A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Imuran Indications, Dosage, Storage, Stability - Azathioprine
Imuran Indications, Dosage, Storage, Stability - Azathioprine
INDICATIONS
Azathioprine is indicated as an adjunct
for the prevention of rejection
in renal homotransplantation.
It is also indicated for the management of severe, active rheumatoid
arthritis unresponsive to
rest, aspirin or other nonsteroidal
anti-intlammatory drugs, or to agents in the class
of which gold is an example
Renal Homotransplantation
Azathioprine is indicated as an adjunct
for the prevention of rejection
in renal homotransplantation.
Experience with over 16,000 transplants shows a five-year patient
survival of 35% to 55%, but
this is dependent on donor, match for HLA
antigens, anti-donor or anti B-cell alloantigen
antibody and other variables. The effect
of azathioprine on these
variables has not been tested in controlled trials.
Rheumatoid Arthritis
Azathioprine is indicated only in adult
patients meeting criteria for classic or definite rheumatoid
arthritis as specified by
the American Rheumatism Association. Azathioprine should be restricted
to patients with severe, active and erosive
disease not responsive to
conventional management including rest, aspirin
or other non-steroidal drugs or to agents in the class
of which gold is an example.
Rest, physiotherapy
and salicylates should be continued while azathioprine
is given, but it may be possible to reduce the dose
of corticosteroids in patients on azathioprine. The combined use of azathioprine
with gold, antimalarials or penicillamine
has not been studied for either added beneht or unexpected adverse effects.
The use of atathioprine with these agents cannot be recommended.
DOSAGE AND ADMINISTRATION
Renal Homotransplantatlon
The dose of azathioprine
required to prevent rejection
and minimize toxicity will vary
with individual patients; this necessitates careful management.
Initial dose is usually 3 to
5 mg/kg daily, beginning at the time
of transplant. Azathioprine is usually given as a single daily dose
on the day of, and in a minority of cases one to three days before, trsnsplantation.
Azathioprine is often initiated with the intravenous
administration of the
sodium salt,
with subsequent use of tablets (at the same dose
level) after the post-operative period. Intravenous administration
of the sodium salt is indicated only in patients unable to tolerate oral
medications. Dose reduction
to maintenance levels of 1 to 3 mg/kg daily is usually possible. The dose
of azathioprine should
not be increased to toxic levels
because of threatened rejection. Discontinuation may be necessary for
severe hematologic or other toxicity,
even if rejection of the
homograft may be a consequence
of drug withdrawal.
Rheumatoid Arthritis
Azathioprine is usually given on a daily basis. The initisl dose
should be approximateiy 1.0 mg/kg (50 to 100 mg) given as a single dose
or on a twice daily schedule. The dose
may be increased, beginning at six to eight weeks and thereafter by steps
at four-week intervals, if there are no serious toxicities and if initial
response is unsatisfactory.
Dose increments should be 0.5 mg/kg daily, up to a maximum
dose of 2.5 mg/kg/day. Therapeutc
response occurs after several weeks of treatment,
usually six to eight; an adequate trial should be a minimum
of 12 weeks. Patients not improved after twelve weeks can be considered
refractory. Azathioprine may be continued long-term in patients with clinical
response, but patients should be monitored carefully, and gradual dosage
reduction should be attempted
to reduce risk of toxicities.
Maintenance therapy should
be at the lowest effective dose, and the dose given can be lowered decrementally
with changes of 0.5 mg/kg or approximately 25 mg
daily every four weeks while other therapy
is kept constant. The optimum duration
of maintenance azathioprine
has not been determined. Azathioprine can be discontinued abruptly, but
delayed effects are possible.
Use in Renal Dysfunction
Relatively oliguric patients, especially those with tubular
necrosis in the immediate
post-cadaveric transplant
period, may have delayed clearance of azathioprine
or its metabolites, may be particularly sensitive
to this drug and may require lower doses.
Procedures for proper handling and disposal of this immunosuppressive
antimetabolite drug should be
considered. Several guidelines on this subject have been published. There
is no general agreement that all
of the procedures recommended in the guidelines are necessary or appropriate.
HOW SUPPLIED
Azathioprlne Tablets USP, 50 mg
Yellow, round, scored tablets (Identified 54 043)
NDC 0054-8084-25; Unit dose, 10 tablets per
strip, 10 strips per shelf pack,
10 shelf packs per
shipper.
NDC 0054-4084-25: Bottles of 100 tablets.
Caution: Federal law prohibits
dispensing without prescription.
Store between 15º-25º C (59º-77º F)
Protect from Light Protect from Moisture
Dispense in tight, light resistant
container as defined in
the USP/NF.
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