Details About Overdose or Poisoning Generic Salt ::  Penicillamine

Penicillamine

    

Drug Pharmacology ::

I. Pharmacology. Penicillamineis a derivative of penicillin that has no antimicrobial activity buteffectively chelates some heavy metals, such as lead, mercury, andcopper. It has been used as adjunctive therapy after initial treatmentwith calcium EDTA [see EDTA, Calcium (Calcium Disodium EDTA, CalciumDisodium Edetate, Calcium Disodium Versenate)] or BAL (dimercaprol; BAL[Dimercaprol]), although its use largely has been replaced by the oralchelator succimer (DMSA, Succimer [DMSA]) because of its poor safetyprofile. Penicillamine is well absorbed orally, and thepenicillamine-metal complex is eliminated in the urine. No parenteralform is available.

Drug Indications ::

Indications

   

Penicillaminemay be used to treat heavy metal poisoning caused by lead (if thepatient is intolerant to succimer, penicillamine may be used alone forminor intoxication or as adjunctive therapy after calcium EDTA or BALin moderate to severe intoxication), mercury (after initial BAL therapyand if intolerant of succimer), and copper (succimer may be analternative for mild to moderate poisoning).

Forlead or mercury poisoning, oral succimer (see Succimer [DMSA]) ispreferable, as it may result in greater metal excretion with feweradverse effects.

For copper poisoning (see Copper) and treatment of Wilson’s disease to remove copper deposits in tissues.

Drug Contra-Indications ::

III. Contraindications./b>

   

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

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

Concomitantadministration with other hematopoietic-depressant drugs (eg, goldsalts, immunosuppressants, antimalarial agents, and phenylbutazone) isnot recommended.

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

Drug Adverse Effects ::

IV. Adverse effects

   

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

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

Hepatitis and pancreatitis.

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

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

F. Use in pregnancy. Birth defects have been associated with its use during pregnancy. No assigned FDA category (see Table III–1).

Drug Lab Interactions ::

Drug or laboratory interactions

   

Penicillaminemay potentiate the hematopoietic-depressant effects of drugs such asgold salts, immunosuppressants, antimalarial agents, and phenylbutazone.

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

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

Drug Dose Management ::

Dosage and method of administration

   

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

Theusual dose is 20–30 mg/kg/day, administered in three or four divideddoses. The usual starting dose in adults is 250 mg four times daily.Initiating treatment at 25% of this dose and gradually increasing tothe full dose over 2–3 weeks may minimize adverse reactions. Themaximum adult daily dose is 2 g. In children with mild to moderate leadpoisoning, a lower dose, 15 mg/kg/day, has been shown to maintainefficacy at lowering blood levels and minimizing adverse effects.

Weeklymeasurement of urinary and blood concentrations of the intoxicatingmetal is indicated to assess the need for continued therapy. Treatmentfor as long as 3 months has been tolerated.

Drug Chemical Formulations ::

Formulations. Note: Although the chemical derivative N-acetylpenicillaminemay demonstrate better CNS and peripheral nerve penetration, it is notcurrently available in the United States.

   

Oral. Penicillamine (Cuprimine, Depen), 125- and 250-mg capsules; 250-mg titratable tablets.

The suggested minimum stocking level to treat a 70-kg adult for the first 24 hours is 1500 mg.

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