arthritis

The pediatric dose of Gold Sodium Thiomalate is proportional to the adult dose on a weight basis. After the initial test dose of 10 mg, the recommended dose for children is one mg per kilogram body weight, not to exceed 50 mg for a single injection. Otherwise, the guidelines given above for administration to adults also apply to children.

Concomitant Drug Therapy—Gold salts should not be used concomitantly with penicillamine.

The safety of coadministration with cytotoxic drugs has not been established. Other measures, such as salicylates, other nonsteroidal anti-inflammatory drugs, or systemic corticosteroids, may be continued when Gold Sodium Thiomalate is initiated. After improvement commences, analgesic and anti-inflammatory drugs may be discontinued slowly as symptoms permit.

Injection Gold Sodium Thiomalate is a light yellow to yellow solution, depending on potency, which must be protected from light. It is supplied as follows:

NDC 11098-533-01 Gold Sodium Thiomalate, 50 mg per mL, 1 mL in 2 mL (partially filled) vials in packages of 6.
NDC 11098-533-10 Gold Sodium Thiomalate, 50 mg per mL, 10 mL vials.

STORAGE: Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature]. Protect from light. Store container in carton until contents have been used.

Taylor Pharmaceuticals, Decatur, IL 62522. Rev. 03/06. FDA revision date: n/a

Last updated on RxList: 11/25/2008

A variety of adverse reactions may develop during the initial phase (weekly injections) of therapy or during maintenance treatment. Adverse reactions are observed most frequently when the cumulative dose of Gold Sodium Thiomalate administered is between 400 and 800mg. Very uncommonly, complications occur days to months after cessation of treatment.

Cutaneous reactions: Dermatitis is the most common reaction. Any eruption, especially if pruritic, that develops during treatment with Gold Sodium Thiomalate should be considered a reaction to gold until proven otherwise. Pruritus often exists before dermatitis becomes apparent, and therefore should be considered a warning signal of impending cutaneous reaction. The most serious form of cutaneous reaction is generalized exfoliative dermatitis which may lead to alopecia and shedding of nails. Gold dermatitis may be aggravated by exposure to sunlight or an actinic rash may develop.

Mucous membrane reactions: Stomatitis is the second most common adverse reaction. Shallow ulcers on the buccal membranes, on the borders of the tongue, and on the palate or in the pharynx may occur as the only adverse reaction, or along with dermatitis. Sometimes diffuse glossitis or gingivitis develops. A metallic taste may precede these oral mucous membrane reactions and should be considered a warning signal.

Conjunctivitis is a rare reaction.

Renal reactions: Gold may be toxic to the kidney and produce a nephrotic syndrome or glomerulitis with hematuria. These renal reactions are usually relatively mild and subside completely if recognized early and treatment is discontinued. They may become severe and chronic if treatment is continued after onset of the reaction. Therefore, it is important to perform a urinalysis before every injection, and to discontinue treatment promptly if proteinuria or hematuria develops.

Hematologic reactions: Blood dyscrasia due to gold toxicity is rare, but because of the potential serious consequences it must be constantly watched for and recognized early by frequent blood examinations done throughout treatment. Granulocytopenia; thrombocytopenia, with or without purpura; hypoplastic and aplastic anemia; and eosinophilia have all been reported. These hematologic disorders may occur separately or in combinations.

Nitritoid and allergic reactions: Reactions of the “nitritoid type” which may resemble anaphylactoid effects have been reported. Flushing, fainting, dizziness and sweating are most frequently reported. Other symptoms that may occur include: nausea, vomiting, malaise, headache, and weakness.

More severe, but less common effects include: anaphylactic shock, syncope, bradycardia, thickening of the tongue, difficulty in swallowing and breathing, and angioneurotic edema. These effects may occur almost immediately after injection or as late as 10 minutes following injection. They may occur at any time during the course of therapy and if observed, treatment with Gold Sodium Thiomalate should be discontinued.

Miscellaneous reactions: Gastrointestinal reactions have been reported, including nausea, vomiting, anorexia, abdominal cramps and diarrhea. Ulcerative enterocolitis, which can be severe or even fatal, has been reported rarely.

There have been rare reports of reactions involving the eye such as iritis, corneal ulcers, and gold deposits in ocular tissues. Peripheral and central nervous system complications have been reported rarely. Peripheral neuropathy, with or without, fasciculations, sensorimotor effects (including Guillain-Barré syndrome) and elevated spinal fluid protein have been reported. Central nervous system complications have included confusion, hallucinations and seizures. Usually these signs and symptoms cleared upon discontinuation of gold therapy.

Hepatitis, jaundice, with or without cholestasis, gold bronchitis, pulmonary injury manifested by interstitial pneumonitis and fibrosis, partial or complete hair loss and fever have also been reported.

Sometimes arthralgia occurs for a day or two after an injection of Gold Sodium Thiomalate; this reaction usually subsides after the first few injections.

Management Of Adverse Reactions

Treatment with Gold Sodium Thiomalate should be discontinued immediately when toxic reactions occur. Minor complications such as localized dermatitis, mild stomatitis, or slight proteinuria generally require no other therapy and resolve spontaneously with suspension of Gold Sodium Thiomalate. Moderately severe skin and mucous membrane reactions often benefit from topical corticosteroids, oral antihistaminics, and soothing or anesthetic lotions.

If stomatitis or dermatitis becomes severe or more generalized, systemic corticosteroids (generally, prednisone 10 to 40 mg daily in divided doses) may provide symptomatic relief.

For serious renal, hematologic, pulmonary, and enterocolitic complications, high doses of systemic corticosteroids (prednisone 40 to 100 mg daily in divided doses) are recommended. The optimum duration of corticosteroid treatment varies with the response of the individual patient. Therapy may be required for many months when adverse effects are unusually severe or progressive.

In patients whose complications do not improve with high-dose corticosteroid treatment, or who develop significant steroid-related adverse reactions, a chelating agent may be given to enhance gold excretion. Dimercaprol (BAL) has been used successfully, but patients must be monitored carefully as numerous untoward reactions may attend its use. Corticosteroids and a chelating agent may be used concomitantly.

Gold Sodium Thiomalate should not be reinstituted after severe or idiosyncratic reactions.

Gold Sodium Thiomalate may be readministered following resolution of mild reactions, using a reduced dosage schedule. If an initial test dose of 5 mg Gold Sodium Thiomalate is well-tolerated, progressively larger doses (5 to 10 mg increments) may be given at weekly to monthly intervals until a dose of 25 to 50 mg is reached.

No information provided.

Last updated on RxList: 11/25/2008

Before treatment is started, the patient's hemoglobin, erythrocyte, white blood cell, differential and platelet counts should be determined, and urinalysis should be done to serve as basic reference. Urine should be analyzed for protein and sediment changes prior to each injection. Complete blood counts including platelet estimation should be made before every second injection throughout treatment. The occurrence of purpura or ecchymoses at any time always requires a platelet count.

Danger signals of possible gold toxicity include: rapid reduction of hemoglobin, leukopenia below 4000 WBC/mm³, eosinophilia above 5 percent, platelet decrease below 100,000/mm³, albuminuria, hematuria, pruritus, skin eruption, stomatitis, or persistent diarrhea. No additional injections of Gold Sodium Thiomalate should be given unless further studies show these abnormalities to be caused by conditions other than gold toxicity.

General

Gold salts should not be used concomitantly with penicillamine.

The safety of coadministration with cytotoxic drugs has not been established.

Caution is indicated in the use of Gold Sodium Thiomalate in patients with the following:

1. a history of blood dyscrasias such as granulocytopenia or anemia caused by drug sensitivity,
2. allergy or hypersensitivity to medications,
3. skin rash,
4. previous kidney or liver disease,
5. marked hypertension,
6. compromised cerebral or cardiovascular circulation.

Diabetes mellitus or congestive heart failure should be under control before gold therapy is instituted.

Carcinogenicity

Renal adenomas have been reported in long-term toxicity studies of rats receiving Gold Sodium Thiomalate at high dose levels (2 mg/kg weekly for 45 weeks, followed by 6mg/kg daily for 47 weeks), approximately 2 to 42 times the usual human dose. These adenomas are histologically similar to those produced in rats by chronic administration of experimental gold compounds and other heavy metals, such as lead. No reports have been received of renal adenomas in man in association with the use of Gold Sodium Thiomalate.

Pregnancy

Pregnancy Category C.

Gold Sodium Thiomalate has been shown to be teratogenic during the organogenetic period in rats and rabbits when given in doses, respectively, of 140 and 175 times the usual human dose. Hydrocephaly and microphthalmia were the malformations observed in rats when Gold Sodium Thiomalate was administered subcutaneously at a dose of 25 mg/kg/day from day 6 through day 15 of gestation. In rabbits, limb malformations and gastroschisis were the malformations observed when Gold Sodium Thiomalate was administered subcutaneously at doses of 20 - 45 mg/kg/day from day 6 through day 18 of gestation.

There are no adequate and well-controlled studies in pregnant women. Gold Sodium Thiomalate should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

Nursing Mothers

The presence of gold has been demonstrated in the milk of lactating mothers. In addition, gold has been found in the serum and red blood cells of a nursing infant. In view of the above findings and because of the potential for serious adverse reactions in nursing infants from Gold Sodium Thiomalate, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. The slow excretion and persistence of gold in the mother, even after therapy is discontinued, must also be kept in mind.

Last updated on RxList: 11/25/2008

No information provided.

Hypersensitivity to any component of this product.

Severe toxicity resulting from previous exposure to gold or other heavy metals.

Severe debilitation.

Systemic lupus erythematosus.

Last updated on RxList: 11/25/2008

The mode of action of Gold Sodium Thiomalate is unknown. The predominant action appears to be a suppressive effect on the synovitis of active rheumatoid disease.

Last updated on RxList: 11/25/2008

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.

Last updated on RxList: 11/25/2008

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

GOLD SODIUM THIOMALATE - INJECTION

(gold So-dee-um thigh-oh-MAL-ate)

COMMON BRAND NAME(S): Aurolate

WARNING: This medication can cause serious (sometimes fatal) side effects, including blood cell problems (e.g., anemia, low white blood cells/platelets), kidney problems, rash, itching, or mouth sores/irritation (stomatitis). Low white blood cells can increase your risk of infection. See Side Effects section for more details. Tell your doctor immediately if you develop any of these side effects.

Your doctor will be closely monitoring certain lab tests (e.g., white blood cells, platelets) before you start therapy and before each injection. It is important that you keep all medical/lab appointments.

USES: This medication is used as part of a complete treatment program to treat active rheumatoid arthritis, including non-drug therapies (e.g., rest, physical therapy). It is used to treat patients with severe rheumatoid arthritis who have not responded to or cannot take other medications.

Gold sodium thiomalate is not a true pain reliever, but it is thought to decrease pain that occurs with arthritis by decreasing inflammation. It is known as a disease-modifying antirheumatic drug (DMARD). It decreases morning stiffness and pain/swelling in joints and can increase grip strength.

HOW TO USE: This medicine is injected into a muscle by a healthcare professional, usually in the buttock. Do not inject into a vein. You will need to lie down during your injection and for 10 minutes afterward to lower the risk of side effects such as dizziness. You will be monitored for 15 minutes after your injection. When you begin therapy, injections are usually given once a week or as directed by your doctor.

This medication should be pale yellow. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid.

Dosage is based on your medical condition and response to therapy. Injections are usually given once a week until improvement occurs or you have received a total of 1 gram. Once improvement occurs, your doctor may decrease your injections to once every 2-3 weeks or less. If your arthritis worsens, your doctor may order weekly injections again.

Use this medication regularly in order to get the most benefit from it. Keep all medical appointments.

If you are changing over from penicillamine, you will usually need to wait 1 month after stopping the penicillamine before starting gold injections. Ask your doctor for more details.

Some decrease in morning stiffness is usually seen in 6-8 weeks. It may take several months of therapy before you see the full benefits of this medication.

Inform your doctor if your condition persists or worsens.

SIDE EFFECTS: See also How to Use section.

Flushing, dizziness, headache, nausea, vomiting, weakness, and sweating may occur soon after the injection. Increased joint pain may occur 1-2 days after your injection. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: eye redness/pain, fainting, hair loss, mental/mood changes (e.g., confusion, hallucinations), numbness/tingling of arms/legs, seizure.

This medication may cause mouth/lip/throat sores (stomatitis). Tell your doctor if you notice a metallic taste in your mouth. This could be the first sign of stomatitis.

Tell your doctor immediately if any of these rare but very serious side effects occur: difficult/painful breathing, signs of low blood count (e.g., fast/pounding heartbeat, pale skin, unusual tiredness), easy bleeding/bruising, black/bloody stools, persistent cough, severe diarrhea, signs of infection (e.g., fever, persistent sore throat), gray/blue skin color, severe stomach/abdominal pain, unusual tiredness, change in the amount/color of urine, vaginal itching/sores, vomit that looks like coffee grounds, yellowing eyes/skin.

A very serious allergic reaction to this drug is uncommon. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: itching, rash, swelling, severe dizziness, trouble breathing.

Skin rash is common with this medication and can be serious. Itching is often the first sign of a severe allergic reaction. Therefore, seek immediate medical attention if you develop any rash or itching.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using gold sodium thiomalate injection, tell your doctor or pharmacist if you are allergic to it; or to any other gold or heavy metal compound; or if you have any other allergies.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: history of reaction to gold compound (e.g., blood disorders, kidney problems, lung problems, severe rash, stomach/intestinal problems), SLE (systemic lupus erythematosus).

Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood circulation problems (e.g., chest pain, heart attack, stroke), blood disorders (e.g., bleeding problems, bone marrow depression), colitis/inflammatory bowel disease, diabetes, eczema, heart problems (e.g., congestive heart failure), certain lung problem (fibrosis), very high blood pressure, kidney disease, liver disease, recent radiation therapy.

This medication may make you more sensitive to the sun. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen and wear protective clothing when outdoors.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor. If you become pregnant or think you may be pregnant, inform your doctor immediately. Consult your doctor for more details.

Injectable forms of gold pass into breast milk. Breast-feeding is not recommended while using this drug. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.

This drug should not be used with the following medication because a very serious interaction may occur: penicillamine.

If you are currently using the medication listed above, tell your doctor or pharmacist before starting gold injections.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: ACE inhibitors (e.g., lisinopril), drugs that suppress the immune system (e.g., azathioprine, cancer chemotherapy), anti-malarial drugs (e.g., chloroquine, primaquine), phenylbutazone, phenytoin.

This medication may interfere with certain laboratory tests (including tuberculin skin test), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Do not share this medication with others.

Laboratory and/or medical tests (e.g., complete blood count, liver/kidney tests, urine tests) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: If you miss an appointment, contact your doctor's office to reschedule.

STORAGE: Store the vial in the carton at room temperature between 59-86 degrees F (15-30 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised August 2008 Copyright(c) 2008 First DataBank, Inc.