Hexadeca-μ-hydroxytetracosahydroxy[μ8-[1,3,4,6-tetra-O-sulfo-β-Dfructofuranosyl-α-D-glucopyranoside tetrakis(hydrogen sulfato)8-hexadecaaluminum
Sucralfate is a cytoprotective agent, an oral gastrointestinal medication primarily indicated for the treatment of active duodenal ulcers. Brand names include Sucramal in Italy; Carafate in U.S.A.; Pepsigard, Sucral, Sucrafil, Hapifate in India; Sutra or Musin in parts of South-East Asia; Sulcrate in Canada; Ulsanic in South Africa and Israel; and Antepsin in Turkey. Sucralfate is also used for the treatment of gastroesophageal reflux disease (GERD) and stress ulcers. Unlike the other classes of medications used for treatment of peptic ulcers, sucralfate is a sucrose sulfate-aluminium complex that binds to the mucosa, thus creating a physical barrier that impairs diffusion of hydrochloric acid in the gastrointestinal tract and prevents degradation of mucus by acid. It also stimulates bicarbonate output and acts like an acid buffer with cytoprotective properties. Sucralfate was approved by the U.S. Food and Drug Administration (FDA) in 1981
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. 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. In addition, it prevents back diffusion of hydrogen ions, and adsorbs both pepsin and bile acids. Recently, it has been indicated that sucralfate also stimulates the increase of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus.
Clinical uses
The only FDA-approved indication for sucralfate is for the treatment of active duodenal ulcers not related to NSAID usage because the mechanism behind these ulcers is secondary to acid oversecretion. It is not technically approved for gastric ulcers because the main mechanism is not due to acid oversecretion but rather from diminished protection. The use for sucralfate in peptic ulcer disease has diminished recently, but it is still the preferred agent for stress ulcer prophylaxis.
Active duodenal ulcer not related to NSAID use—1 g PO four times a day given 1 h before meals and at bedtime for 4–8 weeks
Maintenance therapy for resolved duodenal ulcers—1 g PO bid on empty stomach
Gastric ulcer not related to NSAID use and gastritis due to GERD—1 g PO four times a day 1 h before meals and at bedtime. Triple combination therapy with lansoprazole + cisapride + sucralfate can significantly improve symptoms and quality of life and was more cost-effective than ranitidine combination group.
Aphthous ulcer and stomatitis due to radiation or chemotherapy—5-10 mL PO suspension swish and spit/swallow four times a day.
Proctitis from radiation or ulcerative colitis—3 g/15 mL rectal suspension once or twice daily.
Gastro-esophageal reflux disease during pregnancy -- first-line drug therapy combined with lifestyle and diet modification.
Stress ulcer prophylaxis—The use of sucralfate rather than H2 antagonists for stress ulcer prophylaxis, and measures to prevent aspiration, such as semirecumbent positioning or continuous subglottic suctioning, have all been shown to reduce the risk of ventilator-associated pneumonia (VAP).
Prevention of stricture formation—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
Rectal bleeding and its management after irradiation for uterine cervical cancer
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 patients. 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.
Adverse reactions
The most common side effects seen are constipation 2-3% and bezoar formation. Less commonly reported include flatulence, cephalalgia (headache), hypophosphatemia, and xerostomia (dry mouth). Avoid using this drug in patients with chronic renal failure, it might cause them aluminum-induced nephropathy. Nursing mothers: Uncertain.
Sucralfate is used to treat ulcers. It adheres to damaged ulcer tissue and protects against acid and enzymes so healing can occur.
This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.
How should this medicine be used?
Sucralfate comes as a tablet and liquid to take by mouth. It usually is taken four times a day, 1 hour before meals and at bedtime. Take sucralfate on an empty stomach, 2 hours after or 1 hour before meals. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take sucralfate exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Shake liquid sucralfate well before measuring doses.
This medicine must be taken regularly to be effective. It may take up to 8 weeks for ulcers to heal.
Other uses for this medicine
Sucralfate is also used to protect the stomach lining when taking aspirin and for mouth sores that occur with cancer chemotherapy. Talk to your doctor about the possible risks of using this drug for your condition.
What special precautions should I follow?
Before taking sucralfate,
tell your doctor and pharmacist if you are allergic to sucralfate or any other drugs.
tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially antacids (Mylanta, Maalox), anticoagulants ('blood thinners') such as warfarin (Coumadin), cinoxacin (Cinobac), ciprofloxacin (Cipro), digoxin (Lanoxin), enoxacin (Penetrex), ketoconazole (Nizoral), levofloxacin (Levaquin), lomefloxacin (Maxaquin), nalidixic acid (NegGram), norfloxacin (Noroxin), ofloxacin (Floxin), phenytoin (Dilantin), quinidine, sparfloxacin (Zagam), tetracycline (Sumycin), and vitamins. If you are taking any of these medicines, do not take them within 2 hours of taking sucralfate.
tell your doctor if you have or have ever had heart or kidney disease or diabetes.
tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking sucralfate, call your doctor.
What should I do if I forget a dose?
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
What side effects can this medication cause?
Sucralfate may cause side effects. To avoid constipation, abdominal pain, and gas, eat a high-fiber diet (extra fruits, vegetables, salads, and bran) and drink plenty of fluids.
If you experience any of the following symptoms, call your doctor immediately:
passing red or black stools
coughing up or vomiting material that is bright red or looks like coffee grounds
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088].
What storage conditions are needed for this medicine?Return to top
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.
What other information should I know?
Keep all appointments with your doctor and the laboratory. Your doctor will order certain lab tests to check your response to sucralfate.
Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.
No comments:
Post a Comment