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SUCRALFATE
TABLETS, USP
DESCRIPTION
Sucralfate is an ␣-D-glucopy-
ranoside, ␤-D-fructofuranosyl-,
octakis-(hydrogen sulfate), alu-
minum complex.
Tablets for oral administrationcontain 1 g of sucralfate, USP.
nesium stearate, and colloidalsilicon dioxide.
CLINICAL PHARMACOLOGY
Sucralfate is only minimally
absorbed from the gastrointestinal
tract. The small amounts of the
sulfated disaccharide that are
absorbed are excreted primarily in
the urine.
sucralfate’s ability to acceleratehealing of duodenal ulcers remainsto be fully defined, it is known that itexerts its effect through a local,rather than systemic, action. Thefollowing observations also appearpertinent:1. Studies in human subjects and with animal models of ulcerdisease have shown that sucral-fate forms an ulcer-adherentcomplex with proteinaceousexudate of the ulcer site.
film provides a barrier to dif-fusion of hydrogen ions.
given in doses recommended forulcer therapy inhibits pepsinactivity in gastric juice by 32%.
4. In vitro, sucralfate absorbs bile sucralfate’s antiulcer activity is theresult of formation of an ulcer-adherent complex that covers theulcer site and protects it againstfurther attack by acid, pepsin, andbile salts. There are approximately14 to 16 mEq of acid-neutralizingcapacity per 1-g dose of sucralfate.
Clinical Trials
Acute Duodenal Ulcer
Over 600 patients have participated
in well-controlled clinical trials
worldwide. Multicenter trials con-
ducted in the United States, both of
them placebo-controlled studies
with endoscopic evaluation at 2 and
4 weeks showed:
Treatment
Groups
Ulcer Healing/No. Patients
Treatment
Groups
Ulcer Healing/No. Patients
The sucralfate-placebo differenceswere statistically significant in bothstudies at 4 weeks but not at 2weeks. The poorer result in the firststudy may have occurred becausesucralfate was given 2 hours aftermeals and at bedtime rather than 1 hour before meals and at bedtime, the regimen used in internationalstudies and in the second UnitedStates study. In addition, in the firststudy liquid antacid was utilized asneeded, whereas in the secondstudy antacid tablets were used.
Maintenance Therapy After Healing
of Duodenal Ulcer
Two double-blind randomized
placebo-controlled U.S. multicenter
trials have demonstrated that
sucralfate (1 g bid) is effective as
maintenance therapy following
healing of duodenal ulcers.
performed monthly for 4 months. Ofthe 254 patients who enrolled, 239were analyzed in the intention-to-treat life table analysis presentedbelow.
Duodenal Ulcer Recurrence Rate (%)
In this study, prn antacids were notpermitted.
endoscopies were performed at 6 and 12 months, but for-causeendoscopies, were permitted assymptoms dictated. Median symp-tom scores between the sucralfateand placebo groups were notsignificantly different. A life tableintention-to-treat analysis for the 94patients enrolled in the trial had thefollowing results: Duodenal Ulcer Recurrence Rate (%)
In this study, prn antacids werepermitted.
studies longer than 1 year are notavailable.
INDICATIONS AND USAGE
Sucralfate tablets, USP are indicated
in:
• Short-term treatment (up to 8
weeks) of active duodenal ulcer.
While healing with sucralfate mayoccur during the first week or two,treatment should be continued for4 to 8 weeks unless healing hasbeen demonstrated by x-ray orendoscopic examination.
ulcer patients at reduced dosageafter healing of acute ulcers.
CONTRAINDICATIONS
There are no known contraindi-
cations to the use of sucralfate.
PRECAUTIONS
Duodenal ulcer is a chronic, recur-
rent disease. While short-term
treatment with sucralfate can result
in complete healing of the ulcer, a
successful course of treatment with
sucralfate should not be expected to
alter the posthealing frequency or
severity of duodenal ulceration.
Special Populations:
Chronic Renal Failure
and Dialysis Patients
When sucralfate is
administered orally, small
amounts of aluminum are
absorbed from the
gastrointestinal tract.
Concomitant use of
sucralfate with other
products that contain
aluminum, such as
a l u m i n u m - c o n t a i n i n g
antacids, may increase
the total body burden of
aluminum. Patients with
normal renal function
receiving the recom-
mended doses of
sucralfate and aluminum-
containing products
adequately excrete
aluminum in the urine.
Patients with chronic
renal failure or those
receiving dialysis have
impaired excretion of
absorbed aluminum. In
addition, aluminum does
not cross dialysis
membranes because it is
bound to albumin and
transferrin plasma proteins.
Aluminum accumulation and toxicity
(aluminum osteodystrophy, osteo-
malacia, encephalopathy) have been
described in patients with renal
impairment. Sucralfate should be
used with caution in patients with
chronic renal failure.
Drug Interactions
Some studies have shown that
simultaneous sucralfate adminis-
tration in healthy volunteers reduced
the extent of absorption (bioavail-
ability) of single doses of the
following: cimetidine, digoxin,
fluoroquinolone, antibiotics, keto-
conazole, l-thyroxine, phenytoin,
quinidine, ranitidine, tetracycline,
and theophylline. Subtherapeutic
prothrombin times with con-
comitant warfarin and sucralfate
therapy have been reported in
spontaneous and published case
reports. However, two clinical
studies have demonstrated no
change in either serum warfarin
concentration or prothrombin time
with the addition of sucralfate to
chronic warfarin therapy.
interactions appears to be non-systemic in nature, presumablyresulting from sucralfate binding tothe concomitant agent in thegastrointestinal tract. In all casesstudied to date (cimetidine,ciprofloxacin, digoxin, norfloxacin,ofloxacin, and ranitidine) dosingthe concomitant medication 2 hoursbefore sucralfate eliminated theinteraction. Because of the potentialof sucralfate to alter the absorptionof some drugs, sucralfate should beadministered separately from otherdrugs when alterations in bioavail-ability are felt to be critical. In thesecases, patients should be monitoredappropriately.
SUCRALFATE
TABLETS, USP
Carcinogenesis, Mutagenesis,
Impairment of Fertility
Chronic oral toxicity studies of 24
months’ duration were conducted
in mice and rats at doses up to 1
g/kg (12 times the human dose).
There was no evidence of drug-
related tumorigenicity. A repro-
duction study in rats at doses up to
38 times the human dose did not
reveal any indication of fertility
impairment. Mutagenicity studies
were not conducted.
Pregnancy
Teratogenic effects. Pregnancy
Category B.
Teratogenicity studies have been
performed in mice, rats and rabbits
at doses up to 50 times the human
dose and have revealed no
evidence of harm to the fetus due
to sucralfate. There are, however,
no adequate and well-controlled
studies in pregnant women.
Because animal reproduction
studies are not always predictive of
human response, this drug should
be used during pregnancy only if
clearly needed.
Nursing Mothers
It is not known whether this drug is
excreted in human milk. Because
many drugs are excreted in human
milk, caution should be exercised
when sucralfate is administered to
a nursing woman.
Pediatric Use
Safety and effectiveness in
pediatric patients have not been
established.
Geriatric Use
Clinical studies of Sucralfate
Tablets did not include sufficient
numbers of subjects aged 65 and
over to determine whether they
respond differently from younger
subjects. Other reported clinical
experience has not identified
differences in responses between
the elderly and younger patients. In
general, dose selection for an
elderly patient should be cautious,
usually starting at the low end of
the dosing range, reflecting the
greater frequency of decreased
hepatic, renal, or cardiac function,
and of concomitant disease or
other drug therapy. (See DOSAGE
AND ADMINISTRATION)
This drug is known to be
substantially excreted by the
kidney, and the risk of toxic
reactions to this drug may be
greater in patients with impaired
renal function. (See PRECAUTIONS
Special Populations: Chronic
Renal Failure and Dialysis
Patients) Because elderly patients
are more likely to have decreased
renal function, care should be
taken in dose selection, and it may
be useful to monitor renal function.
ADVERSE REACTIONS
Adverse reactions to sucralfate in
clinical trials were minor and only
rarely led to discontinuation of the
drug. In studies involving over
2700 patients treated with
sucralfate tablets, adverse effects
were reported in 129 (4.7%).
frequent complaint (2%). Otheradverse effects reported in lessthan 0.5% of the patients are listedbelow by body system: Gastrointestinal: diarrhea, nausea,
vomiting, gastric discomfort,
indigestion, flatulence, dry mouth.
Dermatological: pruritus, rash
Nervous System: dizziness,
insomnia, sleepiness, vertigo
Other: back pain, headache
sensitivity reactions, includingurticaria (hives), angioedema,respiratory difficulty, rhinitis,laryngospasm, and facial swellinghave been reported in patientsreceiving sucralfate tablets. Similarevents were reported withsucralfate suspension. However, acausal relationship has not beenestablished.
patients treated with sucralfate.
The majority of patients hadunderlying medical conditions thatmay predispose to bezoar for-mation (such as delayed gastricemptying) or were receivingconcomitant enteral tube feedings.
insoluble sucralfate and itsinsoluble excipients has led to fatalcomplications, including pul-monary and cerebral emboli.
Sucralfate is not intended forintravenous administration.
OVERDOSAGE
Due to limited experience in
humans with overdosage of
sucralfate, no specific treatment
recommendations can be given.
Acute oral toxicity studies in
animals, however, using doses up
to 12 g/kg body weight, could not
find a lethal dose. Sucralfate is only
minimally absorbed from the
gastrointestinal tract. Risks
associated with acute overdosage
should, therefore, be minimal. In
rare reports describing sucralfate
overdose, most patients remained
asymptomatic. Those few reports
where adverse events were
described included symptoms of
dyspepsia, abdominal pain, nausea,
and vomiting.
DOSAGE AND ADMINISTRATION
Active Duodenal Ulcer: The
recommended adult oral dosage
for duodenal ulcer is 1 g four times
a day on an empty stomach.
needed for relief of pain but shouldnot be taken within one-half hourbefore or after sucralfate.
may occur during the first week ortwo, treatment should be continuedfor 4 to 8 weeks unless healing hasbeen demonstrated by x-ray orendoscopic examination.
Maintenance Therapy: The recom-
mended adult oral dosage is 1 g
twice a day.
Elderly: In general, dose selection
for an elderly patient should be
cautious, usually starting at the low
end of the dosing range, reflecting
the greater frequency of decreased
hepatic, renal, or cardiac function,
and of concomitant disease or
other drug therapy. (See
PRECAUTIONS Geriatric Use)
HOW SUPPLIED
Sucralfate 1-g tablets, USP are
supplied in bottles of 100 and 500.
White, scored, oblong tablets
embossed with “N” and “S1”.
Bottles of 100 . . . . . NDC 29033-003-01Bottles of 500 . . . . . NDC 29033-003-05 Store at 20°-25°C (68°-77°F) (SeeUSP Controlled Room Temperature).

Source: http://www.nostrumlabs.com/labels/sucralfate-pi.pdf