penicillamine, Cuprimine, Depen

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GENERIC NAME: penicillamine

BRAND NAMES: Cuprimine, Depen

DRUG CLASS AND MECHANISM: Penicillamine is an anti-rheumatic drug used to treat patients with active rheumatoid arthritis. It also is classified as a metal binding (chelating) agent used for treating Wilson's disease, a genetic disease that causes excessive copper to accumulate in the body. The mechanism of action of penicillamine in rheumatoid arthritis is unknown but it may be related to reduction of collagen formation. (Collagen is a type of tissue compound that forms as part of scar tissue that result from inflammation.) Penicillamine also may result in suppression of the immune system. In patients with rheumatoid arthritis, penicillamine appears to slow the progression of the disease (specifically deformities of the joints) and improve function. For this reason it is considered a disease modifying anti-rheumatic drug (DMARD). Penicillamine binds copper, iron, mercury, lead, and cystine which then are excreted in the urine, and this mechanism is important in treating several non-rheumatic diseases including Wilson's disease. The FDA approved penicillamine in December 1970.

PRESCRIPTION: Yes

GENERIC AVAILABLE: Yes, in other countries

PREPARATIONS: Capsules: 125 and 250 mg; Tablets: 250 mg.

STORAGE: Penicillamine should be stored at room temperature, 15 C to 30 C (59 F to 86 F).

PRESCRIBED FOR: Penicillamine is used to treat active rheumatoid arthritis that has not responded to other drugs. Penicillamine also is used to promote copper excretion from the body in patients with Wilson's disease and is useful for preventing cystine kidney stones in individuals with cystinuria. It has been used in the treatment of lead poisoning.

DOSING:

  • Penicillamine should be taken on an empty stomach, at least one hour before meals or two hours after meals 1-4 times daily. It is usually given with 10-25 mg/day pyridoxine (Vitamin B6).
  • The usual adult dose for treating rheumatoid arthritis is 125 to 250 mg daily. It may be increased by 125 to 250 mg a day every 1 to 3 months up to 500 to 750 mg daily or more if tolerated.
  • Wilson's disease is treated with 250 mg 4 times daily. The dose range is 500 to 1500 mg daily.
  • Cystinuria is treated with 1-4 g daily in 4 doses.
  • Lead poisoning is treated with 1 – 1.5 g/day total orally. The total dose can be divided into twice or three times per day dosing; consult with a toxicologist for dosing and length of time to give medication
  • Pediatric dosing: Dosing is age/weight based and a specialist (pediatric) should be consulted before dosing.

DRUG INTERACTIONS: Penicillamine should not be taken by patients who are also taking gold (gold sodium thiomalate; aurothiomalate [Myochrysine], auranofin [Ridaura], aurothioglucose [Solganal]), antimalarial (hydroxychloroquine [Plaquenil]), phenylbutazone (Butazolidine), or cytotoxic drugs (cyclophosphamide [Cytoxan], azathioprine [Imuran, Azasan], methotrexate [Rheumatrex, Trexall]) because these drugs also affect the bone marrow and kidney and when combined with penicillamine can seriously reduce bone marrow and kidney function.

The absorption of penicillamine is reduced by iron (ferrous sulphate), magnesium and aluminum salts (for example, antacids) because they form unabsorbable complexes with penicillamine in the intestine. Administration of penicillamine and iron containing products or antacids should be separated by 2 hours.

Medically Reviewed by a Doctor on 8/27/2014



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