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

  • Penicillamine is classified as a metal binding (chelating) agent. Penicillamine is 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.
  • Brand names for penicillamine are Cuprimine and Depen.
  • Penicillamine is not available in the US. You need a prescription to obtain penicillamine.

What is penicillamine used for?

Penicillamine is used for treating Wilson's disease.

What are the side effects and warnings of penicillamine?

Common reactions to penicillamine include:

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.

QUESTION

The term arthritis refers to stiffness in the joints. See Answer

What is the dosage for penicillamine?

  • 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.

Which drugs or supplements (contraindications) interact with penicillamine?

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.

SLIDESHOW

Rheumatoid Arthritis (RA) Symptoms & Treatment See Slideshow

Is penicillamine safe to take if you are pregnant or breastfeeding?

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

What else should you know about penicillamine?

What preparations of penicillamine are available?

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

How should I keep penicillamine stored?

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

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Summary

Penicillamine (Cuprimine, Depen) is an antirheumatic drug prescribed for the treatment of rheumatoid arthritis, Wilson's disease, lead poisoning, and The prevention of kidney stones in patients with cystinuria. Side effects, drug interactions, warnings and precautions, and patient information should be reviewed prior to taking any medication.

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Medically Reviewed on 11/14/2019
References
Medically reviewed by John P. Cunha, DO, FACOEP
FDA Prescribing Information

penicillamine (Rx). Medscape.Updated:029.<https://reference.medscape.com/drug/cuprimine-depen-penicillamine-343728>
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