PENICILLAMINE IS GIVEN ORALLY AND SHOULD BE TAKEN ON AN EMPTY STOMACH. A LOW INITIAL DOSE INCREASED GRADUALLY TO THE MINIMUM OPTIMAL MAINTENANCE DOSAGE MAY REDUCE THE INCIDENCE OF ADVERSE EFFECTS AS WELL AS PROVIDE CLOSER CONTROL OF THE CONDITION BEING TREATMENT.
IN THE TREATMENT OF WILSON'S DISEASE, A DOSE OF 1.5 TO 2 G DAILY IN DIVIDED DOSES MAY BE GIVEN INITIALLY. THE OPTIMAL DOSAGE TO ACHIEVE A NEGATIVE COPPER BALANCE SHOULD BE DETERMINED INITIALLY BY REGULAR ANALYSIS OF 24-HOUR URINARY COPPER EXCRETION AND SUBSEQUENTLY BY MONITORING FREE COPPER IN THE SERUM. A MAINTENANCE DOSE OF 0.75 TO 1 G DAILY MAY BE ADEQUATE ONCE CONTROL IS ACHIEVED AND SHOULD BE CONTINUED INDEFINITELY; THE UK MANUFACTURERS RECOMMEND THAT A MAINTENANCE DOSE OF 2 G DAILY SHOULD NOT BE CONTINUED FOR MORE THAN A YEAR. IN CHILDREN, A SUGGESTED DOSE IS UP TO 20 MG/KG DAILY (MINIMUM 500 MG DAILY) IN DIVIDED DOSES. A DOSE OF 20 MG/KG DAILY IS SUGGESTED FOR THE ELDERLY.
IN THE MANAGEMENT OF LEAD POISONING, PENICILLAMINE MAY BE GIVEN IN DOSES OF 1 TO 1.5 G DAILY IN DIVIDED DOSES UNTIL URINARY LEAD IS STABILISED AT LESS THAN 500 MICROGRAMS/DAY. CHILDREN AND THE ELDERLY MAY BE GIVEN 20 MG/KG DAILY IN DIVIDED DOSES.
IN CYSTINURIA, DOSES OF PENICILLAMINE ARE ADJUSTED ACCORDING TO CYSTINE CONCENTRATIONS IN THE URINE. FOR THE TREATMENT OF CYSTINURIA AND CYSTINE CALCULI, THE DOSE IS USUALLY IN THE RANGE OF 1 TO 4 G DAILY IN DIVIDED DOSES; A SUGGESTED DOSE FOR CHILDREN IS 30 MG/KG DAILY IN DIVIDED DOSES. FOR THE PREVENTION OF CYSTINE CALCULI, LOWER DOSES OF 0.5 TO 1 G AT BEDTIME MAY BE GIVEN. AN ADEQUATE FLUID INTAKE IS ESSENTIAL TO MAINTAIN URINE FLOW DURING PENICILLAMINE ADMINISTRATION FOR CYSTINURIA.
IN THE TREATMENT OF SEVERE ACTIVE RHEUMATOID ARTHRITIS, AN INITIAL DOSE OF PENICILLAMINE 125 TO 250 MG DAILY IS INCREASED GRADUALLY BY THE SAME AMOUNT AT INTERVALS OF 4 TO 12 WEEKS. REMISSION IS USUALLY ACHIEVED WITH MAINTENANCE DOSES OF 500 TO 750 MG DAILY IN DIVIDED DOSES, BUT UP TO 1.5 G DAILY MAY BE REQUIRED. IMPROVEMENT MAY NOT OCCUR FOR SEVERAL MONTHS; THE US MANUFACTURERS SUGGEST THAT PENICILLAMINE SHOULD BE DISCONTINUED IF THERE IS NO RESPONSE AFTER TREATMENT FOR 3 TO 4 MONTHS WITH 1 TO 1.5 G DAILY; IN THE UK, A TRIAL FOR 12 MONTHS IS SUGGESTED. AFTER REMISSION HAS BEEN SUSTAINED FOR 6 MONTHS AN ATTEMPT MAY BE MADE GRADUALLY TO REDUCE THE DOSE BY 125 TO 250 MG DAILY EVERY 3 MONTHS BUT RELAPSE MAY OCCUR. LOWER DOSES MAY BE REQUIRED IN THE ELDERLY WHO MAY BE MORE SUSCEPTIBLE TO DEVELOPING ADVERSE EFFECTS. INITIAL DOSES OF 125 MG DAILY ARE RECOMMENDED, GRADUALLY INCREASED TO A MAXIMUM OF 1 G DAILY IF NECESSARY. IN CHILDREN THE MAINTENANCE DOSE IS 15 TO 20 MG/KG DAILY; A SUGGESTED INITIAL DOSE IS 2.5 TO 5 MG/KG DAILY INCREASED GRADUALLY AT 4-WEEK INTERVALS.
IN THE MANAGEMENT OF CHRONIC ACTIVE HEPATITIS, PENICILLAMINE MAY BE GIVEN AFTER LIVER FUNCTION TESTS HAVE INDICATED THAT THE DISEASE HAS BEEN CONTROLLED BY CORTICOSTEROIDS. THE INITIAL DOSE IS 500 MG DAILY IN DIVIDED DOSES, INCREASED GRADUALLY OVER 3 MONTHS TO 1.25 G DAILY, WHILE AT THE SAME TIME REDUCING THE CORTICOSTEROID DOSE.