Reduction in oral penicillamine absorption by food, antacid, and ferrous sulfate

Publisher Website
Google Scholar
Abstract
Plasma levels of penicillamine, urinary recovery of penicillamine and its oxidized metabolites, and urinary Cu excretion were examined after single 500-mg oral doses of penicillamine to 6 healthy men. Penicillamine was given after an overnight fast, a standard breakfast, an antacid and iron(II) sulfate. Following the fasting dose, the mean peak plasma level of 3.05 .mu.g/ml developed at 3.8 h and the drug was cleared from plasma with a t1/2 [half-life] of 2.1 h. Penicillamine levels were reduced to 52, 35 and 66% of those from the fasting dose after food, iron(II) sulfate and antacid. The rates of penicillamine appearance and disappearance from plasma were essentially treatment-independent. There were good correlations between urinary recovery of total penicillamine (r = 0.875), urinary Cu excretion (r = 0.758) and the penicillamine [area under the plasma concentration time curve]. The availability of oral penicillamine is very susceptible to interactions with other substances.