What is penicillamine, and how does it work (mechanism of action)?

Penicillamine is an anti-rheumatic drug used to
treat patients with active
arthritis. It also is classified as a metal binding (chelating) agent used
for treating
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.

What brand names are available for penicillamine?

Cuprimine, Depen

Is penicillamine available as a generic drug?

GENERIC AVAILABLE: Yes, in other countries

Do I need a prescription for penicillamine?


What are the side effects of penicillamine?

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.

Medically Reviewed by a Doctor on 5/15/2017

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