The Journal of Rheumatology 2002; 29:8 1590
Methotrexate (MTX) use in patients with psoriasis may be
associated with considerable hepatotoxicity
1-3
. Liver biop-
sies were therefore recommended after a patient had
achieved a mean cumulative dose of MTX of 1.5 g, and then
again after each additional 1 g
4
. Testing of liver transami-
nase enzyme levels was thought to be of no value in
predicting the development of clinically significant liver
disease (CSLD)
4
.
Because of the reports of liver disease associated with the
use of MTX in psoriatic patients, rheumatologists recog-
nized the need to assess hepatic safety in patients taking
MTX for the treatment of rheumatoid arthritis (RA). With
the more widespread use of MTX in the 1980s, the issue of
determining the hepatic safety profile of the drug in this
group of patients came into sharp focus.
The early prospective studies of MTX in patients with
RA confirmed that its use was accompanied by some
increase in hepatic transaminase enzymes
5
. The implications
of these abnormalities were unclear until prospective studies
could be performed in which frequent monitoring of the
enzyme abnormalities could be correlated with actual
biopsy samples of hepatic tissue. When this was done, it
became possible to examine the relationship between the
abnormalities of blood testing of transaminase enzymes and
serum albumin with the actual evaluation of changes of
hepatic architecture.
With the analysis of liver blood tests and liver biopsy
tissue obtained, certain clinically useful relationships
emerged. Contrary to the doctrine that hepatic changes in
patients with psoriatic arthritis could not be predicted by
abnormalities in liver enzymes
1-4
, it became apparent that
there was indeed a significant correlation between hepatic
aspartate aminotransferase (AST) and progression of histo-
logic deterioration in patients with RA receiving chronic
weekly MTX
6
. The disparity between the seemingly
conflicting data in patients with psoriasis and RA was
resolved when the methodology of blood sampling was
examined more closely. The psoriatic patients had blood
sampling for determination of enzyme levels on the day of
the biopsy
1-3
, while the patients with RA underwent frequent
and regular blood monitoring at regular intervals between
liver biopsies
6
.
Examination of the results of sequential liver biopsies in
patients with RA who were managed to keep the hepatic
AST and serum albumin within the normal range while
avoiding all alcohol actually revealed some improvement in
hepatic histology over prolonged periods of MTX expo-
sure
7,8
. It therefore became apparent that liver toxicity was
not necessarily an inevitable outcome of longterm MTX
treatment
9
.
The pattern of increase of transaminase enzymes, which
actually correlated with hepatic damage seen at the time of
liver biopsy, was of interest. Any elevation of serum AST
into the abnormal range was predictive of hepatic histologic
deterioration
6
. This made sense considering that the mean
value of AST in patients with RA taking MTX more than
doubles from baseline values, even while remaining in the
normal range
10
(Figure 1). This observation, along with the
consideration that the laboratory defined upper limit of
normal is 2 standard deviations from the norm, lends further
credibility to the finding that any increase in AST values
into the abnormal range may be associated with liver
damage, and led to the recommendations in the American
College of Rheumatology guidelines published in 1994,
which indicate that the MTX dose should be adjusted to
keep the transaminase enzyme values within the upper limit
of normal
11
. The utility of these recommendations has been
validated by others
12
, and they have generally served us
well. MTX hepatotoxicity has evolved from a primary
concern limiting drug use into a secondary concern because
of the infrequency of CSLD in the very large number of
patients with RA receiving the drug around the world.
It would therefore be ironic if the reason for the drastic
decrease in MTX induced liver toxicity became the driving
Editorial
Not Yet Time to Change the Guidelines for
Monitoring Methotrexate Liver Toxicity:
They Have Served Us Well
See Monitoring for MTX hepatic toxicity in RA:
Is it time to update the guidelines? page 1586
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