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Propantheline bromide in massive upper gastrointestinal haemorrhage.

The effectiveness of the anticholinergic, propantheline bromide, administered parenterally in patients with upper gastro-intestinal bleeding has been investigated in a double-blind study. The basic material consisted of 99 patients. No differences were found between the group receiving propantheline bromide and the group receiving placebo in regard to clinical factors such as duration of intensive care, total hospital stay and surgical frequency. However, 21 patients under 50 years of age showed a significantly lower blood transfusion requirement with the use of propantheline bromide.

Adult↗

The use of fluorescein diacetate and ethidium bromide as a stain for evaluating viability of mycobacteria.

A method for evaluating the viability of mycobacterial cultures using fluorescein diacetate and ethidium bromide is described. Smears from 2-4 week old cultures of mycobacteria were stained with a 0.005% Dubos albumin broth dilution of fluorescein diacetate for thirty minutes at 37 C. The smears were counterstained with a 0.005% aqueous solution of ethidium bromide for ten minutes at room temperature and blotted dry. One drop of glycerol was placed on the smear and covered with a 22 X 40 mm coverslip. Stained smears were observed with fluorescence microscopy at 450 X. Viable organisms hydrolyzed the fluorescein diacetate and appeared yellow-green while dead organisms absorbed the ethidium bromide and appeared red-orange. Aliquots of material from which the slides were made were concurrently placed on Lowenstein-Jensen media and cultured for growth as a confirmation of viability. Investigation of 104 mycobacterial isolates using the described test showed that the viability of mycobacterial cultures can be determined by this method.

Bacteriological Techniques↗

Inhibition of guinea pig gastric microsomal potassium-stimulated ATPase by nolinium bromide.

Although nolinium bromide (NB) [2-(3,4-dichlorophenylamino)-quinolizinium bromide] inhibited histamine-stimulated acid secretion in vivo in the pylorus-ligated guinea pig, no inhibition of basal or histamine-stimulated acid secretion from the isolated guinea pig gastric fundic disk was observed at serosal or mucosal concentrations from 0.1 to 200 microM. NB did not inhibit carbonic anhydrase in whole stomach homogenates of guinea pig, but did inhibit the potassium-stimulated gastric microsomal ATPase. The IC50 value (compound concentration giving 50% inhibition of the rate of ATP hydrolysis) for the net stimulated reaction (activity with KCl minus activity without KCl) was 65 microM (95% confidence limits = 42-101 microM). The basal reaction (no added KCl) was not inhibited. Inhibition of ATPase by NB was not due to its bromide ion, since NaBr did not, while the chloride analog of NB did, inhibit the enzyme. It was concluded that NB has no direct histamine-H2 receptor blocking activity. Whether ATPase inhibition contributes to its gastric acid antisecretory property is uncertain because of the lack of inhibitory activity in the isolated gastric disk assay.

Adenosine Triphosphatases↗

Induction of antibiotic production with ethidium bromide in Streptomyces hygroscopicus.

Protoplast regeneration carried out in a carriomycin producing organism, Streptomyces hygroscopicus 358 AV2, lose carriomycin productivity without loss of carriomycin-resistance and the ability of formation of aerial mycelium. Ethidium bromide treatment on the 358 AV2 strain generated a bald mutant that produced carriomycin and a new antibiotic curromycin. In some other media, however, the parent strain produced curromycin, indicating that the ethidium bromide treatment altered the regulation of antibiotic production. Ethidium bromide treatment on a protoplast-regenerated strain derived from the parent strain resulted in derivatives capable of producing carriomycin and curromycin. These strains were unstable and tended to lose the recovered antibiotic productivity easily.

Acridine Orange↗

Effectiveness and safety of intranasal ipratropium bromide in common colds. A randomized, double-blind, placebo-controlled trial.

OBJECTIVE: To determine the tolerability and clinical effectiveness of intranasal ipratropium bromide for the treatment of symptoms of common colds. DESIGN: Multicenter, double-blind, randomized trial. SETTING: 3 university student health services. PATIENTS: 411 previously healthy persons 14 to 56 years of age who had cold symptoms that had lasted for no more than 36 hours, rhinorrhea subjectively judged to be of at least moderate severity, and documented nasal discharge of at least 1.5 g over a 1-hour observation period. INTERVENTION: Either 1) ipratropium bromide nasal spray 0.06% in buffered salt solution, two 42-micrograms sprays per nostril administered by metered pump spray; 2) control nasal spray, which consisted of buffered salt solution; or 3) no treatment. Treatments were self-administered three or four times daily during waking hours for 4 days. After receiving their morning dose, patients stayed at the study center for 6 hours on study day 1 and 3 hours on study day 2; symptom severity was recorded and nasal mucus discharges were collected and weighed hourly during these periods. RESULTS: Ipratropium recipients had 26% less nasal discharge than controls (P = 0.0024) and 34% less nasal discharge than untreated patients (P = 0.0001). Severity of rhinorrhea as judged subjectively was reduced in ipratropium recipients by 31% compared with controls and by 78% compared with untreated patients (P = 0.0001 for both comparisons). In addition to being associated with reductions in daily assessments of the severity of rhinorrhea (P < or = 0.003), ipratropium was associated with reduced sneezing on study days 2 (20% difference; P = 0.03) and 4 (30% difference; P = 0.02) but not with reduced nasal congestion compared with the control spray. Ipratropium was generally well tolerated but was associated with higher rates of blood-tinged mucus (16.8% in the ipratropium group compared with 3.6% in the control group; P = 0.01) and nasal dryness (11.7% in the ipratropium group compared with 3.6% in the control group; P = 0.021) than the control spray. Patient assessments of the overall effectiveness of treatment were more favorable for ipratropium than for the control spray (P < or = 0.026) or for no treatment (P < or = 0.002) on each day of inquiry (study days 1, 2, and 5). CONCLUSIONS: Intranasal ipratropium bromide provides specific relief of rhinorrhea and sneezing associated with common colds.

Administration, Intranasal↗

Effects of inhaled methyl bromide gas on the metabolic system and kinetics of bromine ion in rats.

Wistar male rats were exposed to 2000 ppm of methyl bromide gas for one hour (single exposure experiment) or 300 ppm of the gas for 6 hours a day, 3 days a week for 4 or 8 weeks (repeated exposure experiment) to investigate the metabolism of inhaled methyl bromide. After the exposure was completed, the bromine ion concentration in serum was measured up to 60 days. The serum bromine ion concentration was determined by a headspace gas chromatography-mass spectrometry after converting bromine ion to methyl bromide by adding dimethyl sulfate in the serum samples. In the single exposure experiment, the bromine ion concentration decreased quickly within one day after the end of the exposure, and then began to decrease gradually. In the repeated exposure experiment, on the other hand, the bromine ion concentration decreased almost exponentially. A two-compartment model was applied to analyze the clearance rate of bromine ion. The biological half time of serum bromine ion was 9.1 days for the single exposure and 5.4 days for the repeated exposure. The amount of cytochrome P450 (CYP) in liver microsomes was measured after the end of exposure. CYP in liver was not significantly different after the repeated exposure but it decreased after the single exposure.

Administration, Inhalation↗

Individual results of treatment of COPD with low doses of fenoterol compared with treatment with ipratropium bromide.

We compared the effects of 30-day treatments with fenoterol in low doses (4 x 100 mcg) and ipratropium bromide (4 x 40 mcg) on the lung function parameters (LFP), dyspnea and physical capacity of patients with severe chronic obstructive pulmonary disease (COPD) (FEV1 < 35% pred.) and analysed the individual response of patients to the administered therapy. The study included two groups of patients treated with fenoterol (n = 22) and ipratropium bromide (n = 22). The patients were matched by functional characteristics (age: 60 +/- 7 and 57 +/- 9 years; ATS Dyspnea Scale: 2.7 +/- 0.8 and 2.4 +/- 0.9; FEV1%: 25 +/- 7% and 23 +/- 6%; pO2: 62.4 +/- 5.3 mm Hg and 61.0 +/- 9.5 mm Hg; all values mean +/- SD). After 30 days of treatment we measured the lung function parameters (FEV1, FVC), dyspnea indices (ATS dyspnea scale, Borg scale) and the physical capacity of the patients (6-minute walking distance test). The results showed that in an open experiment fenoterol (4 x 100 mcg daily), unlike ipratropium bromide (4 x 40 mcg daily), cannot improve statistically and clinically significantly the lung function parameters, dyspnea and the physical capacity of the group as a whole. However, when the findings were assessed for each patient individually, 32% of the patients proved to have responded positively to the treatment. Therefore efficaciousness of fenoterol in low doses should be determined by assessing the lung function parameters, dyspnea and the physical capacity individually for each patient.

Adrenergic beta-Agonists↗

Pulmonary function profile in chronic congestive heart failure and the effect of ipratropium bromide.

Twenty-five symptomatic patients of chronic heart failure were subjected to spirometry to detect abnormalities of pulmonary function and to assess the effect of ipratropium bromide in reversing or minimising these abnormalities. All the patients exhibited abnormal pulmonary function manifesting as obstructive (15/25) or restrictive (10/25) ventilatory defect. There was overall improvement in lung functions with ipratropium bromide especially in those with obstructive ventilatory defects and mostly comprised of smokers. Forced expiratory volume in one second increased by 47.7 percent (p < 0.02), forced expiratory volume in one second/forced vital capacity ratio by 14.1 percent (p < 0.001) and maximal voluntary ventilation by 40.6 percent (p < 0.05) in these patients. It is concluded that ipratropium bromide can prove as a promising adjunctive therapeutic intervention in improving quality of life in patients of chronic congestive heart failure who are incapacitated by dyspnoea and have clearly documented ventilatory defects.

Adult↗

[Efficacy of early administration of nebulized ipratropium bromide in children with asthmatic crisis].

AIM: To determine the efficacy of adding ipratropium bromide to nebulized salbutamol in the treatment of children with moderate-to-severe acute asthma attacks. METHODS: A total of 102 patients aged between 5 months and 16 years were included in a double-blind randomized trial. All patients were given nebulized salbutamol (0.2 mg/kg) and oral steroids (1 mg/kg). Patients in group A received two doses of nebulized ipratropium bromide (250 mg per dose) and patients in group B were given placebo. Oxygen saturation (SaO2) and a clinical score (heart rate, respiratory rate, dyspnea, retraction of the intercostal spaces, and wheezing) rated from 0 to 5 were measured before treatment and at 120 min. RESULTS: Patients in both groups showed similar SaO2 values and clinical scores at baseline (group A, 93.05% and 4.45; group B, 92.78% and 4.43) and at 120 min (group A, 94.33% and 2.45; group B, 94.03% and 2.74), but the percentage of patients admitted to the hospital was higher in group B than in group A (53% vs 35%, p = 0.07). In the subset of patients with the most severe attacks (baseline score 5), the clinical score after treatment and the percentage of admissions were significantly higher in group B (n = 22) than in group A (n = 23) (3.32 vs 2.69 and 73% vs 39%, p < 0.05). CONCLUSIONS: Coadministration of ipratropium bromide and repeat doses of nebulized salbutamol produced a small beneficial clinical effect compared with administration of nebulized salbutamol alone. This beneficial effect was related to a decrease in the hospitalization rate, particularly in patients with severe asthma attacks.

Administration, Inhalation↗

[Cholinergic crisis following administration of distigmine bromide: a case report].

The long-acting anticholinesterase, distigmine bromide (Ubretid), is widely used for the treatment of underactive neurogenic bladder. Therefore, we emphasize its hazardable side-effect of cholinergic crisis. A 78-year-old man with duodenal ulcer complained of nocturia, and was administered distigmine bromide 10 mg daily under the diagnosis of mild benign prostatic hypertrophy with underactive neurogenic bladder. It seemed that administration slightly improved his symptom but he developed bradycardia, dyspnea and drowsiness suddenly on the 4th day. Blood examination revealed extremely low cholinesterase in his serum, suggesting distigmine bromide intoxication. He was treated intensively with several intravenous injections of atropine, high-concentration oxygen and transfusion of fresh frozen plasma. Nevertheless, his condition did not recover, resulting in death of "cholinergic crisis" on the 6th day.

Aged↗

Use of diazido ethidium bromide as a specific probe for mitochondrial functions.

The diazido derivative of ethidium bromide has been synthesized as a potential photoaffinity label and shown to be at least as effective as a mitochondrial mutagen as the parent compound, with a similar mode of action. Exposure of mitochondria of Saccharomyces cerevisiae to the compound, followed by ultraviolet-irradiation, which converts it to the highly reactive dinitrene, results in its specific binding to a single component which has been tentatively identified as the smallest polypeptide (subunit 9) of the membrane-bound ATPase. An analogus reaction is also obtained with the soluble, oligomycin-sensitive ATPase complex but not with the F1-ATPase itself. The reaction with the ATPase complex can also be monitored by fluorescence enhancement and by this attribute, as well as by other criteria, diazido-ethidium bromide, ethidium bromide itself, euflavine, N,N'-dicyclohexylcarbodiimide, 2,4-dinitrophenol, and 2-azido-4-nitrophenol all appear to compete for the same, lipophilic, binding site. A mitochondrial mutation (73/1) (see Flury, U., Feldman, F., and Mahler, H.R. (1974) J. Biol. Chem. 249, 6630-6637) produces a photoaffinity product with an altered electrophoretic mobility and molecular weight.

Adenosine Triphosphatases↗

[Kinetics of scopolamine bromide release from hydrogel with a filtering membrane].

The hydrated filtration membrane renders possible uniform hydration of hydroxypropylmethylcellulose hydrogel with subsequent uniform release of dissolved scopolamine bromide. Exponential dependence of the diffusion coefficient on the graded medium dimension of the pores of the testing membrane makes possible the estimation of the reactive fractal dimension DR by means of the modified exponent (3-DR). With increasing concentration of scopolamine bromide in xerogel (14.7 to 77.8 mg/cm3), DR decreases within a range of 2.814 to 2.704. A comparison with the structure of a suitable fractal (Menger sponge) leads to a conclusion about suitability of the use of membranes for the testing of concentrations of scopolamine bromide in xerogel, if DR > 2.727.

Chemical Phenomena↗

[Cost effectiveness of the application of inhaled ipratropium bromide in the treatment of adult patients with acute asthma in Uruguay].

BACKGROUND: Administration of multiple doses of inhaled impratropium bromide and salbutamol represents the first-choice treatment for severe asthmatic crisis. However, there is a scarce evidence demonstrating that this therapeutic intervention in cost-effective. OBJECTIVE: To determine cost-effectiveness relationship related to administration of ipratropium bromide in the treatment of severe asthmatic crisis in adults at two hospitals in Montevideo, Uruguay. MATERIAL AND METHODS: The cost of each treatment was estimated in U$S 0.9 when drug was administered by a metered dose pressurized inhaler (MDI) or U$S 1.7 by using a jet nebulizer (NEB). RESULTS: A monetary saving per patient (considering a median of five days of hospitalization and a risk reduction of 0.17) of U$S 30 with MDI or U$S 29 with NEB was observed in the public practice, and a saving of U$S 78 and 77, respectively in the private practice. The total annual monetary saving was of U$S 3,101 with MDI and U$S 2,897 with NEB in the public practice, and of U$S 4,979 and U$S 4,830 in the private practice. A two-way sensitivity analysis taking into account the length of hospitalizations and the risk reduction did not modify significantly the results. CONCLUSIONS: The treatment of adults with severe acute asthma by using ipratropium bromide results cost-effective, leading to a significant saving of resources.

Acute Disease↗

[Manometric effects of pinaverium bromide in irritable bowel syndrome].

The effects of pinaverium bromide on colonic motility were investigated in a controlled, controlled, cross-over study in 32 patients with irritable bowel syndrome. Constipation was clearly predominant in one group of 16 patients, and diarrhea in the other group of 16. Manometric measurements were taken of the colonic motor response generated by distention of a balloon inserted to the rectosigmoid junction. Measurements were taken before and one hour after ingestion of two tablets containing placebo or two tablets each containing 50 mg of pinaverium bromide. Following intake of placebo the motility index increased from the basal value in patients with constipation, and resistance to distention decreased in the diarrhea group. These changes were attributable to repetition of the mechanical stimulus within a relatively brief time lapse, or more probably to the ingestion of liquid which accompanied intake of tablets. Compared with placebo, pinaverium bromide induced inhibition of both effects. From the therapeutic point of view, the decrease in motility index seen in patients with irritable bowel syndrome and constipation is particularly interesting.

Adult↗

Effect of single inhalation of a salbutamol, ipratropium bromide and beclomethasone on mucociliary clearance in patients with chronic obstructive airway disease.

BACKGROUND: Chronic obstructive airway disease (COAD) is associated with hyperplasia and hypertrophy of the mucus producing glands. The beneficial effect of inhaled drug may be due to improved mucociliary function. The present study was done to evaluate the effect of salbutamol, ipratropium bromide and beclomethasone dipropionate inhalation on mucociliary clearance in patients with COAD. METHODS: Ten patients of COAD were taken up, two patients however did not complete the study. Salbutamol, ipratropium bromide, beclomethasone dipropionate and placebo inhalation were given randomly to each patient on four separate days. Radioaerosol inhalation lung cine-scintigraphy after inhalation of the different drugs was followed up to two hours and than after 24 hours. RESULTS: There was no significant visually noticeable increased mucociliary clearance on any of the days. Two patients showed definite steep slope in the time activity curves with salbutamol as compared to other drugs or placebo. All the quantitative indices analysed at the end of one hour and two hours for the three drugs were comparable to placebo. CONCLUSIONS: A single dose of inhaled salbutamol, ipratropium bromide and beclomethasone dipropionate has no appreciable effect on mucociliary clearance in patients with COAD.

Administration, Inhalation↗

Effect of ipratropium bromide in bronchial asthma.

The effect of inhalation of ipratropium bromide was evaluated in 20 patients with bronchial asthma. It was observed that there was no significant improvement in the forced vital capacity and the forced expired volume in one second, while there was significant improvement in the peak expiratory flow rate (PEFR) measured at 9 pm, after inhalation of 2 puffs of ipratropium bromide aerosol (0.02mg/puff) three to four times a day for 2 weeks. Since PEFR is a measure of large airway function and cholinergic mechanisms are primarily involved for airflow obstruction at large airways, improvement in PEFR by ipratropium bromide highlights its role as a useful bronchodilator in patients in whom vagal reflexes are responsible for the provocation of bronchoconstriction.

Administration, Inhalation↗

A comparative study of bronchodilator actions of ipratropium bromide (atrovent) & salbutamol (ventolin) on exercise induced bronchial asthma.

The bronchodilator actions of salbutamol and ipratropium bromide were compared in 30 established cases of bronchial asthma, before and after exercise. It was noticed that after exercise (brisk walk for 3 min.) the PFT values of FVC, PEFR and FEV-1, decreased remarkably from the basal values, the mean fall of 17.91%, 10.68% & 14.8% respectively was noticed. Salbutamol showed improvement in FVC, PEFR, FEV-1, of 20.86%, 15.96% & 17.98% respectively from basal values, while Ipratropium bromide showed improvement by 18.31%, 13.01% & 20.90% respectively. It was also noted that salbutamol is a better drug amongst smokers, patients with family history of bronchial asthma, and in younger age groups. Ipratropium bromide was better in elderly patients (> 40 yrs.) and in those with eosinophillia.

Adult↗

[Analysis of steroids. Part 45: Analytical investigation of pipecuronium bromide (Arduan)].

The following methods are described for the analytical investigation of pipecuronium bromide. 1. HPLC method. Of the several systems tried for the separation and quantification of impurities and degradation products the best results were obtained using silica as the stationary phase and 43:43:14 mixture of methanol, acetonitrile and concentrated aqueous ammonia containing 0.1 mole/l each of ammonium chloride and ammonium carbonate as the eluent. The validation of this method is presented. The above described aggressive eluent can be successfully replaced by an ion-pairing system using silica as the stationary phase and 96:4 mixture of acetonitrile and water containing 0.1 mole/l sodium perchlorate as the eluent. 2. Thin-layer chromatography. TLC systems are described for the separation and densitometric quantification of the impurities and degradation products of pipecuronium bromide. 3. Spectrophotometry. Two methods are described. The ester groups of the molecule can be determined by the iron(III)-hydroxamate method while for the ion-pair extraction of the quaternary ammonium steroid picric acid or bromthymol blue are used as the reagents. 4. Titrimetry. In addition to the titration with acetous perchloric acid for the assay of the bulk material a microtitration method is described for the determination of pipecuronium bromide in individual lyophylized ampoules (potentiometric titration with 0.1 M silver nitrate).

Androstane-3,17-diol↗