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Endoscopic findings after antacid, cimetidine and placebo for peptic ulcer--importance of staging the lesions.

Ninety four adult outpatients entered a randomized trial in which 30 patients were treated openly with antacid hourly and 64 patients with a double-blind regimen of either cimetidine (1 g/day) or placebo. After 4 weeks, 66.3% of the antacid-treated patients, 56.2% of the cimetidine-treated patients and 9.4% of the placebo patients showed ulcer healing. The difference between cimetidine and antacid was not statistically significant. The low percentage in the placebo group as compared to other trials may be attributed to the avoidance of supplementary antacid in this group and or to the criterion of staging the lesions both for entry into study and for evaluating the results.

Adult↗

Decreased bioavailability of prednisone due to antacids in patients with chronic active liver disease and in healthy volunteers.

To investigate the potential action of antacids on prednisone absorption and on prednisolone serum levels, we studied 5 healthy volunteers and 12 patients with chronic active liver disease. Six patients responded to treatment and 6 did not. After administering two 5-mg tablets of prednisone with 60 ml of water, 60 ml of Melox (AlOH 3.75 g/100 ml + MgOH 4.0 g/100 ml), or 60 ml of Aldrox (AlOH 8.0 g/100 ml + MgOH 1.95 g/100 ml), we measured prednisolone by radioimmunoassay. Both peak heights and areas under the serum-concentration curves were significantly reduced when prednisone was administered with antacids. The relative bioavailability of prednisone after prednisone-antacid treatments compared to that after prednisone-water treatment was 74% +/- 13% (p less than 0.05) with Melox and 57% +/- 15% (p less than 0.01) with Aldrox in healthy volunteers. In patients with chronic active liver disease responding to treatment, prednisone bioavailability was 65% +/- 120% (p less than 0.01) and 87% +/- 20%, respectively. Among patients with chronic active liver disease not responding to treatment, this parameter was 76% +/- 12% (p less than 0.05) and 80% +/- 21% (p less than 0.05), respectively. To insure adequate prednisolone levels in patients with chronic active liver disease, prednisone should not be given simultaneously with antacids.

Adult↗

The in vitro adsorption of some antiepileptics on antacids.

The adsorption of the antiepileptics sulthiame, phenytoin, mephenytoin, mesuximide, phensuximide, ethosuximide, and primidone on various antacids or adsorbents was studied at 37 degrees C. The antacids or adsorbents used were magnesium trisilicate, aluminium hydroxide, bismuth oxidcarbonate, magnesium oxide, talc, kaolin and calcium carbonate. Magnesium trisilicate was found to be the strongest adsorbent for most of the antiepileptics tested. The other antacids or adsorbents were without an appreciable effect. Sulthiame exhibited the highest degree of interaction with magnesium trisilicate. Mesuximide, phensuximide and primidone showed intermediate adsorption properties. Mephenytoin and phenytoin had lower adsorption characters, while ethosuximide was the least adsorbed antiepileptic tested. The extent of elution was found to be inversely proportional to adsorption. Alkaline solution gave relatively higher eluting power than acid solution. The mechanism of adsorption of the various antiepileptics on antacids was discussed. The effect of magnesium trisilicate on the bioavailability of coadministered antiepileptics has still to be confirmed by in vivo testing.

Adsorption↗

Some problems with antacids.

The author points out that because a high intake of Vitamin D and calcium is normally encouraged in pregnancy, care should be taken in the prescription of certain antacids likely to cause alkalosis. Calcium-containing antacids are probably best avoided because of nocturnal acid rebound. Because of undesirable fluid retention in some situations in pregnancy caution should be exercised in the use of sodium-containing antacids. The very high sodium content of some antacids is stressed.

Alkalosis↗

[The effectiveness of ranitidine in non-ulcer dyspepsia (functional dyspepsia) in comparison with an antacid].

BACKGROUND: It is generally accepted that functional dyspepsia is caused by heterogeneous pathogenetic factors. From the clinical point of view acid-related symptoms as heartburn, acid regurgitation and epigastric pain (acid-type) can be separated from general dyspeptic symptoms as predominant fullness, nausea/vomiting (dysmotility-type). PATIENTS AND METHODS: In the present study, the influence of a four-week-treatment with ranitidine (twice 150/d, n = 346) in comparison with an antacid (40 mmol/d, n = 340) on the severity and course of symptoms in patients suffering from an acid-related functional dyspepsia was investigated. RESULTS: With ranitidine, acid-related as well as general dyspeptic symptoms disappeared in a significantly higher percentage after two and four weeks compared with antacid. Complete disappearance of symptoms was documented with ranitidine after two weeks in 37% and after four weeks in 66% compared with antacid in 13% and 30% respectively (p < 0.005). Patients with severe symptoms, history of ulcer and long-term dyspepsia and slight endoscopic changes in the upper gastrointestinal tract showed a significant faster and more distinct response. Both kinds of treatment were well tolerated. CONCLUSION: It is concluded that in acid-related functional dyspepsia ranitidine is superior to antacid in relieving symptoms. Therefore, a probative treatment with ranitidine up to four weeks is recommended as a practical therapeutic alternative in this syndrome.

Adolescent↗

Evaluation of commercially available antacid tablets.

Antacids are commonly used for the treatment of acid peptic disease. There is a need to study the relative merits of various brands of antacids available commercially. Twenty three brands of antacid tablet preparations were evaluated with regard to their composition, cost, dispersion time, pH, neutralising capacity and time taken for neutralisation. The cost of various tablets ranged from Rs 0.13 to Rs. 1.48 per tablet and the dispersion time from 20 to 90 minutes. The pH of the dispersed tablet solution ranged from 5.7 to 9.5. The neutralising capacity varied between 8 to 169 meq/tablet and the neutralizing time between 20 and 45 minutes. The cost: neutralizing ratio was calculated and ranged from 102 to 9867 x 10(-3) Rs/meq. A scoring system with a maximum score of 12 has been devised. The study provides a guide for choosing a more potent, quick neutralising and low cost antacid preparation.

Antacids↗

Gastric mucosal calcinosis. Calcified aluminum phosphate deposits secondary to aluminum-containing antacids or sucralfate therapy in organ transplant patients.

We have noticed calcium deposits (gastric mucosal calcinosis, or GMC) in the superficial gastric mucosa of 28 organ transplant patients (OTPs) (11 liver, seven bone marrow, four kidney, three kidney/pancreas, two heart, and one each of liver and kidney transplant) who underwent endoscopic biopsies. The deposits were tinctorially similar to cytomegalovirus inclusions, ranged from 40 to 250 mu in diameter, and were present just beneath the surface epithelium at the tips of the foveolae. An x-ray microanalysis showed that these mucosal deposits contained the elements aluminum, phosphorus, calcium, and chlorine. Clinical chart review showed that all OTPs with GMC were taking aluminum-containing antacids or sucralfate. Review of biopsies from gastric ulcer patients found GMC in a significantly smaller percentage than in transplant patients (32.7% vs. 5.1%, p < 0.0002). In addition, all three ulcer patients with calcified deposits were chronic renal failure patients on long-term aluminum-containing antacid therapy. Gastric mucosal calcinosis appears to be caused by aluminum phosphate accumulation secondary to antacid or sucralfate therapy in organ transplant patients. The presence of GMC in OTPs and chronic renal failure patients rather than other gastric ulcer patients is most likely due to the longer duration of therapy with aluminum-containing compounds in the former two patient groups. The clinical relevance of GMC remains to be seen. In theory, however, accelerated bone demineralization via loss of phosphates and absorption of aluminum in the gastrointestinal tract may be a consequence of long-term aluminum-containing antacid or sucralfate therapy.

Aluminum↗

Comparison of the effects of over-the-counter famotidine and calcium carbonate antacid on postprandial gastric acid. A randomized controlled trial.

OBJECTIVE: To compare an over-the-counter histamine2-receptor antagonist with an antacid as gastric acid reducers. DESIGN: Randomized, double-blind, placebo-controlled crossover trial. SETTING: Gastric secretory research laboratory in a Veterans Affairs medical center. PARTICIPANTS: Eighteen healthy volunteers (10 men and 8 women) aged 25 to 62 years with normal gastric acid secretion rates. INTERVENTIONS: The subjects received the histamine2-receptor antagonist famotidine (Pepcid AC, 10 mg), calcium carbonate antacid tablets (Tums, 1000 mg), or placebo medications 1 hour after a test meal. Two identical meals were taken 2.5 and 6.0 hours after the medication was given. MAIN OUTCOME MEASURES: Intragastric pH was maintained at 4.0 by in vivo intragastric titration with 0.3N sodium bicarbonate for 10 hours (1 hour before and 9 hours after medication). Reduction in sodium bicarbonate titrant use in the 2 treatment groups compared with titrant use with placebo was reflective of acid secretion inhibited by a famotidine or acid neutralized by calcium carbonate tablets. RESULTS: When evaluated in increments of 30 minutes, calcium carbonate had a rapid onset of action, neutralizing 6.7 mmol of acid in the first 30 minutes. However, its duration of effect was only 60 minutes. Famotidine had a delayed onset of action compared with antacid, beginning after 90 minutes. However, famotidine had a duration of effect of at least 540 minutes. At its peak effect, 210 minutes after administration, famotidine reduced acid secretion by 7.3 mmol per 30 minutes. CONCLUSIONS: Recommended over-the-counter doses of famotidine and calcium carbonate tablets have different pharmacokinetic profiles when taken in the postprandial period. The antacid has a rapid onset and short duration of action, while the histamine2-receptor antagonist has a delayed onset and a prolonged duration. Their peak potencies are similar.

Adult↗

In vitro assessment of antacid efficacy using a computer-controlled 'artificial stomach-duodenum' model reproducing gastroduodenal flux regulation.

We have developed an artificial stomach-duodenum model made up of three compartments representing the stomach, (including a fragment of hog gastric mucosa), the proximal duodenum, and the distal duodenum. Gastroduodenal flow rates are controlled by a microcomputer capable of (1) adjusting gastric emptying and alkaline secretion in the proximal duodenum according to intragastric pH; (2) adjusting pancreatic alkaline secretion according to proximal duodenum pH; and (3) simulating acid response to food ingestion. Antacid drugs were added 90 min after simulated food ingestion in near-physiological or duodenal ulcer conditions. Aluminum phosphate-containing antacids resulted in a persistent antacid effect, due to their adsorption to the gastric mucosa; this prolonged the buffering capacity at pH 2.4 to 120 min. Aluminum+magnesium hydroxides and calcium+magnesium carbonate combinations mainly exerted neutralizing activity, inducing an increase in the gastric emptying rate. In the duodenal ulcer simulation, the pH of the gastric contents was lower and the antacid effect was shorter than in the 'physiological' simulation.

Aluminum↗

[in vitro comparison of liquid antacids of commercial use].

The aim of our study was to compare the capacity of several liquid antacids to elevate the pH of a hydrochloric acid solution. An experimental model was designed to measure this capacity in different commercially available liquid antacids. Change in pH of an HCl solution was registered when each of the liquid antacids was added. We found differences between the 4 MgOH - ALOH antacids. Minimal difference was found between the 2 commercially available magaldrates.

Antacids↗

The effect of food and an antacid on the bioavailability of dexketoprofen trometamol.

This randomized three-way, crossover pharmacokinetic study was performed to determine whether food or an antacid alters the bioavailability of dexketoprofen trometamol. A total of 24 healthy volunteers received three single 25 mg doses of dexketoprofen trometamol administered either in fasting condition, after an antacid (Maalox), or after a high-fat breakfast. Each volunteer received the three treatments in a randomized order, with a 7-day washout period between treatments. Blood samples were taken at regular intervals up to 24 h after dose. Plasma dexketoprofen concentrotions were determined by HPLC and the main outcome measures were area under curve of concentration vs. time (AUC0-infinity), maximal plasma concentration (Cmax), and time to reach maximal concentration (t(max)). Administration of an antacid 10 min before dexketoprofen trometamol had no clinically relevant effect on any of the pharmacokinetic parameters. Food did not alter the extent of absorption of dexketoprofen trometamol, but t(max) was significantly increased and C(max). significantly decreased compared with the fasting state. In conclusion, we can state that neither antacid nor food has a significant effect on the overall bioavailability of dexketoprofen trometamol.

Adolescent↗

Effect of antacids on predicted steady-state cimetidine concentrations.

The purpose of this study was to evaluate effects of antacids on predicted steady-state concentrations of cimetidine. Ten healthy volunteers received in random order one week apart, cimetidine and cimetidine and antacid suspension. Blood was obtained at specified times and analyzed for cimetidine. Bioavailability was assessed by comparison of peak concentration, time to peak concentration, area under the curve, and time spent over 0.5 micrograms/ml. Single-dose data were extrapolated to steady-state using computer simulation. Concurrent administration of antacid suspension reduced parameters of bioavailability approximately 30%. When steady-state conditions were simulated, concentrations of cimetidine greater than or equal to 0.5 micrograms/ml were maintained for the entire dosing interval in seven of 10 subjects. These data suggest that temporal separation of cimetidine and antacid suspension may be unnecessary.

Adult↗

Influence of food and antacid administration on fluoride bioavailability from enteric-coated sodium fluoride tablets.

The relative bioavailability of enteric-coated sodium fluoride (NaF) tablets (10 mg F-) has been assessed following administration with a standard calcium-rich breakfast or calcium-poor lunch, and 2 h before or simultaneously with antacid administration (2.4 g aluminum-magnesium hydroxide), versus intake on an empty stomach. Twelve volunteers were studied 3 times according to an open, three-way crossover design over a 24 h period at weekly intervals. Meals were found to decrease the peak serum concentration of NaF from 122 micrograms/L during fasting (after baseline subtraction) to 71 and 88 micrograms/L with breakfast and lunch respectively, and to slow its absorption rate with Tmax increasing from 3.3 to 7.3 and 11.2 hours, without altering its bioavailability. Antacid impaired the bioavailability of NaF by 80% when administered simultaneously, with AUC decreasing from 987 to 155 micrograms.h/L, but had no significant effect when taken 2 h before NaF. In conclusion, the enteric-coated NaF tablets used in this study can be administered with food or after a 2-hour delay following antacid administration, but should not be taken simultaneously with antacid.

Adult↗

A randomized clinical trial comparing ranitidine and antacids in critically ill patients.

In a randomized trial of gastric pH control for stress ulcer prophylaxis, 200 mg/day ranitidine iv was compared to antacids in 86 patients admitted to an ICU. Six (15%) patients receiving ranitidine and six (13%) given antacids failed to maintain greater than 50% of the hourly gastric pH measurements at or above 4. Increasing the ranitidine dosage to 300 mg/day did not provide additional control. One patient in the antacid group developed an overt upper GI bleed secondary to endoscopically proven erosive disease. We conclude that iv ranitidine in a dosage of 200 mg/day is as effective as antacids in reducing gastric acidity and preventing stress ulcer disease in critically ill patients.

Administration, Oral↗

In vitro availability of gliclazide in presence of antacids.

Gliclazide is the most commonly used sulfonylurea derivative for NIDDM therapy. Due to its prolonged therapy, there is always a likelihood of its use with other drugs. On the other hand antacids are commonly prescribed to encounter gastric acidity etc. Present paper deals with the in vitro availability studies of gliclazide in presence of antacids. These studies were carried out in simulated gastric juice and in buffer of pH 7.4 at body and accelerated temperature. The antacids used in these studies were aluminum hydroxide, aluminum trisilicate, magnesium oxide, magnesium trisilicate, sodium bicarbonate, calcium carbonate, magaldrate and simethicone (2,4-dimethoxypoly-siloxane). It has been found that in case of magnesium oxide, magnesium trisilicate and sodium bicarbonate, availability of gliclazide was enhanced while in rest of the antacids retarded the availability of gliclazide.

Journal Article↗

In vitro availability of glibenclamide in presence of antacids.

The in vitro availability studies of glibenclamide in presence of commonly used antacids are present in this paper. Glibenclamide is used for the treatment of Non-Insulin dependent diabetes mellitus. It is a sulfonylurea derivative. Antacids are prescribed to encounter gastric acidity etc. These studies were carried out in simulated gastric juice and in buffer of pH 7.4 at 37 and 48 degrees C. Aluminum hydroxide, aluminum trisilicate, magnesium oxide, magnesium trisilicate, sodium bicarbonate, calcium carbonate, magaldrate and simethicone (2,4-dimethoxypolysiloxane) antacids were used in these studies. It has been observed that in case of magnesium oxide, magnesium trisilicate and sodium bicarbonate, availability of glibenclamide was enhanced while in rest of the antacids retarded the availability of glibenclamide.

Journal Article↗

[Effect of antacids on the bioavailability and therapeutic efficacy of cimetidine].

Five patients with duodenal ulcer received cimetidine and after an interval of four days cimetidine with antacid. Cimetidine in serum was analysed with high performance liquid chromatography. There was no significant difference in the values of the pharmacokinetic parameters of cimetidine (Cmax, tmax and AUC) when taking cimetidine alone and cimetidine plus antacid. 53 outpatients with endoscopically proven duodenal ulcer were evaluated in a randomized study, so as to compare the therapeutic effect of cimetidine and aluminum hydroxide gel plus cimetidine. 18 of 26 patient taking cimetidine alone (69.2%) and 19 of 27 patients taking cimetidine plus antacid (70.4%) had their ulcer completely healed after 4 weeks. The overall healing rates after 8 weeks for the groups taking cimetidine alone and cimetidine plus antacid were 80.0% and 92.6% respectively with no significant difference. This study indicates: (1) Simultaneous administration of aluminum hydroxide gel does not alter the bioavailability of cimetidine. (2) Combined administration of aluminum hydroxide gel and cimetidine does not alter the therapeutic effect of cimetidine in patients with duodenal ulcer.

Adult↗

Absence of in vivo and in vitro interactions of an aluminum hydroxide, magnesium hydroxide containing antacid with cimetidine in patients with peptic ulcer.

In view of contradictory reports on the bioavailability of cimetidine in the presence of concomitantly administered antacids we studied the areas under the plasma concentration time curves (AUC) of cimetidine, the maximal concentrations (cmax) and the time, at which cmax was reached (tmax) in eight patients (five patients with duodenal ulcer, three patients with gastric ulcer) with and without the administration of an aluminum hydroxide magnesium hydroxide containing antacid (Maaloxan). No significant effects of the antacid on AUC, cmax and tmax of cimetidine were found. In vitro studies also showed no adsorption of cimetidine to aluminum hydroxide, magnesium hydroxide or the antacid.

Adult↗