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  1. Pharmacology. Penicillamine is a derivative of penicillin that has no antimicrobial activity but effectively chelates some heavy metals, such as lead, mercury, and copper. It has been used as adjunctive therapy after initial treatment with calcium EDTA (See EDTA, Calcium (Calcium Disodium EDTA, Calcium Disodium Edetate, Calcium Disodium Versenate)) or BAL (dimercaprol [See BAL (Dimercaprol)]), although it largely has been replaced by the oral chelator succimer (DMSA [See Succimer (DMSA)]) because of its poor safety profile. Penicillamine is well absorbed orally, and the penicillamine-metal complex is eliminated in the urine. No parenteral form is available.

  2. Indications

    1. Penicillamine may be used to treat heavy metal poisoning caused by lead (if the patient cannot tolerate succimer, penicillamine may be used alone for minor intoxication or as adjunctive therapy after calcium EDTA or BAL in moderate to severe intoxication), mercury (after initial BAL therapy and if the patient cannot tolerate succimer), and copper (succimer may be an alternative for mild to moderate poisoning). Penicillamine has also been used for arsenic, bismuth, and nickel poisoning, but it is not the agent of choice owing to its toxicity.

    2. For lead or mercury poisoning, oral succimer (See Succimer (DMSA)) is preferable, as it may result in greater metal excretion with fewer adverse effects.

    3. For copper poisoning (See Copper) and treatment of Wilson disease to remove copper deposits in tissues.

  3. Contraindications

    1. Penicillin allergy is a contraindication (penicillamine products may be contaminated with penicillin).

    2. Renal insufficiency is a relative contraindication because the complex is eliminated only through the urine.

    3. Concomitant administration with other hematopoiesis-depressant drugs (eg, gold salts, immunosuppressants, antimalarial agents, and phenylbutazone) is not recommended.

    4. Cadmium poisoning. Penicillamine may increase renal levels of cadmium and the potential for nephrotoxicity.

  4. Adverse effects

    1. Hypersensitivity reactions: rash, pruritus, drug fever, hematuria, antinuclear antibodies, and proteinuria.

    2. Leukopenia, thrombocytopenia, hemolytic anemia, aplastic anemia, and agranulocytosis.

    3. Hepatitis and pancreatitis.

    4. Anorexia, nausea, vomiting, epigastric pain, and impairment of taste.

    5. The requirement for pyridoxine is increased, and the patient may require daily supplementation (See Pyridoxine (Vitamin B6)).

    6. Use in pregnancy. Birth defects have been associated with use during pregnancy. No assigned FDA category (See Introduction in Section III).

  5. Drug or laboratory interactions

    1. Penicillamine may potentiate the hematopoiesis-depressant effects of drugs such as gold salts, immunosuppressants, antimalarial agents, and phenylbutazone.

    2. Several drugs (eg, antacids and ferrous sulfate) and food can reduce GI absorption of penicillamine substantially.

    3. Penicillamine may produce a false-positive test for ketones in the urine.

  6. Dosage and method of administration

    1. Penicillamine should be taken on an empty stomach at least 1 hour before or 3 hours after meals and at bedtime.

    2. The usual dose is 1–1.5 g/d (children: 20–30 mg/kg/d), administered in three or four divided doses. Initiating treatment at 25% of this dose and gradually increasing to the full dose over 2–3 weeks may minimize adverse reactions. Therefore, use a starting dose of 250 mg/d (children: 10 mg/kg/d), then increase to 50% during week 2 and to a full dose by week ...

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