Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: KEGG:D00446 (Sucralfate)
 278 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Two formulations of [99mTc]sucralfate have been used to image gastric and duodenal ulcers and inflammatory bowel disease. One formulation is a complexation of [99mTc]HSA with sucralfate. The second is prepared by directly labeling sucralfate with [99mTc]pertechnetate in the presence of stannous ion. An in vitro study of the factors affecting the production and stability of these labeled sucralfate preparations was conducted. Both formulations were stable at the acidic pH likely encountered in the stomach. However, at pH greater than 6 the albumin-sucralfate complex began to dissociate while directly labeled sucralfate was stable to a pH of 9. Conversely it was shown that directly labeled sucralfate was more susceptible to loss of 99mTc to other chelating species. Sucralfate complexed with [99mTc]HSA was radiochemically stable up to a specific activity of 26 GBq (700 mCi) per gram while directly labeled sucralfate showed decreased 24-hr stability at specific activities greater than 837 mCi (31 GBq) per gram.
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PMID:Chemical aspects of labeling sucralfate with 99mTcO4. 254 93

Conventional stress bleeding prophylaxis with antacids or histamine (H2)-antagonists, as well as the newer mucosa-protective drugs pirenzepine and sucralfate, are satisfying most of the clinicians with regard to efficacy of stress bleeding prevention. Therefore, potential side effects are attaining crucial importance with regard to the drugs to be used. Pharmacologic blockade of cardiac H2-receptors increases the risk of bradycardia and negative inotropic effects as well as coronary vasoconstriction at least in the presence of elevated plasma histamine levels. Intracardiac injection of pirenzepine can lead to temporary tachycardia. Elderly patients have been shown to be at an increased risk of side effects to the central nervous system when treated with H2-antagonists. These drugs can also induce toxic effects in the liver. Cimetidine leads to interactions with a number of drugs used in the intensive care unit. In patients with pre-existing pulmonary diseases, H2-antagonists have been demonstrated to increase pulmonary bronchoconstriction. Alkalinization of the gastric juice is associated with a significant increase in colonization of gram-negative bacteria in the stomach. In intubated patients, aspiration of stomach contents occurs in 30 to 40 percent of the patients. A number of studies have shown a direct correlation between alkalinization of the gastric juice and pulmonary infections. Sucralfate and to a lesser degree pirenzepine can reduce the risk of pulmonary infections. Sucralfate also exerts a bactericidal effect. Recent investigations support the hypothesis that alkalinization of the stomach also increases the risk of systemic infections. This may be the main reason for the observation that at least in ventilated patients sucralfate, unlike H2-antagonists or antacids, leads to a significant reduction of the mortality rate compared with conventional stress bleeding prophylaxis.
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PMID:Side effects of stress bleeding prophylaxis. 256 72

Sucralfate (55 patients), cimetidine (25 patients), ranitidine (30 patients), antacids and cholinolytics (32 patients) were studied and compared in open clinical trials for the efficacy in the treatment of ulcer disease of the stomach and duodenum. During 5 weeks, ulcers completely healed in 100% of the patients given sucralfate (in 94.5% for 4 weeks), in 90% of the patients treated with ranitidine, in 84% on cimetidine, and in 78% of the patients undergoing treatment with antacids and cholinolytics.
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PMID:[A comparative evaluation of the efficacy of sucralfate and H2-histamine blockaders in treating peptic ulcer]. 257 63

Sucralfate possesses site protective and cytoprotective actions and heals ulcers effectively, but its effect on gastric mucosal blood flow is unknown. Using an ex vivo gastric chamber preparation, we studied the effect of sucralfate on gastric mucosal blood flow in rats by laser doppler flowmetry. Under both fasting and fed states, measurements of gastric mucosal blood flow and damage were made in rats after topical application of absolute ethanol alone or after pretreatment with sucralfate. Gastric mucosal damage was assessed by measuring the total area of haemorrhagic mucosal lesions. Ethanol induced gastric mucosal lesions were significantly less with sucralfate pretreatment than without (p less than 0.008). Mucosal blood flow significantly fell after ethanol application (p less than 0.001). The fall was significantly less in fed than in fasted rats (p less than 0.05), and after pretreatment with sucralfate 100 mg or 200 mg than without in both fasted (p less than 0.0008 and 0.00001, respectively) and fed (p less than 0.002 and 0.001, respectively) rats. Graded doses of sucralfate (25-400 mg) resulted in an increase in gastric mucosal blood flow in a dose dependent manner (r = 0.731, p less than 0.001). In conclusion that sucralfate increases gastric mucosal blood flow in rats and lessens the fall in blood flow in rats treated with ethanol, and this action may contribute to its protection against the vascular damage of mucosa by ethanol.
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PMID:Effect of sucralfate on gastric mucosal blood flow in rats. 259 40

Endoscopic distinction between ulcers and erosions is difficult. Consequently, existing literature, which must be taken at face value, may be misleading. Nevertheless, from published studies most gastric and duodenal ulcers associated with nonsteroidal antiinflammatory drugs appear to heal on antacids or H2-antagonists. Sucralfate appears useful for duodenal but not gastric ulcers. Continuing nonsteroidal antiinflammatory drugs does not prevent or delay healing of duodenal or small gastric ulcers; their effects on large gastric ulcers remain uncertain. Thus far, only full doses of H2-antagonists, or their combinations with antacids, have been shown to heal ulcers and prevent recurrences. Ulcer recurrences and complications have occurred in small numbers of patients on maintenance doses of H2-antagonists. Available antiulcer drugs (antacids, H2-antagonists, sucralfate) reduce severe acute injury when taken before or with nonsteroidal antiinflammatory drugs. They also reduce ulcerlike symptoms due to nonsteroidal antiinflammatory drugs. Inexplicably, chronic prophylaxis with H2-antagonists for 4 wk or more appears ineffective in preventing gastric ulcers, although duodenal injury is reduced. As the efficacy of available prophylactic therapy (H2-antagonists, sucralfate, and antacids) has not been established, routine use in all cases seems unjustified at present.
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PMID:Nonsteroidal antiinflammatory drug-induced ulcers: management by traditional therapies. 264 51

To assess the gastric mucosal protective action of sucralfate against alcohol, a double-blind, controlled, randomized study was carried out in 12 healthy adult men. All subjects received four treatments in a random sequence: sucralfate + ethanol, sucralfate + ethanol placebo, sucralfate placebo + ethanol, and sucralfate placebo + ethanol placebo. Fundal, antral, and duodenal mucosae were submitted to endoscopic examinations, and the antral mucosa underwent histologic examination before and after injury. Biopsy specimens were taken from the antral mucosa to determine by radioimmunoassay its capacity to synthesize prostaglandin E2, thromboxane B2, and 6-keto prostaglandin F1 alpha. In both the fundus and the antrum, the mean endoscopic injury score after sucralfate plus ethanol administration was significantly lower than that after ethanol alone. All treatments tended to increase prostanoid values but 6-keto prostaglandin F1 alpha increased significantly when sucralfate was given. Sucralfate did not affect serum ethanol levels, nor did ethanol affect prostanoid synthesis. It is concluded that sucralfate provides significant protection to the human gastric mucosa against ethanol injury, and that this may be partly due to increased prostanoid synthesis.
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PMID:Sucralfate protection of human gastric mucosa against acute ethanol injury. 264 75

Sucralfate as well as colloidal bismuth subcitrate (CBS) and probably also bismuth subsalicylate (BBS) are effective in the acute treatment of peptic ulcer disease. Sucralfate also has positive effects upon symptoms and healing of peptic lesions in reflux esophagitis. Healing rates in gastric and duodenal ulcers are equal to those obtained with H2-antagonists. Side effects are rare, transient and generally mild. Therapy with bismuth compounds should be restricted to 4-8 weeks (cave: bismuth encephalopathy). Healing rates of smokers with duodenal ulcers were the same as in non-smokers during sucralfate therapy. Sucralfate seems to be useful in the treatment (prophylaxis?) of NSAID-induced lesions in the upper gastrointestinal tract. The question of different recurrence rates in peptic ulcer disease after various kinds of medical treatment still remains open. The relationship between the etiology of peptic ulcer disease and Campylobacter pylori infection, as well as possible medical and therapeutic consequences, should be further investigated.
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PMID:Sucralfate and other non-antisecretory agents in the treatment of peptic ulcer disease. 265 80

Sucralfate suspension 1 g/10 ml four times per day was found to be significantly better than placebo for the healing of active duodenal ulcer. An eight-week, double-blind, randomized, placebo-controlled, parallel-group multicenter study was conducted. A total of 292 patients were evaluated. Ulcer healing was evaluated by endoscopy and symptom assessment occurred at baseline and at two, four, and eight weeks, or upon symptom worsening as determined by the investigator. Healing was defined as complete re-epithelialization of the crater, without residual erosion. Patients completed eight weeks of treatment regardless of whether or not they were healed at two or four weeks. Treatment groups were comparable with regard to age, sex, ulcer history, cigarette smoking, alcohol and caffeine consumption, ulcer size, and ulcer symptoms. Analysis of procedurally correct cases demonstrated that sucralfate suspension was significantly more effective in healing duodenal ulcers than placebo at two, four, and eight weeks. Ulcer-healing rates efficacy analysis are as follows. At two weeks, the healing rate of sucralfate suspension was 22 of 125 patients (18 percent) and the healing rate of placebo suspension was eight of 130 patients (6 percent; p = 0.006). At four weeks, 58 of 114 patients (51 percent) for sucralfate and 38 of 112 patients (34 percent) for placebo (p = 0.011) were healed. At eight weeks, 80 of 105 (76 percent) for sucralfate and 53 of 100 (53 percent) for placebo (p = 0.001) were healed. Sucralfate-treated patients experienced significantly greater reductions in both daytime and nighttime pain scores at two weeks. A significant difference between treatment groups was also found for daytime symptoms at four weeks. At four and eight weeks, patients who smoked cigarettes had significantly lower healing rates than those who did not, regardless of treatment group. Sucralfate suspension was found to be effective for the treatment of active duodenal ulcer.
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PMID:Sucralfate suspension 1 g four times per day in the short-term treatment of active duodenal ulcer. 266 May 50

Twice-daily dosing with sucralfate was evaluated by two multicenter trials, trial 1 (eight weeks) and trial 2 (four weeks). Both trials demonstrated significantly better ulcer healing at study completion for the 2-g twice daily (B.I.D.) regimen compared with placebo. Both trials were double-blind, randomized, and placebo-controlled, with parallel groups. Patients received two doses daily consisting of sucralfate 2 g B.I.D., placebo/sucralfate 2 g at bedtime (H.S.), or placebo/placebo. Ulcer healing was assessed by scheduled endoscopy and symptom assessment. Healing was defined as complete absence of erosion or ulceration. Trial 1 evaluations were conducted at four and eight weeks, trial 2 evaluations at two and four weeks. Interim examinations were performed at investigator discretion. Treatment groups were comparable with regard to number of patients, age, sex, smoking status, ulcer size, and presence/absence of baseline symptoms. Sucralfate 2 g B.I.D. was significantly better than H.S. or placebo dosing at the completion of each trial. H.S. dosing was better than placebo only at the four-week analysis of trial 1. At Week 4 of trial 1, 14 of 54 patients (26 percent) were healed with the B.I.D. sucralfate regimen, whereas at Week 8, 41 of 54 (76 percent) were healed (p less than 0.001). For the placebo/sucralfate H.S. group, 17 of 57 patients (30 percent) were healed at Week 4 (p less than 0.05), and 32 of 56 patients (57 percent) were healed at Week 8. For the placebo group, six of 52 (12 percent) and 20 of 51 patients (39 percent) were healed at Weeks 4 and 8, respectively. In trial 2, the B.I.D. group had a 21 percent healing rate at Week 2 (13 of 61 patients) and 62 percent were healed at Week 4 (38 of 61 patients; p less than 0.05). The H.S. group had an 8 percent healing rate (five of 66 patients) at Week 2 and 50 percent (33 of 66 patients) at Week 4. For the placebo group, 10 of 62 patients (16 percent) and 26 of 62 patients (42 percent) were healed at Weeks 2 and 4, respectively. Trial 1 demonstrated significant symptom improvement for active treatment groups at both four and eight weeks, whereas no differences were found in trial 2. Sucralfate 2 g B.I.D. was found to be safe and effective for the treatment of acute duodenal ulcer.
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PMID:Twice-daily sucralfate dosing to heal acute duodenal ulcer. Multicenter Study Group. 266 May 51

Sucralfate 1 g twice daily was found to be significantly better than placebo for the prevention of duodenal ulcer recurrence. This was a double-blind, randomized, placebo-controlled, parallel groups study. A total of 254 patients with a history of two or more duodenal ulcers, the most recent event diagnosed within three months of study entry, were entered into the trial after healing was documented. Patients received sucralfate 1 g twice daily or placebo for four months, or until recurrence. Endoscopies and symptom assessments were scheduled monthly and at investigator discretion upon symptom development. Treatment groups were comparable with regard to number of patients, age, sex, smoking status, and ulcer history. Traditional ulcer prevalence and point prevalence analyses were performed. Traditional ulcer prevalence included all ulcers found at scheduled visits and interim recurrences. Point prevalence included only ulcers found at scheduled visits. In the traditional analysis, sucralfate was significantly better than placebo in reducing ulcer recurrence for all months of the study. The life table estimate of the cumulative percent with ulcer at four months was 42 percent for the sucralfate group and 63 percent for the placebo group (p = 0.002). At four months, there were 49 recurrences among 122 patients in the sucralfate group and 71 among 117 patients for the placebo group. In the point prevalence analysis, sucralfate was significantly better than placebo in reducing ulcer recurrence at Months 2 through 4. The life table estimate of the cumulative percent with ulcer at four months was 36 percent for the sucralfate group and 55 percent for the placebo group (p = 0.005). At four months, there were 38 recurrences among 114 patients in the sucralfate group and 54 among 104 patients for the placebo group. Both analyses demonstrated that sucralfate 1 g twice daily was significantly better than placebo for the prevention of duodenal ulcer recurrence. Symptom development was associated with recurrence in both treatment groups. Smoking was associated with a greater tendency to recur in placebo-treated patients only.
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PMID:Sucralfate tablets 1 g twice a day for the prevention of duodenal ulcer recurrence. 266 May 55


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