Ridaura

Name: Ridaura

Other uses for this medicine

Auranofin is also used sometimes for psoriatic arthritis. Talk to your doctor about the possible risks of using this drug for your condition.

What Is Auranofin?

Auranofin is a form of gold that reduces some of the effects of the inflammatory process in the body.

Auranofin is used to treat rheumatoid arthritis.

Auranofin is usually given when other medications have been tried without successful treatment of symptoms.

Auranofin will not reverse any cartilage or joint damage that has already occurred in your body.

Auranofin may also be used for other purposes not listed in this medication guide.

You should not use this medication if you have ever had a severe reaction to gold therapy that affected your skin, lungs, bone marrow, blood cells, or your stomach or intestines.

Before taking auranofin, tell your doctor if you have a weak immune system, bone marrow disorder, kidney or liver disease, or inflammatory bowel disease.

Auranofin can lower blood cells that help your body fight infections. This can make it easier for you to bleed from an injury or get sick from being around others who are ill. To be sure your blood cells do not get too low, your blood will need to be tested on a regular basis.

Keep using auranofin as directed. Talk with your doctor if your symptoms do not improve after 3 or 4 months of treatment.

Stop taking auranofin and call your doctor at once if you have a skin rash or itching, mouth sores, severe diarrhea, easy bruising or bleeding, blood in your urine or stools, coughing up blood, or unusual weakness, or any signs of infection (fever, chills, flu symptoms).

You should not use this medication if you are allergic to auranofin, or if you have ever had any of these medical problems caused by using gold therapy:

  • an allergic skin reaction;
  • stomach or intestinal problems;
  • a breathing disorder;
  • a bone marrow disorder; or
  • a severe blood cell disorder.

If you have any of these other conditions, you may need a dose adjustment or special tests to safely use this medication:

  • a bone marrow disorder or weak immune system;
  • kidney disease;
  • liver disease; or
  • inflammatory bowel disease.

FDA pregnancy category C. It is not known whether auranofin is harmful to an unborn baby. Before taking this medication, tell your doctor if you are pregnant or plan to become pregnant during treatment.

It is not known whether auranofin passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

Indications

RIDAURA (auranofin) is indicated in the management of adults with active classical or definite rheumatoid arthritis (ARA criteria) who have had an insufficient therapeutic response to, or are intolerant of, an adequate trial of full doses of one or more nonsteroidal anti-inflammatory drugs. RIDAURA should be added to a comprehensive baseline program, including non-drug therapies.

Unlike anti-inflammatory drugs, RIDAURA does not produce an immediate response. Therapeutic effects may be seen after three to four months of treatment, although improvement has not been seen in some patients before six months.

When cartilage and bone damage has already occurred, gold cannot reverse structural damage to joints caused by previous disease. The greatest potential benefit occurs in patients with active synovitis, particularly in its early stage.

In controlled clinical trials comparing RIDAURA with injectable gold, RIDAURA was associated with fewer dropouts due to adverse reactions, while injectable gold was associated with fewer dropouts for inadequate or poor therapeutic effect. Physicians should consider these findings when deciding on the use of RIDAURA in patients who are candidates for chrysotherapy.

Ridaura Drug Class

Ridaura is part of the drug class:

  • Gold preparations

Ridaura Precautions

Serious side effects have been reported with Ridaura including:

  • Gastrointestinal reactions.
    • Diarrhea or loose stools
    • Nausea or vomiting
    • Decreased appetite or anorexia
    • Abdominal cramps
    • Bloody or tar-like stools
  • Dermatitis. An itchy rash may appear after exposure to Ridaura; it may be worsened by exposure to sunlight.
  • Ulcers in the mouth, on the touch, on the palate, or in the throat. These sores may appear with or without dermatitis. A metallic taste may precede the appearance of the ulcers.
  • Blood or protein in the urine.
  • Changes in the composition of blood, including decreased white blood cells and decreased thrombocytes, and aplastic anemia.

Do not take Ridaura if you:

  • are allergic to Ridaura or to any of its ingredients
  • have a history of anaphylactic reactions to gold
  • have or have had necrotizing enterocolitis
  • have or have had pulmonary fibrosis
  • have or have had exfoliative dermatitis
  • have or have had bone marrow aplasia
  • have or had had a severe blood disorder

What should I discuss with my healthcare provider before taking Ridaura (auranofin)?

You should not use this medication if you are allergic to auranofin, or if you have ever had any of these medical problems caused by using gold therapy:

  • an allergic skin reaction;

  • stomach or intestinal problems;

  • a breathing disorder;

  • a bone marrow disorder; or

  • a severe blood cell disorder.

If you have any of these other conditions, you may need a dose adjustment or special tests to safely use this medication:

  • a bone marrow disorder or weak immune system;

  • kidney disease;

  • liver disease; or

  • inflammatory bowel disease.

FDA pregnancy category C. It is not known whether auranofin is harmful to an unborn baby. Before taking this medication, tell your doctor if you are pregnant or plan to become pregnant during treatment.

It is not known whether auranofin passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

Proper Use of Ridaura

In order for this medicine to work, it must be taken regularly as ordered by your doctor. Continue receiving the injections or taking auranofin even if you think the medicine is not working. You may not notice the effects of this medicine until after three to six months of regular use.

For patients taking auranofin:

  • Do not take more of this medicine than ordered by your doctor. Taking too much auranofin may increase the chance of serious unwanted effects.

If you have any questions about this, check with your doctor.

Dosing

The dose medicines in this class will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

    For auranofin
  • For oral dosage form (capsules):
    • For arthritis:
      • Adults—6 milligrams (mg) once a day or 3 mg twice a day. After six months, your doctor may increase the dose to 3 mg three times a day.
      • Children—Dose must be determined by your doctor.
  • For injection dosage form:
    • For arthritis:
      • Adults and teenagers—10 milligrams (mg) for the first dose, then 25 mg once a week for the next two weeks, then 25 or 50 mg once a week. The medicine is injected into a muscle. After several months, the injections may be given less often (25 or 50 mg every two weeks for a while, then every three or four weeks).
      • Children 6 to 12 years of age—2.5 mg for the first dose, then 6.25 mg once a week for the next two weeks, then 12.5 mg once a week. The medicine is injected into a muscle. After several months, the injections may be given less often (6.25 or 12.5 mg every three or four weeks).
      • Children younger than 6 years of age—Dose must be determined by your doctor.
    For gold sodium thiomalate
  • For injection dosage form:
    • For arthritis:
      • Adults and teenagers—10 milligrams (mg) for the first dose, then 25 mg a week later, then 25 or 50 mg once a week. The medicine is injected into a muscle. After several months, the injections may be given less often (25 or 50 mg every two weeks for a while, then every three or four weeks).
      • Children—10 mg for the first dose, then 1 mg per kilogram (about 0.45 mg per pound) of body weight, but not more than a total of 50 mg, once a week. The medicine is injected into a muscle. After several months, the same dose may be given less often (every two weeks for a while, then every three or four weeks).

Missed Dose

Call your doctor or pharmacist for instructions.

For patients taking auranofin: If you miss a dose of this medicine, and your dosing schedule is—

  • One dose a day—Take the missed dose as soon as possible. However, if you do not remember until the next day, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
  • More than one dose a day—Take the missed dose as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using Ridaura

Gold compounds may cause some people to become more sensitive to sunlight than they are normally. These people may break out in a rash after being in the sun, or a skin rash that is already present may become worse. To protect yourself, it is best to:

  • Stay out of direct sunlight, especially between the hours of 10:00 a.m. and 3:00 p.m., if possible.
  • Wear protective clothing.
  • Ask your doctor if you may apply a sun block product. Products that have a skin protection factor (SPF) of at least 15 work best, but some patients may require a product with a higher SPF number, especially if they have a fair complexion.
  • Do not use a sunlamp or tanning bed or booth.

If you have a severe reaction from the sun, check with your doctor.

For patients taking auranofin:

  • Your doctor should check your progress at regular visits. Blood and urine tests may be needed to make certain that this medicine is not causing unwanted effects.

For patients receiving gold injections:

  • Immediately following an injection of this medicine, side effects such as dizziness, feeling faint, flushing or redness of the face, nausea or vomiting, increased sweating, or unusual weakness may occur. These will usually go away after you lie down for a few minutes. If any of these effects continue or become worse, or if you notice any other effects within 10 minutes or so after receiving an injection, tell your health care professional right away.
  • Joint pain may occur for 1 or 2 days after you receive an injection of this medicine. This effect usually disappears after the first few injections. However, if this continues or is bothersome, check with your doctor.

Ridaura Description

Ridaura (auranofin) is available in oral form as capsules containing 3 mg auranofin.

Auranofin is (2,3,4,6-tetra-O-acetyl-1-thio-ß-D-glucopyranosato-S-) (triethyl–phosphine) gold.

Auranofin contains 29% gold and has the following chemical structure:

Each Ridaura capsule, with opaque brown cap and opaque tan body, contains auranofin, 3 mg, and is imprinted with the product name Ridaura. Inactive ingredients consist of benzyl alcohol, cellulose, cetylpyridinium chloride, D&C Red No. 33, FD&C Blue No. 1, FD&C Red No. 40, FD&C Yellow No. 6, gelatin, lactose, magnesium stearate, povidone, sodium lauryl sulfate, sodium starch glycolate, starch, titanium dioxide and trace amounts of other inactive ingredients.

Precautions

General: The safety of concomitant use of Ridaura (auranofin) with injectable gold, hydroxychloroquine, penicillamine, immunosuppressive agents (e.g., cyclophosphamide, azathioprine, or methotrexate) or high doses of corticosteroids has not been established.

Medical problems that might affect the signs or symptoms used to detect Ridaura toxicity should be under control before starting Ridaura (auranofin).

The potential benefits of using Ridaura in patients with progressive renal disease, significant hepatocellular disease, inflammatory bowel disease, skin rash or history of bone marrow depression should be weighed against 1) the potential risks of gold toxicity on organ systems previously compromised or with decreased reserve, and 2) the difficulty in quickly detecting and correctly attributing the toxic effect.

The following adverse reactions have been reported with the use of gold preparations and require modification of Ridaura treatment or additional monitoring. See ADVERSE REACTIONS for the approximate incidence of those reactions specifically reported with Ridaura.

Gastrointestinal Reactions: Gastrointestinal reactions reported with gold therapy include diarrhea/loose stools, nausea, vomiting, anorexia and abdominal cramps. The most common reaction to Ridaura is diarrhea/ loose stools reported in approximately 50% of the patients. This is generally manageable by reducing the dosage (e.g., from 6 mg daily to 3 mg) and in only 6% of the patients is it necessary to discontinue Ridaura (auranofin) permanently. Ulcerative enterocolitis is a rare serious gold reaction. Therefore, patients with gastrointestinal symptoms should be monitored for the appearance of gastrointestinal bleeding.

Cutaneous Reactions: Dermatitis is the most common reaction to injectable gold therapy and the second most common reaction to Ridaura. Any eruption, especially if pruritic, that develops during treatment should be considered a gold reaction until proven otherwise. Pruritus often exists before dermatitis becomes apparent, and therefore should be considered to be a warning signal of a cutaneous reaction. Gold dermatitis may be aggravated by exposure to sunlight or an actinic rash may develop. The most serious form of cutaneous reaction reported with injectable gold is generalized exfoliative dermatitis.

Mucous Membrane Reactions: Stomatitis, another common gold reaction, may be manifested by shallow ulcers on the buccal membranes, on the borders of the tongue, and on the palate or in the pharynx. Stomatitis may occur as the only adverse reaction or with a dermatitis. Sometimes diffuse glossitis or gingivitis develops. A metallic taste may precede these oral mucous membrane reactions and should be considered a warning signal.

Renal Reactions: Gold can produce a nephrotic syndrome or glomerulitis with proteinuria and 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 the onset of the reaction. Therefore it is important to perform urinalyses regularly and to discontinue treatment promptly if proteinuria or hematuria develops.

Hematologic Reactions: Blood dyscrasias including leukopenia, granulocytopenia, thrombocytopenia and aplastic anemia have all been reported as reactions to injectable gold and Ridaura. These reactions may occur separately or in combination at anytime during treatment. Because they have potentially serious consequences, blood dyscrasias should be constantly watched for through regular monitoring (at least monthly) of the formed elements of the blood throughout treatment.

Miscellaneous Reactions: Rare reactions attributed to gold include cholestatic jaundice; gold bronchitis and interstitial pneumonitis and fibrosis; peripheral neuropathy; partial or complete hair loss; fever.

Information for Patients: Patients should be advised of the possibility of toxicity from Ridaura and of the signs and symptoms that they should report promptly. (Patient information sheets are available.)

Women of childbearing potential should be warned of the potential risks of Ridaura therapy during pregnancy (See PRECAUTIONS Pregnancy).

Laboratory Tests: CBC with differential, platelet count, urinalysis, and renal and liver function tests should be performed prior to Ridaura (auranofin) therapy to establish a baseline and to identify any preexisting conditions.

CBC with differential, platelet count and urinalysis should then be monitored at least monthly; other parameters should be monitored as appropriate.

Drug Interactions: In a single patient-report, there is the suggestion that concurrent administration of Ridaura and phenytoin may have increased phenytoin blood levels.

Carcinogenesis/Mutagenesis: In a 24-month study in rats, animals treated with auranofin at 0.4, 1.0 or 2.5 mg/kg/day orally (3, 8 or 21 times the human dose) or gold sodium thiomalate at 2 or 6 mg/kg injected twice weekly (4 or 12 times the human dose) were compared to untreated control animals.

There was a significant increase in the frequency of renal tubular cell karyomegaly and cytomegaly and renal adenoma in the animals treated with 1.0 or 2.5 mg/kg/day of auranofin and 2 or 6 mg/kg twice weekly of gold sodium thiomalate. Malignant renal epithelial tumors were seen in the 1.0 mg/kg/day and the 2.5 mg/kg/day auranofin and in the 6 mg/kg twice weekly gold sodium thiomalate–treated animals.

In a 12-month study, rats treated with auranofin at 23 mg/kg/day (192 times the human dose) developed tumors of the renal tubular epithelium, whereas those treated with 3.6 mg/ kg/day (30 times the human dose) did not.

In an 18-month study in mice given oral auranofin at doses of 1, 3 and 9 mg/kg/day (8, 24 and 72 times the human dose), there was no statistically significant increase above controls in the instances of tumors.

In the mouse lymphoma forward mutation assay, auranofin at high concentrations (313 to 700 ng/mL) induced increases in the mutation frequencies in the presence of a rat liver microsomal preparation. Auranofin produced no mutation effects in the Ames test (Salmonella), in the in vitro assay (Forward and Reverse Mutation Inducement Assay with Saccharomyces), in the in vitro transformation of BALB/T3 cell mouse assay or in the Dominant Lethal Assay.

Pregnancy: Teratogenic Effects Pregnancy Category C. Use of Ridaura (auranofin) by pregnant women is not recommended. Furthermore, women of childbearing potential should be warned of the potential risks of Ridaura therapy during pregnancy. (See below.)

Pregnant rabbits given auranofin at doses of 0.5, 3 or 6 mg/kg/day (4.2 to 50 times the human dose) had impaired food intake, decreased maternal weights, decreased fetal weights and an increase above controls in the incidence of resorptions, abortions and congenital abnormalities, mainly abdominal defects such as gastroschisis and umbilical hernia. Pregnant rats given auranofin at a dose of 5 mg/kg/day (42 times the human dose) had an increase above controls in the incidence of resorptions and a decrease in litter size and weight linked to maternal toxicity. No such effects were found in rats given 2.5 mg/kg/day (21 times the human dose).

Pregnant mice given auranofin at a dose of 5 mg/kg/day (42 times the human dose) had no teratogenic effects.

There are no adequate and well-controlled Ridaura studies in pregnant women.

Nursing Mothers: Nursing during Ridaura therapy is not recommended.

Following auranofin administration to rats and mice, gold is excreted in milk. Following the administration of injectable gold, gold appears in the milk of nursing women; human data on auranofin are not available.

Pediatric Use: Ridaura (auranofin) is not recommended for use in pediatric patients because its safety and effectiveness have not been established.

Overdosage

The acute oral LD50 for auranofin is 310 mg/kg in adult mice and 265 mg/ kg in adult rats. The minimum lethal dose in rats is 30 mg/kg.

In case of acute overdosage, immediate induction of emesis or gastric lavage and appropriate supportive therapy are recommended.

Ridaura overdosage experience is limited. A 50-year-old female, previously on 6 mg Ridaura daily, took 27 mg (9 capsules) daily for 10 days and developed an encephalopathy and peripheral neuropathy. Ridaura was discontinued and she eventually recovered.

There has been no experience with treating Ridaura overdosage with modalities such as chelating agents. However, they have been used with injectable gold and may be considered for Ridaura overdosage.

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