Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
|
pubmed:dateCreated |
1991-8-14
|
pubmed:abstractText |
D-penicillamine (D-PEN) is incompletely recovered during short-term balance studies, despite rapid elimination of D-PEN and its low molecular weight metabolites. Urinary excretion of metabolites of D-PEN also persists long after cessation of chronic therapy. A study was performed to determine whether the formation and later breakdown of a stable disulfide between D-PEN and plasma albumin could explain these aspects of D-PEN pharmacokinetics. Five human volunteers received D-penicillamine, 250 mg orally, daily for 21 days. Plasma concentration-time profiles for D-PEN and D-PEN-albumin disulfide (D-PEN-albumin) were determined during the first day and pre-dose concentrations were measured on five further occasions. The pharmacokinetics of D-PEN on the first day were similar to those reported previously. No D-PEN was found in any of the pre-dose specimens. The concentration of D-PEN-albumin rose rapidly during the first day, with an estimated 8.6% of the bioavailable D-PEN being transformed to D-PEN-albumin. Pseudo-steady-state concentrations of D-PEN-albumin were achieved in three subjects at between 14 and 21 days. The mean trough concentration of D-PEN-albumin at 21 days (19.5 microM) exceeded the peak concentration of D-PEN (during the first day) by 5.7-fold. The terminal elimination half-life of D-PEN-albumin was 1.65 +/- 0.29 days, which compared with an elimination half-life of 59 +/- 8.4 min for D-PEN.(ABSTRACT TRUNCATED AT 250 WORDS)
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:issn |
0090-9556
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
19
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
309-11
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:1676628-Adult,
pubmed-meshheading:1676628-Albumins,
pubmed-meshheading:1676628-Biological Availability,
pubmed-meshheading:1676628-Chromatography, High Pressure Liquid,
pubmed-meshheading:1676628-Female,
pubmed-meshheading:1676628-Half-Life,
pubmed-meshheading:1676628-Humans,
pubmed-meshheading:1676628-Male,
pubmed-meshheading:1676628-Models, Biological,
pubmed-meshheading:1676628-Penicillamine
|
pubmed:articleTitle |
The pharmacokinetics of albumin conjugates of D-penicillamine in humans.
|
pubmed:affiliation |
Department of Clinical Pharmacology and Toxicology, St Vincent's Hospital, Australia.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|