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PubMed1989

Diltiazem multi-dose gastrointestinal diffusion system: preparation and release rate studies.

The present paper is concerned with a multi-dose gastrointestinal diffusion system, releasing diltiazem through a controlled source of diffusional energy. The method calls for: a) encapsulation of the drug in a microball form, and b) coating of the resulting microballs by a porous membrane which controls the diffusion rate of the drug. The system would be expected to deliver the drug at a declining rate, due to the lower solubility of diltiazem hydrochloride in the intestinal than in the stomach fluid. To maintain a constant drug diffusion rate in the intestinal fluid, a membrane-modifying agent soluble in the intestinal tract (EudragitR L.) was introduced into the cellulose acetate microball coating. In this paper in vitro studies of drug release from the unit in relation to microball coating and coating mass are presented. The system provides a zero-order drug deliver in vitro, as the result of an appropriate selection of manufacturing parameters.

Chemistry, Pharmaceutical↗

PubMed2005

Combination treatment with propiverine hydrochloride plus doxazosin controlled release gastrointestinal therapeutic system formulation for overactive bladder and coexisting benign prostatic obstruction: a prospective, randomized, controlled multicenter study.

PURPOSE: We evaluated the efficacy and safety of a therapeutic modality involving propiverine combined with doxazosin in patients with overactive bladder (OAB) and benign prostatic obstruction. MATERIALS AND METHODS: Men 50 years or older with OAB symptoms and urodynamically proven bladder outlet obstruction (Abrams-Griffith score greater than 20) were randomized (1:2) into 2 groups, namely group 1-doxazosin controlled release gastrointestinal therapeutic system formulation (4 mg once daily) only and group 2-propiverine hydrochloride (20 mg once daily) plus doxazosin controlled release gastrointestinal therapeutic system formulation for an 8-week treatment regimen. RESULTS: A total of 211 men, including 69 in group 1 and 142 in group 2, were treated and 198 (93.8%) completed the 8 weeks of treatment. Significant improvements were noted in each group after treatment in urinary frequency, maximum flow rate, average micturition volume and International Prostate Symptom Score. Compared with group 1 improvement rates with regard to urinary frequency (23.5% vs 14.3%, p = 0.004), average micturition volume (32.3% vs 19.2%, p = 0.004), and storage (41.3% vs 32.6%, p = 0.029) and urgency (p = 0.019) International Prostate Symptom Score symptoms were more significant in group 2. Post-void residual urine was found to be significantly increased only in group 2 but this was not accompanied by urinary retention. Patient satisfaction rates were found to be significantly higher in group 2 than in group 1 (p = 0.002). Overall adverse event rates were higher in group 2 (p = 0.002), although discontinuation rates and discontinuation rates due to adverse events were not different between the 2 groups. CONCLUSIONS: This study reveals that combination therapy consisting of alpha1-adrenoceptor antagonists with antimuscarinics represents an effective and relatively safe treatment modality in select patients with OAB coexisting with benign prostatic obstruction.

Adrenergic alpha-Antagonists↗

PubMed1987

Antihypertensive effectiveness of the nifedipine gastrointestinal therapeutic system.

The results of a multicenter trial conducted in order to determine the therapeutic efficacy of the gastrointestinal therapeutic system (GITS) formulation of nifedipine in comparison with hydrochlorothiazide and placebo in the management of mild to moderate essential hypertension are presented. During a one-week wash-out phase, antihypertensive therapy was discontinued in all patients. After a three-week single-blind placebo period, eligible patients were randomly assigned in a double-blind fashion to one of three treatment groups for a one-week titration period and a nine-week efficacy period. Patients received either nifedipine GITS, 30 or 60 mg daily; hydrochlorothiazide, 25 or 50 mg daily; or placebo. Sitting and standing blood pressures decreased by an average 11.6/10.4 and 10.8/10.8 mm Hg, respectively, with nifedipine GITS therapy, and 14.8/10.8 and 14.3/8.2 mm Hg, respectively, with hydrochlorothiazide therapy. Compared with placebo, these changes were highly significant for both sitting (p less than or equal to 0.005) and standing (p less than or equal to 0.02) measurements. Heart rate remained essentially unchanged in all three groups. It was therefore concluded that monotherapy with nifedipine GITS, at doses of 30 or 60 mg given once daily, effectively reduces blood pressure in patients with hypertension to a degree comparable with that seen in hydrochlorothiazide therapy.

Adult↗

PubMed2002

Persistence of antihypertensive efficacy after missed doses: comparison of amlodipine and nifedipine gastrointestinal therapeutic system.

OBJECTIVE: In this randomized, double-blind, crossover study, the antihypertensive efficacy of amlodipine and nifedipine gastrointestinal therapeutic system (GITS) was compared following missed doses. Design and methods In a randomized crossover design, 42 patients were randomized to receive amlodipine (5-10 mg) or the GITS formulation of nifedipine (nifedipine GITS) (30-60 mg) once daily for 12 weeks, then vice versa. During weeks 8, 10 and 12 of each treatment period, compliance failures were simulated by patients missing 0, 1 or 2 doses of their medication, and ambulatory systolic (SBP) and diastolic (DBP) blood pressure measurements were obtained. RESULTS: Following steady-state treatment (i.e. 'perfect compliance'), there was no difference between amlodipine and nifedipine GITS in SBP (140.1 versus 134.2 mmHg) or DBP (84.0 versus 85.8 mmHg) at 0-24 h post-dose. When compliance was not perfect, i.e. when one or two doses were missed, DBP was maintained at a significantly lower level with amlodipine compared with nifedipine GITS at 24-48 h post-dose (83.1 versus 86.4 mmHg, P = 0.005) and at 48-72 h post-dose (84.2 versus 89.7 mmHg, P < 0.001). Plasma concentrations of amlodipine were better maintained than those of nifedipine GITS. At 72 h post-dose, the plasma concentration of amlodipine was 61% (17.0 +/- 11.2 ng/ml) compared with < 25% (28.3 +/- 49.9 ng/ml) for nifedipine GITS. CONCLUSION: During short periods of non-compliance, antihypertensive efficacy remains more predictable with amlodipine than with nifedipine GITS.

Adult↗

PubMed2000

Diagnostic criteria for gastrointestinal carcinomas in Japan and Western countries: proposal for a new classification system of gastrointestinal epithelial neoplasia.

BACKGROUND: Large differences have been found between Western and Japanese pathologists in their diagnosis of adenoma/dysplasia and early carcinoma for gastric, colorectal and oesophageal epithelial neoplastic lesions. Common worldwide terminology based on clinical usefulness, that is, on neoplastic severity and depth of invasion, is needed. METHODS: Thirty-one pathologists from 12 countries reviewed 35 gastric, 20 colorectal and 21 oesophageal biopsy and resection specimens. The extent of diagnostic agreement between those with Western and Japanese viewpoints was assessed by kappa statistics. RESULTS: Suspected or definite carcinoma was diagnosed in 17-66% 'of gastric, in 5-40% of colorectal, and in 10-67% of oesophageal slides by pathologists with a Western viewpoint, but in 77-94% of gastric, in 45-75% of colorectal and in 81-100% of oesophageal slides by pathologists with a Japanese viewpoint (from Japan, Germany, Austria and UK). Overall, there was poor agreement between the conventional Western and Japanese diagnoses (kappa values lower than 0.3 for gastric, colorectal and oesophageal lesions). There was much better agreement among the pathologists (kappa values higher than 0.5 for gastric and colorectal lesions) when the original assessments of the slides were regrouped into the five categories of the following classification of GI epithelial neoplasia we hereby propose: C1, negative for neoplasia; C2, indefinite for neoplasia; C3, mucosal low-grade neoplasia (low-grade adenoma/dysplasia); C4, mucosal high-grade neoplasia (high-grade adenoma/dysplasia plus mucosal carcinoma); C5, submucosal invasion of neoplasia. CONCLUSIONS: The intercountry differences in the diagnoses of adenoma/dysplasia and early carcinoma can, in large part, be resolved by adopting terminology based on neoplastic severity and depth of invasion. Problems with defining intramucosal invasion are thus avoided. Moreover, grouping high-grade adenoma/dysplasia and mucosal carcinoma together in one category is clinically useful, as patients with small mucosal neoplastic lesions can be cured by endoscopic local resection.

Adenoma↗

PubMed2006

Abdominal heterotopic tissues: review of 24 cases diagnosed on postoperative histological evaluation.

BACKGROUND/AIMS: Heterotopy is defined as abnormal localization of well-differentiated tissue. Heterotopic tissues usually tend to be asymptomatic and noncomplicated but sometimes may cause serious clinical problems. Malignancy potential is the most important issue in this clinical entity. In this study we reviewed medical records of 24 patients with heterotopic tissues. METHODS: Between 1995-2004, 24 patients with heterotopic tissues who were diagnosed during gastrointestinal system or abdominal wall surgery or upper gastrointestinal endoscopy were included in this study. Patients' medical data were retrospectively reviewed. RESULTS: Sixteen patients with heterotopy were younger than 30 years and eight patients were older than 30 years. Nineteen (0.21%) heterotopic tissues were diagnosed in 8,945 patients who underwent gastrointestinal system surgery or upper gastrointestinal endoscopy, whereas five (0.21%) heterotopic tissues were diagnosed in 2,320 patients who underwent abdominal wall surgery. Overall, 24 (0.21%) heterotopic tissues were found in a total of 11,265 patients. The majority were pancreatic heterotopy, followed in decreasing order by gastric, adrenal and osseous heterotopy. In patients who underwent gastrointestinal surgery-endoscopy, pain was the main symptom (n=13)(68.4%), followed by dyspepsia (n=3)(15.7%) and vomiting- nausea (n=2)(10.5%). The main symptom in patients who underwent abdominal wall surgery was palpable mass. heterotopic tissues presented as wall thickening in 13, polypoid mass in five and whole solitary mass or intraparenchymal lesion in six patients. CONCLUSION: Although incidence of heterotopic tissues is low, in case of its suspicion or diagnosis, early treatment should be performed by surgical or endoscopic resection or patients must be followed up carefully due to risk of malignancy.

Abdomen↗

PubMed2000

Gastrointestinal endoscopic surgery.

A working knowledge of normal endoscopic anatomy and the effects of positioning must be mastered to take advantage of endoscopic procedures involving the gastrointestinal system. Endoscopic procedures involving the gastrointestinal system offer advantages over conventional surgery in that they are less invasive and provide direct visualization. Laparoscopy can be used to evaluate horses with abdominal pain before and after surgery. It can be used to evaluate and biopsy abdominal masses and parenchymal organs such as the spleen, liver, and kidney. Endoscopic gastrointestinal surgical procedures such as colopexy and adhesionolysis are limited at this time but should continue to be developed as instrumentation and technology evolve.

Abdominal Pain↗

PubMed1991

Nifedipine GITS (gastrointestinal therapeutic system) bezoar.

In a patient with a gastroplasty, gastric outlet obstruction developed after the dosage of nifedipine GITS (gastrointestinal therapeutic system) was increased from 30 to 60 mg/d. The hard, insoluble shell for this extended-release tablet appears causative.

Adult↗

PubMed1987

Gastrointestinal therapeutic system delivering of a water insoluble drug: isosorbide dinitrate (ISDN).

An oral therapeutic system can only be effective for soluble drugs. If no suitable salt of a drug can be found, then an osmotic agent such as sodium chloride or mannitol has to be used in a modified two-chamber system, or the osmotic dispenser with collapsible supply container. A one-chamber gastrointestinal therapeutic system (GTS) is proposed which is capable of delivering insoluble drug at a relatively constant rate. The unit consists of a tablet containing the insoluble drug and the soluble carrier, surrounded by a rate-controlling membrane with a delivery orifice. If the unit is in contact with fluid, water will pass constantly through the membrane into the tablet, dissolve the carrier which will be pumping out the insoluble drug through the delivery orifice. The effect was studied of variable content and weight of the tablet, size of the delivery orifice and thickness of the membrane on the rate of insoluble drug release from the GTS.

Excipients↗

PubMed2005

Effect of doxazosin gastrointestinal therapeutic system on platelet degranulation and platelet-leukocyte microaggregate formation induced by physiologic shear stress in hypertension.

INTRODUCTION: In this prospective, ex vivo, single-blind study, the effect of doxazosin on platelet function was studied in patients with hypertension. MATERIALS AND METHODS: Platelet activation by shear stress was measured in whole blood samples of 22 hypertensive patients and 22 normotensive controls, using flow cytometry. Sheared samples were evaluated for CD62 expression, microaggregate formation, and Ca2+ mobilization. Results were collected at baseline and after 1 and 2 months of single-dose (4 mg/d) extended-release doxazosin gastrointestinal therapeutic system therapy. RESULTS: Doxazosin normalized blood pressure in hypertensive patients after 1 and 2 months of treatment. Hypertensive patients had a higher baseline percentage (mean+/-SD) of degranulated platelets (CD62+) than the normotensive control group (4.14+/-1.05 vs. 2.47+/-0.68, P<0.01). After 2 months of doxazosin gastrointestinal therapeutic system treatment, the percentage of CD62+ in the experimental group significantly decreased (P<0.05). At baseline, the number of platelet-leukocyte aggregates in vivo was greater in hypertensive patients (P<0.01); doxazosin did not normalize this measurement. Following shearing, platelet expression of CD62 increased significantly in the hypertensive group (P<0.001 vs. control). Shear stress-induced platelet activation and microaggregate formation were also greater in hypertensive patients. Intraplatelet-free calcium concentration was higher in hypertensive patients at baseline than in the normotensive group (P<0.001). At 2 months, doxazosin significantly reduced thrombin-stimulated Ca2+ mobilization in hypertensive patients (P<0.01 vs. baseline). CONCLUSIONS: Platelets from hypertensive patients are more readily activated by shear stress and demonstrate significant alterations in cytoplasmic-free calcium mobilization. Doxazosin treatment reduced blood pressure and normalized alterations in platelet function.

Blood Platelets↗

PubMed1999

[Pharmacological analysis of atypical beta-adrenoceptors in the guinea pig gastrointestinal tissue systems].

The purpose of the present study was to characterize the atypical beta-adrenoceptors involved in relaxant responses in guinea pig gastric fundus, duodenum and ileum in functional experiments with catecholamines (isoprenaline, noradrenaline and adrenaline), beta 3-adrenoceptor agonists (BRL37344 and CGP12177A) and a non-selective beta 1-, beta 2- and beta 3-adrenoceptor antagonist bupranolol, and to obtain further evidence to clarify whether there is a tissue difference in atypical beta-adrenoceptors in the guinea pig gastrointestinal tissue systems. The atypical beta-adrenoceptors are present in gastric fundus, duodenum and ileum of guinea pig. In the presence of propranolol (1 microM) or atenolol (100 microM) plus butoxamine (100 microM), bupranolol caused a concentration-dependent rightward shift of the concentration-response curves for catecholamines and beta 3-adrenoceptor agonists. There was not a significant difference of pA2 values for bupranolol against these agonists between gastric fundus, duodenum and ileum of guinea pig. These results suggest that guinea pig gastric fundus, duodenum and ileum relaxation are mediated predominantly by an atypical beta-adrenoceptor population whereas the classical beta 1- or/and beta 2-adrenoceptors play a subordinate function role and that the receptors of three tissues are pharmacological identified by functional approaches. There is not a tissue difference in atypical beta-adrenoceptors in the guinea pig gastrointestinal tissue systems between stomach and ileum.

Adrenergic beta-Agonists↗

PubMed1993

Comparative efficacy of nifedipine gastrointestinal therapeutic system versus diltiazem when added to beta blockers in stable angina pectoris.

To determine the relative efficacy of nifedipine gastrointestinal therapeutic system (GITS) and diltiazem, 20 patients with angina pectoris and coronary artery disease were studied in a double-blinded, placebo-controlled randomized crossover trial. All patients were taking concomitant beta blockers. Efficacy was assessed by symptoms, exercise treadmill testing, and ambulatory ST-segment monitoring at baseline and after 6 weeks on each medication. Mean daily dose was titrated to 119 +/- 7 mg (nifedipine GITS) and 342 +/- 59 mg (diltiazem). The addition of either nifedipine GITS or diltiazem resulted in a significant reduction in angina frequency, improvement in exercise treadmill duration (7 vs 7 and 8 minutes; baseline vs nifedipine GITS and diltiazem), time to angina onset (4 vs 7 and 7 minutes; baseline vs nifedipine GITS and diltiazem), and time to ST-segment depression (5 vs 6 and 7 minutes; baseline vs nifedipine GITS and diltiazem). There was no significant difference between nifedipine GITS and diltiazem with respect to the magnitude of improvement in anginal symptoms or exercise test parameters. Both nifedipine GITS and diltiazem reduced the overall frequency and duration of ischemic episodes on ambulatory monitoring, but this reduction was not statistically different. Thus, nifedipine GITS and diltiazem at maximally tolerated doses were equally effective at reducing angina and increasing exercise tolerance as beta blockers alone.

Adrenergic beta-Antagonists↗

PubMed1995

Nifedipine gastrointestinal therapeutic system (GITS). A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in hypertension and angina pectoris.

Nifedipine 'gastrointestinal therapeutic system' (GITS) is a recently developed formulation that slowly releases the drug into the intestinal tract over a 24-hour period. When administered once daily, it is of similar efficacy to sustained release formulations of felodipine, verapamil, and diltiazem and at least as effective as standard formulations of lisinopril and enalapril, and long-acting propranolol and atenolol in the treatment of patients with mild to moderate essential hypertension. Substitution of nifedipine GITS for conventional formulations of nifedipine, diltiazem or verapamil, maintained adequate control of anginal symptoms in patients with stable angina pectoris. Nifedipine GITS appears to maintain quality of life and is apparently better tolerated than those formulations of nifedipine which require 2 or 3 times daily administration in both elderly and younger patients. In addition, it has minimal effect on lipid and glucose metabolism and reverses left ventricular hypertrophy, and is thus suitable for treatment of the majority of patients with mild to moderate hypertension or angina pectoris.

Administration, Oral↗

PubMedDate not supplied

Nifedipine gastrointestinal therapeutic system (GITS) for hypertensive patients in a primary care setting: results of the Extended Release Adalat Canadian Trial (EXACT).

Nifedipine gastrointestinal therapeutic system (GITS) is an extended-release dosage formulation that provides sustained blood concentrations of nifedipine over 24 hours. A 20-week, postmarketing surveillance study of the effectiveness and patient tolerability of nifedipine GITS 30 or 60 mg was conducted in the offices of 187 Canadian general practitioners from September 1992 to March 1994. A total of 1700 patients previously or newly diagnosed with mild-to-moderate essential hypertension (sitting diastolic blood pressure, 95 to 114 mm Hg) were included. The 20-week treatment period was completed by 1326 patients. Patients received nifedipine GITS 30 mg initially; the dose could be titrated upward to 60 mg after 3 and 6 weeks. Of all patients entered, 605 (35.6%) reported one or more adverse events. The three most frequently occurring adverse events were headache (12.2%), peripheral edema (8.1%), and dizziness (2.9%). The frequency of adverse events was highest in the first 3 weeks and decreased subsequently. The overall incidence of adverse events was 29.8% in patients receiving 30 mg of nifedipine GITS and 25.3% in those receiving 60 mg; adverse events were the cause of study discontinuation in 12.3% of patients. The overall health status of patients as measured by the SF-36 questionnaire was comparable to that previously reported for healthy individuals. At baseline, mean (+/- SE) systolic/diastolic blood pressure values for all patients were 160.1 +/- 0.4/97.4 +/- 0.2 mm Hg. Final blood pressure readings after 20 weeks of treatment in the 30-mg group (141.5 +/- 0.4/84.8 +/- 0.2 mm Hg) and the 60-mg group (146.6 +/- 0.8/88.8 +/- 0.4 mm Hg) were significantly decreased from baseline. At week 20, the 30-mg dose was sufficient to maintain blood pressure in 74.5% of patients; 25.5% of patients required 60 mg. Subgroup analysis revealed similar responses in patients who had received blood pressure medication before study initiation and those who had not. Response was also independent of age and type of previous antihypertensive therapy. In general medical practice, the 30-mg and 60-mg doses of nifedipine GITS were both effective and well tolerated and had minimal or no negative effects on the overall health status of treated individuals.

Adult↗

PubMed1998

Systemic amyloidosis and the gastrointestinal tract.

Systemic amyloidosis is caused by a variety of different diseases and frequently involves the gastrointestinal tract. Each type of amyloid affects the gastrointestinal tract differently. This article reviews the unique pathogenesis, pattern of gastrointestinal disposition, diagnosis, and treatment of the five systemic amyloidoses, and discusses the gastrointestinal diseases that cause systemic amyloidosis: inflammatory bowel disease and familial Mediterranean fever.

Amyloidosis↗

PubMed1996

Safety and Efficacy of Once-Daily Captopril Plus Hydrochlorothiazide versus Nifedipine Gastrointestinal Therapeutic System in Black Patients with Mild to Moderate Hypertension.

The safety and efficacy of captopril plus hydrochlorothiazide (HCTZ) were compared to nifedipine gastrointestinal therapeutic system (GITS) in 145 randomly assigned black patients with mild to moderate hypertension. Following a 4-week placebo lead-in, patients received captopril plus HCTZ 25/15 mg or nifedipine GITS 30 mg for up to 12 weeks. Upward dose titration was permitted at weeks 3 and 6. Mean seated systolic and diastolic blood pressures decreased 16.1 ± 13.5 mm Hg and 11.5 ± 7.4 mm Hg, respectively, with captopril plus HCTZ. Statistically similar decreases were observed with nifedipine GITS: systolic, 19.3 ± 12.2 mm Hg; diastolic, 13.8 ± 7.2 mm Hg. There were no clinically significant between-group differences in serum chemistries. Edema was reported in 20.3% of nifedipine GITS patients versus 1.4% of captopril plus HCTZ patients (p = 0.001). The two regimens were equally effective in controlling blood pressure in black patients; however, a higher incidence of edema occurred with nifedipine GITS compared to captopril plus HCTZ.

Journal Article↗

PubMed1994

Trough and peak effects of a single daily dose of nifedipine gastrointestinal therapeutic system (GITS) as assessed by ambulatory blood pressure monitoring. Italian Nifedipine GITS Study Group.

AIM: To evaluate the antihypertensive efficacy of nifedipine gastrointestinal therapeutic system (GITS), a slow-release formulation of nifedipine. PATIENTS AND METHODS: A randomly allocated, double-blind, placebo-controlled trial was set up with 126 essential hypertensives who were assessed by ambulatory blood pressure monitoring. A 2-week placebo run-in phase was followed by treatment with nifedipine GITS at 30 mg (n = 42) or 60 mg (n = 42) or with a placebo (n = 42) once a day for 4 weeks. At the end of each period, 24- to 36-h ambulatory blood pressure was measured at 15-min intervals by a SpaceLabs 90202 or 90207 device. The peak effect of nifedipine was assessed as the lowest average hourly value of systolic/diastolic blood pressure 2-6 h after drug intake subtracted from the baseline value for the same hour, and the trough effect as the mean systolic/diastolic blood pressure obtained 24 h after the dose subtracted from the baseline value for the same hour. RESULTS: In the 81 patients with 24-h valid ambulatory blood pressure data, 24-h, daytime and night-time mean systolic and diastolic blood pressures were significantly decreased by nifedipine GITS at both doses, but were not changed by the placebo. The trough: peak ratios for systolic and diastolic blood pressure were 90.5 and 76.3% for 30 mg nifedipine GITS and 109.3 and 98.6% for 60 mg nifedipine GITS. Correction by trough and peak effects in the placebo group further increased the trough: peak ratios. In 51 patients with 36-h ambulatory blood pressure data, trough: peak ratios above the United States Food and Drug Administration recommended value of 50% were found 30 h after the dose, and systolic blood pressure was still significantly lower 36 h after the nifedipine GITS dose.

Blood Pressure↗

PubMed2002

Influence of clinical factors, diet, and drugs on the human upper gastrointestinal glutathione system.

BACKGROUND: Glutathione (GSH) and the cytosolic glutathione S-transferases (GSTs) protect the gastrointestinal mucosa against the toxic effects of a wide variety of compounds, such as reactive oxygen species and electrophiles. AIMS: We wished to investigate the distribution along the upper gastrointestinal mucosa and the influence of clinical variables on components of the GSH system to learn more about factors which control its cytoprotective properties. METHODS: Antral and duodenal biopsies of normal appearing mucosa were collected from 202 patients (104 males, 98 females; mean age 62 years) undergoing upper gastrointestinal endoscopy. GSH content was examined by high pressure liquid chromatography, GST enzyme activity by 1-chloro-, 2, 4-dinitrobenzene conjugation, and levels of the GST classes alpha, pi, and theta by western blot. RESULTS: GSH, GST enzyme activity, and GST alpha levels were significantly lower (p<0.001) in the antrum than in the duodenum (antrum v duodenum: GSH 23.0 (0.7) v 35.0 (1.0) nmol/mg protein; GST activity 626 (19) v 832 (22) nmol/mg protein/min; GST alpha 4.5 (0.5) v 20.0 (0.7) microg/mg protein) while GST pi content was significantly higher (p<0.001) in antral than in duodenal biopsies (16.5 (0.7) v 11.2 (0.5) microg/mg protein). Antral GSH and GST activities were markedly lower in males compared with females (p<0.01). Some drugs (cisapride, diuretics, cortisol, analgesics) increased GST pi and GST alpha content but cytostatic drugs suppressed duodenal GST activity. High intake (>3 days a week) of vegetables enhanced duodenal GST alpha and GST pi and high intake of fruits the antral content of GST theta 1. CONCLUSIONS: The gastrointestinal GSH system represents the antitoxic barrier of the mucosa; its activity is influenced by localisation, sex, and drugs, and its enzymes are stimulated by a high intake of vegetables and fruits.

Adolescent↗