C H A P T E R 1 6
Anti-inflammatory, antiarthritis and related agents
253
Clinically important drug–drug interactions
These drugs should not be combined with penicillamine,
antimalarials, cytotoxic drugs or immunosuppressive
agents other than low-dose corticosteroids because of
the potential for severe toxicity.
D
isease
-
modifying antirheumatic drugs
Other antiarthritis drugs, called disease-modifying
antirheumatic drugs (DMARDs), are available for
treating arthritis and aggressively affect the process
TABLE 16.3
DRUGS IN FOCUS Antiarthritis agents
Drug name
Dosage/route
Usual indications
Gold compounds
auranofin (Ridaura)
Adult: 6 mg/day PO; monitor geriatric people
carefully
Paediatric: 0.1–0.15 mg/kg per day PO
Oral agent for long-term therapy of
rheumatic disorders
sodium aurothiomalate
(Myocrisin)
Adult: 10 mg IM, then 25 mg IM every other
week; use caution in geriatric people
Paediatric: 10 mg IM, then 1 mg/kg IM every
other week
Injected drug for early treatment of
rheumatic disorders
Other antiarthritis drugs
anakinra (Kineret)
Adult: 100 mg/day SC
Reduction of signs and symptoms of
rheumatoid arthritis in people ≥18 years
if one or more other arthritis agents have
failed
etanercept (Enbrel)
Adult: 25 mg SC two times per week or 50 mg
SC once a week
Paediatric (4–17 years): 0.4 mg/kg SC two
times per week with 72–96 hours between
doses; not recommended for children
<4 years
Reduction of signs and symptoms of
severe rheumatoid arthritis in people
whose disease is unresponsive to other
therapy; prevention of damage early in
the disease; ankylosing spondylosis;
psoriatic arthritis
hyaluronidase (Hyalase)
2 mL once a week for 3 weeks injected into
the affected knee
Relief of pain in the knees of people with
arthritis whose disease is unresponsive
to conventional treatment
leflunomide (Arava)
100 mg PO daily for 3 days, then 20 mg PO
daily
Treatment of active rheumatoid arthritis, to
relieve signs and symptoms and to slow
the progression of disease in adults
penicillamine
(D-Penamine)
250 mg/day PO for 1 month, increasing to
dose of 1500 mg/day PO
Treatment of severe, active rheumatoid
arthritis in adults whose disease is
unresponsive to conventional therapy
sodium hyaluronate
(Fermathron)
20 mg once a week for 5 weeks injected into
affected knee
Relief of pain in the knees of people with
arthritis whose disease is unresponsive
to conventional treatment
Prototype summary: Auranofin
Indications:
Treatment of selected cases of adult and
juvenile rheumatoid arthritis, most effective early in
disease.
Actions:
Although the mechanism of action has
not been fully elucidated, auranofin exhibits a
variety of anti-inflammatory, antiarthritic and
immunoregulatory activities. These properties
include: stimulation of cell-mediated immunity,
suppression of immunoglobulin synthesis and
antibody-dependent cytotoxicity, suppression of the
respiratory burst/superoxide radicals, inhibition
of neutrophil release of lysosomal enzymes and
secretion of inflammatory eicosanoids, inhibition
of platelet aggregation, serotonin production and
protein kinase C activity.
Pharmacokinetics:
Route
Onset
Peak
Oral
Rapid
2 hours
T
1/2
:
10 to 30 days; excreted mainly in faeces and
some in urine.
Adverse effects:
Dermatitis, nausea, diarrhoea,
anaemia, membranous glomerulonephritis and
nephrotic syndrome.
