Læknablaðið : fylgirit - 01.07.1978, Page 92

shown by Huskisson et al (1974) and others
to be effective, but its place in the
treatment of patients with rheumatoid
arthritis has still to be determined.
Azapropazone has a pyrazolidine ring
like phenylbutazone, but in azapropazone
the ring is coupled with a 1, 2, 4, benzo-
triazine ring. So far azapropazone has
caused dyspepsia and an occasional skin
rash, but not any of the serious complica-
tions associated with phenylbutazone.
Azapropazone is effective in rheumatoid
arthritis, and probably will find a useful
place in management (Brooks and Buchanan,
1976).
Feprazone has a terpene group condensed
together with a pyrazolidine ring. It was
developed with the intention of combining
the ulcer-healing properties of the terpenes
with the anti-inflammatory effects of the
pyrazolidines. The drug appears to have
an anti-inflammatory effect comparable
with other non-steroidal anti-inflammatory
analgesics as indomethacin (Rooney et al,
1974) . Dyspepsia has been found trouble-
some and 5 per cent of patients develop
rashes.
Tolmetin is a pyrrole derivative with
some structural similarities to indomethacin.
The drug has been found to be effective,
but further studies will be required before
its place in the management of rheumatoid
arthritis is established.
Alclofenac is a substituted aryl acetic
acid. A considerable amount of work has
been done on this drug's ability to displace
a natural anti-inflammatory substance from
the protein-binding site (Aylward et al,
1975) . However, this has by no means
been proved. Alclofenac will also uncouple
oxidative phosphorylation, inhibit
prostaglandin synthetase, and interfere
with the release of ADP from platelets.
It has been suggested that alclofenac will
fundamentally alter the disease process,
but again this has not been proved. Drug
rashes are common occuring in 10 per
cent of patients, and vasculitis has been
reported.
Sulindac is a new, non-steroidal anti-
inflammatory, analgesic, antipyretic agent
produced by Merck, Sharp and Dohme.
Chemically it rejoices in the formula;
(Z) - 5 - fluoro - 2 - methyí - 1
(p-methylsulfinyl) pheiiyl) methylene - IH -
indene - 3 - acetic acid. The drug has
been proven of cUnical value in rheumatoid
arthritis (Huskisson and Franchimont,
1976, Reynolds et al, 1977) and appears
to be weU tolerated. Sulindac has now
been extensively studied in a variety of
rheumatic disorders including osteoarthritis,
ankylosing spondylitis, painful shoulder
syndromes and aeute gout, where it has
been proven beneficial. We have
also recently been able to show that the
drug has definite anti-inflammatory
properties in man, as evidenced by
shrinkage of digital joint circumference
and reduction in radioactive technetium
uptake in the joints in rheumatoid arthritis.
So far no serious side effects have been
reported, and the major problem is that
of otner non-steroidal antiinflammatory
drugs, namely dyspepsia.
The Anti - Malarials
The 4-aminoquinalone antimalarial drugs
have been used in the treatment of
rheumatoid arthritis for nearly quarter of
a century. The major problem associated
with their use is the development of
serious retinal damage. Many rheuma-
tologists indeed now consider that this
compUcation outweighs the clinical benefit
derived from their administration.
Evidence that antimalarial drugs are
beneficial in rheumatoid arthritis rests
essentially on two studies in which the
drug was compared with placebo for a
year or more (Popert et al, 1961,
Hamilton and Scott, 1962). The drugs
most commonly prescribed are hydroxy-
chloroquine sulphate in a dose of 200 mg
twice daily and chloroquine sulphate 250
mg once daily. Improvement occurs
slowly, maximum benefit not occuring for
three to six months. Antimalarials should
not be prescribed in patients with psoriasis
because of the danger of developing
exfoliative dermatitis (Baker, 1966) and
they should not be given to children, who
may develop cardio-respiratory arrest
even after as Httle as 1 g (Markowitz and
McGinley, 1964). Pregnancy is a definite
contraindication. Rarelj' leucopenia and
peripheral neuropathy may occur wit
chronic administration of anti-malarials.
Surprisingly patients, who develop side
effects to chloroquine, such as vomiting,
diarrhoea and skin rashes, may tolerate
hydr oxychlor oquine.
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