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    Other Drugs for Peptic Ulcer and Gastro-Esophageal Reflux Disease/GERD

    DEA CLASS

    Rx

    DESCRIPTION

    Oral aluminum-containing sucrose sulfate complex; forms adherent, protective barrier at sites of damaged GI mucosa, shields mucosa from pepsin, acid, and bile; used for esophagitis, GERD, GI ulceration, and stomatitis.

    COMMON BRAND NAMES

    Carafate

    HOW SUPPLIED

    Carafate/Sucralfate Oral Susp: 1g, 10mL
    Carafate/Sucralfate Oral Tab: 1g

    DOSAGE & INDICATIONS

    For the treatment of duodenal ulcer not related to NSAID use.
    For active disease.
    Oral dosage
    Adults

    1 g PO four times per day, given 1 hour before meals and at bedtime for 4—8 weeks or less if healing has been effectively demonstrated.

    For maintenance therapy of duodenal ulcer.
    Oral dosage (tablets only)
    Adults

    1 g PO two times per day on an empty stomach.

    For the treatment of gastric ulcer† not related to NSAID use or for treatment of esophagitis† associated with gastroesophageal reflux disease (GERD)†.
    Oral dosage
    Adults

    1 g PO four times per day given one hour before meals and at bedtime.

    For NSAID-induced ulcer prophylaxis†.
    Oral dosage
    Adults

    Several studies have evaluated sucralfate as an agent to prevent NSAID-induced ulcers. In a small study of healthy males, sucralfate 1 g PO four times per day was superior to placebo in preventing gastric injury due to aspirin. Endoscopy was not used in this study. However, some clinicians feel that sucralfate has no place in the prevention or therapy of NSAID-induced gastric ulcer and does not appear to prevent NSAID-associated duodenal ulcer. In a comparison with misoprostol to prevent the development of NSAID-induced gastric ulcer in patients during 3 months of continuous NSAID administration, the incidence of gastric ulcer was 1.6% in the misoprostol group and 16% in the sucralfate group. The sucralfate dose in this study was 1 g PO four times per day given one hour before meals and at bedtime.

    For stress gastritis prophylaxis†.
    Oral dosage
    Adults

    Although the use of sucralfate in this setting has been questioned , doses of 4, 6, or 9 g/day in divided doses have been used.

    For the palliative treatment of aphthous ulcer†, or for the palliative treatment of stomatitis† due to chemotherapy or radiation therapy.
    Oral rinse dosage (sucralfate suspension)
    Adults

    5—10 ml (500 mg to 1 g) PO swished in the mouth for several minutes and spit or swallowed, four times per day. Retain in the mouth for several minutes while swishing to insure contact time with affected oral mucosal surfaces.

    For the alternative treatment of proctitis† due to ulcerative colitis or radiation injury.
    Rectal dosage (rectal suspension retention enema, commercial dosage form not available in U.S)
    Adults

    Doses range from 2—4 g per 15—20 ml (3 g/15 ml is a common dosage for radiation proctitis) PR once or twice daily or as 20 g/100 ml PR once or twice daily (for ulcerative proctosigmoiditis) in literature reports. Prophylactic use (rectally or orally) to prevent radiation injury does not appear to be effective. Extemporaneous compounds vary and have not been adequately characterized for stability or other attributes (see Administration). One case report described using the commercially available oral suspension to deliver a 2 g/20 ml dosage PR twice daily ; however, the effect of formulation excipients on the rectal mucosal or in regard to safety, efficacy, or tolerability are not known.

    †Indicates off-label use

    MAXIMUM DOSAGE

    Adults

    4 g/day PO.

    Elderly

    4 g/day PO.

    Adolescents

    4 g/day PO.

    Children

    Maximum dosage not established. 80 mg/kg/day PO or alternatively, up to 2000 mg/day PO has been suggested for most indications.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Renal Impairment

    CrCl > 30 ml/min: Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
    CrCl <= 30 ml/min: Sucralfate contains aluminum; systemically absorbed in small amounts. Patients with renal failure can develop aluminum accumulation due to impaired aluminum excretion. Use with caution in patients with renal failure.
     
    Intermittent hemodialysis
    Sucralfate contains aluminum, which may be systemically absorbed in small amounts. Aluminum does not cross dialysis membranes because of high plasma protein binding, and may accumulate in patients on dialysis.

    ADMINISTRATION

    Oral Administration

    Take on an empty stomach at least one hour prior to a meal and at bedtime. If antacids are being administered, do not give antacids within 30 minutes before or 1 hour after sucralfate.

    Oral Solid Formulations

    Tablets: Do not crush or chew (the tablet dosage form is not amenable to crushing or chewing). The sucralfate tablet is scored and may be cut into two pieces for ease of administration.

    Oral Liquid Formulations

    Sucralfate suspension is for oral administration only. Fatal complications, including pulmonary and cerebral emboli, have occurred with the inadvertent intravenous administration of sucralfate suspension.
    Shake sucralfate well prior to administration; measure dosage with calibrated device. For enteral tube administration, flush the tube with 30 mL of water (adults) before and after administering the drug.

    Extemporaneous Compounding-Oral

    Slurry†: For patients with difficulty swallowing whole or halved sucralfate tablets, a slurry may be prepared just prior to administration by slowly dissolving (the tablet dosage form is not amenable to crushing) a 1 gram tablet in 10 mL of distilled water, allowing to stand for 15 to 20 minutes. Equal parts of sorbitol 70% and cherry syrup may be added if desired. Shake well before administration. Some references state that a prepared slurry is stable for up to 2 weeks at room temperature.

    Rectal Administration

    Marketed formulations are not available in the U.S. While doses have been characterized in literature reports, extemporaneous formulations for those doses have not been standardized. Water, or 5% or 10% methylcellulose solutions, have been used as diluents for the oral tablets for compounding the dosages reported. Stability data and expiration date recommendations are generally not available for these extemporaneous enemas.
    One article reports a case of rectal administration of the commercially available 10% sucralfate oral suspension to deliver a 2 g/20 mL dosage rectally twice daily; however, the effect of formulation excipients on the rectal mucosal or with regard to safety, efficacy, or tolerability are not known.
    Another article reported an extemporaneous formula for 10% sucralfate rectal enema as follows: Crush one-hundred-twenty (120) sucralfate 1-g tablets to a fine powder using a large mortar and pestle. Add the powder to 300 mL of 10% methylcellulose solution, mixing well. This will form a paste until the rest of the methylcellulose is added and it is important to allow this phase to occur to establish 'high-shear' forces that will allow the powder to be well distributed when the enema suspension is finished. Then, add more methylcellulose to make a final volume of 1200 mL. Package in disposable enema bottles or rectal syringes in 2 g/20 mL packages. Label with 'refrigerate', 'shake well', and 'protect from light'. Because stability data are not available, the author recommended no longer than a 2-week expiration date.

    STORAGE

    Carafate:
    - Storage information not available

    CONTRAINDICATIONS / PRECAUTIONS

    General Information

    NOTE: Sucralfate can interfere with the absorption of other medications if administered concomitantly (see Drug Interactions).

    Dialysis, renal failure, renal impairment

    Small amounts of aluminum can be absorbed following oral administration of sucralfate. Each 1 g tablet contains roughly 207 mg of aluminum. Sucralfate 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. However, patients with renal failure or those receiving dialysis can develop aluminum accumulation due to impaired aluminum excretion. Aluminum does not cross dialysis membranes because of high plasma protein binding. Aluminum intoxication in the form of aluminum osteodystrophy, osteomalacia, or encephalopathy has been described in patients with renal impairment. Sucralfate should be used with caution in patients with renal failure.

    Diabetes mellitus

    Use sucralfate suspension cautiously in patients with diabetes mellitus. Cases of hyperglycemia have been reported in diabetic patients being treated with this product. Close monitoring of blood sugar is recommended; antidiabetic therapy may need adjustment in some patients during concomitant treatment with sucralfate suspension.

    Dysphagia, gag reflex depression

    Isolated reports of sucralfate tablet aspiration with accompanying respiratory complications have been received. Therefore, sucralfate tablets should be used with caution by patients who have known conditions that may impair swallowing, such as recent or prolonged intubation, tracheostomy, prior history of aspiration, dysphagia, or any other conditions that may alter gag and cough reflexes (e.g., conditions causing gag reflex depression) or diminish oropharyngeal coordination or motility.

    Geriatric

    Clinical studies of sucralfate did not include sufficient numbers of geriatric patients to determine whether they respond differently compared to younger patients; however, no differences have been reported during clinical experience. Because of an increased frequency of renal and hepatic impairment in the elderly and because of the possibility of comorbidity and concomitant drug use, careful dose selection (usually starting at the low end of the dosing range) should be observed.

    Children, infants, neonates

    Safe and effective use of sucralfate in children, infants, and neonates has not been established.

    Pregnancy

    Sucralfate is classified in FDA pregnancy category B. Animal studies have not indicated a potential for fetal harm. However, because animal studies are not always indicative of human response, sucralfate should be used in pregnancy only when clearly needed. Epidemiologic evidence, including evidence from a prospective, randomized controlled trial, suggests a lack of association of sucralfate with congenital events. The American College of Gastroenterology generally considers the use of sucralfate safe during gestation in women with normal renal function, due to the local rather than systemic action of the drug and the available clinical data.

    Breast-feeding

    Because only small portions of sucralfate are absorbed systemically in the mother, and virtually no excretion is expected into breast milk, sucralfate is considered to be compatible with breast-feeding by the American College of Gastroenterology.

    Intravenous administration

    Sucralfate suspension is for oral administration only. Fatal complications, including pulmonary and cerebral emboli, have occurred with the inadvertent intravenous administration of sucralfate suspension. Do not administer sucralfate suspension intravenously.

    ADVERSE REACTIONS

    Severe

    bezoar / Delayed / Incidence not known
    angioedema / Rapid / Incidence not known
    anaphylactoid reactions / Rapid / Incidence not known
    aluminum toxicity / Delayed / Incidence not known

    Moderate

    constipation / Delayed / 2.0-2.0
    edema / Delayed / Incidence not known
    dyspnea / Early / Incidence not known
    hypophosphatemia / Delayed / Incidence not known
    hyperglycemia / Delayed / Incidence not known

    Mild

    dizziness / Early / 0-0.5
    headache / Early / 0-0.5
    nausea / Early / 0-0.5
    rash / Early / 0-0.5
    flatulence / Early / 0-0.5
    vomiting / Early / 0-0.5
    back pain / Delayed / 0-0.5
    drowsiness / Early / 0-0.5
    xerostomia / Early / 0-0.5
    pruritus / Rapid / 0-0.5
    vertigo / Early / 0-0.5
    urticaria / Rapid / Incidence not known

    DRUG INTERACTIONS

    Abacavir; Dolutegravir; Lamivudine: (Moderate) Administer dolutegravir 2 hours before or 6 hours after taking sucralfate. The chemical structure of sucralfate contains aluminum, which can bind dolutegravir in the GI tract. Taking these drugs simultaneously may result in reduced bioavailability of dolutegravir.
    Alendronate: (Moderate) Concomitant administration of oral alendronate with aluminum-containing medications (e.g., sucralfate) may interfere with the absorption of alendronate. Separation of administration is advised. At least 30 minutes should elapse after an alendronate dose before taking aluminum-containing drugs.
    Alendronate; Cholecalciferol: (Moderate) Concomitant administration of oral alendronate with aluminum-containing medications (e.g., sucralfate) may interfere with the absorption of alendronate. Separation of administration is advised. At least 30 minutes should elapse after an alendronate dose before taking aluminum-containing drugs.
    Amoxicillin; Clarithromycin; Lansoprazole: (Moderate) Sucralfate has been shown to delay absorption and reduce the bioavailability of lansoprazole by about 17%. Lansoprazole should be taken no less than 30 minutes before sucralfate if these drugs are to be used concomitantly.
    Amoxicillin; Clarithromycin; Omeprazole: (Minor) Proton pump inhibitors should be taken at least 30 minutes prior to sucralfate. Sucralfate has been shown to delay absorption and reduce the bioavailability of omeprazole by about 16%.
    Antacids: (Major) 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.
    Aspirin, ASA; Omeprazole: (Minor) Proton pump inhibitors should be taken at least 30 minutes prior to sucralfate. Sucralfate has been shown to delay absorption and reduce the bioavailability of omeprazole by about 16%.
    Bictegravir; Emtricitabine; Tenofovir Alafenamide: (Moderate) Concomitant administration of bictegravir and sucralfate may result in decreased bictegravir plasma concentrations. The chemical structure of sucralfate contains aluminum, which can bind bictegravir in the GI tract, resulting in reduced bioavailability of bictegravir. Caution and close monitoring are advised if these drugs are used together.
    Calcium Acetate: (Major) Oral antacids, including calcium salts, potentially interfere with gastric mucosal binding of sucralfate. This interaction can be minimized by staggering the doses of these agents as much as possible.
    Calcium Carbonate: (Major) Oral antacids, including calcium carbonate, potentially interfere with gastric mucosal binding of sucralfate. This interaction can be minimized by staggering the doses of these agents as much as possible.
    Calcium Carbonate; Magnesium Hydroxide: (Major) Oral antacids, including calcium carbonate, potentially interfere with gastric mucosal binding of sucralfate. This interaction can be minimized by staggering the doses of these agents as much as possible.
    Calcium Carbonate; Risedronate: (Major) Oral antacids, including calcium carbonate, potentially interfere with gastric mucosal binding of sucralfate. This interaction can be minimized by staggering the doses of these agents as much as possible.
    Calcium Chloride: (Major) Calcium salts potentially interfere with gastric mucosal binding of sucralfate. This interaction can be minimized by staggering the doses of these agents as much as possible.
    Calcium Citrate: (Major) Oral antacids, including calcium salts, potentially interfere with gastric mucosal binding of sucralfate. This interaction can be minimized by staggering the doses of these agents as much as possible.
    Calcium Gluconate: (Major) Oral antacids, including calcium salts, potentially interfere with gastric mucosal binding of sucralfate. This interaction can be minimized by staggering the doses of these agents as much as possible.
    Ciprofloxacin: (Major) Administer oral ciprofloxacin at least 2 hours before or 6 hours after sucralfate. Ciprofloxacin absorption may be reduced as quinolone antibiotics can chelate with sucralfate. This interaction appears to be the result of chelation by the aluminum content of sucralfate.
    Delafloxacin: (Major) Administer oral delafloxacin at least 2 hours before or 6 hours after sucralfate. Delafloxacin absorption may be reduced as quinolone antibiotics can chelate with sucralfate. This interaction appears to be the result of chelation by the aluminum content of sucralfate.
    Dexlansoprazole: (Moderate) Sucralfate has been shown to delay the absorption and reduce the bioavailability of oral lansoprazole by about 17%. Dexlansoprazole should be taken no less than 30 minutes before sucralfate if these drugs are to be used concomitantly. Concurrent administration of oral dexlansoprazole and antacids may reduce the bioavailability of dexlansoprazole; except when the antacids are given at least 30 minutes to one hour before dexlansoprazole administration.
    Digoxin: (Moderate) Sucralfate, because it contains aluminum in its structure and due to its mechanism of action, can bind with digoxin in the GI tract, reducing its bioavailability. Sucralfate should be given 2 hours before or after the oral administration of digoxin. In addition, the manufacturer of digoxin recommends measuring serum digoxin concentrations prior to initiation of sucralfate. Continue monitoring during concomitant treatment and increase the digoxin dose by 20 to 40% as necessary.
    Diphenhydramine; Naproxen: (Moderate) Concomitant administration of sucralfate and enteric-coated or delayed-release naproxen tablets can delay the absorption of naproxen. Periodic use should not be problematic as long as sucralafatge and naproxen administration are separated by at least 2 hours.
    Dolutegravir: (Moderate) Administer dolutegravir 2 hours before or 6 hours after taking sucralfate. The chemical structure of sucralfate contains aluminum, which can bind dolutegravir in the GI tract. Taking these drugs simultaneously may result in reduced bioavailability of dolutegravir.
    Dolutegravir; Rilpivirine: (Moderate) Administer dolutegravir 2 hours before or 6 hours after taking sucralfate. The chemical structure of sucralfate contains aluminum, which can bind dolutegravir in the GI tract. Taking these drugs simultaneously may result in reduced bioavailability of dolutegravir.
    Enteral Feedings: (Minor) The risk of bezoar formation may be increased when sucralfate is combined with enteral feedings; additionally, continuous enteral feedings have been reported to interfere with the therapeutic efficacy of sucralfate for selected indications. When sucralfate is given via a feeding tube, careful attention to proper administration technique is recommended. In patients receiving continuous enteral feedings, the selection of an alternative agent to sucralfate may be warranted.
    Esomeprazole: (Minor) Sucralfate may delay absorption and reduce the bioavailability of lansoprazole. Lansoprazole should be taken no less than 30 minutes before sucralfate. This interaction is theoretical and is based on the interaction between sucralfate and lansoprazole; sucralfate has been shown to delay absorption and reduce the bioavailability of lansoprazole by about 17%. No information is available to determine if a similar interaction occurs with esomeprazole.
    Esomeprazole; Naproxen: (Moderate) Concomitant administration of sucralfate and enteric-coated or delayed-release naproxen tablets can delay the absorption of naproxen. Periodic use should not be problematic as long as sucralafatge and naproxen administration are separated by at least 2 hours. (Minor) Sucralfate may delay absorption and reduce the bioavailability of lansoprazole. Lansoprazole should be taken no less than 30 minutes before sucralfate. This interaction is theoretical and is based on the interaction between sucralfate and lansoprazole; sucralfate has been shown to delay absorption and reduce the bioavailability of lansoprazole by about 17%. No information is available to determine if a similar interaction occurs with esomeprazole.
    Ethotoin: (Major) The oral absorption of ethotoin may be reduced by sucralfate. Although the magnitude of this interactions is not great, an occasional patient may be affected and the interaction may lead to subtherapeutic ethotoin concentrations. Sucralfate should be given 2 hours before or after the ethotoin.
    Furosemide: (Major) According to the manufacturer for furosemide, simultaneous administration of sucralfate and furosemide may reduce its natriuretic and antihypertensive effects. Patients receiving both drugs should be observed closely to determine if the desired diuretic and/or antihypertensive effect of furosemide is achieved. The intake of furosemide and sucralfate is recommended to be separated by at least two hours.
    Gemifloxacin: (Major) Administer sucralfate at least 3 hours before or 2 hours after gemifloxacin. Gemifloxacin absorption may be reduced as quinolone antibiotics can chelate with sucralfate. This interaction appears to be the result of chelation by the aluminum content of sucralfate.
    Ketoconazole: (Major) Concomitant administration of oral ketoconazole with sucralfate may interfere with the absorption of ketoconazole. Separation of administration is advised.
    Lansoprazole: (Moderate) Sucralfate has been shown to delay absorption and reduce the bioavailability of lansoprazole by about 17%. Lansoprazole should be taken no less than 30 minutes before sucralfate if these drugs are to be used concomitantly.
    Lansoprazole; Naproxen: (Moderate) Concomitant administration of sucralfate and enteric-coated or delayed-release naproxen tablets can delay the absorption of naproxen. Periodic use should not be problematic as long as sucralafatge and naproxen administration are separated by at least 2 hours. (Moderate) Sucralfate has been shown to delay absorption and reduce the bioavailability of lansoprazole by about 17%. Lansoprazole should be taken no less than 30 minutes before sucralfate if these drugs are to be used concomitantly.
    Lanthanum Carbonate: (Major) Oral compounds known to interact with antacids, like sucralfate, should not be taken within 2 hours of dosing with lanthanum carbonate. If these agents are used concomitantly, space the dosing intervals appropriately. Monitor serum concentrations and clinical condition.
    Levofloxacin: (Major) Administer sucralfate at least 2 hours before or 2 hours after orally administered levofloxacin. Levofloxacin absorption may be reduced as quinolone antibiotics can chelate with sucralfate. This interaction appears to be the result of chelation by the aluminum content of sucralfate. Chelation of divalent cations with levofloxacin is less than with other quinolones.
    Moxifloxacin: (Major) Administer oral moxifloxacin at least 4 hours before or 8 hours after sucralfate. Moxifloxacin absorption may be reduced as quinolone antibiotics can chelate with sucralfate. This interaction appears to be the result of chelation by the aluminum content of sucralfate.
    Naproxen: (Moderate) Concomitant administration of sucralfate and enteric-coated or delayed-release naproxen tablets can delay the absorption of naproxen. Periodic use should not be problematic as long as sucralafatge and naproxen administration are separated by at least 2 hours.
    Naproxen; Pseudoephedrine: (Moderate) Concomitant administration of sucralfate and enteric-coated or delayed-release naproxen tablets can delay the absorption of naproxen. Periodic use should not be problematic as long as sucralafatge and naproxen administration are separated by at least 2 hours.
    Naproxen; Sumatriptan: (Moderate) Concomitant administration of sucralfate and enteric-coated or delayed-release naproxen tablets can delay the absorption of naproxen. Periodic use should not be problematic as long as sucralafatge and naproxen administration are separated by at least 2 hours.
    Norfloxacin: (Major) Administer sucralfate at least 2 hours before or 2 hours after norfloxacin. Norfloxacin absorption may be reduced as quinolone antibiotics can chelate with sucralfate. This interaction appears to be the result of chelation by the aluminum content of sucralfate.
    Ofloxacin: (Major) Administer sucralfate at least 2 hours before or 2 hours after ofloxacin. Ofloxacin absorption may be reduced as quinolone antibiotics can chelate with sucralfate. This interaction appears to be the result of chelation by the aluminum content of sucralfate.
    Omeprazole: (Minor) Proton pump inhibitors should be taken at least 30 minutes prior to sucralfate. Sucralfate has been shown to delay absorption and reduce the bioavailability of omeprazole by about 16%.
    Omeprazole; Sodium Bicarbonate: (Major) 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. (Minor) Proton pump inhibitors should be taken at least 30 minutes prior to sucralfate. Sucralfate has been shown to delay absorption and reduce the bioavailability of omeprazole by about 16%.
    Phenytoin: (Major) Sucralfate, because it contains aluminum in its structure and due to its mechanism of action, can bind with certain drugs in the GI tract, including phenytoin, reducing the bioavailability of these agents. Sucralfate should be given 2 hours before or after the oral administration of these agents. Be alert to altered clinical response to phenytoin and monitor blood concentrations as clinically indicated.
    Phosphorus: (Moderate) Serum phosphorus should be checked routinely in patients treated chronically with sucralfate; sucralfate may cause hypophosphatemia and some patients may require phosphorus repletion. This nutrient interaction should be considered in patients receiving phosphates for dietary supplementation. It appears that sucralfate chelates phosphorus in the gut, forming nonabsorbable complexes. Because of sucralfate's therapeutic effect, this interaction may not be prevented by separating times of oral administration.
    Posaconazole: (Major) The manufacturer suggests drugs that increase gastric pH, such as sucralfate, may decrease the absorption of posaconazole. The manufacturer recommends monitoring patients for breakthrough fungal infections.
    Sodium Bicarbonate: (Major) 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.
    Tetracyclines: (Major) Divalent or trivalent cations readily chelate with tetracycline antibiotics, forming insoluble compounds. The oral absorption of these antibiotics will be significantly reduced by other orally administered compounds that contain aluminum salts, calcium salts, iron salts, magnesium salts, and/or zinc salts. Sucralfate, because it contains aluminum in its structure and due to its mechanism of action, can bind with tetracyclines in the GI tract, reducing the bioavailability of these agents. Sucralfate should be given 2 hours before or after the oral administration of tetracyclines.
    Theophylline, Aminophylline: (Major) Sucralfate, because it contains aluminum in its structure and due to its mechanism of action, can bind with certain drugs in the GI tract, including aminophylline, reducing its bioavailability. Sucralfate should be given 2 hours before or after the oral administration of aminophylline. (Major) Sucralfate, because it contains aluminum in its structure and due to its mechanism of action, can bind with certain drugs in the GI tract, including theophylline, reducing its bioavailability. Sucralfate should be given 2 hours before or after the oral administration of theophylline.
    Thyroid hormones: (Major) Concurrent use of sucralfate may reduce the efficacy of levothyroxine and other thyroid hormones by binding and delaying or preventing absorption, potentially resulting in hypothyroidism. Administer levothyroxine at least 4 hours apart from a dose of sucralfate. Patients treated concomitantly with these drugs should be monitored for changes in thyroid function. Consider an alternative to sucralfate, if appropriate.
    Warfarin: (Moderate) Sucralfate has been reported to interfere with warfarin absorption. While isolated reports have shown that sucralfate can inhibit warfarin oral absorption, other studies have shown no clinical effect.

    PREGNANCY AND LACTATION

    Pregnancy

    Sucralfate is classified in FDA pregnancy category B. Animal studies have not indicated a potential for fetal harm. However, because animal studies are not always indicative of human response, sucralfate should be used in pregnancy only when clearly needed. Epidemiologic evidence, including evidence from a prospective, randomized controlled trial, suggests a lack of association of sucralfate with congenital events. The American College of Gastroenterology generally considers the use of sucralfate safe during gestation in women with normal renal function, due to the local rather than systemic action of the drug and the available clinical data.

    Because only small portions of sucralfate are absorbed systemically in the mother, and virtually no excretion is expected into breast milk, sucralfate is considered to be compatible with breast-feeding by the American College of Gastroenterology.

    MECHANISM OF ACTION

    Mechanism of Action: Sucralfate exerts its action locally rather than systemically and its effect on gastric acid is negligible with a low acid-neutralizing capacity (14—16 mEq/dose). 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. In vivo, recommended doses of sucralfate inhibit pepsin activity in gastric juice by 32%. Recent data indicate that production of prostaglandin E2 and gastric mucus may be increased. Sucralfate also absorbs bile salts in vitro.

    PHARMACOKINETICS

    Sucralfate is administered orally. 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. Animal studies indicate that the majority of an oral dose (> 90%) is excreted in the feces within 48 hours. Any systemically absorbed drug is excreted primarily in the urine.

    Oral Route

    Following oral administration, minimal amounts of sucralfate are absorbed systemically (3—5%).