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At least 325 records · Page 18Linked to original sources
PubMed1992

The effect of antacid and ranitidine on droxicam pharmacokinetics.

Droxicam is a nonsteroidal anti-inflammatory drug that is a pro-drug of piroxicam. The influence of concomitant administration of antacid or ranitidine on droxicam pharmacokinetics has been investigated. On three separate phases, 15 healthy volunteers received a single oral 20-mg dose of droxicam either alone, with antacid (400 mg aluminum hydroxide + 400 mg magnesium hydroxide, three times/day), or with ranitidine (300 mg, two times/day) for 6 days. Piroxicam, the active substance from droxicam, was quantified by high-performance liquid chromatography. The pharmacokinetic parameters for droxicam given alone were: maximum peak plasma concentration (Cmax) = 1.53 +/- .21 micrograms/mL (mean +/- SD), time to peak concentration (Tmax) = 7.5 +/- 2.1 hr, t1/2a = 1.38 +/- .82 hour, t1/2el = 53.3 +/- 11.9 hr, Cl/F = 2.98 +/- .71 mL/min, volume of distribution (Vd/F) = 13.2 +/- 1.8 L and area under the curve (AUC) = 117.6 +/- 26.8 micrograms/hour/mL. The subject effect was significant for all the pharmacokinetic parameters except for the absorption half-life (P < .05). Concomitant antacid or ranitidine administration had no significant effect on any of the droxicam pharmacokinetic parameters. The results of this study suggest that antacid or ranitidine do not significantly alter the oral absorption or pharmacokinetic disposition of single-dose droxicam.

Administration, Oral↗
PubMed2006

Interactions between sparfloxacin and antacids - dissolution and adsorption studies.

Sparfloxacin is a broad-spectrum oral fluoroquinolone antimicrobial agent with a long elimination half-life, extensively used against both Gram-positive as well as Gram-negative microorganism. Concurrent administration of antacids and sparfloxacin decreases the gastrointestinal absorption of sparfloxacin and therapeutic failure may result. The present study was designed to evaluate the influence of some antacids on the availability of sparfloxacin. The release of sparfloxacin from tablets in the presence of antacids like sodium bicarbonate, calcium hydroxide, calcium carbonate, aluminum hydroxide, magnesium hydroxide, magnesium carbonate, magnesium trisilicate and magaldrate has been studied on BP 2003 dissolution test apparatus. These studies were carried out in simulated gastric and intestinal juices for three hours at 37 degrees C. The results confirmed that the dissolution rate of tablets was markedly retarded in the presence all of antacids studied, whereas magaldrate and calcium carbonate exhibited relatively higher adsorption capacities in simulated gastric juice and magnesium trisilicate and calcium hydroxide in simulated intestinal juice.

Adsorption↗
PubMed1991

[The effect of pH and amount of antacids on bile acid binding in a quasi-natural reflux milieu].

Bile acid adsorption may be one therapeutical mechanism of antacids. Little is known about the effect of pH and amount of antacid on bile acid adsorption. Therefore we carried out the following investigations using a lattice [correction of lettuce] layer antacid as a model substance. 5 ml of "quasi-natural reflux milieu" were mixed with 0.5, 1 or 2 ml of hydrotalcite and adjusted to pH 3, 5 or 7. The highest total bile acid adsorption was found at pH 3, the degree of bile acid adsorption correlated with bile acid lipophilicity, i.e. the most lipophilic and toxic bile acids are adsorbed best. High adsorption of lipophilic and particularly toxic bile acids even at low gastric pH may help to explain the good therapeutic effect of low-dose antacids in gastric ulcer.

Adsorption↗
PubMedDate not supplied

[Treatment of duodenal ulcers with antacid mixtures and sulpiride. A double-blind controlled study (author's transl)].

A total of 108 patients with duodenal ulcers were divided into 4 groups in a double-blind study controlled by endoscopic examinations. Patients in each group were given either an antacid mixture or sulpiride alone, antacid mixture plus sulpiride, or a placebo. The highest complete recovery rate (84 per cent) was noted in the antacid mixture plus sulpiride group, while partial healing (more than 50 per cent reduction in ulcer size) was highest in the sulpiride group (84,6 per cent). As sulpiride has both healing effects on the ulcer and an analgesic effect against pain it can be prescribed in association with antacid mixtures for the treatment of duodenal ulcers.

Antacids↗
PubMed1990

Protection of the upper gastrointestinal mucosa: the role of antacids.

Experiments performed in animals and in healthy human subjects suggest that antacids increase prostaglandin synthesis and have a cytoprotective effect on gastroduodenal mucosa. To investigate this hypothesis, the ability was evaluated of an antacid containing an aluminium/magnesium hydroxide combination (Maalox TC) to modify prostanoid production at the gastric level in 28 patients with gastric antral ulcer of various sizes in different stages of activity with or without erosive gastritis. After the antacid treatment, a significant prostaglandin E2 reduction was observed, together with a significant 6-keto-prostaglandin F1 alpha increase, but there was no thromboxane B2 variation at antrum level, nor any significant modification of prostanoid production at body level. The decreased prostaglandin E2 levels, detected after treatment with the antacid combination, may be due to lesion improvement, decreased synthesis or increased catabolism by mucosal cells, to a drop in this prostaglandin production by inflammatory cells. As far as 6-keto-prostaglandin F1 alpha is concerned, the obtained data confirm the results reported by other authors in healthy human subjects. The increase of this prostaglandin could enhance blood flow, resulting in a protective effect.

6-Ketoprostaglandin F1 alpha↗
PubMed1975

In vivo studies on the neutralizing effect of antacids using the Heidelberg capsule.

The effects on gastric pH of various forms of administration of antacids have been studied in healthy volunteers. Gastric pH was recorded using a radiotelemetric technique (Heidelberg Capsules). In one series of experiments the Heidelberg Capsules were compared with a conventional aspiration method of measuring gastric pHqt lower pH-levels (pH smaller than 2) the Heidelberg Capsules recorded lower values than what was found with the aspiration technique. However, when the pH-response to an antacid dose was studied the two techniques gave concordant results. In another series of experiments, four antacids with the same acid-neutralizing capacity in vitro were compared in fasting subjects, using a crossover design. A liquid preparation and a chewable tablet gave almost equal results with a short latency time and a duration of action of more than one hour (mean 69 minutes and 82 minutes, respectively, with pH above the basal level). Two other tablet antacids designed to be swallowed whole gave less prompt effects and a shorter duration of action (mean 45 minutes for both, with pH above the basal level).

Adult↗
PubMed1990

The effect of concomitantly administered antacids on the bioavailability of lornoxicam, a novel highly potent NSAID.

Antacids are used in the treatment of upper gastrointestinal side-effects during therapy with nonsteroidal anti-inflammatory drugs (NSAIDs). Since pharmacokinetic interactions between antacids and NSAIDs have been reported, it was investigated whether aluminium and magnesium hydroxide (Maalox as oral suspension) or aluminium hydroxide and calcium carbonate (Solugastril as oral gel) influenced the bioavailability of Lornoxicam (rINN), a new potent NSAID from the chemical group of the oxicams. Eighteen male volunteers were given 4 mg of Lornoxicam as a film-coated tablet either alone or together with 10 ml of Maalox or 10 g of Solugastril in an open, randomized, three-way cross-over study. The levels of Lornoxicam in plasma were determined by HPLC following solid-phase extraction. It was found that none of the antacids changed significantly any of the following pharmacokinetic parameters: elimination half-life (t1/2 beta), concentration at peak time (Cmax), time to reach the peak (tmax) and area under the curve to infinity (AUCo-infinity). The results indicate that the concomitant administration of antacids did not influence the pharmacokinetic profile of Lornoxicam. Furthermore they confirm the short elimination half-life of Lornoxicam in man, which is markedly shorter than that of other oxicam-type compounds.

Adult↗
PubMed1989

Influence of antacids on the bioavailability of glibenclamide.

A single oral dose of glibenclamide (2.5 mg) was given to eight healthy volunteers in a randomized cross-over study after a standardized fasting and breakfast (374 kcal), with or without a concomitant intake of 10 ml of antacid suspension. Serum glibenclamide levels were determined by means of a specific radioimmunoassay method. The areas under the blood concentration-time curves (AUC0-infinity), with or without antacid, were 408.17 +/- 168.25 and 307.9 +/- 84.13 ng/ml (p less than 0.05), respectively. The peak concentrations of 96.88 +/- 49.9 and 66.19 +/- 32.35 ng/ml/h (p less than 0.05) with or without antacid, were reached in 4.13 and 3.81 h, respectively. Values of tmax, Vd and t1/2 were not affected by the presence of the antacid. A 33% increase in bioavailability of glibenclamide emerged, as seen from the respective AUC values, but no clinically remarkable effect was observed in the subjects.

Adult↗
PubMed1989

Antacids in the treatment of peptic ulcer disease.

In peptic ulcer disease, antacids present a therapeutic effect by neutralizing gastric acid and reducing acid delivery to the duodenum. Furthermore, they reduce the activity of pepsin and have the capacity to bind bile acids. Despite the opinion of most clinicians, the effect of antacids relieving pain in patients with peptic ulcer has not been definitely demonstrated. Furthermore, antacids do not seem to improve the healing rate of gastric ulcer. Earlier studies showed that antacids could hasten the healing of duodenal ulcer when administered at a very high dose. However, recent papers demonstrate that this therapeutic effect is also achieved with a dose with very low neutralizing capacity. Severe side effects are rare, although they can occur in high-risk patients. However, minor problems, such as changes in bowel habits, are more frequent.

Antacids↗
PubMedDate not supplied

[Prolonged effect of an antacid treatment on changes in gastric potential difference induced by aspirin in man].

In ten healthy volunteers, we evaluated the effects of a 6 days antacid treatment (Rocgel) on the aspirin induced changes in gastric potential difference (PD). In this placebo controlled cross-over study, PD was measured twelve hours after the last take of the antacid. Aspirin induced drop of PD was less pronounced after antacid compared to placebo; maximal fall of PD and area upper the curve decreased (p less than 0.001). This effect was observed twelve hours after the last take of the antacid. It may suggested a long-term protective effect on the gastric mucosa.

Action Potentials↗
PubMed1989

[Bile acid binding by antacids in a "quasi-natural" reflux milieu].

In a "quasi-physiological" reflux mixture obtained from non-stimulated gastric juice and hepatic bile the bile acid adsorption of 7 antacids is investigated with an newly developed HPLC method. The antacids produce pH values varying from 3.7 to 7.6. With increasing pH and increasing polarity of bile acids the bile acid binding to antacids decreases. The theoretically desirable combination of high pH and good bile acid binding is difficult to achieve. The relatively good total bile acid binding (over 60%) by Trigastril at a high pH (7.53) contrast with better bile acid adsorption by Maaloxan and Aludrox (about 90%) at a lower pH (4.5-4.9). Interestingly, toxic nonpolar bile acids are particularly well adsorbed by antacids.

Antacids↗
PubMed1986

Antacid protection of gastric mucosa.

Antacids containing aluminum hydroxide are protective for the stomach in that they prevent grossly visible mucosal necrosis and hemorrhages produced by noxious agents such as aspirin or absolute ethanol. Histologically, this protective effect is confined mainly to the tissue located deep in the gastric mucosa, essentially comprising gastric glands, while the damage to the surface epithelium is not significantly lessened. Accordingly, integrity parameters of the superficial epithelial layer (potential difference, mucus secretion, cell desquamation) do not indicate a protective action of antacids against damage by necrotizing agents. By contrast, significantly diminished microbleeding rates do suggest that protection by antacids works at a level deeper within the mucosa. The protective action of antacids may be mediated, at least in part, by endogenous prostaglandins, which were found to be elevated in this context.

Aluminum Hydroxide↗
PubMed1987

[Prostaglandin synthesis in stomach and duodenal mucosa of the human: effect of aspirin with and without antacid].

A decreased PG E2 content in gastric mucosa of humans receiving a longterm antirheumatic therapy has been reported to be partially reversed after a one week treatment with an antacid (Reimann et al., Fortschr Med 102 [1984], 25-26). Therefore the effect of an Aspirin treatment of healthy volunteers with or without an antacid on the prostaglandin synthesis in gastric or duodenal mucosa was investigated. 14C-labelled arachidonic acid was used as substrate during in vitro incubation of the mucosal homogenate for determination of the endogenous formation of prostaglandins. Aspirin suppressed the total prostaglandin synthesis to less than 10% of control after one week treatment. The addition of a high dose antacid did not influence this inhibition, and no significant effect on the prostaglandin profile was detectable. It is concluded that antacids do not influence the suppression of the endogenous prostaglandin synthesis by NOSAC's, however another effect, eg a prolonged stability of PG E2 in a less acidic environment is more likely.

Adult↗
PubMed1978

Effects of bile acids, antacids, and cholestyramine on transmural electrical potential difference in man.

The effect of glycocholic acid (GCA) on functional changes of the gastric mucosal barrier was examined by measurement of transmural gastric potential difference (PD) in humans in the presence and absence of cholestyramine and of A1(OH)3-containing antacids possessing potent bile acid binding properties. Intagastric instillation of GCA induced reduction of PD which could be prevented by the more potent buffering Mg-A1(OH)3-containing antacid, but not by cholestyramine or the less potent A1(OH)3-containing antacid. It is concluded that for the prevention of bile acid induced damage of gastric mucosa potent antacids are superior to potent bile acid binding agents loosing the binding properties at low pH-values.

Aluminum Hydroxide↗
PubMed1977

Antacid and placebo produced similar pain relief in duodenal ulcer patients.

The effectiveness of antacid and placebo in relieving single episodes of spontaneous duodenal ulcer pain were compared in two double blind, controlled, randomized trials. The trials compared the effects on ulcer pain of individual doses of a liquid antacid and placebo, rather than the effects of therapeutic regimens with antacid or placebo. Thirty patients were studied. There were no significant differences between antacid and placebo in time to onset, degree, or duration of pain relief. These results suggest that factors other than gastric acid neutralization are important in acute relief of spontaneous duodenal ulcer pain.

Adult↗
PubMed1978

Cimetidine versus intensive antacid therapy for duodenal ulcer: a multicenter trial.

In a randomized double blind multicenter trial, patients treated with cimetidine (800 or 1200 mg daily) or an intensive regimen of Al-Mg antacid (210 ml daily) had similar rates of duodenal ulcer healing and pain relief. After 4 weeks of treatment, the proportion of patients with ulcer healing by endoscopy were: cimetidine (1200 mg), 21 of 33 (64 percent); cimetidine (800 mg), 19 of 32 (59 percent); and antacids, 15 of 29 (52 percent). These proportions did not differ significantly. Eighty per cent of cimetidine-treated patients became asymptomatic by week 4, as did 63 percent of antacid-treated patients (P greater than 0.1). No untoward effects were observed during cimetidine treatment. Twenty-seven per cent of antacid-treated patients reported diarrhea.

Adult↗
PubMed1987

Adsorption of bile acids by sucralfate, antacids, and cholestyramine in vitro.

Sucralfate, one of the newer drugs shown to be effective in the treatment of peptic ulcer and esophagitis; cholestyramine, a known bile acid binder; and commercial antacid preparations of pure aluminum hydroxide, pure magnesium hydroxide, and a combination of aluminum hydroxide, magnesium hydroxide, and magnesium carbonate were tested in vitro for bile acid-binding capacity. Cholestyramine was found to be the most effective bile acid binder, with more than 90% of bile acids adsorbed at all of the pH values studied. Sucralfate proved efficacious at pH 4, 6, and 8, adsorbing about 50% of the bile acids, but its binding capacity decreased at pH 2. Pure aluminum hydroxide was the most effective of the various antacid preparations; it adsorbed about 90% of bile acids at pH 2, although this percentage was significantly reduced at pH 6 and 8. Sucralfate was significantly more effective as a bile acid absorbent at pH 4 than either the magnesium hydroxide or aluminum-magnesium hydroxide plus magnesium carbonate antacids, as effective as the aluminum hydroxide antacid, and significantly less effective than cholestyramine.

Adsorption↗
PubMed1987

Prophylaxis of upper gastrointestinal tract bleeding in mechanically ventilated patients. A randomized study comparing the efficacy of sucralfate, cimetidine, and antacids.

Sixty-two mechanically ventilated patients were randomized into three study groups to compare the efficacy of sucralfate vs cimetidine and antacid regimens for the prevention of upper gastrointestinal tract bleeding. Only five study patients (8%) developed bright-red blood per nasogastric tube; four patients received the antacid regimen and one received cimetidine. None of the patients receiving sucralfate developed acute upper gastrointestinal tract bleeding. Bleeding was not severe enough in any patient to require endoscopy or surgery. There were no significant differences in the three groups when several major risk factors for gastrointestinal tract bleeding were analyzed, including sepsis, hypotension, steroid use, adult respiratory distress syndrome, gastric pH of 4 or less, previous peptic ulcer disease, peritonitis, and jaundice. A significantly higher incidence of acute renal failure was noted in the antacid-treated group when compared with the cimetidine and sucralfate groups. We find preliminary evidence that sucralfate is as efficacious as and more cost-effective than either cimetidine or antacids for prophylaxis of stress-related gastrointestinal tract bleeding in the critically ill ventilator-dependent patient.

Acute Kidney Injury↗