medication
Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to medical diagnosis, diagnose, cure, treat, or preventive medicine, prevent disease. Drug therapy (pharmaco ...
used to treat
stomach ulcers
Peptic ulcer disease is when the inner part of the stomach's gastric mucosa (lining of the stomach), the first part of the small intestine, or sometimes the lower esophagus, gets damaged. An ulcer in the stomach is called a gastric ulcer, while ...
,
gastroesophageal reflux disease
Gastroesophageal reflux disease (GERD) or gastro-oesophageal reflux disease (GORD) is a chronic upper gastrointestinal disease in which stomach content persistently and regularly flows up into the esophagus, resulting in symptoms and/or ...
stress ulcer
A stress ulcer is a single or multiple mucosal defect usually caused by physiological (not psychological) stress which can become complicated by upper gastrointestinal bleeding. These ulcers can be caused by shock, sepsis, trauma or other con ...
s. Its usefulness in people infected by '' H. pylori'' is limited. It is used by mouth (for upper GIT ulcers) and rectally (for radiation proctitis).
Common side effects include
constipation
Constipation is a bowel dysfunction that makes bowel movements infrequent or hard to pass. The Human feces, stool is often hard and dry. Other symptoms may include abdominal pain, bloating, and feeling as if one has not completely passed the ...
. Serious side effects may include
bezoar
A bezoar stone ( ) is a mass often found trapped in the gastrointestinal system, though it can occur in other locations. A pseudobezoar is an indigestible object introduced intentionally into the digestive system.
There are several varieties o ...
formation and
encephalopathy
Encephalopathy (; ) means any disorder or disease of the brain, especially chronic degenerative conditions. In modern usage, encephalopathy does not refer to a single disease, but rather to a syndrome of overall brain dysfunction; this syndrome ...
. Use appears to be safe in
pregnancy
Pregnancy is the time during which one or more offspring gestation, gestates inside a woman's uterus. A multiple birth, multiple pregnancy involves more than one offspring, such as with twins.
Conception (biology), Conception usually occurs ...
and
breastfeeding
Breastfeeding, also known as nursing, is the process where breast milk is fed to a child. Infants may suck the milk directly from the breast, or milk may be extracted with a Breast pump, pump and then fed to the infant. The World Health Orga ...
. How it works is unclear but is believed to involve binding to the ulcer and protecting it from further damage.
Sucralfate was approved for medical use in the United States in 1981. It is available as a
generic medication
A generic drug is a pharmaceutical drug that contains the same chemical substance as a drug that was originally protected by chemical patents. Generic drugs are allowed for sale after the patents on the original drugs expire. Because the active ch ...
. In 2022, it was the 214th most commonly prescribed medication in the United States, with more than 1million prescriptions.
Medical uses
Sucralfate is used for the treatment of active duodenal ulcers not related to the use of
nonsteroidal anti-inflammatory drug
Non-steroidal anti-inflammatory drugs (NSAID) are members of a Indication (medicine), therapeutic drug class which Analgesic, reduces pain, Anti-inflammatory, decreases inflammation, Antipyretic, decreases fever, and Antithrombotic, prevents bl ...
s (NSAIDs), as the
mechanism
Mechanism may refer to:
*Mechanism (economics), a set of rules for a game designed to achieve a certain outcome
**Mechanism design, the study of such mechanisms
*Mechanism (engineering), rigid bodies connected by joints in order to accomplish a ...
behind these ulcers is due to acid oversecretion. It is not FDA approved for gastric ulcers, but is widely used because of evidence of efficacy. The use for sucralfate in
peptic ulcer disease
Peptic ulcer disease is when the inner part of the stomach's gastric mucosa (lining of the stomach), the first part of the small intestine, or sometimes the lower esophagus, gets damaged. An ulcer in the stomach is called a gastric ulcer, while ...
has diminished recently, but it is still the preferred agent for
stress ulcer
A stress ulcer is a single or multiple mucosal defect usually caused by physiological (not psychological) stress which can become complicated by upper gastrointestinal bleeding. These ulcers can be caused by shock, sepsis, trauma or other con ...
prevention.
Sucralfate has also been used for the following conditions:
* Active
duodenal ulcer
Peptic ulcer disease is when the inner part of the stomach's gastric mucosa (lining of the stomach), the first part of the small intestine, or sometimes the lower esophagus, gets damaged. An ulcer in the stomach is called a gastric ulcer, while ...
not related to NSAID use
* Maintenance therapy for resolved duodenal ulcers
* Gastric ulcer not related to NSAID use and
gastritis
Gastritis is the inflammation of the lining of the stomach. It may occur as a short episode or may be of a long duration. There may be no symptoms but, when symptoms are present, the most common is upper abdominal pain (see dyspepsia). Othe ...
due to GERD—Triple
combination therapy
In mathematics, a combination is a selection of items from a set that has distinct members, such that the order of selection does not matter (unlike permutations). For example, given three fruits, say an apple, an orange and a pear, there are ...
symptom
Signs and symptoms are diagnostic indications of an illness, injury, or condition.
Signs are objective and externally observable; symptoms are a person's reported subjective experiences.
A sign for example may be a higher or lower temperature ...
s and
quality of life
Quality of life (QOL) is defined by the World Health Organization as "an individual's perception of their position in life in the context of the culture and value systems in which they live and in relation to their goals, expectations, standards ...
and was more cost-effective than
ranitidine
Ranitidine, previously sold under the brand name Zantac among others, is a medication used to decrease stomach acid production. It was commonly used in treatment of peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellis ...
combination group.
*
Aphthous ulcer
Aphthous stomatitis, or recurrent aphthous stomatitis (RAS), commonly referred to as a canker sore or salt blister, is a common condition characterized by the repeated formation of benignity, benign and non-contagious disease, contagious mouth ...
radiation
In physics, radiation is the emission or transmission of energy in the form of waves or particles through space or a material medium. This includes:
* ''electromagnetic radiation'' consisting of photons, such as radio waves, microwaves, infr ...
or
chemotherapy
Chemotherapy (often abbreviated chemo, sometimes CTX and CTx) is the type of cancer treatment that uses one or more anti-cancer drugs (list of chemotherapeutic agents, chemotherapeutic agents or alkylating agents) in a standard chemotherapy re ...
radiotherapy
Radiation therapy or radiotherapy (RT, RTx, or XRT) is a treatment using ionizing radiation, generally provided as part of cancer therapy to either kill or control the growth of malignant cells. It is normally delivered by a linear particle ...
randomized controlled trial
A randomized controlled trial (or randomized control trial; RCT) is a form of scientific experiment used to control factors not under direct experimental control. Examples of RCTs are clinical trials that compare the effects of drugs, surgical ...
pregnancy
Pregnancy is the time during which one or more offspring gestation, gestates inside a woman's uterus. A multiple birth, multiple pregnancy involves more than one offspring, such as with twins.
Conception (biology), Conception usually occurs ...
Stress ulcer
A stress ulcer is a single or multiple mucosal defect usually caused by physiological (not psychological) stress which can become complicated by upper gastrointestinal bleeding. These ulcers can be caused by shock, sepsis, trauma or other con ...
prophylaxis
Preventive healthcare, or prophylaxis, is the application of healthcare measures to prevent diseases.Hugh R. Leavell and E. Gurney Clark as "the science and art of preventing disease, prolonging life, and promoting physical and mental health a ...
—The use of sucralfate rather than H2
antagonists
An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.aspiration, such as continuous subglottic suctioning, have been shown to reduce the risk of
ventilator-associated pneumonia
Ventilator-associated pneumonia (VAP) is a type of lung infection that occurs in people who are on mechanical ventilation breathing machines in hospitals. As such, VAP typically affects critically ill persons that are in an intensive care unit (I ...
(VAP). Sucralfate is less effective for prophylaxis against gastrointestinal bleeding than either a PPI or H2-blocker. For that reason, it is not commonly used for stress ulcer prophylaxis.
* Prevention of stricture formation—Sucralfate has an inhibitory effect on stricture formation in experimental
corrosive
Corrosion is a natural process that converts a refined metal into a more chemically stable oxide. It is the gradual deterioration of materials (usually a metal) by chemical or electrochemical reaction with their environment. Corrosion engine ...
burns and can be used in the treatment of corrosive esophageal burns to enhance
mucosal
A mucous membrane or mucosa is a membrane that lines various cavities in the body of an organism and covers the surface of internal organs. It consists of one or more layers of epithelial cells overlying a layer of loose connective tissue. It is ...
healing and suppress stricture formation
* Proctitis from
ulcerative colitis
Ulcerative colitis (UC) is one of the two types of inflammatory bowel disease (IBD), with the other type being Crohn's disease. It is a long-term condition that results in inflammation and ulcers of the colon and rectum. The primary sympto ...
prostate
The prostate is an male accessory gland, accessory gland of the male reproductive system and a muscle-driven mechanical switch between urination and ejaculation. It is found in all male mammals. It differs between species anatomically, chemica ...
bleeding
Bleeding, hemorrhage, haemorrhage or blood loss, is blood escaping from the circulatory system from damaged blood vessels. Bleeding can occur internally, or externally either through a natural opening such as the mouth, nose, ear, urethr ...
experienced immediate relief with sucrasulfate
enema
An enema, also known as a clyster, is the rectal administration of a fluid by injection into the Large intestine, lower bowel via the anus.Cullingworth, ''A Manual of Nursing, Medical and Surgical'':155 The word ''enema'' can also refer to the ...
for 1 month.
** Grade 2 bleeding, sucrasulfate enema] and/or
coagulation
Coagulation, also known as clotting, is the process by which blood changes from a liquid to a gel, forming a thrombus, blood clot. It results in hemostasis, the cessation of blood loss from a damaged vessel, followed by repair. The process of co ...
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
In epidemiology, a risk factor or determinant is a variable associated with an increased risk of disease or infection.
Due to a lack of harmonization across disciplines, determinant, in its more widely accepted scientific meaning, is often use ...
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
In anatomy, a fistula (: fistulas or fistulae ; from Latin ''fistula'', "tube, pipe") is an abnormal connection (i.e. tube) joining two hollow spaces (technically, two epithelialized surfaces), such as blood vessels, intestines, or other h ...
or stricture.
* 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
The esophagus (American English), oesophagus (British English), or œsophagus (Œ, archaic spelling) (American and British English spelling differences#ae and oe, see spelling difference) all ; : ((o)e)(œ)sophagi or ((o)e)(œ)sophaguses), c ...
prior to the battery's endoscopic removal.
*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.
Side effects
The most common
side effect
In medicine, a side effect is an effect of the use of a medicinal drug or other treatment, usually adverse but sometimes beneficial, that is unintended. Herbal and traditional medicines also have side effects.
A drug or procedure usually use ...
seen is
constipation
Constipation is a bowel dysfunction that makes bowel movements infrequent or hard to pass. The Human feces, stool is often hard and dry. Other symptoms may include abdominal pain, bloating, and feeling as if one has not completely passed the ...
(2–3%). Less commonly reported side effects (<0.5%) include
flatulence
Flatulence is the expulsion of gas from the Gastrointestinal tract, intestines via the anus, commonly referred to as farting. "Flatus" is the medical word for gas generated in the stomach or bowels. A proportion of intestinal gas may be swal ...
,
headache
A headache, also known as cephalalgia, is the symptom of pain in the face, head, or neck. It can occur as a migraine, tension-type headache, or cluster headache. There is an increased risk of Depression (mood), depression in those with severe ...
,
hypophosphatemia
Hypophosphatemia is an electrolyte disorder in which there is a low level of phosphate in the blood. Symptoms may include weakness, trouble breathing, and loss of appetite. Complications may include seizures, coma, rhabdomyolysis, or soft ...
,
xerostomia
Xerostomia, also known as dry mouth, is a subjective complaint of dryness in the mouth, which may be associated with a change in the composition of saliva, reduced salivary flow, or have no identifiable cause.
This symptom is very common and is o ...
(dry mouth), and
bezoar
A bezoar stone ( ) is a mass often found trapped in the gastrointestinal system, though it can occur in other locations. A pseudobezoar is an indigestible object introduced intentionally into the digestive system.
There are several varieties o ...
formation.
Use of this drug is not recommended for people with
chronic kidney failure
Chronic kidney disease (CKD) is a type of long-term kidney disease, defined by the sustained presence of abnormal kidney function and/or abnormal kidney structure. To meet criteria for CKD, the abnormalities must be present for at least three mo ...
, as it might cause aluminium accumulation and
toxicity
Toxicity is the degree to which a chemical substance or a particular mixture of substances can damage an organism. Toxicity can refer to the effect on a whole organism, such as an animal, bacteria, bacterium, or plant, as well as the effect o ...
.
A few well-controlled studies have been carried out investigating the safety and efficacy of sucralfate in children and pregnant women (
Pregnancy Category
The pregnancy category of a medication is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. It does ''not'' include any risks conferred by pharmaceutical agents or their ...
B).
Mechanism of action
Sucralfate is a locally acting
substance
Substance may refer to:
* Matter, anything that has mass and takes up space
Chemistry
* Chemical substance, a material with a definite chemical composition
* Drug, a chemical agent affecting an organism
Arts, entertainment, and media Music
* ' ...
that in an acidic environment (pH < 4) reacts with
hydrochloric acid
Hydrochloric acid, also known as muriatic acid or spirits of salt, is an aqueous solution of hydrogen chloride (HCl). It is a colorless solution with a distinctive pungency, pungent smell. It is classified as a acid strength, strong acid. It is ...
in the
stomach
The stomach is a muscular, hollow organ in the upper gastrointestinal tract of Human, humans and many other animals, including several invertebrates. The Ancient Greek name for the stomach is ''gaster'' which is used as ''gastric'' in medical t ...
to form a cross-linking,
viscous
Viscosity is a measure of a fluid's rate-dependent resistance to a change in shape or to movement of its neighboring portions relative to one another. For liquids, it corresponds to the informal concept of ''thickness''; for example, syrup h ...
, paste-like material capable of acting as an acid buffer for as long as 6 to 8 hours after a single dose. It also attaches to
protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metab ...
s on the surface of ulcers, such as
albumin
Albumin is a family of globular proteins, the most common of which are the serum albumins. All of the proteins of the albumin family are water- soluble, moderately soluble in concentrated salt solutions, and experience heat denaturation. Alb ...
and
fibrinogen
Fibrinogen (coagulation factor I) is a glycoprotein protein complex, complex, produced in the liver, that circulates in the blood of all vertebrates. During tissue and vascular injury, it is converted Enzyme, enzymatically by thrombin to fibrin ...
, to form stable
insoluble
In chemistry, solubility is the ability of a substance, the solute, to form a solution with another substance, the solvent. Insolubility is the opposite property, the inability of the solute to form such a solution.
The extent of the solub ...
complexes. These complexes serve as protective barriers at the ulcer surface, preventing further damage from
acid
An acid is a molecule or ion capable of either donating a proton (i.e. Hydron, hydrogen cation, H+), known as a Brønsted–Lowry acid–base theory, Brønsted–Lowry acid, or forming a covalent bond with an electron pair, known as a Lewis ...
,
pepsin
Pepsin is an endopeptidase that breaks down proteins into smaller peptides and amino acids. It is one of the main digestive enzymes in the digestive systems of humans and many other animals, where it helps digest the proteins in food. Pe ...
, and
bile
Bile (from Latin ''bilis''), also known as gall, is a yellow-green/misty green fluid produced by the liver of most vertebrates that aids the digestion of lipids in the small intestine. In humans, bile is primarily composed of water, is pro ...
. In addition, sucralfate prevents back
diffusion
Diffusion is the net movement of anything (for example, atoms, ions, molecules, energy) generally from a region of higher concentration to a region of lower concentration. Diffusion is driven by a gradient in Gibbs free energy or chemical p ...
of
hydrogen ion
A hydrogen ion is created when a hydrogen atom loses or gains an electron. A positively charged hydrogen ion (or proton) can readily combine with other particles and therefore is only seen isolated when it is in a gaseous state or a nearly particl ...
s, and absorbs both pepsin and
bile acid
Bile acids are steroid acids found predominantly in the bile of mammals and other vertebrates. Diverse bile acids are synthesized in the liver in peroxisomes. Bile acids are conjugated with taurine or glycine residues to give anions called bile ...
s.
It has been thought that sucralfate also stimulates the production of
prostaglandin
Prostaglandins (PG) are a group of physiology, physiologically active lipid compounds called eicosanoids that have diverse hormone-like effects in animals. Prostaglandins have been found in almost every Tissue (biology), tissue in humans and ot ...
bFGF
Fibroblast growth factor 2 (FGF-2), also known as basic fibroblast growth factor (bFGF) and FGF-β, is a growth factor and signaling protein encoded by the ''FGF2'' gene. It binds to and exerts effects via specific fibroblast growth factor rece ...
peptic ulcer disease
Peptic ulcer disease is when the inner part of the stomach's gastric mucosa (lining of the stomach), the first part of the small intestine, or sometimes the lower esophagus, gets damaged. An ulcer in the stomach is called a gastric ulcer, while ...
(PUD))
* Absorption: <5% Orally
* Duration: Up to 6 hours due to high affinity for defective mucosa ( PUD)
*
Bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation.
By definition, when a medication is administered intravenously, its bioavailability is 100%. H ...
: 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
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