The P-I-E-N-O Parkinsn's List Drug Database
sucralfate/ CarafateTM
GASTROINTESTINAL:
Antiulcer
Description: Sucralfate is an oral gastrointestinal drug. Chemically, it is a sucrose sulfate complex. Sucralfate is indicated for the treatment of active duodenal ulcers and as maintenance therapy following resolution of a duodenal ulcer. The efficacy of sucralfate in the treatment of gastric ulcers is comparable to cimetidine. Sucralfate has been used in the relief of GI symptoms occurring with NSAIDs, although in one study, sucralfate was significantly less effective than misoprostol in this setting.I Other uses for sucralfate include treatment of gastroesophageal reflux disease (GERD) as well as prophylaxis and treatment of stress-induced mucosal damage. Sucralfate was approved by the FDA in 1981.
Mechanism of Action: Unlike HA-antagonists, sucralfate does not appear to affect gastric acid concentration. In addition, sucralfate exerts its action locally rather than systemically. Sucralfate reacts with hydrochloric acid in the stomach to form an adherent, paste-like substance capable of acting as an acid buffer. Subsequently, sucralfate adheres electrostatically to proteins on the surface of an ulcer, such as albumin and fibrinogen, forming insoluble, stable complexes. These ulcer-bound complexes act as a protective barrier at the ulcer site, which facilitates recovery by shielding the ulcer from the ulcerogenic properties of pepsin, acid, and bile. Sucralfate predominantly binds to damaged GI mucosa, although binding to normal mucosa occurs to a minimal extent. This agent also inhibits back-diffusion of hydrogen ions, and adsorbs both pepsin and bile acids. Recent data indicate that production of prostaglandin EA and gastric mucus may be increased.
Pharmacokinetics: Sucralfate is administered orally. Following oral administration, minimal amounts of sucralfate are absorbed systemically (3-5%). Sucralfate predominantly acts locally, with the duration of action dependent upon the length of contact at the ulcer site. Binding to ulcer sites has been demonstrated for up to 6 hours. It is unknown whether sucralfate crosses the placenta or is distributed into breast milk. Animal studies indicate that the majority of an oral dose (>90%) is excreted in the feces within 48 hours.
CONTRAINDICATIONS/PRECAUTIONS: Small amounts of aluminum can be absorbed following oral administration of sucralfate. This agent should not be given concomitantly with other agents containing aluminum (e.g., aluminum-containing antacids) because the total body burden of aluminum can increase. Aluminum is cleared by the kidneys in patients with normal renal function; patients with renal disease, however, can develop aluminum accumulation and intoxication in the form of aluminum osteodystrophy, osteomalacia, or encephalopathy.
Sucralfate can interfere with the absorption of other medications if administered concomitantly (see Drug Interactions).
DRUG INTERACTIONS: Sucralfate can bind with certain drugs in the GI tract, including cimetidine, ranitidine, digoxin, phenytoin, tetracyclines, and theophylline, reducing the bioavailability of these agents. Sucralfate should be given 2 hours before or after the oral administration of these agents.
Antacids can interfere with the binding capacity of sucralfate to the GI mucosa, decreasing its effectiveness. Antacids should not be administered within 30 minutes of sucralfate. In addition, antacids or other aluminum-containing agents should be used cautiously with sucralfate in patients with chronic renal failure due to the aluminum content of sucralfate and the potential for aluminum toxicity.
Concomitant administration of sucralfate with quinolone antibiotics, such as ciprofloxacin, norfloxacin, or ofloxacin, can decrease the absorption of these antibiotics and substantially reduce their serum concentrations. This interaction appears to be the result of chelation by the aluminum content of sucralfate. These antibiotics should not be administered within 2 hours of sucralfate. Fleroxacin oral bioavailability is decreased by approximately 23% when coadministered with sucralfate. Although sucralfate contains aluminum and it is known that divalent and trivalent cations can bind with fluoroquinolone antibiotics, the mechanism of this interaction is not clear at this time since antacids do not affect the bioavailability of fleroxacin as much as other fluoroquinolones. Since fleroxacin is essentially completely absorbed, the remaining 77% of a fleroxacin dose is still bioavailable and may be sufficient to make this interaction not clinically significant.¥
Sucralfate has been shown to decrease the bioavailability of ketoconazole when these two drugs were administered together. Staggering the times of administration may alleviate this pharmacokinetic interaction.
Simultaneous administration of levothyroxine with sucralfate has been reported to interfere with the clinical response to levothyroxine. Although the mechanism is yet to be determined, it is possible that sucralfate may reduce levothyroxine bioavailability.
Sucralfate has been shown to delay absorption and reduce the bioavailability of lansoprazole. Lansoprazole should be taken no less than 30 minutes before sucralfate if these drugs are to be used concomitantly.
ADVERSE REACTIONS: Sucralfate is well tolerated, with few adverse effects reported. Constipation is the most frequent adverse effect, occurring in 2% of patients.
Adverse effects reported in fewer than 0.5% of patients include diarrhea, nausea/vomiting, gastric discomfort, indigestion, flatulence, dry mouth, rash, pruritis, headache, dizziness, back pain, drowsiness, and vertigo, which rarely require discontinuation of sucralfate.
There have been reports of hypersensitivity reactions to sucralfate. These include urticaria (hives), angioedema, respiratory difficulty and rhinitis. A causal relationship haa not yet been established.
PATIENT INFORMATION:
What do sucralfate tablets do?
Sucralfate (CarafateTM ) helps to treat or prevent the recurrence of stomach or duodenal ulcers; to prevent ulcers in hospitalized patients or patients using nonsteroidal antiinflammatory drugs (NSAIDS). Sucralfate coats and protects ulcers or irritated stomach lining from the effects of acid. Generic sucralfate tablets are not yet available.
What should my doctor, dentist, or pharmacist know before I take sucralfate?
They need to know if you have any of these conditions:
How should I take this medicine?
Take sucralfate tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Sucralfate works best if taken on an empty stomach, at least 1 hour before or 2 hours after meals. Take your doses at regular intervals. Do not take your medicine more often than directed.
Special precautions for use in children:
This medicine is not for use in children.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
What other medicines can interact with sucralfate?
Tell your doctor or pharmacist: about all other medicines you are taking, including non-prescription medicines; if you are a frequent user of drinks with caffeine or alcohol; if you smoke; or if you use illegal drugs. These may affect the way your medicine works. Check before stopping or starting any of your medicines.
What side effects may I notice from taking sucralfate?
Serious side effects with sucralfate are rare and are more likely in patients over 60 years old or patients with severe kidney problems. They include:
Call your doctor as soon as you can if you get any of these side effects.
Minor side effects with sucralfate include:
Let your doctor know about these side effects if they do not go away or if they annoy you.
What do I need to watch for while I take sucralfate?
Check with your doctor if your condition does not improve, or if it gets worse. Although healing with sucralfate can occur within two weeks, you should continue treatment until your doctor has examined your stomach to make sure healing is complete.
If you need to take antacid, take it at least 2 hours after a dose of sucralfate or more than 30 minutes before.
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30C (59 and 86F). Keep container tightly closed. Throw away any unused medicine after the expiration date.
Parkinsn's Archive Treasures Page
John Cottingham is the webmaster of this site.
