PENICILLAMINE

Background and Date of Approval

Penicillamine is an antirheumatic medication approved by the Food and Drug Administration (FDA) on 21 July 1970. It is indicated for the treatment of rheumatoid arthritis, Wilson's disease (a genetic disorder characterised by copper accumulation), cystinuria (a kidney stone disorder), and as a chelating agent in heavy metal poisoning, including lead and mercury toxicity.

Uses

Penicillamine treats Wilson's disease, a genetic disorder that causes copper to accumulate in organs like the liver and brain. It promotes copper excretion and prevents further damage to these organs. The medication also treats cystinuria, a condition where excessive cystine excretion leads to stone formation in the urinary tract, by reducing cystine levels and preventing stone formation. Additionally, penicillamine helps patients with severe active rheumatoid arthritis who haven't responded to conventional treatments by reducing inflammation and improving symptoms. While it is sometimes considered for ankylosing spondylitis, research suggests it is not effective for this condition.

How is it administered?

Take penicillamine on an empty stomach at least one hour before meals or two hours after meals. Take it at least one hour apart from any other drug, food, or milk to ensure optimal absorption. Do not break, chew, or crush the tablets. Since penicillamine increases your need for pyridoxine, you may need to take a daily pyridoxine supplement.

Side Effects

Side effects are unwanted symptoms caused by medicines. Although all drugs can cause side effects, not everyone experiences them. Common side effects of Penicillamine: Generalised pruritus Rashes Pemphigus Drug eruptions with fever, arthralgia, or lymphadenopathy Anorexia Epigastric pain Nausea and vomiting Occasional diarrhoea Loss of taste Oral ulcerations Cheilosis Glossitis Gingivostomatitis Leukopenia (Rare) Thrombocytopenia (Rare) Proteinuria Hematuria Serious side effects of Penicillamine: Lupus erythematosus-like syndrome Urticaria Exfoliative dermatitis Hepatic dysfunction Pancreatitis Reactivated peptic ulcer Toxic hepatitis Aplastic anaemia Nephrotic syndrome Renal failure Optic neuritis Peripheral neuropathies Muscular weakness Visual and psychic disturbances

Warnings

Serious reactions : Penicillamine can cause fatalities from conditions like aplastic anaemia, agranulocytosis, thrombocytopenia, Goodpasture's syndrome, and myasthenia gravis. Monitoring : Regular lab tests (urinalysis, WBC, haemoglobin, platelet count) are required, particularly in the first month. Blood disorders : Discontinue if WBC falls below 3500/mm³ or platelet count below 100,000/mm³. Renal risks : Monitor for proteinuria or haematuria, which may indicate nephrotic syndrome. Liver Function : Liver tests should be done every six months during therapy. Neurological effects : New neurological symptoms may develop, including myasthenia gravis. Pemphigus : Discontinue if pemphigus is suspected. Pregnancy risk : Penicillamine can cause fetal harm. It should be avoided unless the benefits outweigh the risks.

Precautions

Penicillamine may cause drug fever, skin rashes, and allergic reactions, such as lupus-like syndrome and oral ulcers. It can also lead to taste disturbances and skin issues, including bruising and excessive wrinkling. Patients should avoid using it with certain medications, including gold therapy. Doctors should exercise caution when prescribing it to patients with impaired renal function and monitor them closely. Pregnant women should not use penicillamine, and doctors should be cautious when prescribing it to the elderly or those with renal issues.

Word of Advice

Patients prescribed penicillamine should monitor closely for fever, rashes, or mouth ulcers. Inform your doctor immediately if you experience unusual symptoms such as joint pain or swelling. Avoid concurrent use with certain medications, particularly gold therapy. Regular kidney function monitoring is essential, especially in patients with pre-existing kidney disease. Patients who are pregnant or elderly require doctor assessment before starting treatment.

References

Michael C. Byrns and Trevor M. Penning, Environmental Toxicology: Carcinogens and Heavy Metals, Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 13th edition, 2018, 1297-1315. Gerard Laboratories, EMC, [Revised on October 2021] [Accessed on June 2023] https://www.medicines.org.uk/emc/product/2713/smpc https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/19853s012,014lbl.pdf Mejias SG, Ramphul K. Penicillamine. 2023 Mar 27. In: StatPearls [Internet]. https://pubmed.ncbi.nlm.nih.gov/30020688/

Frequently Asked Questions

Is penicillamine a penicillin?

No, penicillamine is not a penicillin. It is a synthetic drug used for treating conditions like Wilson's disease and rheumatoid arthritis. Although its name is similar, it has different properties and functions.

Is penicillamine an Immunosuppressant?

Yes, penicillamine is considered an immunosuppressant. It works by suppressing the immune system, which helps in conditions like rheumatoid arthritis and Wilson's disease.

Does penicillamine affect the kidneys?

Yes, penicillamine can affect the kidneys. It may cause proteinuria and hematuria and, in rare cases, lead to kidney damage, such as membranous glomerulopathy. Regular monitoring of kidney function is recommended during treatment.

How long does it take for Penicillamine to show its therapeutic effects?

The time it takes for Penicillamine to demonstrate its therapeutic effects can vary depending on the individual and the treatment condition. Following the prescribed treatment plan and having regular follow-up appointments with your healthcare provider to monitor the progress is important.

Can Penicillamine cause allergic reactions?

Yes, Penicillamine can potentially cause allergic reactions in some individuals. It is important to inform your healthcare provider if you have a history of allergic reactions to medications or if you experience any signs of an allergic reaction, such as rash, itching, swelling, or difficulty breathing while taking this medicine.

Available Brands 3

Written By: Muskan Patel, M.Pharm

Reviewed By: Dr. Vishwa Patel, MBBS