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Penicillamine

Penicillamine

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

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.

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.

Common side effects

The most common side effects include:

  • rash or itchy skin
  • a loss of taste
  • not feeling hungry
  • vomiting
  • diarrhea
  • bleeding
  • fever
  • infection
  • ulcers or sores in the mouth
  • protein in the urine, which can cause kidney failure
  • low platelets and low white blood cells
  • Symptoms and signs of kidney problems may include:
  • swelling of the hands, feet, or face
  • cloudy or foamy urine
  • Mild side effects may disappear within a few days or a couple of weeks. If side effects are severe or do not go away, it is important to speak to a doctor.

Food and drug interactions

Penicillamine can interact with other medications, herbs, vitamins, and other supplements, so it is important to talk to the doctor about any existing medications.

Having all prescriptions filled at the same pharmacy can help reduce this risk, because the pharmacist can check for possible drug interactions.

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