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[Effectiveness and tolerance of selected Polish antacids in the therapy of duodenal ulcer disease. A placebo- and ranitidine-controlled study].

In a randomized, open clinical trial we compared the efficiency of selected Polish antacids Alugastrin, Gastrin and Wikalina with ranitidine and placebo in the healing of duodenal ulcer, pain relief and drug toleration. One hundred and ten outpatients completed the study. The trial showed that antacids and ranitidine had similar rates of duodenal ulcer healing which were significantly better than placebo. After 4 weeks of treatment with Alugastrin, Gastrin, Wikalina and ranitidine the healing rates were 70%, 76%, 71% and 81%, respectively, compared to placebo 44%. Efficiency of antacids in pain relief was similar to placebo and slightly lower than ranitidine. Antacids were well tolerated, except for hypermagnezemia and urine alkalization caused by Gastrin and Wikalina. We conclude that studied antacids are as effective as ranitidine in promoting healing of duodenal ulcer, but because of side effects they are not recommended for maintenance therapy.

Adult↗

Ranitidine and antacids in the prevention of duodenal ulcer relapse in Greece.

The present study was undertaken to compare the efficacy of ranitidine 150 mg/nocte with that of antacids taken "on demand" in the prevention of recurrence of duodenal ulcer (DU). Two groups (A, B) of patients with DU recently healed by ranitidine or antacids were studied. Patients of Group A (110) healed by ranitidine were put on maintenance treatment with ranitide, and patients of Group B (32) healed by antacids were given antacids "on demand" for a period of one year. Endoscopy was performed at the end of the 6th and 12th months, as well as whenever symptoms appeared. Patients were followed up clinically at 2-month intervals. Relapse rates of 11% (group A) and 34% (group B) were found at the end of the 6th month, (p less than 0.005), while the total relapse rates at the end of the 12th month were 19% and 47%, respectively (p less than 0.005). Recurrences were asymptomatic in 62% (Group A) and 27% (Group B) of patients. No significant side effects were observed. It is concluded that ranitidine 150 mg nocte is significantly superior to antacids "on demand" as far as the recurrence of DU is concerned.

Adult↗

[Role of bile acids in the development of peptic lesions. Studies on the bile acid-binding capacity of a new kind of antacid].

Bile acids are a factor in the pathogenesis of peptic lesions of the mucosa. The introduction in the literature of the term type C gastritis reflects the recognition of this fact. It is possible that antacids develop their effect not merely via the neutralization of hydrochloric acid, but, to an appreciable extent, through the adsorption of toxic substances. Since antacids often elevate the gastric pH only slightly, we investigated bile acid binding not only as a function of dose, but also at low pH values. The aim of the study was, in a follow-on to previous studies of a layer-lattice antacid to describe the characteristics of an antacid of the mixed type (aluminium-magnesium hydroxide + smectite). Already at neutral pH, Gelofalk manifests a high level of bile acid absorption, which increases further at low pH values. The high bile acid absorption capacity of Gelofalk shows no correlation with decreasing bile acid polarity; the dose-dependency is lower at high than at low pH levels. This indicates that bile acid absorption by Gelofalk must, at least in part, involve other mechanisms than those operative in the case of pure layer-lattice antacids.

Adsorption↗

Treatment of childhood peptic oesophagitis with famotidine or alginate-antacid.

Both antacids and H2 receptor antagonists have a potential role in treating peptic oesophagitis associated with acid reflux. The aim of this study is to assess the efficacy and tolerability of famotidine and alginate-antacid in children with endoscopically documented peptic oesophagitis. We compared clinical, endoscopic and histological response to alginate-antacid (1 tablet to be chewed 30 min after each meal and at bed time) or famotidine (1 mg/kg before supper at 7 pm) in 49 children (mean age 9 years, 34 males). Twenty-four of them were randomly allocated to alginate-antacid treatment (group A), twenty-five to famotidine (group B). Both treatments were protracted for six months and endoscopy was then repeated. Symptoms disappeared in 43.4% and improved in 47.8% of children of group A and disappeared in 91.6% of those of group B (p less than .05). Mean time for symptom disappearance was 17 weeks for group A and 5 weeks for group B (p less than .01). After six months, at endoscopy oesophagitis was healed in 43.4% in group A and in 41.6% of group B, the difference between the two groups was not significant, however the improvement of endoscopic grades induced by famotidine was significantly better (p less than .05). Histology showed a healed peptic oesophagitis in 52.2% of the children in group A and in 70.8% of group B (p less than .001). No toxicity was observed with either treatment. We conclude that famotidine is superior to alginate-antacid in treating peptic oesophagitis associated with acid reflux, since it induces a better symptomatic response and a greater improvement of endoscopic lesions.

Adolescent↗

Low-dose antacids versus 400 mg cimetidine twice daily for reflux oesophagitis. A comparative, placebo-controlled, multicentre study.

Ninety-one patients with reflux oesophagitis were randomly allocated to treatment with one chewable antacid tablet (acid-neutralizing capacity, 30 mmol) four times daily, 400 mg cimetidine twice daily, or placebo. The study was double-blind, with a double-dummy technique. Endoscopy was performed before inclusion and after 8 weeks' treatment. Symptoms were recorded on diary cards and on visual analogue scales. Statistically significant healing of oesophagitis was achieved in all three treatment groups, but none of the active regimens were significantly superior to placebo. Symptoms were significantly reduced with both cimetidine and antacids compared with placebo. Patients taking antacids consumed significantly less extra antacids for pain relief and had significantly better global assessment score than patients taking cimetidine during the first and second half of the study, respectively. In conclusion, neither cimetidine nor antacids were significantly superior to placebo in healing of reflux oesophagitis. Both the active regimens were superior to placebo for symptomatic relief.

Administration, Oral↗

[Length of effectiveness of calcium-containing and calcium-free antacids. A double-blind study].

The effect of a Ca-containing and Ca-free antacid on meal-stimulated acid secretion was examined by intragastric titration with pH being measured extragastrically. The Ca-containing antacid was more effective in neutralisation of the intragastric content (pH greater than 5,8) and increasing the pH (p less than 0,002). The acid secretion was reduced (p less than 0,04) by the Ca-free antacid and remained constant after administration of the Ca-containing antacid. There were no significant differences between acid secretion before and after the administration of the Ca-free and the Ca-containing antacid.

Antacids↗

The effect of antacids on the absorption of simultaneously ingested iron.

Most discussions of iron therapy include a statement about the ineffectiveness of iron ingested simultaneously with antacids. This study was designed to determine whether or not antacids inhibit iron absorption. A small-dose iron tolerance test was used to compare absorption of iron with and without various antacids. Liquid antacid containing aluminum hydroxide and magnesium hydroxide did not significantly decrease iron absorption. Sodium bicarbonate and calcium carbonate caused the plasma iron increase to be 50% and 67% less than the control values, respectively. However, when calcium carbonate was present in a multivitamin-plus-minerals tablet, the plasma iron change was not significantly different from control trials. Presumably the competitive binding of iron by ascorbic acid in the vitamin pill allowed uninhibited absorption of the iron. Our results suggest that certain antacids may be combined with iron therapy without reducing the efficacy of the iron.

Adult↗

[Evaluation of antacids "in vitro"].

Five different antacids were compared "in vitro" through titration with NaOH 0.5 N to observe their neutralising power towards HCl 1.0 N. Eight pH measurements were done for each antacid. The neutralising capacity of the antacid was calculated with a specific formula for each pH measure reading, with this information statistical calculation were made to compare the antacids among themselves, with suggest that the method can be useful in the valuation of newly produced antacid before their clinical application.

Antacids↗

Effect of antacid suspension on the pharmacokinetics of ibuprofen.

The effect of antacid administration on the pharmacokinetics of ibuprofen was evaluated in a randomized, crossover study of eight healthy volunteers. Doses of 62 mL of aluminum and magnesium hydroxide suspension and single doses of ibuprofen 400 mg were used. Subjects received each of the following treatments at one-week intervals: ibuprofen alone; ibuprofen administered concurrently with one dose of antacid; antacid administered one hour after the ibuprofen dose; and antacid administered concurrently with the ibuprofen dose, plus three more antacid doses given every five hours. Blood samples were taken at various time intervals up to 24 hours after the ibuprofen dose. Serum samples were assayed for ibuprofen content using high-performance liquid chromatography. Values for AUC, Cmax, tmax, and k were not significantly different among treatment groups. The ranges of mean (+/- S.D.) values were 113.97 +/- 21.5 to 127.53 +/- 29.3 micrograms.hr/mL for AUC, 35.30 +/- 6.40 to 41.00 +/- 10.00 micrograms/mL for Cmax, 0.95 +/- 0.30 to 1.28 +/- 0.54 hr for tmax, and 0.346 +/- 0.026 to 0.388 +/- 0.040 hr-1 for k. For the doses used, concurrent administration of aluminum and magnesium hydroxide suspension and ibuprofen does not alter ibuprofen pharmacokinetics.

Adult↗

[Antacids in combination with other anti-ulcer agents].

Antacids should not be combined with other anti-ulcer drugs such as carbenoxolone, metoclopramide, domperidone, sulpiride, di-citrato-bis-muthate and alginic acid. The effect of each single drug can be negatively influenced by combined application. H2-receptor-antagonists and sucralfate seem to be useful in combination with antacids. There is no evidence up to now that goals of therapy can be attained more effectively and in a shorter time than with either a drug alone. Before pirenzepine will be given in combination with antacids, bioavailability of the drug should be proved during antacid treatment. Today antacids in combination with other antiulcer drugs cannot be recommended for routine ulcer therapy.

Aluminum↗

[Prevention of acute stress hemorrhages of the upper gastrointestinal tract with pirenzepine and antacids. A controlled comparison between pirenzepine and cimetidine].

H2-antagonists, antacids and pirenzepine are effective drugs for prophylaxis of stress ulcer bleeding. Combined medication seems to be superior to single medication, but investigations of the effectiveness of a pirenzepine-antacid prophylaxis have not been carried out. We therefore evaluated the effect of this combination on gastric pH and on prevention of stress bleeding in ICU patients. In a prospective controlled randomized study 33 patients in each group received 50 mg. pirenzepine intravenously as a basic medication and alternatively 2000 mg. cimetidine i.v. or 2-hourly 10 ml. antacid. Gastric pH was determined three times per day. Stress bleeding was defined as bloody gastric juice, haematemesis or melaena. Two stress bleedings could be detected in each group. The pirenzepine-antacid combination proved to be superior to ensure a gastric pH of more than 3.5 than the pirenzepine-cimetidine group. After removal of the nasogastric tube the 2-hourly application of antacids proved to be impracticable.

Antacids↗

Antacids and hormones.

Antacids are neutralizing compounds which have been shown to hasten ulcer healing and to prevent bleeding from stress ulcerations. Owing to gastric alkalinization, gastrin will be released following antacid ingestion, a condition similar to that following the ingestion of a meal. Gastrin release and, more important, acid rebound also occur when the gastric mucosa comes into contact with calcium chloride. These findings indicate that acid rebound is independent of antral neutralization. Acid rebound and gastrin release will also be induced in duodenal ulcer patients by magnesium hydroxide. The magnitude of acid rebound represents one fourth to one third of the peak acid response to pentagastrin and is more marked following calcium than magnesium antacid intake. The mechanism of acid rebound may be in part due to gastrin release, but may also be due to the direct effect of calcium on the parietal cell. In the duodenum, calcium and magnesium evoke pancreatic enzyme secretion and gall bladder emptying. This effect of both cations is attributed to the release of cholecystokinin. Owing to their chemical composition, antacids stimulate the release of gastrointestinal hormones, cause acid secretion and stimulate pancreatic enzyme secretion and gall bladder concentration. So far, it has not been proven that these effects of antacids and of their chemical constituents will limit their therapeutic use.

Antacids↗

[Metabolic effects of antacids and interactions with other drugs].

The incidence of side effects from antacids is low, but patients with renal insufficiency are at risk to develop alkalosis with high doses of calcium carbonate or magnesium hydroxides, or to develop hypercalcemia due to insufficient calcium elimination by the kidneys.--A great potential exists for drug interactions with antacids. In most instances, the effectiveness of other drugs is decreased in the presence of antacids, but effectiveness may be increased for L-dopa (less degradation in stomach) or quinidine (renal elimination reduced). Interactions at the absorption level can be avoided by administering the antacid one hour after intake of the other drugs (one hour after meals) which is also the optimum dosing schedule to ensure good antacid effect. Interactions through changes of urine pH are not eliminated by observing special dosing time schedules, but by modifying the dose or by selecting alternative drug treatment.

Absorption↗

[In vitro determination of the neutralizing capacity of antacids].

The in vitro evaluation of antacids provides information about their therapeutic effectiveness. By testing the ability of antacids to buffer acid in vitro, the dependency of the neutralization or buffer capacity from the pH of the endpoint of titration should be taken into consideration. Practical and physiologic reasons suggest to use pH 3.5 as the standard reference value. Furthermore antacids, mostly those containing aluminum hydroxide, loose a considerable percentage of the buffer capacity, if they are tested in a protein solution. Finally, with regard to other indications for antacid therapy besides peptic ulcer disease like biliary reflux or alkaline gastritis, the individual ability of an antacid to bind bile acids should be tested in vitro.

Antacids↗

In vitro and In vivo evaluations of a tableted antacid and sucralfate, a new antiulcer agent.

Sucralfate is a nonsystemic drug used in the therapy of peptic ulcer disease. It is an aluminum salt of a sulfated disaccharide which adheres to ulcerated sites and forms a cytoprotective barrier to acid peptic digestion. The purposes of this study were to determine whether sucralfate had antacid activity in humans and to test the validity of the in vitro antacid qualifying test by comparing its results for tableted products with those of in vivo studies. In the in vitro antacid qualifying test Maalox #1 (4 tablets) passes and sucralfate (1 gm.) failed. These findings were consistent with the results of in vivo tests utilizing a telemetric device, the Heidelberg capsule and tube aspirations. We conclude that sucralfate does not possess antacid properties and that the results of the standard in vitro antacid qualifying test correlated well with those of in vitro studies.

Adult↗

[Antacids: A comparison of their in vitro neutralizing capacity in hydrochloric acid and in acidified peptone solution (author's transl)].

Using a simple and reproducible in vitro-test the neutralizing capacity of different liquid commercial antacids was measured at pH 2.0 and at pH 3.5 in diluted hydrochloric acid and in acidified peptone solution. In peptone solutions corresponding to postprandial gastric juice, antacids containing aluminum hydroxide and aluminate forming components demonstrated a marked loss in their neutralizing capacity when compared to peptone free hydrochloric acid as control. This loss in buffering capacity is dependent on the reaction time, the pH of the reaction mixture, the concentration of peptone in the solution and the amount of aluminum in the different antacid compounds. Furthermore the neutralizing capacity of aluminum hydroxide is also diminished by dibasic organic acids which mimicked fasting gastric juice in the experiment. The different availability of neutralizing potency of aluminum hydroxide containing antacids in acid and in acidified peptone solution will need to be considered when antacids are recommended for the treatment of patients with peptic ulcer disease.

Aluminum Hydroxide↗

[Radiotelemetric study of the effects of antacids and cimetidine on intragastric pH (author's transl)].

Radiotelemetric measurement of intragastric pH constitutes a simple method for assessing the activity of surface antacids and antisecretory agents in man. The time during which the intragastric pH is maintained at 3.5 or above is the bet criterion of therapeutic effectiveness. One hundred and fifty-two measurements were performed to evaluate the effects of six antacids administered in the usual doses and of cimetidine, milk (250 ml) and a standard continental breakfast. The results showed that the effects of antacids were extremely brief (less than 30 minutes). The delay in onset of cimetidine activity (more than 45 minutes) and the time it maintained intragastric pH above 3.5 were determined. These in vivo results correlated positively with in vitro measurements. The authors suggest that the dosage of surface antacids should be expressed in anti-acid mEq, knowing that 50 mEq produce as therapeutic effect lasting approximately 30 minutes. The data provided by radiotelemetry could be used to adjust the anti-acid treatment to the diet and the time of the day. The method also seems to be applicable to the study of new antacids and antisecretory drugs.

Adolescent↗

[Complicated ulcer; prevention and therapy of upper gastrointestinal bleeding; indications for antacid therapy].

Antacids reduce gastric acidity by neutralization, diminish peptic activity by increasing luminal pH above that optimal for proteolysis and provide thereby the rational for their use in ulcer disease. In clinical trials antacids fastened ulcer healing in patients with duodenal ulcer but not with gastric ulcer when compared to placebo. Furthermore, the prophylactic use of antacid medication can significantly reduce the frequency of acute bleeding when gastric content is titrated to a pH greater 3.5 on an hourly basis. Cimetidine does not adequately protect seriously ill patients from acute upper gastrointestinal tract bleeding. Antacids are better for this purpose. So far the efficacy of an antacid therapy has not been proven in controlled trials in patients with chronic ulcer disease, in patients with recurring ulcers following gastric surgery and in patients bleeding from acute or chronic gastroduodenal lesions.

Antacids↗