CARAFATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CARAFATE (CARAFATE).
Sucralfate, a sulfated sucrose-aluminum complex, forms a viscous adhesive barrier at the ulcer site by binding to positively charged proteins in the gastric mucosa, especially in acidic environments (pH < 4). It inhibits pepsin and adsorbs bile salts, promoting ulcer healing.
| Metabolism | Sucralfate is minimally absorbed (3-5% of dose). The small absorbed fraction is primarily excreted unchanged in urine. No significant hepatic metabolism. |
| Excretion | Primarily fecal (∼90%) as unabsorbed drug; small amount absorbed drug is excreted unchanged in urine via glomerular filtration and tubular secretion; biliary excretion is minimal. |
| Half-life | 2–4 hours for the absorbed portion (if any), but clinical duration is dependent on local binding to gastrointestinal mucosa rather than systemic elimination. |
| Protein binding | Negligible (<1%); does not bind significantly to plasma proteins. |
| Volume of Distribution | Not applicable for IV; negligible systemic absorption; no meaningful Vd. |
| Bioavailability | <5% (oral) due to poor absorption; acts locally in gastrointestinal tract. |
| Onset of Action | 30–60 minutes (oral) for binding to ulcer site; effect on mucosal protection begins immediately upon coating. |
| Duration of Action | Up to 6 hours due to prolonged retention in gastric mucosa and formation of protective barrier; dosing typically 4 times daily. |
1 g orally four times daily on an empty stomach (1 hour before meals and at bedtime).
| Dosage form | SUSPENSION |
| Renal impairment | No specific dose adjustment required; however, use caution in patients with chronic renal failure due to aluminum absorption. |
| Liver impairment | No dose adjustment needed; not metabolized by the liver. |
| Pediatric use | Not established for children <18 years; limited data suggest 40-80 mg/kg/day divided every 6 hours, not to exceed 4 g/day. |
| Geriatric use | No specific dose adjustment; use lowest effective dose and monitor for constipation due to decreased gastrointestinal motility. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CARAFATE (CARAFATE).
| Breastfeeding | Sucralfate is minimally absorbed systemically (<5%) and is not expected to be excreted into breast milk in clinically significant amounts. M/P ratio not determined. Considered compatible with breastfeeding. |
| Teratogenic Risk | Pregnancy Category B. No evidence of teratogenicity in animal studies. Insufficient human data in first trimester; risk cannot be excluded. In second and third trimesters, no known fetal risks from topical gastrointestinal action. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to sucralfate or any component of the formulation"]
| Precautions | ["Aluminum accumulation may occur in patients with chronic renal failure, especially those on dialysis, leading to aluminum toxicity (osteomalacia, encephalopathy).","Constipation is common due to formation of aluminum-sucrose complex.","May bind to other drugs in GI tract, reducing absorption. Separate administration by at least 2 hours.","Use with caution in patients with diabetes due to sucrose content (about 1.6 g per gram of sucralfate)."] |
| Food/Dietary | Avoid taking with food or antacids; food reduces binding efficacy. Do not take within 2 hours of antacids. High-protein meals may decrease effectiveness. Administer on empty stomach. |
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| No specific monitoring required beyond routine prenatal care. Monitor for constipation, a common adverse effect, which may be exacerbated in pregnancy. |
| Fertility Effects | No known effects on fertility based on animal studies and limited human data. Sucralfate is not systemically absorbed and is unlikely to impact reproductive function. |
| Clinical Pearls | Carafate (sucralfate) forms a protective barrier over ulcer sites; administer on an empty stomach 1 hour before or 2 hours after meals. Separate from other oral medications by at least 2 hours to avoid binding. Use with caution in renal impairment due to aluminum absorption. Ineffective for GERD without erosive esophagitis. |
| Patient Advice | Take this medication on an empty stomach, 1 hour before or 2 hours after meals. · Separate Carafate from other oral medications by at least 2 hours. · Common side effects include constipation; drink plenty of fluids. · Do not crush or chew the tablet; swallow whole. · Complete the full course as prescribed even if symptoms improve. · Inform your doctor if you have kidney problems or are on dialysis. |