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PubMed1979

Fate of oral neutralizing antacid and its effect on postprandial gastric secretion and emptying.

The fate and neutralizing efficiency of oral antacids (aluminum and magnesium hydroxides) as well as their effect on postprandial gastric function were quantified in 6 patients with duodenal ulcer disease. We employed a double-marker technique for measurement of gastric secretion and emptying and combined this with back-titration of the gastric samples and analysis of aluminum to trace the fate of antacid in the stomach and duodenum. These studies show that: (a) antacid therapy with aluminum and magnesium hydroxides significantly increases gastric secretion; (b) intragastric neutralization of gastric acid produces a significant and substantial decrease in net acid output (acid secreted minus acid neutralized), but the beneficial effects of neutralization are partially offset by incomplete intragastric formation of aluminum trichloride; (c) most but not all of the ingested antacid is utilized in acid neutralization in the stomach (average 78.6% in our 6 patients); and (d) antacid therapy does not modify the absolute rate of postprandial gastric emptying, but increases dilution of gastric contents, expanding the intragastric volume. Thus, the fractional gastric emptying rate declines, and this, in turn, should enhance antacid utilization by delaying its emptying.

Administration, Oral↗
PubMed1985

Clinical evaluation of triletide versus antacids in the treatment of duodenal ulcer out-patients.

Thirty out-patients with endoscopically assessed, active duodenal ulcer of mild to moderate intensity were randomly assigned to 8-weeks' treatment with either antacids (0.8 g/day each of aluminium hydroxide and magnesium hydroxide), triletide (1.5 g/day) or a combination of the two treatments. Every other week, the intensity of subjective symptoms and of objective signs was scored and recorded, and the endoscopic outcome assessed at the 8th week. Three patients on antacids alone and 1 on triletide alone were withdrawn at the 4th week because of therapeutic failure. Symptoms and signs improved in the three groups significantly faster, to a significantly greater extent, and in more patients with triletide, alone or in combination, than with antacids. Endoscopic evidence of therapeutic response was detected in significantly more patients given triletide, alone or in combination, in comparison with the group who had antacids. A significant influence on promoting ulcer healing could be attributed to triletide (p less than 0.05, multiple linear regression) and not to antacids. Tolerance was complete in all patients. It is concluded that triletide appears to be equally well tolerated as, but significantly more effective than, antacids in relieving symptoms and promoting healing in patients with mild to moderate duodenal ulcer.

Adult↗
PubMed1979

[Cimetidine versus antacids].

The rationale of ulcer therapy with cimetidine or antacids is to block or neutralize gastric acid secretion intragastrically. 5 tablets of cimetidine can inhibit gastric acid secretion in duodenal ulcer patients by more than 50% over a 24-hour period. Approximately 250 ml per day of a highly active antacid is necessary to achieve a similar effect. The effect of cimetidine on night secretion is superior. In acute ulcer attack cimetidine brings about healing of the ulcer in duodenal ulcer disease in about 80% of all patients in about 4-6 weeks, and a maintenance dose of 200 mg in the evening may prevent a recurrence within a year in about 50% of all patients. According to American studies, antacid therapy in the above-mentioned dosage may achieve a similar healing rate in duodenal ulcer patients in acute attack. However, it is unknown whether high antacid therapy prevents ulcer recurrences. If acceptability of the treatment by the patient, side effects and costs are taken into account, cimetidine appears to be superior to high doses of antacid. However, it must be considered that in many European countries, including Switzerland, the spontaneous healing rate is up to 60% in placebo studies. It is thus legitimate to continue treating uncomplicated ulcers with the small antacid doses customary in Europe.

Antacids↗
PubMed1982

Antacid therapy for duodenal and gastric ulcer: the experience in the United States.

An intensive antacid regimen, 15 to 30 ml 1 and 3 hours after each meal and at bedtime, has a significant effect on duodenal ulcer healing as compared to placebo and is as effective as cimetidine in endoscopically assessed trials. The healing rates at 4 weeks for placebo, antacid, and cimetidine are about 24%, 59%, and 62%, respectively. Smoking reduces the frequency of ulcer healing irrespective of therapy. Ulcer recurrences are as frequent after antacid as after cimetidine. Extensive placebo-controlled trials have not been reported for antacid treatment of gastric ulcer, but regular antacid dosing was as effective as cimetidine in one trial. Both the acute relief of ulcer pain and the pain relief during several weeks of therapy are similar between antacid and placebo, but pain relief per se is not a reliable indicator of ulcer healing.

Antacids↗
PubMed1982

Methods for the assessment of antacids. In-vitro and in-vivo investigations with gastric aspiration.

In-vitro investigations offer a simple and reproducible method to estimate antacid potency and reactivity. The acid-neutralizing capacity, the onset and duration of action and the buffering capacity of an antacid can be determined by these tests. In vivo- tests can, to some extent, approximate in-vivo conditions and the in-vivo potency of an antacid can be predicted with reasonable accuracy by means of in-vitro tests. In vitro tests are needed to control and standardize various antacid preparations which vary in composition and content. In-vivo tests are needed to assess antacid potency in various physiological conditions and to study the principles of an optimal antacid therapy. The most conventional of these methods has been the aspiration technique. pH-recording by means of repeated gastric aspirates is more laborious than in other methods but will give reliable results when a proper and careful aspiration technique is used.

Antacids↗
PubMed1980

Failure of gastric pH control by antacids or cimetidine in the critically ill: a valid sign of sepsis.

To compare the ability of antacids and cimetidine to control gastric pH and potential hemorrhage, 77 critically ill patients were randomized into two groups initially receiving either antacids (37 patients) or cimetidine (40 patients). Gastric pH was monitored hourly and the dosage of medication adjusted as required to maintain gastric pH above 4. Forty-nine patients maintained a pH above 4 while receiving a standard dose of antacids (29 patients) or cimetidine (20 patients). Only 8 of these 49 patients proved to be septic, compared to 20 of the 28 patients who required additional medication to maintain pH above 4 (P less than 0.001). There were five episodes of gastrointestinal hemorrhage occurring in septic patients who had a gastric pH consistently below 4 despite treatment. Excluding septic patients, 8 of 23 failed to maintain a gastric pH of 4 on cimetidine compared to 0 of 26 receiving antacids (P less than 0.005). The data suggest that (1) persistent failure of antacids and/or cimetidine to maintain gastric pH above 4 is yet another indicator of often unappreciated infection, (2) maintaining gastric pH above 4 largely prevents gastrointestinal hemorrhage, and (3) cimetidine is not as consistently effective as antacids in maintaining gastric pH above 4.

Adolescent↗
PubMed1980

Acute relief of epigastric pain by antacid in duodenal ulcer patients.

Thirty-six duodenal ulcer patients participated in a randomized controlled trial of the immediate effect of a liquid antacid preparation (Link) and placebo on epigastric pain. The patients recorded the effect of a total of 143 doses of antacid and 148 doses of placebo. Marked or complete relief of pain 30 min after ingestion was found after 62% of the antacid doses and after 52% of the placebo doses. The average effect of antacid was better than the effect of placebo in 21 patients, worse in 8 and equal in 7 patients. This difference in favour of antacid is statistical significant (p less than 0.05) and therefore it is concluded that antacid is more effective than placebo in relieving epigastric pain in duodenal ulcer patients, although the therapeutic gain is small.

Antacids↗
PubMed1978

Rapid fall of serum phosphorus secondary to antacid therapy.

Two patients with marked hypophosphatemia secondary to antacid therapy are described, 1 asymptomatic and the other symptomatic. In contrast to previous reports, these 2 patients were on aluminum hydroxide-containing antacids for relatively short periods of time before the hypophosphatemia occurred. Hypophosphatemia developed after only moderate doses of antacid in the symptomatic patient who was on a low phosphorus diet. An adequate intake of dietary phosphorus or phosphorus-containing antacids may be necessary to avoid a low serum phosphorus in patients taking aluminum hydroxide antacids even when the duration of therapy is as short as 2 weeks and the dose of antacids is not large.

Aged↗
PubMed1980

In vitro antidiabetics-antacid interactions.

The adsorption of the oral antidiabetics metformin hydrochloride, glibenclamide, acetohexamide, tolbutamide, carbutamide, tolazamide and glymidine on various antacids or adsorbents was studied at 37 degrees C. The antacids or adsorbents used were magnesium trisilicate, aluminium hydroxide, calcium carbonate, magnesium oxide, bismuth oxycarbonate, talc, kaolin as well as charcoal. None of the substances tested, with the exception of charcoal, exhibited superior adsorptive properties for all the drugs. Magnesium trisilicate and calcium carbonate were the best adsorbents for metformin hydrochloride. Acetohexamide and glibenclamide were adsorbed to an appreciable extent on most antacids. Tolbutamide showed an adsorption tendency towards talc. Most antacids slightly adsorbed carbutamide, while magnesium trisilicate showed a higher adsorption capacity for tolazamide and glymidine. The dissolution rate of acetohexamide in magnesium oxide suspension (5:400) increased about 40-fold after 10 min, whle in magnesium trisilicate suspension (5:400) it increased about 7-fold. On the other hand, magnesium trisilicate did not influence the dissolution rate of metformin hydrochloride. The probable variation in the bioavailability of orally administered antidiabetics when coadministered with antacids was discussed. However, further in vivo studies are needed before a final assessment for such drug-antacid interaction can be confirmed.

Adsorption↗
PubMed1994

Antacid activity of calcium carbonate and hydrotalcite tablets. Comparison between in vitro evaluation using the "artificial stomach-duodenum" model and in vivo pH-metry in healthy volunteers.

Antacid activity of calcium carbonate (CAM, Rennie) and of hydrotalcite (HYD) containing tablets has been assessed in vitro using computer-controlled "artificial stomach-duodenum" model, including or not a piece of hog gastric mucosa in the gastric reservoir, and simulating the constant flux system or the normal gastroduodenal flux regulation. The data obtained under the latter condition were compared to those obtained in vivo by pH-metry in 12 healthy volunteers, in response to one administration of 2 tablets. The theoretical maximal capacity was similar when 1 tablet of CAM or of HYD was added to the gastric contents, including or not a piece of gastric mucosa, close to 95 H+ mmol. The reduction of acid load penetrating into the duodenum and the duodenal pH were of the same magnitude in response to both antacids. When normal gastroduodenal flux regulation was simulated, a dose-response curve, constructed by 1, 2 or 3 tablets, resulted in the same antacid characteristics in response to both antacids. The maximal gastric and the mean duodenal pH values obtained with CAM were, however, higher than with HYD, corresponding to a greater neutralizing activity developed by CAM than by HYD. The comparison between in vivo administration of two tablets of each antacid and the in vitro model simulating normal gastroduodenal flux regulation in response to the addition of two tablets resulted in similar data. The maximal pH values obtained in in vivo assays were slightly lower than in vitro, depending on the ratio of antacid amount to gastric acid content, well established in in vitro conditions and unknown in in vivo situations.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1976

The in vitro adsorption of some antibiotics on antacids.

The adsorption of oxytetracycline hydrochloride, tetracycline hydrochloride, doxycycline hyclate, triacetyloleandomycin, chloramphenicol, ampicillin, and cloxacillin sodium was studied on various antacids namely, magnesium trisilicate, magnesium oxide, calcium carbonate, bismuth oxycarbonate, aluminium hydroxide, and kaolin. The adsorption of the various antibiotics by milk was also tested as milk is frequently used as an antacid. Charcoal was included in the present study as a model adsorbent having a large hydrophobic surface. The adsorption of the various antibiotics on the different antacids and other adsorbents in most cases obeyed the Freundlich adsorption isotherm. Magnesium trisilicate and magnesium oxide showed the highest adsorptive capacity, relative to other antacids used, for most antibiotics. Calcium carbonate and aluminium hydroxide and intermediate power while kaolin and bismuth oxycarbonate had the least adsorptive power. Charcoal exhibited a marked adsorption for all antibiotics tested. Tetracyclines were found to be more highly adsorbed than other antibiotics studied. Triacetyloleandomycin and chloramphenicol had intermediate values. Ampicillin was only adsorbed to a slight extent while cloxacillin was not adsorbed on the antacids used. The extent of adsorption was correlated to the structure of both the adsorbent and adsorbate, the pH of the adsorbent suspension, and to the polarity of the antibiotic in such pH. The reversibility of the adsorption process was studied in different media and at pH values similar to those of the gastrointestinal tract. The extent of elution was found to be inversely proportional to the adsorptive capacity of the different adsorbents. In general, 0.0143 n NaHCO3 solution was found to possess higher eluting properties than 0.01 n HCl. An exception to this pattern was observed with tetracyclines adsorbed on aluminium hydroxide where the elution with acid resulted in a higher degree of desorption. Careful in vitro and in vivo testing of drug availability is advisable prior to the concomitant administration of antibiotics with antacids or other adsorbents.

Adsorption↗
PubMed1996

In vitro evaluation of magaldrate antacid efficacy in the presence of some drugs and its effect on their dissolution rates: Part I.

A comparison of the antacid efficacy of magaldrate powder and its dosage forms on an equal weight basis by an in vitro technique revealed that: suspensions > chew tablets > powder. This was also evidenced by acid neutralizing capacity test USP XXIII, which also showed that riopan and rioplus suspensions were equipotent. All tested doses of different antacid dosage forms were found to regulate acid level to pH 3.0 within 10 seconds. This rapidity of action depends on its dose, dosage forms, and extent of chewing the tablets. The antacid efficacy of tested antacid was not affected by the concomitant presence of two tablets of duspatalin, faverin and panadol (group I) or their equivalent weights of pure powders, whilst, the duration of action, buffering capacity and total acid consumption was significantly suppressed with two dosage units of inderal, aspirin, and indocid (group II) or their equivalents of pure powder. However, antacid tested was still regulating gastric acid level within the comfort zone for a period of 70-110 min, and possessing (20.01-25.10 mEq/g) with group (II). These results are consistent with that obtained from acid neutralizing capacity test. The dissolution of magaldrate was pH dependent, with fast magnesium release and sustained aluminum hydroxide conversion. A significant (p < 0.05) retardation of the release rates of group (II), whilst, a non significant (p > 0.05) effect on that of group (I) was observed in the presence of different doses of antacid tested in all dissolution media. The presence of riopan suspension (20 ml) had a significant suppression on the release rates in all systems.

Aluminum Hydroxide↗
PubMed1997

Effect of acarbose and simultaneous antacid therapy on blood glucose.

In a single-centre, placebo-controlled, clinical study, the influence of an antacid containing magnesium hydroxide and aluminium hydroxide (Maalox 70; 10 ml) on the pharmacodynamics of the oral antidiabetic drug acarbose (Glucobay 100, Bay g 5421, CAS 56180; 100 mg) was tested in 24 healthy male volunteers. The drugs were given alone or in combination and were compared with placebo. Volunteers were randomized into four different treatment groups. The daily medication over 4 days was 1 x 1 placebo tablet, or 1 x 1 tablet containing 100 mg acarbose, or 1 x 1 tablet containing 100 mg acarbose plus 10 ml antacid suspension, or 1 x 1 placebo tablet plus 10 ml antacid suspension, interrupted by wash-out phases of 6-10 days between successive treatments. Efficacy was assessed on the basis of postprandial blood glucose and serum insulin levels after administration of 75 g sucrose, and was measured as maximal concentrations and 'area under the curve' (0-4 h). No influence of the antacid on the blood glucose and insulin-lowering effect of acarbose could be detected. Hence, there does not appear to be a significant interaction between acarbose and the antacid tested. Antacids similar to that tested do not need to be classified as a contraindication when used in combination with acarbose.

Acarbose↗
PubMed1998

The management of acid-related dyspepsia in general practice: a comparison of an omeprazole versus an antacid-alginate/ranitidine management strategy. Compete Research Group [corrected].

BACKGROUND: There is need for an evidence-based comparison of clinical management strategies to provide the rationale for selection of a particular therapeutic approach to treatment. Ideal dyspepsia treatment should quickly and conveniently alleviate patient symptoms whilst also minimizing the use of healthcare resources. AIM: To examine dyspepsia symptom relief over 16 weeks and compare an omeprazole clinical management strategy with a commonly used combination of antacid-alginate followed by H2-antagonist. METHODS: Seven hundred and twenty-five patients participated in this randomized, open, parallel group comparison over 16 weeks. Patients were randomized to receive either an omeprazole treatment strategy (363) consisting of omeprazole 10 mg stepping up to 20 mg and 40 mg as required, or an antacid-alginate/ranitidine treatment strategy (362) consisting of antacid-alginate 10 mL q.d.s. stepping up to ranitidine 150 mg b.d. and 150 mg q.d.s. as required. RESULTS: A greater proportion of patients receiving the omeprazole clinical management strategy had achieved the stringent health target of complete symptom relief (61 vs. 40%, P < 0.0001) at 16 weeks. Forty-six per cent of omeprazole-treated patients were symptom free after the first 10 mg step compared to only 17% in the antacid-alginate treated group (P = 0.0001). Total relief of heartburn, the most common symptom at entry, was achieved by more patients in the omeprazole treatment group than the antacid-alginate/ranitidine treatment group, 62 vs. 36%, respectively, at 4 weeks, and 81 vs. 60% at 16 weeks (P = 0.0001). CONCLUSION: Treatment with the omeprazole clinical management strategy was superior to the antacid-alginate/ranitidine management strategy in providing relief of acid-related dyspepsia symptoms after 16 weeks. In addition, the omeprazole treatment strategy involved fewer GP consultations and thus minimized the use of other healthcare resources.

Abdominal Pain↗
PubMed1985

[Therapy of stomach ulcer with low-dose antacid gel and cimetidine. A multicenter double-blind study].

In a multi-centre double-blind (double-dummy) trial the effectiveness of low-dose antacid gel (6 X 12 ml/d; neutralisation capacity 120 mmol) was compared with that of a standard dose of cimetidine (1 g/d) in the curative treatment of gastric ulcer. Antacid gel was given to 65 patients, cimetidine to 60. Diagnosis was confirmed by endoscopic biopsy, which was also employed in a serial follow-up. After 4 weeks antacid gel and cimetidine produced cures in 43% and 52%, respectively; after 8 weeks 76% and 89%, respectively, the difference between the two methods not being statistically significant. There was also no statistically significant difference with regard to ulcer pain. In one case each in the antacid and cimetidine groups, the treatment had to be stopped because of side effects. Diarrhoea was more common on cimetidine than on antacid gel. It is concluded that both low-dose antacids gels and cimetidine are suitable in the treatment of gastric ulcers.

Adult↗
PubMed1987

[Binding of bile salts and lysolecithin by various antacids in biological media].

The in vitro capacity of several commercial antacids to bind bile acids and lysolecithin was measured in three different test media: 0.1 n HCl, natural human gastric juice and human gastric juice enriched with 5% protein. Antacids bind bile salts variably. In HCl and in natural and protein-enriched gastric juice the capacity to bind conjugated bile salts was higher (47-72%) for antacids with high aluminium content, such as Alucol, Andursil, Muthesa than for antacids with less aluminium such as Calamox and Riopan (17-18%). Binding of unconjugated bile salts did not show any corresponding difference. The test medium had little effect on binding capacity when pH was comparable. Natural gastric juice was slightly better with regard to binding of conjugated bile salts. The addition of protein had only minimal effect. Lysolecithin was equally heavily adsorbed by all tested antacids and in all three test conditions (85-100%). Since duodenogastral reflux contains mainly unconjugated bile salts, our results suggest that antacids with higher aluminium content should be preferred if binding of bile salt reflux is attempted.

Bile Acids and Salts↗
PubMed1981

Effect of antacids on activity of oral hypoglycemics.

The effect of some antacids on the dissolution and hypoglycemic activity of acetohexamide, tolazamide, and tolbutamide tablets was investigated, as was the adsorption of the three drugs onto the antacids. The dissolution rates of the three drugs in the presence of magnesium oxide, aluminum hydroxide, magnesium carbonate, and calcium carbonate increased (0.5-1 hr) and then plateaued or decreased (1-3 hr). Magnesium trisilicate directly suppressed the dissolution of the three drugs. The antacids reduced the hypoglycemic activity of tolbutamide in the following order:magnesium trisilicate greater than magnesium oxide greater than aluminum hydroxide greater than magnesium carbonate greater than calcium carbonate. The same order occurred for the first three antacids with acetohexamide and tolazamide. Decreased hypoglycemic activity of the drugs may have been due to their adsorption to the coadministered antacids.

Adsorption↗
PubMed1985

Influence of antacids on the gastric antisecretory activity of the synthetic prostanoid (8R,11R,12S,15R,5Z,13E)-15-(acetyloxy)- 11,16,16-trimethyl-9-oxoprosta-5,13-dien-1-oic acid in dogs.

Liquid antacids that contain aluminum-magnesium hydroxides reduce the absorption of various therapeutic agents. To assess the potential for such an interaction with the synthetic anti-ulcer prostanoid (8R,11R,12S,15R,5Z,13E)-15-(acetyloxy)-11, 16,16-trimethyl-9-oxoprosta-5,13-dien-1-oic acid (1; Ro 22-6923), we studied the effect of Mylanta and DiGel liquid on the gastric antisecretory activity of this drug in dogs. Dogs were prepared with a modified Pavlov (innervated) pouch. Compound 1 was administered alone or with liquid antacid into the main stomach while acid secretion into the pouch was measured. Mylanta (30 mL) and DiGel (35 mL) failed to significantly reduce the ability of 1 (0.5 mg/kg, orally) to inhibit histamine (25 micrograms/kg/h)-stimulated secretion. Neither the onset nor the duration of action of 1 was affected by either antacid. The total acid output over the 4 h after administration of 1 was not significantly affected by the antacids. The results suggest that Mylanta and DiGel, or antacids of a composition similar to that of these products are not likely to interfere with the antisecretory activity of 1 in humans.

Animals↗