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penicillamine (Rx)Brand and Other Names:Cuprimine, Depen

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 250mg

capsule

  • 125mg
  • 250mg
more...

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
more...

Lead Poisoning

Considered 3rd-line therapy

20-40 mg/kg/day PO divided q8hr  

Wilson's Disease

20 mg/kg/day PO divided q12hr  

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

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Interactions

Interaction Checker

penicillamine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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

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            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

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            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.

            more...
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            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

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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