From the Guidelines
Penicillamine is a chelating agent and disease-modifying antirheumatic drug (DMARD) that works by binding to metals in the body, particularly copper, lead, and mercury, allowing them to be excreted in urine. This chelating property makes it effective for treating Wilson's disease, where it helps remove excess copper from the body 1. Penicillamine is also used to treat certain forms of rheumatoid arthritis due to its immunomodulatory effects, which can reduce inflammation and slow disease progression 1. Additionally, it can be prescribed for cystinuria, a condition where it helps prevent kidney stone formation by binding to cystine.
The typical dosage ranges from 250mg to 1500mg daily, depending on the condition being treated, and it's usually taken on an empty stomach to maximize absorption 1. Common side effects include rash, loss of taste, nausea, and reduced white blood cell count. Regular blood monitoring is essential during treatment to check for potential adverse effects on kidney function and blood cell counts 1. It's also important to note that penicillamine can cause severe side effects, such as nephrotoxicity, bone marrow toxicity, and dermatologic toxicities, which may require discontinuation of the drug 1.
Some key points to consider when prescribing penicillamine include:
- Starting with incremental doses to enhance tolerability
- Administering the drug 1 hour prior to or 2 hours after meals to minimize absorption interference
- Regularly monitoring 24-hour urinary copper excretion to assess treatment efficacy
- Providing supplemental pyridoxine to prevent deficiency
- Being aware of the potential for severe side effects and adjusting treatment accordingly
Overall, penicillamine is a valuable treatment option for Wilson's disease and other conditions involving metal toxicity, but its use requires careful consideration of the potential benefits and risks, as well as close monitoring of patients to minimize adverse effects 1.
From the FDA Drug Label
Penicillamine is 3-mercapto-D-valine, a disease modifying antirheumatic drug. The type of drug is a disease modifying antirheumatic drug 2.
- Key characteristics:
- Freely soluble in water
- Slightly soluble in alcohol
- Insoluble in ether, acetone, benzene, and carbon tetrachloride
- Chemical properties:
- Empirical formula: C5H11NO2S
- Molecular weight: 149.21
- Structural formula: reacts readily with formaldehyde or acetone to form a thiazolidine-carboxylic acid
From the Research
Type of Drug
Penicillamine is classified as a:
- Chelating agent, specifically a heavy metal chelator 3, 4, 5
- Disease Modifying Antirheumatic Drug (DMARD) 6
Uses
The drug is used to treat various conditions, including:
- Wilson's disease, an autosomal recessive disorder characterized by excessive accumulation of copper in the liver and other organs 3, 4, 5
- Rheumatoid arthritis, a severe disease that can cause joint destruction and radiological progression 4, 7, 6
- Cystinuria, a condition characterized by the formation of cystine stones in the kidneys 4
- Systemic sclerosis, a dermatologic condition 4
Mechanism of Action
Penicillamine acts as a reductive chelator, binding to heavy metals such as copper and removing them from the body 3