Dosing & Uses
Dosage Forms & Strengths
tablet
- 250mg
capsule
- 125mg
- 250mg
Wilson's Disease
250 mg PO QID; dosage range 500-1500 mg/day
Pregnancy: Not to exceed 500-750 mg/day
Planned cesarean section: Reduce dose to 250 mg/day for the last 6 weeks of pregnancy and postoperatively until wound healing completed
Dosing considerations
- Adjust dose to achieve urinary copper excretion of 0.5-1 mg/day
- Free copper levels in serum: Maintain at <10 mcg/dL
Arsenic Poisoning
100 mg/kg/day PO divided q6hr x5 days
If used for chronic arsenic poisoning, endpoint: 24 hours urinary arsenic <50 mcg/L
Rheumatoid Arthritis
Initial: 125-250 mg/day PO
Maintenance: May be increased by 125-250 mg/day q1-3Months up to 500-750 mg/day, may be increased further if no response and patient tolerates
Lead Poisoning
1-1.5 g qDay PO or divided BID-TID x1-6 months
Administration
Usually given with 10-25 mg/day pyridoxine
Take on empty stomach; last dose given at least 3 hr after evening meal
Other Indications & Uses
Cystinuria
Off-label: Lead toxicity (used following Ca-EDTA or dimercaprol; succimer preferred); copper, mercury, arsenic poisoning (chronic-only if BAL/DMSA unavailable); primary biliary cirrhosis
Dosage Forms & Strengths
tablet
- 250mg
capsule
- 125mg
- 250mg
Lead Poisoning
Considered 3rd-line therapy
20-40 mg/kg/day PO divided q8hr
Wilson's Disease
Cystinuria
30 mg/kg/day PO divided BID/QID; not to exceed 1 g/day
Juvenile Rheumatoid Arthritis
1st step (2 months): 5 mg/kg PO qDay x2 months
2nd step (4 months): 10 mg/kg PO qDay x4 months
Administration
Usually given with 10-25 mg/day pyridoxine
Take on empty stomach; last dose given at least 3 hours after evening meal
Cystinuria: drink plenty of fluids
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (2)
- gold sodium thiomalate
gold sodium thiomalate, penicillamine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Increased potential for serious bone marrow suppression or renal toxicity.
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate increases toxicity of penicillamine by Other (see comment). Avoid or Use Alternate Drug. Comment: Administer penicillamine at least 2 hr before and no less than 6 hr after each dose to avoid chelation with magnesium. .
Monitor Closely (28)
- aluminum hydroxide
aluminum hydroxide decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- calcium carbonate
calcium carbonate decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- carbonyl iron
carbonyl iron decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- copper
copper decreases effects of penicillamine by pharmacodynamic antagonism. Use Caution/Monitor.
- ferric maltol
ferric maltol decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- ferrous fumarate
ferrous fumarate decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- ferrous gluconate
ferrous gluconate decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- ferrous sulfate
ferrous sulfate decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- iron dextran complex
iron dextran complex decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- iron sucrose
iron sucrose decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- magnesium chloride
magnesium chloride decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- magnesium citrate
magnesium citrate decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- magnesium hydroxide
magnesium hydroxide decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- magnesium oxide
magnesium oxide decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- magnesium sulfate
magnesium sulfate decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- magnesium supplement
magnesium supplement will decrease the level or effect of penicillamine by Other (see comment). Modify Therapy/Monitor Closely. Drug may form a chelate with polyvalent cations; may decrease absorption by the intestinal tract; applies to oral forms; may administer 1 hr from polyvalent cation administration
- peramivir
penicillamine increases levels of peramivir by decreasing renal clearance. Use Caution/Monitor. Caution when peramivir coadministered with nephrotoxic drugs.
- polysaccharide iron
polysaccharide iron decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- promazine
promazine increases toxicity of penicillamine by unspecified interaction mechanism. Use Caution/Monitor. Enhanced myelosuppression.
- rose hips
rose hips decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Interaction only with oral iron administration.
- selenium
selenium will decrease the level or effect of penicillamine by cation binding in GI tract. Modify Therapy/Monitor Closely. Separate penicillamine administration from ingestion of polyvalent cations by at least 1 h.
- sodium bicarbonate
sodium bicarbonate decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- sodium citrate/citric acid
sodium citrate/citric acid decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- sodium picosulfate/magnesium oxide/anhydrous citric acid
sodium picosulfate/magnesium oxide/anhydrous citric acid decreases levels of penicillamine by cation binding in GI tract. Use Caution/Monitor. Take at least 2 hours before and not less than 6 hours after administration of sodium picosulfate, magnesium oxide and anhydrous citric acid to avoid magnesium chelation .
- sodium sulfate/?magnesium sulfate/potassium chloride
sodium sulfate/?magnesium sulfate/potassium chloride decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Administer penicillamine at least 2 hr before and no less than 6 hr after each dose to avoid chelation with magnesium. .
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate decreases levels of penicillamine by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Administer penicillamine at least 2 hr before and no less than 6 hr after each dose to avoid chelation with magnesium. .
- tenofovir DF
penicillamine, tenofovir DF. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Use Caution/Monitor.
penicillamine increases levels of tenofovir DF by decreasing renal clearance. Use Caution/Monitor. - zinc
zinc will decrease the level or effect of penicillamine by cation binding in GI tract. Modify Therapy/Monitor Closely. Separate administration of penicillamine and oral polyvalent cation containing products by at least 1 hr.
Minor (3)
- digoxin
penicillamine decreases levels of digoxin by unknown mechanism. Minor/Significance Unknown.
- pyridoxine
penicillamine decreases levels of pyridoxine by unspecified interaction mechanism. Minor/Significance Unknown.
- pyridoxine (Antidote)
penicillamine decreases levels of pyridoxine (Antidote) by unspecified interaction mechanism. Minor/Significance Unknown.
Adverse Effects
>10%
Worsening neurologic symptoms (10-50% pts with Wilson's disease)
Adverse effects requiring discontinuation of treatment
- Discontinued in 20-30% of pts with Wilson's disease
- Diarrhea (17%)
- Taste alteration (12%)
1-10%
Proteinuria (6%)
Rash (early and late 5%)
Thrombocytopenia (4-5%)
Leukopenia (2-5%)
Frequency Not Defined
Nausea/vomiting
Fever
Anorexia
Pemphigus
Oral lichenoid reaction
Myasthemia gravis
Neuropathy
Optic neuritisTinnitus
Goodpasture's syndrome
Renal failure
positive ANA
Hepatitis
Pancreatitis
Hemolytic anemia
Warnings
Contraindications
Penicillin allergy, discontinue if immune reactions
History of penicillamine-related aplastic anemia, agranulocytosis
Renal insufficiency (avoid if CrCl <50 mL/min)
Concurrency with gold salts, antimalarials, immunosuppressants, phenylbutazone
Cautions
Antacids, digoxin and iron (PO) decr levels and/or activity
Reactive airway disease
Associated with obliterative bronchiolitis
Increases the body's requirement for pyridoxine
Potential for development of (reversible) myasthenia gravis and other neurologic symptoms
Pregnancy & Lactation
Pregnancy Category: D; allowed only in Wilson's: not to exceed 750 mg/d; contraindicated for rheumatoid arthritis and cystinuria
Lactation: little information available, mfr states do not nurse
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Absorption: 40-70%
Peak Plasma Time: 1-3 hr
Peak Plasma Concentration: (250 mg dose) 1-2 mg/L
Metabolism: small amount in liver
Protein Bound: >80%
Excretion: urine
Mechanism of Action
Chelates gold, copper, mercury, and arsenic
Cystinuria: forms disulfide bonds with cysteine and facilitates excretion of cysteine-penicillamine complex rather than cystine
Rheumatoid arthris: unknown; depresses T-cell activity in vitro
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| penicillamine oral - | 250 mg capsule |  | |
| penicillamine oral - | 250 mg capsule |  | |
| penicillamine oral - | 250 mg capsule |  | |
| penicillamine oral - | 250 mg capsule |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
penicillamine oral
PENICILLAMINE - ORAL
(PEN-i-SIL-a-meen)
COMMON BRAND NAME(S): Cuprimine, Depen
USES: This medication is used to treat rheumatoid arthritis, Wilson's disease (a condition in which high levels of copper in the body cause damage to the liver, brain, and other organs), and a certain disorder which causes kidney stones (cystinuria). For the treatment of rheumatoid arthritis, penicillamine is known as a disease-modifying antirheumatic drug (DMARD). It helps to decrease pain/tenderness/swelling in the joints. For the treatment of Wilson's disease, penicillamine binds to copper and helps it to be removed from the body. Decreasing copper levels helps to improve liver function and the mental/mood/nerve problems (such as confusion, difficulty speaking/walking) caused by the disease. For the treatment of cystinuria, penicillamine helps to decrease the amount of a certain substance (cystine) in the urine which can cause kidney stones.
HOW TO USE: Take this medication by mouth on an empty stomach (1 hour before or 2 hours after meals) as directed by your doctor. Take this medication at least 1 hour apart from other drugs (especially antacids), milk, or food.Dosage is based on your medical condition and response to treatment.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day.Your doctor may also direct you to take vitamin B6 (pyridoxine) and iron. Follow your doctor's instructions carefully. If you need to take iron or other products that contain minerals (such as zinc), take it at least 2 hours before or after taking penicillamine. Consult your doctor before taking any products containing minerals since they may block the absorption of penicillamine.For the treatment of rheumatoid arthritis, it may take 2 to 3 months before you see any improvement in your condition.For the treatment of Wilson's disease, follow the diet recommended by your doctor to get the most benefit from this medication. Your condition may not improve for 1 to 3 months and may actually get worse when you start this medication. Tell your doctor right away if your condition continues to worsen after a month of treatment.For the treatment of cystinuria, follow the diet recommended by your doctor to get the most benefit from this medication. Drink plenty of water unless your doctor directs you otherwise.Tell your doctor if your condition does not improve or if it worsens.
SIDE EFFECTS: Stomach/abdominal pain, nausea/vomiting, loss of appetite, diarrhea, and decreased sense of taste may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: signs of infection (such as sore throat that doesn't go away, fever, swollen lymph nodes), easy bruising/bleeding, coughing up blood, shortness of breath, unusual tiredness, rapid breathing, skin blisters, mouth sores, new or worsening joint pain, thinning/wrinkling skin, signs of kidney problems (such as change in the amount of urine, bloody urine), muscle weakness, eye problems (such as drooping eyelids, blurred vision), signs of liver problems (such as nausea/vomiting that doesn't stop, severe stomach/abdominal pain, dark urine, yellowing eyes/skin).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking penicillamine, tell your doctor or pharmacist if you are allergic to it; or to penicillins; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: a previous severe reaction to penicillamine (such as aplastic anemia, agranulocytosis), kidney disease, blood/bone marrow disorders (such as thrombocytopenia).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using penicillamine. Penicillamine may harm an unborn baby. However, it may sometimes be used during pregnancy in certain situations (such as treating Wilson's disease). If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: digoxin, gold salts (such as auranofin), drugs to treat malaria (such as chloroquine), phenylbutazone, other drugs that decrease bone marrow function (such as azathioprine, cancer chemotherapy, trimethoprim/sulfamethoxazole).
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as complete blood count, hematocrit/hemoglobin, liver function, urine test, physical exam) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised January 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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