Penicillamine
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From MedlinePlus, U.S. National Library of Medicine
Boxed warning
Physicians planning to use penicillamine should thoroughly familiarize themselves with its toxicity, special dosage considerations, and therapeutic benefits. Penicillamine should never be used casually. Each patient should remain constantly under the close supervision of the physician. Patients should be warned to report promptly any symptoms suggesting toxicity.
Antirheumatic Agent
Dosing in kidney impairment
Because of its potential for causing renal damage, penicillamine should not be administered to rheumatoid arthritis patients with a history or other evidence of renal insufficiency. WARNINGS The use of penicillamine has been associated with fatalities due to certain diseases such as aplastic anemia, agranulocytosis, thrombocytopenia, Goodpasture’s syndrome, and myasthenia gravis.
Because of the potential for serious hematological and renal adverse reactions to occur at any time, routine urinalysis, white and differential blood cell count, hemoglobin determination, and direct platelet count must be done twice weekly, together with monitoring of the patient’s skin, lymph nodes, and body temperature, during the first month of therapy, every two weeks for the next 5 months, and monthly thereafter.
When penicillamine is used in cystinuria, an annual x-ray for renal stones is advised. Cystine stones form rapidly, sometimes in 6 months. Up to one year or more may be required for any urinary abnormalities to disappear after penicillamine has been discontinued. Because of rare reports of intrahepatic cholestasis and toxic hepatitis, liver function tests are recommended every 6 months for the duration of therapy.
Supplement interactions
Dietary supplement interactions
1 noted- Zinc can reduce the absorption and action of penicillamine, a drug used to treat rheumatoid arthritis and Wilson disease. To minimize this interaction, people should take zinc supplements and penicillamine at least 1 hour apart.
Contraindications
Except for the treatment of Wilson’s disease or certain patients with cystinuria, use of penicillamine during pregnancy is contraindicated (see WARNINGS ). Although breast milk studies have not been reported in animals or humans, mothers on therapy with penicillamine should not nurse their infants. Patients with a history of penicillamine-related aplastic anemia or agranulocytosis should not be restarted on penicillamine (see WARNINGS and ADVERSE REACTIONS ). Because of its potential for causing renal damage, penicillamine should not be administered to rheumatoid arthritis patients with a history or other evidence of renal insufficiency.
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
ALikelihood score A: Well established cause of clinically apparent liver injury.
Penicillamine is chelating agent used to decrease copper stores in Wilson disease, which also has immunomodulatory activity in rheumatic diseases such as rheumatoid arthritis, scleroderma and systemic lupus erythematosus. Penicillamine is capable of causing hypersensitivity reactions, some of which are accompanied by liver injury which is typically cholestatic.
ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.
Pregnancy and lactation
Pregnancy
Pregnancy Penicillamine can cause fetal harm when administered to a pregnant woman. Penicillamine has been shown to be teratogenic in rats when given in doses six times higher than the highest dose recommended for human use. Skeletal defects, cleft palates, and fetal toxicity (resorptions) have been reported. There are no controlled studies on the use of penicillamine in pregnant women. Although normal outcomes have been reported, characteristic congenital cutis laxa and associated birth defects have been reported in infants born of mothers who received therapy with penicillamine during pregnancy.
Penicillamine should be used in women of childbearing potential only when the expected benefits outweigh the possible hazards. Women on therapy with penicillamine who are of childbearing potential should be apprised of this risk, advised to report promptly any missed menstrual periods or other indications of possible pregnancy, and followed closely for early recognition of pregnancy. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Pregnancy (see WARNINGS, Pregnancy )
Lactation
Nursing Mothers See CONTRAINDICATIONS .
Breastfeeding (LactMed)
Limited information indicates that penicillamine is not detectable in breastmilk and no adverse effects have been reported among breastfed infants whose mothers were taking the drug. Copper and zinc levels in breastmilk are reduced in some mothers receiving penicillamine. Penicillamine has been used with apparent safety during nursing of several infants. Based on available data, it appears that penicillamine is acceptable to use during breastfeeding.
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Supply and cost
Drug shortage status
Recalls (last 24 months)
Therapeutic equivalence (Orange Book)
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