Sucralfate

Sucralfate, sold under various brand names, is

Sucralfate
a medication used to treat stomach ulcers,
gastroesophageal reflux disease (GERD),
radiation proctitis, and stomach inflammation
and to prevent stress ulcers.[3][4][5] Its
usefulness in people infected by H. pylori is
limited.[3] It is used by mouth (for upper GIT
ulcers) and rectally (for radiation
proctitis). [3][5]

Common side effects include constipation.[3]

Serious side effects may include bezoar
formation and encephalopathy.[6] Use appears
to be safe in pregnancy and breastfeeding.[6] Clinical data
How it works is unclear but is believed to Trade names Carafate
involve binding to the ulcer and protecting it AHFS/Drugs.com Monograph (https://www.drugs.co
from further damage.[3][6]
m/monograph/sucralfate.html)

Sucralfate was approved for medical use in the MedlinePlus a681049 (https://medlineplus.gov/d
United States in 1981.[3] It is available as a ruginfo/meds/a681049.html)
generic medication.[6][7] In 2022, it was the License data US DailyMed: Sucralfate (https://dai
214th most commonly prescribed medication lymed.nlm.nih.gov/dailymed/searc
in the United States, with more than 1 million h.cfm?labeltype=all&query=Sucralf
prescriptions.[8][9] ate)
Routes of By mouth, rectal
administration
Medical uses ATC code A02BX02 (WHO (https://www.whoc
c.no/atc_ddd_index/?code=A02BX
Sucralfate is used for the treatment of active 02))
duodenal ulcers not related to the use of
Legal status
nonsteroidal anti-inflammatory drugs
Legal status US: ℞-only
[1]
(NSAIDs), as the mechanism behind these
ulcers is due to acid oversecretion.[1] It is not In general: ℞ (Prescription only)
FDA approved for gastric ulcers, but is widely Pharmacokinetic data
used because of evidence of efficacy.[10] The Bioavailability 3-5% (local acting)
use for sucralfate in peptic ulcer disease has
Metabolism GI; liver: unknown
diminished recently, but it is still the preferred
Elimination unknown
agent for stress ulcer prevention.[11][12][13][14]
half-life
Sucralfate has also been used for the following Excretion Feces, urine
conditions: Identifiers
Active duodenal ulcer not related to IUPAC name
NSAID use Hexadeca-μ-hydroxytetracosahydroxy[μ8-[1,3,4,6-tetra-O-
Maintenance therapy for resolved sulfo-β-Dfructofuranosyl-α-D-glucopyranoside tetrakis
duodenal ulcers
(hydrogen sulfato)8-)]]hexadecaaluminum[2]
Gastric ulcer not related to NSAID use
and gastritis due to GERD—Triple CAS Number 54182-58-0 (https://commonchemi
combination therapy with lansoprazole stry.cas.org/detail?cas_rn=54182-5
+ cisapride + sucralfate can 8-0)
significantly improve symptoms and
quality of life and was more cost- PubChem CID 6398525 (https://pubchem.ncbi.nl
effective than ranitidine combination m.nih.gov/compound/6398525)
group. [15]
DrugBank DB00364 (https://www.drugbank.c
Aphthous ulcer and stomatitis due to
a/drugs/DB00364)
radiation or chemotherapy—The 2013
guidelines of the International Society ChemSpider 4911161 (https://www.chemspider.
of Oral Oncology does not com/Chemical-Structure.4911161.
recommended sucralfate for the
html)
prevention of oral mucositis in head
and neck cancer patients receiving UNII XX73205DH5 (https://precision.fda.
radiotherapy or chemoradiation due to gov/uniisearch/srs/unii/XX73205D
a lack of efficacy found in a H5)
randomized controlled trial.[16]
KEGG C07314 (https://www.kegg.jp/entry/
Gastro-esophageal reflux disease
during pregnancy—First-line drug C07314)
therapy combined with lifestyle and ChEMBL ChEMBL611727 (https://www.ebi.a
diet modification.[17]
c.uk/chembl/explore/compound/Ch
Stress ulcer prophylaxis—The use of EMBL611727)
sucralfate rather than H2 antagonists
for stress ulcer prophylaxis, and CompTox DTXSID1048966 (https://comptox.
measures to prevent aspiration, such Dashboard (EPA)
epa.gov/dashboard/chemical/detail
as continuous subglottic suctioning, s/DTXSID1048966)
have been shown to reduce the risk of
ventilator-associated pneumonia ECHA InfoCard 100.053.636 (https://echa.europa.e
(VAP).[18] Sucralfate is less effective u/substance-information/-/substanc
for prophylaxis against gastrointestinal einfo/100.053.636)
bleeding than either a PPI or H2- Chemical and physical data
blocker. For that reason, it is not
commonly used for stress ulcer Formula C12H54Al16O75S8
prophylaxis. Molar mass 2 086.67 g·mol−1
Prevention of stricture formation— (what is this?) (verify)
Sucralfate has an inhibitory effect on
stricture formation in experimental
corrosive burns and can be used in the treatment of corrosive esophageal burns to enhance
mucosal healing and suppress stricture formation[19]
Proctitis from ulcerative colitis[20]
Rectal bleeding due to proctitis from radiation to treat cancers of the cervix, prostate, and
colon.[5]
Grade 1 bleeding experienced immediate relief with sucrasulfate enema for 1 month.
Grade 2 bleeding, sucrasulfate enema] and/or coagulation were effective.
Grade 3 bleeding lasted for 1 year despite frequent transfusions and coagulation.
 Grade 2 and 3 rectal bleeding occurred in 8.5% of people. The most significant risk
factor was the ICRU-CRBED. Prompt treatment with a combination of sucrasulfate
enema and coagulation is effective in controlling Grade 1 and 2 rectal bleeding without
the development of fistula or stricture.[21]
Treatment of anastomotic ulcer after gastric bypass surgery
Sucralfate suspension is recommended by the US-based National Capital Poison Center
(Poison Control) as an intervention for known or suspected button battery ingestions to
reduce the risk and severity of injury to the esophagus prior to the battery's endoscopic
removal.[22][23]
Protection against ventilator-associated pneumonia - Reductions in gastric acidity and
volumes increase bacterial overgrowth and the incidence of ventilator-associated
pneumonia. Sucralfate may be considered to have the advantage over H2-blockers and
PPIs in this regard because sucralfate does not change the pH of gastric fluid. A majority of
meta-analyses found that sucralfate therapy decreased the incidence of ventilator-
associated pneumonia compared to H2-antagonists.[10]

Side effects
The most common side effect seen is constipation (2–3%). Less commonly reported side effects (<0.5%)
include flatulence, headache, hypophosphatemia, xerostomia (dry mouth), and bezoar
formation.[24][25][26] Use of this drug is not recommended for people with chronic kidney failure, as it
might cause aluminium accumulation and toxicity. A few well-controlled studies have been carried out
investigating the safety and efficacy of sucralfate in children and pregnant women (Pregnancy Category
B).[1][27][28]

Mechanism of action
Sucralfate is a locally acting substance that in an acidic environment (pH < 4) reacts with hydrochloric
acid in the stomach to form a cross-linking, viscous, paste-like material capable of acting as an acid
buffer for as long as 6 to 8 hours after a single dose.[29] It also attaches to proteins on the surface of
ulcers, such as albumin and fibrinogen, to form stable insoluble complexes. These complexes serve as
protective barriers at the ulcer surface, preventing further damage from acid, pepsin, and bile.[29] In
addition, sucralfate prevents back diffusion of hydrogen ions, and absorbs both pepsin and bile acids. [30]

It has been thought that sucralfate also stimulates the production of prostaglandin E2, epidermal growth
factors (EGF), bFGF, and gastric mucus.[1][31]

Pharmacokinetics
Onset: 1–2 hr (initial onset for peptic ulcer disease (PUD))
Absorption: <5% Orally
Duration: Up to 6 hours due to high affinity for defective mucosa (PUD)
Bioavailability: 5%, sucralfate is considered non-systemic, sucrose octasulfate: 5%,
aluminum: 0.005%
Metabolism: Not metabolized, excreted unchanged in urine
 Excretion: Primarily in feces as unchanged drug[28][32]

Society and culture

Brand names
Brand names include Carafate in the US, Sucramal in Italy, Sucrafil, Sufrate, Sucralpro, Sucralcoat,
Pepsigard, Sucral, Hapifate, Sucralpro tablets and Sucralpro cream in India, Sutra or Musin in parts of
South-East Asia, Sulcrate in Canada, Discral (sucralfato) in México, Ulsanic in South Africa and Israel,
Andapsin in Sweden, Antepsin in Turkey, Sucracell in India, and Ulsidex in Indonesia

References
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