Medications and Drugs

Rheumatoid Arthritis Slideshow Joint-Friendly Exercises Slideshow

Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD

GENERIC NAME: penicillamine

BRAND NAMES: Cuprimine, Depen

DRUG CLASS AND MECHANISM: Penicillamine is an antirheumatic 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 that forms a part of scar tissue that results from inflammation) and 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 nonrheumatic diseases including Wilson's disease. The FDA approved penicillamine in December 1970.

PRESCRIPTION: Yes

GENERIC AVAILABLE: No

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

STORAGE: Penicillamine should be stored at room temperature, 15 to 30 C (59 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. The usual adult dose is 125-750 mg daily. Some patients may require up to 1 g daily administered in 4 doses.
• Wilson's disease is treated with 750-1.5 g daily in 4 doses.
• Cystinuria is treated with 1-4 g daily in 4 doses.

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.

PREGNANCY: Penicillamine should not be taken by pregnant women unless it is for a life-threatening condition, because of potential harm to the fetus.

NURSING MOTHERS: Penicillamine should not be used by nursing mothers because of potential adverse effects in the infant.

SIDE EFFECTS: Common reactions to penicillamine include abdominal pain, cramps, rash, allergic reactions, weight loss, diarrhea, dysgeusia (loss of sense of taste), nausea, lip swelling, itching, and vomiting.

Penicillamine can cause bone marrow suppression [anemia, low blood platelets (thrombocytopenia) and white blood cells (neutropenia)] and serious kidney disease. All patients who take penicillamine require regular blood and urine testing to monitor for these side effects.

Penicillamine can increase the requirement for vitamin B6 (pyridoxine), and supplements of pyridoxine are advised. Penicillamine has an unusual risk of inducing immune-related diseases, such as systemic lupus erythematosus, polymyositis, Goodpasture's syndrome, and myasthenia gravis.

Reference: FDA Prescribing Information

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