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Sample records for cimetidine

  1. Compound list: cimetidine [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available cimetidine CIM 00035 ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Human/i...n_vitro/cimetidine.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vi...tro/cimetidine.Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liv...er/Single/cimetidine.Rat.in_vivo.Liver.Single.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates

  2. Effects of cimetidine on haematopoiesis in vitro.

    Science.gov (United States)

    Calzado, M. C.; Garcia-Castellano, J. M.; Manzanares, R. M.; Martinez, F.; Prieto, B.; Torres, A.

    1982-01-01

    The possible modifications in haematopoiesis induced by cimetidine were studied in normal bone marrow cultures in vitro. When cimetidine was added in the therapeutic range, there was no significant change in either granulocytic-macrophagic (CFU-GM) or erythroid (BFU-E) colony growth. However, when cimetidine was added to the culture at 2 to 25 times the therapeutic range, a small but significant inhibition of both types of colony growth was found. We conclude that cimetidine in the therapeutic range does not induce inhibition of haematopoiesis in vitro but does in doses above the therapeutic range when inhibition is dose-dependent. PMID:7186818

  3. Interaction between succinylcholine and cimetidine in rats.

    Science.gov (United States)

    Mishra, Y; Ramzan, I

    1992-04-01

    The hypothesis that histamine H2 receptor blockade adversely affects neuromuscular function was tested, in vivo, in rats anaesthetised with urethane during mechanical pulmonary ventilation. Succinylcholine was administered as a bolus and constant-rate infusion to maintain 49.2% (+/- 1.5 SEM) twitch suppression in 19 rats. Cimetidine iv, 3.2, 7.5, 10, 17.8, 23.7, 31.6, or 56.2 mg.kg-1 was then administered in groups of two to three rats. Cimetidine produced an immediate potentiation of twitch suppression followed by a transient reversal and then a continued potentiation. Peak potentiation occurred within 19.0 (+/- 2.7) sec and was maintained in 11 rats at steady-state. Reversal was evident 4.1 (+/- 0.4) min after cimetidine administration. There was a good relationship between peak potentiation and serum cimetidine concentration with 50% potentiation occurring at 46.5 (+/- 4.6) micrograms.ml-1. Potentiation at steady-state was not correlated to serum cimetidine concentration but there was a weak relationship between reversal and serum cimetidine concentration. These results support reports from patients of an interaction between cimetidine and succinylcholine. PMID:1314141

  4. Effect of cimetidine on the absorption of orally administered tetracycline.

    OpenAIRE

    Fisher, P; House, F; Inns, P; Morrison, P. J.; Rogers, H. J.; Bradbrook, I D

    1980-01-01

    1 Six healthy female subjects received orally two 250 mg tetracycline tablets either with 400 mg cimetidine or placebo. In a separate experiment six healthy female volunteers received 500 mg tetracycline as a suspension on the fifth day of a 6 day regime of 400 mg cimetidine or placebo, 8 hourly and at bedtime. 500 mg tetracycline as tablets was also given with cimetidine only. 2 Following a single dose of cimetidine the mean peak tetracycline plasma concentration was significantly reduced by...

  5. Cortisol and dexamethasone elimination during treatment with cimetidine.

    OpenAIRE

    Peden, N R; Rewhorn, I; Champion, M C; Mussani, R; Ooi, T C

    1984-01-01

    In a randomised cross-over study of treatment for 7 days with cimetidine 600 mg twice daily and placebo, cimetidine had no effect on the pharmacokinetics of a single intravenous dose of dexamethasone sodium phosphate. Likewise the elimination characteristics of endogenous cortisol in the dexamethasone suppressed state were not affected by cimetidine.

  6. Effect of cimetidine on survival after gastric cancer

    DEFF Research Database (Denmark)

    Tønnesen, H; Knigge, U; Bülow, Steffen;

    1988-01-01

    The effect of cimetidine on survival was investigated in 181 patients with gastric cancer. Immediately after operation or the decision not to operate, the patients were randomised in double-blind fashion to placebo or cimetidine 400 mg twice daily for two years or until death, with review every...

  7. Biowaiver monographs for immediate release solid oral dosage forms: cimetidine.

    NARCIS (Netherlands)

    Jantratid, E; Prakongpan, S; Dressman, J B; Amidon, G L; Junginger, H E; Midha, K K; Barends, D M

    2006-01-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing cimetidine are reviewed. According to the current Biopharmaceutics Classification System (BCS), cimetidine would be assigned

  8. Cimetidine as pre-anesthetic agent for cesarean section

    DEFF Research Database (Denmark)

    Qvist, N; Storm, K; Holmskov, A

    1985-01-01

    In a prospective randomized study of 39 consecutive cesarean sections, 20 patients received cimetidine 400 mg intramuscularly as a pre-anesthetic, an 19 control patients were given NaCl. No perinatal effects on the infants were observed by cardiotocography before delivery, and K, Na, pH, PCO2, HCO...

  9. Intragastric nitrites, nitrosamines, and bacterial overgrowth during cimetidine treatment.

    OpenAIRE

    Stockbrugger, R W; Cotton, P B; Eugenides, N; Bartholomew, B. A.; Hill, M.J.; Walters, C L

    1982-01-01

    A six week course of cimetidine (1 g/day) healed peptic ulcers in 20 of 23 patients (14 with duodenal ulcer, nine with gastric ulcer). Reduction of basal acid output by 73% and peak acid output by 36% led to a rise in concentrations of intragastric aerobic bacteria and nitrate-reducing bacteria. While the mean intragastric concentration of nitrate was unchanged by treatment, there were statistically significant rises in nitrite and N-nitrosamine concentrations. The conversion from nitrates to...

  10. Cimetidine Pharmacodynamics and Pharmacokinetics in Healthy Subjects: A Comparison of Tablets and Suspension

    Directory of Open Access Journals (Sweden)

    ABR Thomson

    1994-01-01

    Full Text Available The objective of this study was to compare the effect of cimetidine 200 mg tablet with that of cimetidine suspension (200 mg/10 mL, a 20 mL suspension of 800 mg magnesium hydroxide and 912 mg aluminum hydroxide, and matching placebo on intragastric pH of healthy volunteers. There were 13 males and seven females, mean age 23 years (range 20 to 32 and mean weight 72 kg (range 55 to 89. The intragastric pH of each subject was measured over 6 h starting immediately before dosing on each of five study days. Cimetidine plasma levels were measured for 6 h after dosing on each of the cimetidine study days. Cimetidine tablet and suspension were superior to placebo tablet or suspension or to the magnesium hydroxide/aluminum hydroxide suspension in the area under the pH time curve from 0 to 6 h, percentage time pH of at least 3.5, change from pretreatment pH area under the pH time curve (0 to 6 h and maximum increase in pH. Mean plasma cimetidine levels were significantly and positively correlated to mean intragastric pH for both cimetidine tablets and cimetidine suspension. Comparing cimetidine concentration (Cmax and lower percentage time plasma cimetidine concentration was at least 0.5 μg/mL (the minimum therapeutic level. These pharmacokinetic variations between cimetidine suspension and tablets may have partially explained the pharmacodynamic differences of the lower area under the pH time curve (0 to 6 h. The results indicate that both cimetidine tablets and cimetidine suspension significantly increase intragastric pH relative to the magnesium hydroxide/aluminum hydroxide suspension, placebo tablets or placebo suspension. Based on the assumption that elevation of intragastric pH is an important factor for alleviation of the symptoms and for the healing of peptic disorders, the results of this study suggest that both cimetidine tablets and cimetidine suspension should be effective treatment.

  11. Mitigation of cimetidine induced testicular toxicity in mice by Kaempferia parviflora Wall. Ex Baker rhizome extract

    Directory of Open Access Journals (Sweden)

    Ampa Luangpirom

    2011-06-01

    Full Text Available Kaempferia parviflora Wall. Ex Baker is a herb belonging to the family Zingiberaceae, its rhizomes were used as tea or wine and well known as Thai ginseng. This present study is to evaluate the mitigative effect of aqueous rhizome extract of K. parviflora (KPE against testicular toxicity induced by subcutaneous injection of cimetidine 2 mg / 100 gBW for 14 days in male mice. The extracts at oral doses of 5, 10 and 20 mg / 100 gBW were pretreated for 7 days and co-treated with cimetidine for 14 days exhibited the significant results of mitigation by elevating seminal quality, higher than the cimetidine treated group (P K. parviflora rhizome extract as mitigative agent against testicular toxicity induced by cimetidine.

  12. [Effect of calcitonin, somatostatin and cimetidine on stress ulcer in rats].

    Science.gov (United States)

    Jakesz, R; Hofbauer, F; Lehr, L; Schiessel, R

    1978-05-01

    The prophylactic effect of calcitonin, somatostatin and cimetidine on stress ulcer formation in rats was investigated in two stress models: restraint + ketamin (4 h) and hypovolemia (4 h). The basis of the comparative study was a 70% inhibition of acid secretion for 4 h in pyloric ligated animals. This was achieved with 1000 microgram/kg somatostatin s.c., 10 microgram/kg calcitonin s.c., and 2 X 100 mumol/kg cimetidine s.c. In restraint stress and ketamin with calcitonin and cimetidine a significantly lower frequency of gastric lesions was found than with somatostatin. The most potent substance in hypovolemia was calcitonin, with a significant difference in the frequency of mucosal lesions to the groups with cimetidine and somatostatin.

  13. Therapeutic effects of oral rebamipide and in combination with cimetidine on experimental gastritis in rats.

    Science.gov (United States)

    Kishimoto, S; Fujimura, J; Machino, H; Shimamoto, T; Kobayashi, H; Shimizu, S; Haruma, K; Kajiyama, G; Sakurai, K; Yamasaki, K

    1992-12-01

    The present study evaluated the therapeutic effects of rebamipide alone and in combination with cimetidine on experimental gastritis established by the administration of 5 mM sodium taurocholate (TCA) for 6 months in rats. Morphological and biochemical analyses were performed to determine the effects of rebamipide, administered alone or in combination with cimetidine, on chronic, atrophic and erosive gastritis. Rebamipide and cimetidine were administered to rats as a dietary admixture for 4 weeks after withdrawal of TCA. Rebamipide dose-dependently reduced the total length of the erosion, normalized the mucosal thickness and increased the number of parietal and total cells, and tended to reduce interstitial infiltration of inflammatory cells and proliferation of collagenous fibers. Moreover, histochemical and biochemical studies also showed rebamipide to be effective. Rebamipide increased the PAS-positive mucus and normalized the reduced gastric mucosal SOD activity. The therapeutic effect of rebamipide on the experimental gastritis was enhanced by the combined use of cimetidine. These results suggest that rebamipide has a therapeutic effect on chronic atrophic erosive gastritis induced by TCA, and that the mechanism of the therapeutic effect is partially due to the increase in PAS-positive mucus and gastric mucosal SOD activity. Furthermore, the enhanced effect of the combination therapy of rebamipide with cimetidine was considered to be due to the actions of both cimetidine and rebamipide. PMID:1335596

  14. Functional and structural changes of human erythrocyte catalase induced by cimetidine: proposed model of binding.

    Science.gov (United States)

    Yazdi, Fatemeh; Minai-Tehrani, Dariush; Jahngirvand, Mahboubeh; Almasirad, Ali; Mousavi, Zahra; Masoud, Masoudeh; Mollasalehi, Hamidreza

    2015-06-01

    In erythrocyte, catalase plays an important role to protect cells from hydrogen peroxide toxicity. Hydrogen peroxide is a byproduct compound which is produced during metabolic pathway of cells. Cimetidine, a histamine H2 receptor antagonist, is used for gastrointestinal tract diseases and prevents the extra release of gastric acid. In this study, the effect of cimetidine on the activity of human erythrocyte catalase was investigated. Erythrocytes were broken by hypotonic solution. The supernatant was used for catalase assay and kinetics study. Lineweaver-Burk plot was performed to determine the type of inhibition. The kinetics data revealed that cimetidine inhibited the catalase activity by mixed inhibition. The IC50 (1.54 μM) and Ki (0.45 μM) values of cimetidine determined that the drug was bound to the enzyme with high affinity. Circular dichroism and fluorescence measurement showed that the binding of cimetidine to the enzyme affected the content of secondary structure of the enzyme as well as its conformational changes. Docking studies were carried out to detect the site in which the drug was bound to the enzyme. Molecular modeling and energy calculation of the binding showed that the cyanoguanidine group of the drug connected to Asp59 via two hydrogen bonds, while the imidazole group of the drug interacted with Phe64 in the enzyme by a hydrophobic interaction. In conclusion, cimetidine could bind to human erythrocyte catalase, and its interaction caused functional and conformational changes in the enzyme.

  15. Effects of cimetidine on adenylate cyclase activity of guinea pig gastric mucosa stimulated by histamine, sodium fluoride and 5'-guanylylimidodiphosphate.

    Science.gov (United States)

    Anttila, P; Westermann, E

    1976-08-01

    Cimetidine, a recently developed histamine H2-receptor blocking agent has been shown to be a potent inhibitor of histamine-stimulated gastric acid secretion in rat, cat, dog and man. To study the mode of action of cimetidine the modification of stimulatory effects of histamine, sodium flouride and 5'-guanylylimidodiphosphate by cimetidine on the adenylate cyclase activity of guinea pig gastric mucosa was studied. The effect of cimetidine was also compared to that of metiamide, an older histamine H2-receptor antagonist. The effect of cimetidine was qualitatively similar to that of metiamide, i.e. a selective blockade of histamine H2-receptors. Quantitatively cimetidine was about 10-fold more potent than metiamide.

  16. Cimetidine inhibits in vivo growth of human colon cancer and reverses histamine stimulated in vitro and in vivo growth.

    OpenAIRE

    Adams, W J; Lawson, J. A.; Morris, D. L.

    1994-01-01

    The effect of histamine and cimetidine on the growth of four human colon cancer cell lines was studied. Histamine significantly stimulated the uptake of tritiated thymidine in vitro in a dose dependent manner, to a maximum of 120% and 116% of controls for C170 and LIM2412, respectively. This effect was antagonised by cimetidine, but not diphenhydramine. Histamine also stimulated a dose dependent increase in cyclic adenosine monophosphate accumulation in C170 cells, antagonised by cimetidine. ...

  17. Cooperative inhibitory effects of antisense oligonucleotide of cell adhesion molecules and cimetidine on cancer cell adhesion

    Institute of Scientific and Technical Information of China (English)

    Nan-Hong Tang; Yan-Ling Chen; Xiao-Qian Wang; Xiu-Jin Li; Feng-Zhi Yin; Xiao-Zhong Wang

    2004-01-01

    AIM: To explore the cooperative effects of antisense oligonucleotide (ASON) of cell adhesion molecules and cimetidine on the expression of E-selectin and ICAM-1 in endothelial cells and their adhesion to tumor cells.METHODS: After treatment of endothelial cells with ASON and/or cimetidine and induction with TNF-α, the protein and mRNA changes of E-selectin and ICAM-1 in endothelial cells were examined by flow cytometry and RT-PCR,respectively. The adhesion rates of endothelial cells to tumor cells were measured by cell adhesion experiment.RESULTS: In comparison with TNF-α inducing group, lipoASON and lipo-ASON/cimetidine could significantly decrease the protein and mRNA levels of E-selectin and ICAM-1 in endothelial cells, and lipo-ASON/cimetidine had most significant inhibitory effect on E-selectin expression (from 36.37±1.56% to 14.23±1.07%, P<0.001). Meanwhile,cimetidine alone could inhibit the expression of E-selectin (36.37±1.56% vs 27.2±1.31%, P<0.001), but not ICAM-1 (69.34±2.50% vs68.07±2.10%,P>O.05)and the two kinds of mRNA, either. Compared with TNF-αα inducing group, the rate of adhesion was markedly decreased in lipo-E-selectin ASON and lipo-E-selectin ASON/cimetidine treated groups(P<0.05),and Jipo-E-selectin ASON/cimetidine worked better than lipo-E-selectin ASON alone except for HepG2/ECV304 group(P<0.05). However, the decrease of adhesion was not significant in lipo-ICAM-1 ASON and lipo-ICAM-1 ASON/cimetidine treated groups except for HepG2/ECV304 group (P >0.05).CONCLUSION: These data demonstrate that ASON in combination with cimetidine in vitro can significantly reduce the adhesion between endothelial cells and hepatic or colorectal cancer cells, which is stronger than ASON or cimetidine alone. This study provides some useful proofs for gene therapy of antiadhesion.

  18. Tubular transport and metabolism of cimetidine in chicken kidneys

    International Nuclear Information System (INIS)

    Renal tubular transport and renal metabolism of [14C]cimetidine (CIM) were investigated by unilateral infusion into the renal portal circulation in chickens (Sperber technique). [14C]CIM was actively transported at a rate 88% that of simultaneously infused p-aminohippuric acid, and its transport was saturable. The following organic cations competitively inhibited the tubular transport of [14C]CIM with decreasing potency: CIM, ranitidine, thiamine, procainamide, guanidine and choline. CIM inhibited the transport of [14C]thiamine, [14C]amiloride and [14C]tetraethylammonium. During CIM infusion, two renal metabolites, CIM sulfoxide and hydroxymethylcimetidine, were found in urine. When CIM sulfoxide was infused, its transport efficiency was 32% and not saturable. CIM sulfoxide did ot inhibit the simultaneous renal tubular transport of p-aminohippuric acid or tetraethylammonium. CIM is transported by the organic cation transport system and the kidney metabolizes CIM. Transport of CIM and other cationic drugs could produce a drug interaction to alter drug excretion

  19. Protective effects of cimetidine on micronucleated polychromatic erythrocytes in mice irradiated with 0.7Gy

    Directory of Open Access Journals (Sweden)

    Jun-ling ZHANG

    2016-01-01

    Full Text Available Objective  To study the radioprotective effect of cimetidine on single low-dose irradiated mice with radiosensitive detection indexes. Methods  Forty-eight healthy male C57BL/6 mice were randomly divided into normal control group, model control group, positive group (200mg/kg WR2721 and cimetidine groups (7.5mg/kg, 15mg/kg and 30mg/kg. The mice were given intraperitoneal injection of cimetidine 2h before irradiation in cimetidine groups and WR2721 before irradiation once a day for two days in positive group. All the mice except those in normal control group were irradiated with 0.7Gy 60Co γ-ray at 5.83mGy/min rate. Peripheral blood cells, superoxide dismutase (SOD activity and malondialdehyde (MDA content both in serum and liver, bone marrow DNA content and frequency of micronucleated polychromatic erythrocytes (fMPEs were determined 24h after irradiation. Results  Compared with normal control group, the peripheral white blood cells (WBCs of irradiated mice decreased significantly (P<0.01, and fMPEs increased significantly (P<0.01 after irradiation. Except for 15mg/kg cimetidine group, the bone marrow DNA content was decreased significantly after irradiation (P<0.01, P<0.05. The SOD activity and MDA content in irradiated mice showed no significant difference compared with that of normal mice. Compared with model control group, peripheral WBCs and bone marrow DNA content showed no significant changes in treatment groups. The f MPE of 7.5mg/kg cimetidine group was 0.027‰, which was decreased significantly compared with that of model control group (P<0.01, and the dose reduction factor (DRF of 7.5mg/kg cimetidine group was 3.338. Conclusion  Cimetidine has good protective effect on micronucleated polychromatic erythrocytes (MPEs in mice irradiated by 0.7Gy in single low-dose. DOI: 10.11855/j.issn.0577-7402.2015.12.03

  20. Cimetidine suspension as adjuvant to energy restricted diet in treating obesity

    DEFF Research Database (Denmark)

    Rasmussen, M H; Andersen, T; Breum, Leif;

    1993-01-01

    OBJECTIVE--To study the effect of cimetidine suspension compared with placebo suspension on weight loss in moderately obese patients taking a 5 MJ/day diet supplemented with dietary fibre. To determine the relation between the effectiveness of the blinding and weight loss. DESIGN--Randomised doub...

  1. Preventive effect of cimetidine on chronic erosive gastritis induced by taurocholate in rats.

    Science.gov (United States)

    Kishimoto, S; Kobuke, K; Kobayashi, H; Kajiyama, G; Miyoshi, A; Daitoku, K

    1991-01-01

    We studied the preventive effect of cimetidine at the microscopic level on chronic erosive gastritis induced experimentally by 6-months of administration of drinking water containing 5 mmol/l of the sodium salt of taurocholic acid (TCA) in rats. The chronic erosive gastritis was characterized by mucosal erosions, reduction of mucosal thickness and reduction in the number of parietal cells per unit area, infiltration of inflammatory cells which were mainly lymphocytes and plasmocytes, and proliferation of collagenous fibers in the gastric mucosa. A standard meal including cimetidine 0.4 and 0.8%, which was administered ad libitum with TCA, reduced the total length of erosions, normalized the mucosal thickness and the number of parietal cells, and reduced inflammatory cell infiltration in the gastric mucosa. However, cimetidine did not show any effect on the proliferation of collagenous fibers in the interstitial space of the mucosa. The doses administered were 400 mg/kg/day and 800 mg/kg/day for 6 months. Cimetidine, thus, had a preventive effect on experimental chronic erosive gastritis in rats. PMID:2024066

  2. A comparison of oral omeprazole and intravenous cimetidine in reducing complications of duodenal peptic ulcer

    Directory of Open Access Journals (Sweden)

    Khaleghian Farzaneh

    2006-01-01

    Full Text Available Abstract Background Gastrointestinal bleeding is a common problem and its most common etiology is peptic ulcer disease. Ulcer rebleeding is considered a perilous complication for patients. To reduce the rate of rebleeding and to fasten the improvement of patients' general conditions, most emergency departments in Iran use H2-blockers before endoscopic procedures (i.e. intravenous omeprazole is not available in Iran. The aim of this study was to compare therapeutic effects of oral omeprazole and intravenous cimetidine on reducing rebleeding rates, duration of hospitalization, and the need for blood transfusion in duodenal ulcer patients. Methods In this clinical trial, 80 patients with upper gastrointestinal bleeding due to duodenal peptic ulcer and endoscopic evidence of rebleeding referring to emergency departments of Imam and Sina hospitals in Tabriz, Iran were randomly assigned to two equal groups; one was treated with intravenous cimetidine 800 mg per day and the other, with 40 mg oral omeprazole per day. Results No statistically significant difference was found between cimetidine and omeprazole groups in regards to sex, age, alcohol consumption, cigarette smoking, NSAID consumption, endoscopic evidence of rebleeding, mean hemoglobin and mean BUN levels on admission, duration of hospitalization and the mean time of rebleeding. However, the need for blood transfusion was much lower in omeprazole than in cimetidine group (mean: 1.68 versus 3.58 units, respectively; p Conclusion This study demonstrated that oral omeprazole significantly excels intravenous cimetidine in reducing the need for blood transfusion and lowering rebleeding rates in patients with upper gastrointestinal bleeding. Though not statistically significant (p = 0.074, shorter periods of hospitalization were found for omeprazole group which merits consideration for cost minimization.

  3. Dissociation between changes in immunoreactive parathormone and its biological indices induced by cimetidine in primary hyperparathyroidism.

    Science.gov (United States)

    van der Velden, P C; Fischer, H R; Hackeng, W H; Schopman, W; Koorevaar, G; den Ottolander, G J; Silberbusch, J

    1981-01-01

    In three out of four patients with primary hyperparathyroidism, 2 000 mg of cimetidine daily caused a reduction of immunoreactive parathormone (iPTH) when measured at 8.30 and 11.30 on days 16 and 17 on treatment. Serum Ca, PO4 and maximal tubular reabsorption of PO4 remained unchanged. Excretion of cAMP/100 ml GFR remained elevated to at least the same extent as before treatment. Two patients, in whom cimetidine treatment was continued for an additional 4 weeks, did not show further hormonal or biochemical changes compared with the evaluation on days 16 and 17. We conclude that reduction of iPTH is not accompanied by any change in biological activity of this hormone. The reason for this discrepancy remains unclear. PMID:6277160

  4. Effect of ethanol, cimetidine and propranolol on toluene metabolism in man

    DEFF Research Database (Denmark)

    Døssing, M; Bælum, Jesper; Hansen, S H;

    1984-01-01

    In a climatic exposure chamber four healthy volunteers were exposed to 100ppm toluene, 100ppm toluene + ethanol, 100ppm toluene + cimetidine, and 100ppm toluene + propranolol for 7h each at random over four consecutive days. A control experiment and 3.5h of exposure to 200ppm toluene were also pe......-cresol or hippuric acid in biological monitoring of persons occupationally exposed to toluene, the consumption of ethanol should be considered....

  5. EFFECTS OF PERIOPERATIVE CIMETIDINE ADMINISTRATION ON NATURAL KILLER CELLS IN PATIENTS WITH GASTROINTESTINAL CANCER

    Institute of Scientific and Technical Information of China (English)

    LI Yan; BAI De-jiao; WANG Kun; YANG Guo-liang; YUAN Hong-yin; SHAO Hua

    1999-01-01

    Objective: To study the effects of perioperative use of cimetidine on natural killer (NK) cells in gastrointestinal (GI) cancer patients. Methods: 49 GI cancer patients were randomized into treatment group which took cimetidine in the perioperative period, and control group which did not take the drug. NK cells were measured by immunocytochemical method, using mouse-anti-human CD57 monoclonal antibody as the primary antibody. Blood samples from 20 healthy volunteers were treated in the same way as normal control. Comparisons were made within and between groups. Results: The NK cell percentage of normal control was 18.50±2.31. Both groups of patients had significantly lower than normal NK percentages before treatment (P<0.05). NK cell percentages at admission,before operation, on the 2nd and the 10th postoperative days were 14.60±3.91, 15.64±3.61, 17.40±3.28, 20.68±4.13, respectively, for the treatment group, and 14.88±2.76, 13.17±2.93, 14.50±2.77, 15.67±2.55, respectively,for control group. The difference between the two groups was statistically significant. Conclusion: Perioperative cimetidine application can help restore NK cells. The drug may be useful to reverse postoperative immuno-depression in GI cancer patients.

  6. [Therapy of duodenal ulcer and pyloric ulcer with 800 mg cimetidine nightly].

    Science.gov (United States)

    Schütze, K; Hentschel, E; Weiss, W; Kratochvil, P; Brandstätter, G; Menthe, W; Okulski, G

    1986-04-18

    The efficacy of cimetidine 400 mg b.i.d. as compared with a single evening dose 800 mg was evaluated in a single-blind multicentre trial involving 86 patients with endoscopically proven duodenal or pyloric ulcer. After four weeks of treatment the healing rates were 64.4% (29/45) with 400 mg cimetidine twice daily and 78% (32/41) with 800 mg nocte; after eight weeks the corresponding rates were 77.7% (35/45) and 85.3% (35/41). Administration of 800 mg cimetidine every evening is, consequently, at least as effective as a twice-daily regimen. In the second half of the treatment period it was significantly more effective in reducing pain and antacid consumption. The single noctural dose takes the pathogenetic importance of overnight gastric acidity into consideration, entails a simplification of therapy and may improve patient compliance. It should, therefore, take preference over the conventional twice-daily regimen. PMID:3521103

  7. Metabolic changes in cimetidine treatment for scald injury on the peritoneo-serosal surface in far-advanced gastric cancer patients treated by intraperitoneal hyperthermic perfusion.

    Science.gov (United States)

    Fujimoto, S; Takahashi, M; Kobayashi, K; Kokubun, M; Shrestha, R D; Kiuchi, S; Konno, C

    1993-01-01

    Since pretreatment with cimetidine results in the prevention of scald injury on the peritoneo-serosal surface caused by intraperitoneal hyperthermic perfusion (IPHP) for advanced gastric cancer, the diverse influence of IPHP on patients who were either given or not given cimetidine was studied both during and after IPHP treatment. Cimetidine 50 mg/kg was injected intravenously into 12 patients immediately prior to IPHP. There were no statistical background differences between the cimetidine and control groups (those not given cimetidine). The inflow and outflow temperatures of the hyperthermic perfusate in the control and cimetidine groups were 46.1 +/- 0.1 degree C and 44.1 +/- 0.1 degree C and 46.3 +/- 0.1 degree C and 44.2 +/- 0.04 degree C, respectively. Either the pre-IPHP hypothermia or IPHP in the control group resulted in a considerable increase in serum noradrenaline and adrenaline. The intravenous administration of cimetidine led to a stransient but moderate drop in the mean blood pressure as well as a delayed appearance of high concentrations of noradrenaline and adrenaline, induced by high concentrations of circulating histamine released with cimetidine. These results suggest that the sympathetic nervous responses were activated either by hypothermia or hyperthermia. The transient hypotension and delayed increases of both serum catecholamines were attributed to a marked increase in circulating histamine, released with the intravenous cimetidine. PMID:8324332

  8. Effect of omeprazole and cimetidine on healing of chronic gastric ulcers and gastric acid secretion in rats

    DEFF Research Database (Denmark)

    Poulsen, Steen Seier

    1988-01-01

    The effect of omeprazole and cimetidine on healing of chronic gastric ulcers and gastric acid secretion was investigated in rats. The effect of three doses of omeprazole given orally once daily for 25 days was investigated. In controls median ulcer healing was 19.6% after 25 days. Omeprazole...... increased median ulcer healing from 36% at 145 mumole/kg/day to 80% at 580 mumole/kg/day. Basal and pentagastrin stimulated gastric acid secretion decreased dose-dependently by nearly 90% at a dose of 580 mumole/kg/day 22-24 hr after the last dose of omeprazole. Cimetidine given twice daily, in a dose...... that initially inhibits gastric acid secretion by 95%, reduced acid secretion by only 50% 11 hr after the last dose. Median ulcer healing after treatment with cimetidine for 25 days was 41%. This study demonstrates that omeprazole has a more long-acting inhibitory effect on gastric acid secretion compared...

  9. Thermoanalytical studies of cimetidine and complexes with Mn(II Co(II and Ni(II

    Directory of Open Access Journals (Sweden)

    Ana Carolina Mendes Hacke

    2014-02-01

    Full Text Available Cimetidine is an important hydrogen histamine receptor and can coordinate metal ions in blood plasma. The stability of cimetidine and its complexes with Mn(II, Co(II and Ni(II was evaluated by studies of thermogravimetry (TG and differential thermal analysis (DTA. Cimetidine was thermally stable up to near 190 °C and above this temperature the thermal decomposition occurred in two stages. Complexes of [Mn(HCm2]Cl2, [Co(Cm2]Cl2 and [Ni(Cm2]Cl2 showed a similar behavior. The pyrolytic decomposition occurred in two stages at temperatures above 250 oC. A residue for each complex was detected at the end of the decomposition process. This probably corresponds to the respective metal oxide.

  10. Very-low dose antacid in treatment of duodenal ulcer. Comparison with cimetidine.

    Science.gov (United States)

    Zaterka, S; Cordeiro, F; Lyra, L G; Toletino, M M; Miszputen, S J; Jorge, J L; Silva, E P; Vieira, F E; Modena, J L; Massuda, H K

    1991-10-01

    Antacid (AA) in a very low dose (88 mmol/day) was compared to the standard 800-mg dose of cimetidine in healing duodenal ulcers. The influence of sex, age, symptom duration at entry, night pain, smoking, coffee consumption, and alcohol on ulcer healing was studied. The antacid was given in two different schedules: group I--20 ml 1 hr after breakfast and at bedtime; group II--10 ml 1 hr after breakfast and lunch and 20 ml at bedtime. Cimetidine (group III) was given in two divided doses: 400 mg 1 hr after breakfast and 400 mg at bedtime. Endoscopic control was performed after four weeks and, if necessary, after eight weeks of treatment. The healing rate after four weeks of treatment was, respectively, for groups I, II, and III, 45.5%, 55.8%, and 69.4% (group I = group II, and group III different from groups I and II). After eight weeks of treatment the healing rate was 61.5%, 80.8%, and 88.0% for groups I, II, and III, respectively (group II = group III, and group I different from groups II and III). Except for group I, smoking did not influence healing rate. Age, sex, symptoms at entry, night pain, and coffee consumption did not influence the treatment results. The authors concluded that the very low dose of magaldrate (88 mmol/day), when administered in three divided doses (10 ml after breakfast and lunch and 20 ml at bedtime) for eight weeks was as effective as 800 mg of cimetidine (400 mg twice a day) in healing duodenal ulcer. PMID:1914758

  11. FORMULATION AND EVALUATION OF FLOATING IN SITU GEL BASED GASTRO RETENTIVE DRUG DELIVERY OF CIMETIDINE

    OpenAIRE

    Bhargav D. Jayswal; Varun T. Yadav; Kunal N. Patel; Bhavana A. Patel; Poras A. Patel

    2012-01-01

    The present investigation deals with the formulation and evaluation of sodium alginate and pectin basedIn situ gel of Cimetidine. Sodium alginate and pectin were used as a polymer and CaCO3 was used as across-linking agent. In-situ forming polymeric formulations drug delivery systems is in sol form beforeadministration in the body, but once administered, undergoes gelation in-situ to form a gel. Theformulation of gel depends upon factors like temperature modulation, pH changes, presence of io...

  12. The effects of cimetidine on creatinine excretion, glomerular filtration rate and tubular function in renal transplant recipients

    DEFF Research Database (Denmark)

    Olsen, N V; Ladefoged, S D; Feldt-Rasmussen, B;

    1989-01-01

    The renal clearance of endogenous creatinine (CCr), sodium (CNa) and lithium (CLi) was determined before and after a single intravenous bolus of cimetidine in nine renal transplant recipients. The glomerular filtration rate (GFR) was measured with 125I-iothalamate clearance (CTh). The initial CCr...... of sodium decreased throughout the study (p less than 0.05); CLi was unchanged. In conclusion cimetidine, when measured during 1-h clearance periods, interferes with tubular creatinine secretion in the denervated kidney of transplant recipients without affecting the glomerular filtration rate or proximal...

  13. Cimetidine and Clobenpropit Attenuate Inflammation-Associated Colorectal Carcinogenesis in Male ICR Mice

    Directory of Open Access Journals (Sweden)

    Takuji Tanaka

    2016-02-01

    Full Text Available Histamine and histamine receptors (Hrhs have been identified as critical molecules during inflammation and carcinogenesis. This study was conducted to determine the effects of Hrh1-Hrh3 antagonists on inflammation-associated colorectal carcinogenesis. Male ICR mice were treated with azoxymethane (AOM, 10 mg/kg bw, i.p. and 1.5% dextran sodium sulfate (DSS, drinking water for 7 days to induce colorectal carcinogenesis. The mice were then fed diets containing test chemical (500 ppm terfenadine, 500 ppm cimetidine or 10 ppm clobenpropit for 15 weeks. At week 18, feeding with the diets containing cimetidine (Hrh2 antagonist and clobenpropit (Hrh3 antagonist/inverse agonist significantly lowered the multiplicity of colonic adenocarcinoma. Terfenadine (Hrh1 antagonist did not affect AOM-DSS-induced colorectal carcinogenesis. Adenocarcinoma cells immunohistochemically expressed Hrh1, Hrh2, Hrh3 and Hrh4 with varied intensities. Because clobenpropit is also known to be a Hrh4 receptor agonist, Hrh2, Hrh3 and Hrh4 may be involved in inflammation-related colorectal carcinogenesis. Additional data, including the mRNA expression of pro-inflammatory cytokines and inducible inflammatory enzymes in the colonic mucosa, are also presented.

  14. EFFECTS OF PERIOPERATIVE CIMETIDINE ADMINISTRATION ON TUMOR CELL NUCLEAR MORPHOMETRY AND DNA CONTENT IN PATIENTS WITH GASTROINTESTINAL CANCER

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    Objective: To explore the effects of perioperative cimetidine administration on tumor cell nuclear morphometric parameters and DNA content in patients with gastrointestinal adenocarcinoma. Methods: 49 patients with pathologically confirmed gastrointestinal adenocarcinoma were randomized into test group (n=25) and control group (n=24). The test group started oral cimetidine intake 400 mg, tid, 7-10d before operation, followed by standard curative operation. The control group did not receive cimetidine. Tumor specimens were paraffin embedded for microsection and stained with hematoxylin and eosin (HE) and Feulgen stain. Morphometric studies and DNA content of tumor nuclei were performed on IBAS Image Analyzer. Results: The tumor cell nuclear area (m m2), nuclear perimeter (m m), maximal nuclear diameter (m m) for test group/control group were 23.54 ± 5.08/34.69± 10.08 (Pquintuple ploidy tumor cells for test group/control group were 16.64± 2.58/5.33± 2.14 (P0.50), 12.42± 5.00/14.48± 0.74 (P>0.20), 31.11± 6.86/ 45.97± 3.82 (P<0.005), respectively. Conclusion: Perioperative administration of cimetidine in gasgtrointestinal cancer patients could decrease the nuclear size and raise the percentage of diploid tumor cells, and convert high aneuploid tumor cells into low-aneuploid tumor cells, which might help reduce the invasiveness of tumor cells.

  15. Cimetidine Injection

    Science.gov (United States)

    ... effects of your treatment using laboratory tests and physical examinations. It is important to keep all appointments ... health care provider as soon as possible: tenderness warmth irritation drainage redness swelling pain ¶ These branded products ...

  16. Effects of dietary fruits, vegetables and a herbal tea on the in vitro transport of cimetidine: comparing the Caco-2 model with porcine jejunum tissue

    OpenAIRE

    Tarirai, Clemence; Hamman, Josias H.; Alvaro M. Viljoen

    2012-01-01

    Context: Dietary botanicals are often consumed together with allopathic medicines, which may give rise to pharmacokinetic interactions. In vitro intestinal models are useful to identify botanical-drug interactions, but they may exhibit different expressions of transporters or enzymes. Objective: To compare the effects of selected dietary botanical extracts on cimetidine transport across two in vitro intestinal models. Materials and Methods: Bi-directional transport of cimetidine was m...

  17. FORMULATION AND EVALUATION OF FLOATING IN SITU GEL BASED GASTRO RETENTIVE DRUG DELIVERY OF CIMETIDINE

    Directory of Open Access Journals (Sweden)

    Bhargav D. Jayswal

    2012-05-01

    Full Text Available The present investigation deals with the formulation and evaluation of sodium alginate and pectin basedIn situ gel of Cimetidine. Sodium alginate and pectin were used as a polymer and CaCO3 was used as across-linking agent. In-situ forming polymeric formulations drug delivery systems is in sol form beforeadministration in the body, but once administered, undergoes gelation in-situ to form a gel. Theformulation of gel depends upon factors like temperature modulation, pH changes, presence of ions andultra-violet irradiation, from which drug gets released in sustained and controlled manner. The objectiveof this study was to develop a novel in- situ gel system for sustained drug delivery using naturalbiodegradable polymers. The system utilizes polymers that exhibit sol-to-gel phase transition due tochange in specific physico-chemical parameters. In-situ gel was formed at a biological pH. In vitrorelease studies were conducted in simulated gastric fluid and cumulative amount of drug release wasanalyzed by spectrophotometry. From designed set of experiments, it was evident that formulationcontaining 1.2% of sodium alginate and 1.5% of pectin control the release of drug for longer duration.The in-situ gel exhibited the expected, viscosity, drug content, pH, in vitro gelling capacity, in vitrofloating ability, water uptake ability and sustained drug release.The drug release from the in situ gelsfollows the fickian diffusion type of release.

  18. Continuous intragastric pH monitoring in the evaluation of ebrotidine, cimetidine and placebo on gastric acidity in healthy volunteers.

    Science.gov (United States)

    Muñoz-Navas, M; Honorato, J; Reina-Ariño, M; Márquez, M; Herrero, E; Villamayor, F; Torres, J; Roset, P N; Fíllat, O; Camps, F; Ortiz, J A

    1997-04-01

    This study was conducted to determine the efficacy and tolerance of ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]-4-thiazolyl) methyl]thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamide, CAS 100981-43.9, FI-3542), a new H2-receptor antagonist, on reducing gastric acidity after a single 800 mg dose, compared with cimetidine 800 mg once daily and placebo by means of a continuous intragastric pH monitoring. A total of 30 healthy volunteers were allocated to receive in a double blind, parallel design the study medication. Clinical observations, physical examinations and visual analogue scales (VAS) were performed during the study to assess the tolerability of the three treatments. Ebrotidine and cimetidine caused a greater and longer-lasting gastric acid inhibition than placebo. With ebrotidine, significantly (p < 0.05) higher median pH values (and interquartile range, IQR) were reached in the post-administration (2.61, IQR 2.02-3.93), postprandial (3.38, IQR 2.82-3.91) and nocturnal (2.83, IQR 1.69-3.77) periods than with placebo: 1.82 (IQR, 1.66-2.09), 2.81 (IQR, 2.02-3.28), and 1.89 (IQR, 1.44-2.13), respectively. Cimetidine showed significant differences compared to placebo in the post-administration (2.36, IQR 1.89-3.46) and nocturnal (2.46, IQR 1.88-4.33) periods. No statistical differences were observed between the active treatments. Ebrotidine caused a significantly higher percentage of time above pH 2.0 in the post-administration and nocturnal periods compared to placebo (p < 0.05), and above pH 3.0 in the post-administration, postprandial and nocturnal periods. No serious adverse effects, or disturbances in the VAS or in the vital signs were reported, and all medications were well tolerated. It is concluded that a single dose of ebrotidine 800 mg is as effective as cimetidine 800 mg in reducing total and nocturnal intragastric acidity. The study also confirms the excellent safety profile of the new drug.

  19. The effects of cimetidine, ranitidine and famotidine on the single-dose pharmacokinetics of naproxen and its metabolites in humans.

    Science.gov (United States)

    Vree, T B; van den Biggelaar-Martea, M; Verwey-van Wissen, C P; Vree, M L; Guelen, P J

    1993-12-01

    We studied the effects of cimetidine, ranitidine and famotidine on the kinetics of naproxen. The mean t1/2 beta of naproxen in 6 subjects was 25.7 +/- 5.4 h (range 16 to 36). Naproxen acyl glucuronide accounts for 50.9 +/- 6.9% of the dose, its isomerized isoglucuronide for 6.8 +/- 2.6%, O-desmethylnaproxen acyl glucuronide for 14.3 +/- 4.1% and its isoglucuronide for 5.5 +/- 1.5% (n = 6). Naproxen (1.3 +/- 1.1%) and O-desmethylnaproxen (0.6 +/- 0.4%) are excreted in negligible amounts. Cimetidine, ranitidine and famotidine all reduced significantly the t1/2 beta of naproxen by 50% from 25 h to 13 h and the t1/2 alpha from 4.0 h to 1.1 h. No effect of the H2 antagonists was observed on the absorption of naproxen. They also reduced the Vss of naproxen by 50%. The amount of naproxen acyl glucuronide, naproxen isoglucuronide and O-desmethylnaproxen acyl glucuronide excreted in the urine, remained unchanged, 60%, 7%, and 14% respectively. PMID:8314361

  20. An Overview of Analytical Determination of Diltiazem, Cimetidine, Ranitidine, and Famotidine by UV Spectrophotometry and HPLC Technique

    Directory of Open Access Journals (Sweden)

    Nighat Shafi

    2013-01-01

    Full Text Available This review article recapitulates the analytical methods for the quantitative determinations of diltiazem and three H2 receptor antagonists (cimetidine, ranitidine, and famotidine by one of the spectroscopic technique (UV spectrophotometery and separation technique such as high-performance liquid chromatography (HPLC. The clinical and pharmaceutical analysis of these drugs requires effective analytical procedures for quality control, pharmaceutical dosage formulations, and biological fluids. An extensive survey of the literature published in various analytical and pharmaceutical chemistry-related journals has been compiled in its review. A synopsis of reported spectrophotometric and high-performance liquid chromatographic methods for individual drug is integrated. This appraisal illustrates that majority of the HPLC methods reviewed are based on the quantitative analysis of drugs in biological fluids, and they are appropriate for therapeutic drug monitoring purpose.

  1. Synergistic and additive effects of cimetidine and levamisole on cellular immune responses to hepatitis B virus DNA vaccine in mice.

    Science.gov (United States)

    Niu, X; Yang, Y; Wang, J

    2013-02-01

    We and others have previously shown that both cimetidine (CIM) and levamisole (LMS) enhance humoral and cellular responses to DNA vaccines via different mechanisms. In this study, we investigated the synergistic and additive effects of CIM and LMS on the potency of antigen-specific immunities generated by a DNA vaccine encoding the hepatitis B surface antigen (HBsAg, pVax-S2). Compared with CIM or LMS alone, the combination of CIM and LMS elicited a robust HBsAg-specific cellular response that was characterized by higher IgG2a, but did not further increase HBsAg-specific antibody IgG and IgG1 production. Consistent with these results, the combination of CIM and LMS produced the highest level of IL-2 and IFN-γ in antigen-specific CD4(+) T cells, whereas the combination of CIM and LMS did not further increase IL-4 production. Significantly, a robust HBsAg-specific cytotoxic response was also observed in the animals immunized with pVax-S2 in the presence of the combination of CIM and LMS. Further mechanistic studies demonstrated that the combination of CIM and LMS promoted dendritic cell (DC) activation and blocked anti-inflammatory cytokine IL-10 and TGF-β production in CD4(+) CD25(+) T cells. These findings suggest that CIM and LMS have the synergistic and additive ability to enhance cellular response to hepatitis B virus DNA vaccine, which may be mediated by DC activation and inhibition of anti-inflammatory cytokine expression. Thus, the combination of cimetidine and levamisole may be useful as an effective adjuvant in DNA vaccinations for chronic hepatitis B virus infection. PMID:23298196

  2. Effects of transdermal scopolamine, alone or in combination with cimetidine, on total 24 hour gastric acid secretion in patients with duodenal ulcer.

    OpenAIRE

    Richardson, C T; M. Feldman

    1986-01-01

    Transdermal scopolamine is an antimuscarinic preparation approved for use in the United States for prevention of motion sickness. A recent study using this drug (0.5 mg/patch) suggested that enough scopolamine was absorbed through the skin to reduce basal gastric acid secretion in patients with duodenal ulcer. We have compared the effect of transdermal scopolamine and oral cimetidine (400 mg twice daily) in seven men with chronic duodenal ulcer, both alone and in combination, on acid secretio...

  3. Ecotoxicological assessment of cimetidine and determination of its potential for endocrine disruption using three test organisms: Daphnia magna, Moina macrocopa, and Danio rerio.

    Science.gov (United States)

    Lee, Saeram; Jung, Dawoon; Kho, Younglim; Ji, Kyunghee; Kim, Pilje; Ahn, Byeongwoo; Choi, Kyungho

    2015-09-01

    Cimetidine is a histamine H2-receptor antagonist used for treatment of gastrointestinal disorders. It is often detected in aquatic environments, but its ecotoxicological effects have not been well studied. Thus, ecotoxicity of cimetidine was evaluated using Daphnia magna and Moina macrocopa, and zebrafish (Danio rerio), and a predicted no effect concentration (PNEC) was derived. In D. magna, 48 h immobilization EC50 was determined at 394.9 mg L(-1). However, reproduction damages in D. magna were not found even at the maximum exposure level (30 mg L(-1)). For M. macrocopa, 48 h EC50 was found at 175.8 mg L(-1) and the 7 d reproduction no observed effect concentration (NOEC) was 1.1 mg L(-1). For D. rerio, 40 d growth NOEC was determined at 100 mg L(-1), the highest experimental concentration. The PNEC of cimetidine was estimated at 0.1 mg L(-1) based on M. macrocopa 7d reproduction NOEC. In 14 d adult zebrafish exposure, endocrine disruption potentials of cimetidine were observed. In male, decrease in plasma 17β-estradiol and testosterone levels, up-regulation of gonadal cyp17, and down-regulation of hepatic erα were observed at 300 mg L(-1). In female, increase in plasma E2 level and down-regulation of hepatic cyp1a were noted at 3 mg L(-1). Endocrine disruption effects were also observed in early life stage exposure. Up-regulation of erβ at 17d, and cyp19a and vtg at 40 d post fertilization were detected at 100 mg L(-1), and co-occurrence of ovary and putative testis was observed at as low as 1.1 mg L(-1). The results indicate that there is little evidence for cimetidine to cause direct ecological impact at the current ambient levels in the aquatic environment. However potential consequences of endocrine disruption following long-term exposure in aquatic environment deserves further investigation. PMID:25957140

  4. The pharmacokinetics of naproxen, its metabolite O-desmethylnaproxen, and their acyl glucuronides in humans. Effect of cimetidine.

    Science.gov (United States)

    Vree, T B; Van Den Biggelaar-Martea, M; Verwey-Van Wissen, C P; Vree, M L; Guelen, P J

    1993-05-01

    1. The pharmacokinetics of 500 mg naproxen given orally were described in 10 subjects using a direct h.p.l.c. analysis of the acyl glucuronide conjugates of naproxen and its metabolite O-desmethylnaproxen. 2. The mean elimination half-life of naproxen was 24.7 +/- 6.4 h (range 7 to 36 h). 3. Naproxen acyl glucuronide accounted for 50.8 +/- 7.3% of the dose recovered in the urine, its isomerised conjugate isoglucuronide for 6.5 +/- 2.0%, O-desmethylnaproxen acyl glucuronide for 14.3 +/- 3.4%, and its isoglucuronide for 5.5 +/- 1.3%. Naproxen and O-desmethylnaproxen were excreted in negligible amounts (< 1%). 4. Even though the urine pH of the subjects was kept acid in order to stabilize the acyl glucuronides, isomerisation took place in blood. 5. The extents of plasma binding of the unconjugated compounds were 98% (naproxen) and 100% (O-desmethylnaproxen), while naproxen acyl glucuronide binding was 92%; that of its isomer isoglucuronide 66%. O-desmethylnaproxen acyl glucuronide was 72% bound and its isoglucuronide was 42% bound. 6. Cimetidine (400 mg twice daily) decreased the t1/2 of naproxen by 39-60% (mean 47.3 +/- 11.5%; P = 0.0014) from 24.7 +/- 6.4 h to 13.2 +/- 1.0 h. It increased (10%) the urinary recovery of naproxen acyl glucuronide (P = 0.0492). The urinary recoveries of naproxen isoglucuronide and O-desmethylnaproxen acyl glucuronide remained unchanged. PMID:8512758

  5. Detection method of improvement the Cimetidine Capsule dissolution rate%改进西咪替丁胶囊溶出度的测定方法

    Institute of Scientific and Technical Information of China (English)

    秦松; 张蓓

    2016-01-01

    目的:探讨改进西咪替丁胶囊溶出度的测定方法。方法采用HPLC法测定西咪替丁胶囊的溶出度,同时将改进方法的测定结果与《中国药典》的方法进行比较。结果在0.02~0.2 mg/ml浓度范围内峰面积与浓度呈良好的线性关系(r=0.9998),回收率为99.82%,RSD为0.33%(n=6)。结论改进后的方法准确、精密、科学,且专属性强。%Objective To explore the detection method of improvement the Cimetidine Capsule dissolution rate. Meth-ods HPLC was used to determine the dissolutionrate of Cimetidine Capsule.The measurement results of improved method were compared with Chinese Pharmacopeia. Results On the concentrationscale from 0.02 to 0.2 mg/ml,the peak area had nice linear relationship with concentration,and r,recovery rate and RSD were respectively 0.9998,99.82% and 0.33% (n=6). Conclusion The improved method has advantages of more accurate,more exact,more scientific and strong specificity.

  6. Resposta cronotrópica ao teste cardiopulmonar após o uso de cimetidina Effects of cimetidine on chronotropic response to cardiopulmonary exercise t esting

    Directory of Open Access Journals (Sweden)

    Gicela Risso Rocha

    2006-03-01

    Full Text Available OBJETIVO: Testar a hipótese, por meio de ensaio clínico randomizado, de que a administração de cimetidina altera a resposta cronotrópica ao exercício. MÉTODOS: Foram selecionados 24 indivíduos saudáveis, com idade entre 20 e 68 anos, não-atletas, os quais concordaram em ser submetidos a testes cardiopulmonares, após uso de placebo e de cimetidina, 400 mg, duas vezes ao dia, durante uma semana. Os testes foram realizados em esteira rolante, com protocolo de rampa com análises diretas dos gases expirados. Foi avaliada freqüência cardíaca máxima atingida, além da freqüência cardíaca de repouso e do limiar anaeróbico. RESULTADOS: Os indivíduos estudados foram igualmente distribuídos por sexo, com idade média (± desvio padrão de 43 ±11 anos. Os exames com placebo e com cimetidina tiveram igual duração (578±90 seg vs 603±131 seg e igual VO2 pico (35±8 ml/kg.min vs 35±8 ml/kg.min. A administração de cimetidina não apresentou efeito significativo na freqüência cardíaca de repouso (75±10 vs 74±8 bpm, no pico do esforço (176±12 vs 176±11 bpm e, da mesma forma, também não houve diferença entre as variações das freqüências cardíacas (pico - repouso, nos dois estudos (101±14 vs 101±13 bpm. CONCLUSÃO: A administração de cimetidina por sete dias não altera a resposta cronotrópica ao exercício.OBJECTIVE: To test the hypothesis that the administration of cimetidine will modify the chronotropic response to exercise testing through a random clinical trial. METHODS: The study selected 24 eligible healthy subjects, ages between 20 and 68 years, not athletes, who agreed to undergo cardiopulmonary exercise testing after the administration of placebo and 400 mg of cimetidine twice a day for one week. The tests were performed on a treadmill using a ramp protocol and direct analysis of the expired gases. Peak, resting and anaerobic threshold heart rate were recorded. RESULTS: The twenty subjects studied were

  7. Thermally induced solid-state transformation of cimetidine. A multi-spectroscopic/chemometrics determination of the kinetics of the process and structural elucidation of one of the products as a stable N{sub 3}-enamino tautomer

    Energy Technology Data Exchange (ETDEWEB)

    Calvo, Natalia L.; Simonetti, Sebastian O.; Maggio, Rubén M.; Kaufman, Teodoro S., E-mail: kaufman@iquir-conicet.gov.ar

    2015-05-22

    Highlights: • Thermally stressed cimetidine above its melting point affords a stable N{sub 3} tautomer. • Multi-spectroscopic/chemometric approach developed to monitor tautomerization. • First combined use of NMR, UV and IR spectroscopies with chemometrics. • Solid cimetidine suffers first order degradation upon submission to dry heat. • Theoretical chemistry analysis confirmed the relative stability of cimetidine tautomer. - Abstract: Exposure of cimetidine (CIM) to dry heat (160–180 °C) afforded, upon cooling, a glassy solid containing new and hitherto unknown products. The kinetics of this process was studied by a second order chemometrics-assisted multi-spectroscopic approach. Proton and carbon-13 nuclear magnetic resonance (NMR), as well as ultraviolet and infrared spectroscopic data were jointly used, whereas multivariate curve resolution with alternating least squares (MCR-ALS) was employed as the chemometrics method to extract process information. It was established that drug degradation follows a first order kinetics. One of the products was structurally characterized by mono- and bi-dimensional NMR experiments. It was found to be the N{sub 3}-enamino tautomer (TAU) of CIM, resulting from the thermal isomerization of the double bond of the cyanoguanidine moiety of the drug, from the imine form to its N{sub 3}-enamine state. The thus generated tautomer demonstrated to be stable for months in the glassy solid and in methanolic solutions. A theoretical study of CIM and TAU revealed that the latter is less stable; however, the energy barrier for tautomer interconversion is high enough, precluding the process to proceed rapidly at room temperature.

  8. Analyze the Effect of Cetirizine and Cimetidine in Treatment of Eczema of Vulva%西替利嗪与西咪替丁治疗外阴湿疹临床效果分析

    Institute of Scientific and Technical Information of China (English)

    罗振增

    2015-01-01

    目的:探究外阴湿疹患者采用患西替利嗪和西咪替丁治疗的方法和效果。方法选取2014年3月~2015年6月收治的62例外阴湿疹患者进行治疗,随机分成两组,实验组38例患者选择西替利嗪和西咪替丁的综合治疗,对照组24例患者选择西替利嗪的治疗,对比两组治疗效果。结果实验组治疗的总有效率为94.74%,对照组治疗的总有效率为79.17%。实验组治疗效果更好,差异比较具有统计学意义(P<0.05)。结论外阴湿疹患者采用患西替利嗪和西咪替丁综合治疗,可及时缓解患者的身体不适,提高治疗效果。%Objective To explore the effect of cetirizine and cimetidine in treating eczema of vulva.Methods62 cases of patients with eczema of vulva were chosen from March 2014 to June 2015 for treatment, and randomly divided into two groups. 38 patients in study group are given comprehensive treatment of cetirizine and cimetidine,24 patients in control group are given cetirizine treatment only, and then observe and compare treatment effects between two groups.ResultsThe total effective rate was in study group was 94.74%, which is higher than 79.17% in control group; there was a differential between two groups and such a differential has statistic value (P<0.05).Conclusion Comprehensive treatment of cetirizine and cimetidine is effective for eczema of vulva, and it is conducive to relieving patients’ symptoms and promoting treatment efficacy, thus, such a treatment method is quite worthwhile to be promoted widespread.

  9. Analyze the Effect of Cetirizine and Cimetidine in Treatment of Eczema of Vulva%西替利嗪与西咪替丁治疗外阴湿疹临床效果分析

    Institute of Scientific and Technical Information of China (English)

    罗振增

    2015-01-01

    Objective To explore the effect of cetirizine and cimetidine in treating eczema of vulva.Methods62 cases of patients with eczema of vulva were chosen from March 2014 to June 2015 for treatment, and randomly divided into two groups. 38 patients in study group are given comprehensive treatment of cetirizine and cimetidine,24 patients in control group are given cetirizine treatment only, and then observe and compare treatment effects between two groups.ResultsThe total effective rate was in study group was 94.74%, which is higher than 79.17% in control group; there was a differential between two groups and such a differential has statistic value (P<0.05).Conclusion Comprehensive treatment of cetirizine and cimetidine is effective for eczema of vulva, and it is conducive to relieving patients’ symptoms and promoting treatment efficacy, thus, such a treatment method is quite worthwhile to be promoted widespread.%目的:探究外阴湿疹患者采用患西替利嗪和西咪替丁治疗的方法和效果。方法选取2014年3月~2015年6月收治的62例外阴湿疹患者进行治疗,随机分成两组,实验组38例患者选择西替利嗪和西咪替丁的综合治疗,对照组24例患者选择西替利嗪的治疗,对比两组治疗效果。结果实验组治疗的总有效率为94.74%,对照组治疗的总有效率为79.17%。实验组治疗效果更好,差异比较具有统计学意义(P<0.05)。结论外阴湿疹患者采用患西替利嗪和西咪替丁综合治疗,可及时缓解患者的身体不适,提高治疗效果。

  10. 外用西咪替丁、甲硝唑联合激光治疗智齿冠周炎疗效观察%Observe the efficacy of topical cimetidine, metronidazole combined laser treatment on pericoronitis

    Institute of Scientific and Technical Information of China (English)

    姚冬梅

    2014-01-01

    Objective:To observe treatment effect of cimetidine,metronidazole combined laser acute on pericoronitis.Methods:79 cases with acute pericoronitis were randomly divided into experimental group and control group.In experimental group,irradiation 5 minutes by Mandi Sen infrared laser treatment after cimetidine,metronidazole liquid alternately flushing,and then taken powder researched by two tablets into blind pouch.In the control group,also irradiated with infrared laser treatment for 5 minutes afer partial hydrogen peroxide and saline flush,then taken iodine glycerin into blind bag.1 time/day,evaluated the efficacy after 5 days.Results:The effective rate in the experimental group were higher than in the control group(P<0.01),and no adverse reactions occur.Conclusion:Cimetidine,metronidazole combined laser is an effective method of acute pericoronitis treatment.%目的:观察西咪替丁、甲硝唑联合激光治疗急性智齿冠周炎效果。方法:选取急性智齿冠周炎79例,随机分为试验组和对照组。试验组西咪替丁、甲硝唑液交替冲洗后,用曼迪森红外激光治疗仪照射5分钟,然后将两药片剂研成的药粉放进盲袋内;对照组局部双氧水、生理盐水冲洗后,也用红外激光治疗仪照射5分钟,盲袋内置入碘甘油,1次/日,5天后复诊评价疗效。结果:试验组的显效率均较对照组高(P<0.01),无不良反应发生。结论:西咪替丁、甲硝唑联合激光是一种治疗急性智齿冠周炎的有效方法。

  11. Thermally induced solid-state transformation of cimetidine. A multi-spectroscopic/chemometrics determination of the kinetics of the process and structural elucidation of one of the products as a stable N3-enamino tautomer.

    Science.gov (United States)

    Calvo, Natalia L; Simonetti, Sebastian O; Maggio, Rubén M; Kaufman, Teodoro S

    2015-05-22

    Exposure of cimetidine (CIM) to dry heat (160-180°C) afforded, upon cooling, a glassy solid containing new and hitherto unknown products. The kinetics of this process was studied by a second order chemometrics-assisted multi-spectroscopic approach. Proton and carbon-13 nuclear magnetic resonance (NMR), as well as ultraviolet and infrared spectroscopic data were jointly used, whereas multivariate curve resolution with alternating least squares (MCR-ALS) was employed as the chemometrics method to extract process information. It was established that drug degradation follows a first order kinetics. One of the products was structurally characterized by mono- and bi-dimensional NMR experiments. It was found to be the N3-enamino tautomer (TAU) of CIM, resulting from the thermal isomerization of the double bond of the cyanoguanidine moiety of the drug, from the imine form to its N3-enamine state. The thus generated tautomer demonstrated to be stable for months in the glassy solid and in methanolic solutions. A theoretical study of CIM and TAU revealed that the latter is less stable; however, the energy barrier for tautomer interconversion is high enough, precluding the process to proceed rapidly at room temperature.

  12. Clinical efficacy of cimetidine combined with Bifico prevention of necrotizing enterocolitis in preterm children%西咪替丁联合培菲康防治早产儿坏死性小肠结肠炎的临床疗效

    Institute of Scientific and Technical Information of China (English)

    鲁玉湘

    2015-01-01

    目的:观察西咪替丁联合培菲康(双歧杆菌三联活菌散)防治早产儿坏死性小肠结肠炎的临床疗效。方法:选取100例早产儿坏死性小肠结肠炎患儿,随机分为两组,每组50例。对照组单纯服用培菲康治疗,试验组给予西咪替丁与培菲康联合治疗,对比两组临床疗效及不良反应。结果:试验组总有效率为96%,明显优于对照组的78%,差异具有统计学意义( P﹤0.05)。两组均未见明显不良反应。结论:西咪替丁联合培菲康方案治疗早产儿坏死性小肠结肠炎具有较好的防治效果,安全性高,值得推广应用。%Objective To observe the clinical efficacy of cimetidine combined with Bifico( triple viable Bifidobacterium bulk)prevention of necrotizing enterocolitis in preterm children. Method 100 cases of patients with preterm children necrotizing enterocolitis were randomly divided into two groups,50 cases of each group. The control group received Bifico treatment,the experimental group received cimetidine and Bifico combination therapy. Treatment effects of the two groups were observed and statistically analyzed. Results Total efficiency rate of exper-imental group was 96%,which was significantly higher than 78% of the control group,there was statistical significance(P﹤0. 05). The two groups had no significant adverse reactions. Conclusion The effect of cimetidine combined with Bifico in the treatment of necrotizing enteroco-litis in preterm children is better,high safety,it is worthy of popularization and application.

  13. Efeitos hemodinâmicos do atracúrio e do cisatracúrio e o uso de difenidramina e cimetidina Efectos hemodinámicos del atracurio y del cisatracurio y el uso de la difenidramina y la cimetidina Hemodynamic effects of atracurium and cisatracurium and the use of diphenhydramine and cimetidine

    Directory of Open Access Journals (Sweden)

    Claudia Maria Nogueira Correa

    2010-02-01

    humans, the hemodynamic effects of atracurium and cisatracurium as well as the hemodynamic protection of diphenhydramine and cimetidine were investigated in rats. METHODS: 1 Wistar rats were anesthetized with sodium pentobarbital and prepared according to Brown et al. to evaluate different doses of atracurium and cisatracurium in the reduction of T4/T1 equal or greater than 95%. 2 Assessment of the hemodynamic changes caused by the intravenous administration of atracurium and cisatracurium by monitoring the blood pressure in the carotid artery and the electrocardiogram of rats. 3 Observation of the hemodynamic protection of prior treatment with the intravenous administration of diphenhydramine (2 mg.kg-1 and/or cimetidine (4 mg.kg-1. Statistical analysis: Student t test and ANOVA. RESULTS: Doses of 1 mg.kg-1 and 0.25 mg.kg-1 of atracurium and cisatracurium respectively did not change the mean arterial pressure (MAP. Doses of 4 mg.kg-1 of atracurium and cisatracurium decreased MAP to 62.8 ± 4.5% and 82.5 ± 2.3% respectively when compared to control levels. When the rats were pre-treated with diphenhydramine and cimetidine, diastolic pressure was reduced to 95.4% ± 2.5%. With cimetidine, diastolic pressure was reduced to 82.7 ± 8.4% when compared to the control group. The effects on systolic and diastolic blood pressure were reflected in the levels of MAP. CONCLUSIONS: The isolated administration of diphenhydramine and cimetidine did not prevent the reduction in mean arterial pressure induced by atracurium. However, the association of both drugs was able to prevent the hemodynamic effects of atracurium. The doses of cisatracurium used in this study did not cause a reduction in blood pressure significant enough to justify the use of the preventive measures used in the atracurium groups.

  14. High-Resolution Solid-State NMR Spectroscopy: Characterization of Polymorphism in Cimetidine, a Pharmaceutical Compound

    Science.gov (United States)

    Pacilio, Julia E.; Tokarski, John T.; Quiñones, Rosalynn; Iuliucci, Robbie J.

    2014-01-01

    High-resolution solid-state NMR (SSNMR) spectroscopy has many advantages as a tool to characterize solid-phase material that finds applications in polymer chemistry, nanotechnology, materials science, biomolecular structure determination, and others, including the pharmaceutical industry. The technology associated with achieving high resolution…

  15. The pharmacokinetics of naproxen, its metabolite O-desmethylnaproxen, and their acyl glucuronides in humans. Effect of cimetidine.

    OpenAIRE

    Vree, T.B.; van den Biggelaar-Martea, M; Verwey-Van Wissen, C P; Vree, M L; Guelen, P J

    1993-01-01

    1. The pharmacokinetics of 500 mg naproxen given orally were described in 10 subjects using a direct h.p.l.c. analysis of the acyl glucuronide conjugates of naproxen and its metabolite O-desmethylnaproxen. 2. The mean elimination half-life of naproxen was 24.7 +/- 6.4 h (range 7 to 36 h). 3. Naproxen acyl glucuronide accounted for 50.8 +/- 7.3% of the dose recovered in the urine, its isomerised conjugate isoglucuronide for 6.5 +/- 2.0%, O-desmethylnaproxen acyl glucuronide for 14.3 +/- 3.4%, ...

  16. Histologic evaluation of preventive measures for scald injury on the peritoneo-serosal surface due to intraoperative hyperthermic chemoperfusion for patients with gastric cancer and peritoneal metastasis.

    Science.gov (United States)

    Fujimoto, S; Takahashi, M; Kobayashi, K; Mutou, T; Toyosawa, T; Izawa, E; Numai, T; Kondoh, F; Ohkubo, H

    1998-01-01

    To histologically assess the preventive efficacy of cimetidine against scald injury on the peritoneo-serosal surface during intraperitoneal hyperthermic chemoperfusion (IHCP) for advanced gastric cancer, a randomized histologic study using cimetidine, a histamine H2-receptor antagonist, was performed for 20 patients with advanced or recurrent gastric cancer and peritoneal metastasis. Cimetidine 50 mg/kg was administered intravenously to 10 patients just prior to the IHCP (cimetidine group), and the remaining 10 patients underwent the IHCP without cimetidine (control group). The background factors and IHCP treatments of these two groups were nearly the same. Although the antitumour efficacy of the IHCP was not histologically different between the two groups, the histological analysis revealed that the peritoneo-serosal surface in the cimetidine group was protected against scald injury, compared with the control group. This finding suggests that pre-IHCP cimetidine is of great benefit for protecting the peritoneo-serosal surface from scald injury due to IHCP. PMID:9483448

  17. In Vivo Effects of the H2 Receptor Antagonist Cimetidine on Anamnestic Response of Humoral Immunity in Chicks%西咪替丁对鸡回忆性体液免疫应答反应的作用

    Institute of Scientific and Technical Information of China (English)

    乔彦良; 盛英霞; 杨汉春; 李翠梅; 付兴伦; 原培勋

    2001-01-01

    本试验系统观察了西咪替丁对鸡回忆性体液免疫应答反应的作用,并与同类咪唑类化合物左旋咪唑进行了比较.28日龄鸡,免疫注射绵羊红细胞+牛血清白蛋白(SRBC+BSA)悬液,或稀释的布氏杆菌(BA)抗原.56日龄时,以10.0、100.0mg/kg西咪替丁或10.0mg/kg左旋咪唑饮水给药,连用3天,给药第二天同时进行第2次免疫注射.结果表明西咪替丁(10.0~100mg/kg)可使二次免疫鸡体内对颗粒性胸腺依赖性抗原SRBC和非胸腺依赖性抗原BA抗体滴度回忆性免疫应答反应明显升高;但使鸡对可溶性胸腺依赖性抗原BSA抗体滴度回忆性免疫应答反应明显降低.与西咪替丁比较,左旋咪唑(10.0mg/kg)也存在着非常类似的作用.

  18. 甲氰咪胍加阿昔洛韦治疗水痘患者16例报告%Report on the results of treatment of 16 chickenpox patients with cimetidine and aciclovir

    Institute of Scientific and Technical Information of China (English)

    周建南; 麦世萍

    2004-01-01

    水痘是儿科、皮肤科等常见的疾病,易在群体中传播,以往采取传统方法治疗,疗效不明显,病程绵长,易出现感染等合并症以致遗留瘢痕。我们采用甲氰咪胍加阿昔洛韦软膏治疗16例患者,临床疗效明显,现报道如下。

  19. 聚肌胞、西咪替丁联合治疗小儿水痘34例疗效观察%Observation for Unite Treatment with Polyinosinic and Cimetidine for 34 Children with Chickenpox

    Institute of Scientific and Technical Information of China (English)

    郑丽英; 董彩琴

    2003-01-01

    目的:观察聚肌胞、西咪替丁联合治疗小儿水痘的疗效.方法:观察组34例每次应用聚肌胞0.07~0.1mg/kg,隔日1次肌注,西咪替丁每日15 mg/kg,分3次口服,疗程5~7 d.对照组30例应用病毒唑每日10~15 mg/kg,分2次肌注,维生素B12每次250μg,隔日1次肌注,疗程5~7 d.结果:观察组退热、皮疹隐退、疱疹结痂、痂皮脱落,所需平均天数分别为1.65,3.13,4.50,9.58.对照组退热、皮疹隐退、疱疹结痂、痂皮脱落,所需平均天数分别为4.33,4.83,6.28,12.05.两组比较,观察组疗效明显优于对照组,各项指标比较均有显著差异,均为P<0.01.结论:聚肌胞、西咪替丁联合治疗小儿水痘疗效满意,可起到减轻症状,缩短病程,预防并发症的作用;并且见效较快,无严重不良反应.

  20. Human breast cancer resistance protein : Interactions with steroid drugs, hormones, the dietary carcinogen 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine, and transport of cimetidine

    NARCIS (Netherlands)

    Pavek, P; Merino, G; Wagenaar, E; Bolscher, E; Novotna, M; Jonker, JW; Schinkel, AH

    2005-01-01

    The breast cancer resistance protein (BCRP/ABCG2) is an ATP-binding cassette drug efflux transporter that extrudes xenotoxins from cells, mediating drug resistance and affecting the pharmacological behavior of many compounds. To study the interaction of human wild-type BCRP with steroid drugs, hormo

  1. Effects of Cimetidine on portal hemodynamics in dogs with cirrhosis and portal hypertension%甲氰咪胍对肝硬化门脉高压症犬门脉血液动力学的影响

    Institute of Scientific and Technical Information of China (English)

    王延龄; 陈云波; 丁巍; 李桂英; 王淑敏; 李爱景

    2005-01-01

    目的:探讨甲氰咪胍对肝硬化门脉高压症犬门脉血液动力学的影响.方法:以胆总管结扎法成功制备胆汁性肝硬化门脉高压症模型犬11只,随机分为两组,即甲氰咪胍组(n=7)和盐水对照组(n=4);另取4只正常犬作正常对照组.经股动脉、股静脉、右颈外静脉分别插管,以多导生理记录仪、电磁流量计等检测门脉及全身血液动力学变化,使用RF-3000型荧光分光光度计测量血浆组织胺浓度.结果:甲氰咪胍组静脉注射甲氰咪胍(剂量0.012 g·kg-1)5、15、30、60、90和120 min后,自由门脉压平均值分别较注射前下降5.2%、14.1%、13.7%、12.9%、9.3%和6.5%(P<0.05,P<0.01,P<0.01,P<0.01,P<0.01,P<0.05),肝静脉楔入压、肝静脉压梯度、门静脉阻力均同步下降.肝动脉血流量无显著改变,门静脉血流量及全肝血流量轻度增多.肝静脉自由压、下腔静脉压、腹主动脉平均压及心率均无明显变化.自由门静脉压下降最大幅度与股静脉血血浆组织胺浓度呈显著正相关(r=0.787 4,P<0.05).盐水对照组及正常对照组上述各指标均无显著变化.结论:甲氰咪胍通过拮抗肝硬化门脉高压症犬血中异常升高的组织胺的作用,舒张肝血管床,降低门脉血流阻力,从而降低门脉压力,同时使门脉及全肝血流量轻度增加,而对全身血流动力学无不良影响.

  2. Treatment of acne vulgaris with anti androgens

    OpenAIRE

    Vaswani Neena; Pandhi R

    1990-01-01

    This study was conducted to compare the relative efficacy of spironolactone and cimetidine in moderately severe acne vulgaris. Fifteen women were treated with spironolactone (100 mg daily) given cyclically, while 14 women were given cimetidine (1400 mg daily) cyclically. The response was evaluated at 12 weeks. Spironolactone produced a good to excellent response in 11 (73. 3%) acne patients while with cimetidine 6 (42.8%) patients showed a good to excellent response. The mean re...

  3. Treatment of acne vulgaris with anti androgens

    Directory of Open Access Journals (Sweden)

    Vaswani Neena

    1990-01-01

    Full Text Available This study was conducted to compare the relative efficacy of spironolactone and cimetidine in moderately severe acne vulgaris. Fifteen women were treated with spironolactone (100 mg daily given cyclically, while 14 women were given cimetidine (1400 mg daily cyclically. The response was evaluated at 12 weeks. Spironolactone produced a good to excellent response in 11 (73. 3% acne patients while with cimetidine 6 (42.8% patients showed a good to excellent response. The mean reduction of the non-inflammatory and inflammatory lesion count was 29. 3 + 3. 6 and 9. 7 + 1. 3 respectively with spironolactone and 18.6 + 5.8 and 6.4 + 2.1 respectively with cimetidine. The response of acne vulgaris to spironolactone was superior to that of cimetidine and this difference was statistically significant (p< .05. The side effects were minimal and did not necessitate withdrawal of treatment.

  4. Cimetidine test in correcting creatinine clearance rate in chlidren with renal dysfunction and its evaluation%西咪替丁试验纠正肾功能不全患儿肌酐清除率方法及评价

    Institute of Scientific and Technical Information of China (English)

    孙良忠; 陈述枚

    2003-01-01

    1 使用肌酐清除率评价肾小球滤过率的偏差 肾小球滤过率(GFR)的检测对观察肾脏疾病的进展和预后、药物治疗疗效、透析充分性和移植肾的功能等均有重要意义.目前准确评价GFR的指标是菊粉清除率(Cin)或同位素51铬-乙二胺四乙酸(51Cr-EDTA)等的清除率;临床上用来评价GFR最常用的指标仍然是肌酐清除率(Ccr).Ccr与实际GFR存在一定的偏差.导致Ccr偏离GFR的主要原因是肾小管可分泌少量的肌酐,使Ccr高于GFR.血清肌酐(Scr)在正常水平时,肾小管分泌肌酐量很少,对Ccr影响不大,Ccr/GFR为1.1~1.4;且由于肾小管对肌酐的分泌存在昼夜规律,对肌酐的分泌主要集中在夜间,因此采用4h晨尿Ccr会比24h Ccr的偏差小.但是如果肾小球功能降低,Scr水平升高时,肾小管就会失去分泌肌酐的昼夜规律,分泌肌酐量会显著增多,使测得的Ccr远高于实际GFR;在GFR小于20mL*(min*1.73m2)-1时,Ccr/GFR比值可达到1.7[1,2].这样,用Ccr来反映GFR就会很不准确.

  5. Flibanserin

    Science.gov (United States)

    ... receptor 2A antagonist. It works by changing the activity of serotonin and other natural substances in the ... the following: antidepressants such as fluoxetine (Prozac, Sarafem); antifungals; cimetidine (Tagamet); digoxin (Lanoxin); diphenhydramine (Benadryl); medications for ...

  6. Zidovudine Injection

    Science.gov (United States)

    ... severe side effects, such as liver damage, blood toxicities, and muscle disorders. If you experience any of ... prescription and nonprescription medications you are taking, especially acetaminophen, acyclovir (Zovirax), aspirin, cancer chemotherapy, cimetidine (Tagamet), fluconazole ( ...

  7. Oral administration of synthetic human urogastrone promotes healing of chronic duodenal ulcers in rats

    DEFF Research Database (Denmark)

    Poulsen, Steen Seier; Nexø, Ebba

    1986-01-01

    The effect of oral administration of synthetic human epidermal growth factor/urogastrone (EGF/URO) on healing of chronic duodenal ulcers induced by cysteamine in rats was investigated and compared with that of cimetidine, a H2-receptor antagonist. After 25 and 50 days of treatment, synthetic human...... EGF/URO significantly increased healing of chronic duodenal ulcers to the same extent as cimetidine. Combined treatment with synthetic human EGF/URO and cimetidine for 25 days was more effective than synthetic human EGF/URO given alone, whereas combined treatment for 50 days was significantly more...... effective than cimetidine alone. These results show that a combination of an agent inhibiting gastric acid secretion and the cytoprotective and growth-stimulating peptide EGF/URO seems to be more effective with regard to duodenal ulcer healing than individual administration of the two substances. Synthetic...

  8. H2-receptor blockade and exercise-induced asthma.

    OpenAIRE

    Nogrady, S G; Hahn, A G

    1984-01-01

    While in vitro studies suggest that H2-receptor blockade enhances mediator release from bronchial mast cells and leads to bronchoconstriction, in vivo studies have given conflicting results. Eight asthmatic subjects were given cimetidine 800 mg and placebo double-blind on different days. Baseline values of forced expiratory volume in one second (FEV1) were obtained before an 8 min standardized exercise test using a bicycle ergometer. Subjects inhaled cold, dry air and exercise on cimetidine a...

  9. Measurements of intestinal villi non-specific and ulcer-associated duodenitis-correlation between area of microdissected villus and villus epithelial cell count.

    OpenAIRE

    M. Hasan; Ferguson, A.

    1981-01-01

    Measurements of villus height, villus area, together with counts of epithelial cells in individual villi, were performed on endoscopic duodenal biopsies from five groups of patients: controls, ulcer-associated duodenitis, mild and severe non-specific (non-ulcerative) duodenitis, cimetidine healed ulcer-associated duodenitis and cimetidine healed non-specific duodenitis. The objectives of the study were two-fold: to establish if epithelial cell count correlated with simpler measurements of vil...

  10. Titanium dioxide nanofibers integrated stainless steel filter for photocatalytic degradation of pharmaceutical compounds.

    Science.gov (United States)

    Ramasundaram, Subramaniyan; Yoo, Ha Na; Song, Kyung Guen; Lee, Jaesang; Choi, Kyoung Jin; Hong, Seok Won

    2013-08-15

    A photocatalytically active stainless steel filter (P-SSF) was prepared by integrating electrospun TiO2 nanofibers on SSF surface through a hot-press process where a poly(vinylidene fluoride) (PVDF) nanofibers interlayer acted as a binder. By quantifying the photocatalytic oxidation of cimetidine under ultraviolet radiation and assessing the stability of TiO2 nanofibers integrated on the P-SSF against sonication, the optimum thickness of the TiO2 and PVDF layer was found to be 29 and 42 μm, respectively. At 10L/m(2)h flux, 40-90% of cimetidine was oxidized when the thickness of TiO2 layer increased from 10 to 29 μm; however, no further increase of cimetidine oxidation was observed as its thickness increased to 84 μm, maybe due to limited light penetration. At flux conditions of 10, 20, and 50 L/m(2) h, the oxidation efficiencies for cimetidine were found to be 89, 64, and 47%, respectively. This was attributed to reduced contact time of cimetidine within the TiO2 layer. Further, the degradation efficacy of cimetidine was stably maintained for 72 h at a flux of 10 L/m(2) h and a trans-filter pressure of 0.1-0.2 kPa. Overall, our results showed that it can potentially be employed in the treatment of effluents containing organic micropollutants. PMID:23721729

  11. Mechanism for high PCO2 in gastric juice: roles of bicarbonate secretion and CO2 diffusion.

    Science.gov (United States)

    Stevens, M H; Thirlby, R C; Feldman, M

    1987-10-01

    The partial pressure of CO2 (PCO2) in gastric juice often exceeds the PCO2 of blood. CO2 in gastric juice may originate from blood and enter luminal fluid by diffusion, or CO2 may be produced in the lumen of the stomach from the reaction of HCO3- and H+. Because CO2 production from HCO3- is dependent on acid (low pH), we suppressed acid secretion with intravenous cimetidine to estimate to what extent appearance of CO2 in luminal fluid is due to production from HCO3-. When denervated fundic pouches of dogs were distended with saline, the PCO2 of the solution increased to the PCO2 of blood in approximately 20 min, with the initial rate of appearance of CO2 in the pouch solution only minimally affected by cimetidine. Thereafter, PCO2 of luminal fluid continued to increase to 50-60 mmHg in the absence of cimetidine, whereas PCO2 of luminal fluid remained approximately equal to that of blood when cimetidine was infused (P less than 0.001, cimetidine vs. control). The mean pH in the pouch solution remained between 6.3 and 6.9 during cimetidine infusion but decreased to 4.75 without cimetidine (P less than 0.001). In additional experiments, an acidic solution with high PCO2 (242 +/- 3 mmHg) was infused into the fundic pouches. PCO2 in luminal fluid decreased rather slowly toward plasma PCO2, requiring 240 min for luminal fluid PCO2 to decrease to 56 +/- 2 mmHg. Thus the permeability of the gastric mucosa to luminal CO2 was relatively low.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:3116857

  12. Modulation of drug efflux by aloe materials: An In Vitro investigation across rat intestinal tissue

    Directory of Open Access Journals (Sweden)

    Beneke Carien

    2013-01-01

    Full Text Available Background: Clinically, significant herb-drug interactions have been previously documented and can be pharmacodynamic and/or pharmacokinetic in nature. Pharmacokinetic interactions have been attributed to induction or inhibition of either metabolic enzymes or efflux transporters. Objective: The effect of gel and whole leaf materials from 3 different aloe species namely Aloe ferox, Aloe marlothii, and Aloe vera as well as polysaccharides precipitated from the A. vera materials on the bi-directional transport of cimetidine across rat intestinal tissue was investigated. Materials and Methods: Cimetidine transport studies were performed across excised rat intestinal tissue mounted in Sweetana-Grass diffusion chambers in both the apical-to-basolateral and basolateral-to-apical directions. Results: While A. vera gel and whole leaf materials did not inhibit the efflux of cimetidine, the polysaccharides precipitated from them did show a reduction of cimetidine efflux. On the other hand, both A. ferox and A. marlothii gel and whole leaf materials exhibited an inhibition effect on cimetidine efflux. Conclusions: This study identified a modulation effect of efflux transporters by certain aloe materials. This may cause herb-drug pharmacokinetic interactions when drugs that are substrates for these efflux transporters are taken simultaneously with aloe materials. On the other hand, these aloe materials may be used for drug absorption enhancement for drugs with low bioavailability due to extensive efflux.

  13. Efficacy and safety of ecabet sodium on functional dyspepsia :A prospective, double-blinded, randomized, multi-center controlled trial

    Institute of Scientific and Technical Information of China (English)

    Jun Haeng Lee; Soo Teik Lee; Eun Hyun Lee; Jong Chul Rhee; Jae J Kim; Ki-Baik Hahm; Dong Ho Lee; Nayoung Kim; Sung Kook Kim; Jong Jae Park; Seok Reyol Choi; Jong Hun Lee

    2006-01-01

    AIM: To compare ecabet sodium and cimetidine in relieving symptoms of functional dyspepsia.METHODS: We performed a multi-center, prospective,randomized, double-blinded controlled trial to compare the clinical efficacy of ecabet sodium and cimetidine in patients with functional dyspepsia. Two-hundred and seventy-two patients with dyspeptic symptoms fulfilling the Rome-Ⅱ criteria were enrolled from 7 centers. In the study group (115 patients), 1.5 g ecabet sodium was given twice a day. In the control group (121 patients),400 mg cimetidine was given twice a day. Symptoms and parameters of quality of life were analyzed at baseline, 3,14, and 28 d after initiating the treatment.RESULTS: Two-hundred and thirty-six patients completed the clinical trial. After 4 wk of treatment,the rates of improvement in patients with dyspeptic symptoms were not different between two groups (77.4% in the ecabet group and 79.3% in the cimetidine group, respectively, P > 0.05). Likewise, the rates of symptomatic improvement were not different at 3 d and 14 d. The parameters of quality of life did not change significantly during the study period in both groups.There was no clinically significant adverse event in both groups.CONCLUSION: In patients with functional dyspepsia,ecabet sodium has similar clinical efficacy with cimetidine.

  14. Role of central histaminergic mechanism in behavioural depression (swimming despair) in mice.

    Science.gov (United States)

    Nath, C; Gulati, A; Dhawan, K N; Gupta, G P

    1988-01-01

    The role of the central histaminergic system in depression was studied by using swimming despair test in mice - a behavioural model of depression. In this test, immobility of mice reflects a state of depression. Intracerebral (ic) injection of histamine (50-200 micrograms) increased significantly the immobility. The H1-receptor blocker mepyramine (2.5-20 mg/kg ip) had no effect while H2-receptor blocker cimetidine (100-200 micrograms ic) caused a significant decrease in immobility. The histamine induced facilitation was blocked completely by cimetidine and antidepressant drugs-imipramine and desipramine, but remained unaffected in mice pretreated with mepyramine or atropine. The H2 agonist impromidine (20-40 micrograms ic) also enhanced significantly, the immobility which was blocked by cimetidine and antidepressant drugs. It has been concluded that central H2-receptors facilitate depression and antidepressant drugs block central H2-receptors.

  15. Histamine delays gastric emptying of solid food in man through histamine, receptors

    International Nuclear Information System (INIS)

    The authors have shown that histamine (H) contracts the cat pylorus and duodenum through H/sub 1/ receptor mechanisms. The authors investigated the effect of H infusion on gastric emptying (GE) and the role of H/sub 1/ and H/sub 2/ receptor blockade in healthy volunteers. Radionuclide GE studies were performed using chicken liver labeled in vivo with /sup 99m/Technetium-sulfur colloid as a marker of solid food. Study days were as follows: a baseline GE study (Day 1); H infused continuously IV at a rate of 40 μg/kg/hr during the GE study (Day 2); an IV bolus of 50 mg of diphenhydramine (Day 3), or 300 mg cimetidine (Day 4) given just prior to the continuous infusion of H; a final day when cimetidine was given alone (Day 5). GE was monitored for 2 hours on each day. The results of days 1, 2 and 3 are summarized below (+p<0.05 vs baseline or Day 1). Pretreatment with cimetidine (Day 4) augmented the delay in GE induced by H infusion, while cimetidine without H (Day 5) had no effect on GE. The authors conclude that: 1) H given at a dose which elicits maximal acid secretory response in man significantly delays GE; and 2) H/sub 1/ receptor blockade but not H/sub 2/ blockade prevented this effect. Histamine may play a modulatory role in human gastric emptying through an H/sub 1/ receptor mechanism

  16. Disease: H00374 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available (Flat wart) Human papillomavirus 4 [VGNM:NC_001457] (Pigmented wart) Human papill...aris / Common wart) Human papillomavirus 60 [VGNM:NC_001693] (Pigmented wart) Human papillomavirus 63 [VGNM:...NC_001693] (Punctate wart) Human papillomavirus 65 (Pigmented wart) Human papillomavirus 88 [VGNM:NC_010329]...00] (Condyloma acuminatum, Myrmecia, Pigmented wart, Punctate wart, Verrucous papule, Flat wart) Cimetidine

  17. Tranexamic acid for upper gastrointestinal bleeding

    DEFF Research Database (Denmark)

    Gluud, Lise Lotte; Klingenberg, Sarah Louise; Langholz, Ebbe

    2012-01-01

    Tranexamic acid reduces haemorrhage through its antifibrinolytic effects. In a previous version of the present review, we found that tranexamic acid may reduce mortality. The present review includes updated searches of randomised trials on tranexamic acid versus placebo, cimetidine or lansoprazole....

  18. The role of a defined formula diet in the prevention of stress-induced gastric mucosal injury in the rat.

    Science.gov (United States)

    Mabogunje, O A; Andrassy, R J; Isaacs, H; Mahour, G H

    1981-12-01

    The role of a defined formula diet, Vivonex HN, in the prevention of gastric mucosal injury was evaluated in the cold, restrained rat model. The mean grade of gastric bleeding and mean number of gastric lesions were 3.95 and 7.35 +/- 1.02, respectively, in the stressed, unprotected control group. In four random groups of rats given Vivonex HN, Maalox, Cimetidine (20 mg/kg) and Cimetidine (60 mg/kg) prior to stress, the mean grade of gastric bleeding was 0; 1.55; 2.33; 1.75; and the mean number of gastric lesions was 0; 1.2 +/0 0.31; 2.83 +/0 0.82; 2.2 +/- 0.65, respectively. The differences were statistically significant. Our experiments show that Vivonex HN was more effective than Maalox or Cimetidine in high dose in preventing gastric bleeding and gastric mucosal lesions in the cold, restrained rat. Cimetidine in a standard dose was the least protective. Clinical trials are needed to establish the role of Vivonex HN in the prevention of stress ulcers in patients at risk.

  19. Evaluation of the Anti-ulcer Properties of the Aqueous Methanolic Leaf Extract of Palisota hirsuta and its Fractions in mice

    Directory of Open Access Journals (Sweden)

    Aruh O Anaga

    2013-06-01

    Full Text Available Objective: This study evaluated the effects of aqueous methanolic leaf extract of Palisota hirsuta (MLEPH, against experimentally induced gastric ulceration in mice. Materials and methods: The plant material was extracted with 70% methanol for 48h and concentrated in vacuo with rotary evaporator, yielding 8.77%w/w MLEPH. MLEPH (50, 100, 150 mg/kg and MLEPH fractions (MLEPHfr (50 mg/kg were studied in various ulcer models: acetyl salicylic acid (ASA, HCl-ethanol and cold restraint stress-induced ulcer models. Results: MLEPH at all doses used significantly reduced (P0.05 and gave a UPI of 33%. In cold restraint stress, MLEPH (50 and 100 mg/kg decreased both MNU and MUI. However this was not significant (P>0.05 compared with the control. Both doses produced UPI of 57% compared with cimetidine (95%. The MLEPHfr7 (50 mg/kg, significantly decreased (P<0.05 MNU compared with both distilled water and cimetidine and MUI compared with cimetidine in HCl-ethanol-induced gastric ulceration. The UPI for MLEPHfr7 was 58% compared with cimetidine. The phytochemical constituents of MLEPHfr7 include tannins and reducing sugars. Conclusion: Our study shows that MLEPH and MLEPHfr exhibited promising antiulcer properties, mediated by tannins and reducing sugars through cytoprotective mechanisms. [J Intercult Ethnopharmacol 2013; 2(3.000: 141-146

  20. Titanium dioxide nanofibers integrated stainless steel filter for photocatalytic degradation of pharmaceutical compounds

    Energy Technology Data Exchange (ETDEWEB)

    Ramasundaram, Subramaniyan; Yoo, Ha Na; Song, Kyung Guen; Lee, Jaesang [Center for Water Resource Cycle Research, Korea Institute of Science and Technology, Hwarangno 14-gil 5, Seongbuk-gu, Seoul 136-791 (Korea, Republic of); Choi, Kyoung Jin [School of Mechanical and Material Science Engineering, Ulsan National Institute of Science and Technology, Ulsan (Korea, Republic of); Hong, Seok Won, E-mail: swhong@kist.re.kr [Center for Water Resource Cycle Research, Korea Institute of Science and Technology, Hwarangno 14-gil 5, Seongbuk-gu, Seoul 136-791 (Korea, Republic of)

    2013-08-15

    Highlights: • A photocatalytic metal filter was fabricated with electrospun nanofibrous TiO{sub 2}. • PVDF layer effectively acted as a binder between TiO{sub 2} nanofibers and metal filter. • The photocatalytic efficacy of P-SSF was evaluated against pharmaceuticals. • The photocatalytic efficacy was highly dependent on water flux thru P-SSF. •Almost 90% of cimetidine was removed at a flux of 10 L/m{sup 2} h and 0.1–0.2 kPa TMP. -- Abstract: A photocatalytically active stainless steel filter (P-SSF) was prepared by integrating electrospun TiO{sub 2} nanofibers on SSF surface through a hot-press process where a poly(vinylidene fluoride) (PVDF) nanofibers interlayer acted as a binder. By quantifying the photocatalytic oxidation of cimetidine under ultraviolet radiation and assessing the stability of TiO{sub 2} nanofibers integrated on the P-SSF against sonication, the optimum thickness of the TiO{sub 2} and PVDF layer was found to be 29 and 42 μm, respectively. At 10 L/m{sup 2} h flux, 40–90% of cimetidine was oxidized when the thickness of TiO{sub 2} layer increased from 10 to 29 μm; however, no further increase of cimetidine oxidation was observed as its thickness increased to 84 μm, maybe due to limited light penetration. At flux conditions of 10, 20, and 50 L/m{sup 2} h, the oxidation efficiencies for cimetidine were found to be 89, 64, and 47%, respectively. This was attributed to reduced contact time of cimetidine within the TiO{sub 2} layer. Further, the degradation efficacy of cimetidine was stably maintained for 72 h at a flux of 10 L/m{sup 2} h and a trans-filter pressure of 0.1–0.2 kPa. Overall, our results showed that it can potentially be employed in the treatment of effluents containing organic micropollutants.

  1. Characterization of histamine receptors in isolated pig basilar artery by functional and radioligand binding studies

    International Nuclear Information System (INIS)

    Histamine receptors in pig basilar arteries were investigated in vitro by radioligand binding assays and by measuring the contractile and relaxant responses to histamine. Histamine and 2-pyridyethylamine (H1-agonist) induced concentration-dependent contractions, whereas impromidine (H2-agonist) induced concentration-dependent relaxations. These responses were independent of the presence of endothelial cells. Diphenhydramine (H1-antagonist) partially reversed the histamine-induced contractions to relaxations. Cimetidine (Hα2-antagonist) potentiated the contraction in a concentration-dependent manner. In the presence of cimetidine, the pEC50 value of histamine for the contraction was 6.30, and diphenhydramine competitively antagonized the histamine-induced contractions (pA2, 7.77). In the presence of diphenhydramine, the pEC50 value of histamine for the relaxation was 5.93, and cimetidine competitively antagonized the histamine-induced relaxations (pA2, 6.62). In the binding studies, the Kd value of [3H]mepyramine was 2.1 nM and the Bmax value was 95.6 fmol/mg protein. A competition experiment with diphenhydramine showed that the pKi value (7.51) was similar to the pA2 value. The Kd value for [3H]cimetidine was 126.0 nM and the Bmax value was 459.8 fmol/mg protein. The pKd (6.90) for [3H]cimetidine was similar to the pA2 for cimetidine. The Hill coefficients for these experiments were not significantly different from unity. The present findings indicate that the number of H1-receptors, in terms of the Bmax value for [3H]mepyramine, is smaller than that of H2-receptors, in terms of the Bmax value for [3H]cimetidine. However, the contractile response to histamine is predominantly mediated through stimulation of H1-receptors on vascular smooth muscle cells in pig basilar artery

  2. Titanium dioxide nanofibers integrated stainless steel filter for photocatalytic degradation of pharmaceutical compounds

    International Nuclear Information System (INIS)

    Highlights: • A photocatalytic metal filter was fabricated with electrospun nanofibrous TiO2. • PVDF layer effectively acted as a binder between TiO2 nanofibers and metal filter. • The photocatalytic efficacy of P-SSF was evaluated against pharmaceuticals. • The photocatalytic efficacy was highly dependent on water flux thru P-SSF. •Almost 90% of cimetidine was removed at a flux of 10 L/m2 h and 0.1–0.2 kPa TMP. -- Abstract: A photocatalytically active stainless steel filter (P-SSF) was prepared by integrating electrospun TiO2 nanofibers on SSF surface through a hot-press process where a poly(vinylidene fluoride) (PVDF) nanofibers interlayer acted as a binder. By quantifying the photocatalytic oxidation of cimetidine under ultraviolet radiation and assessing the stability of TiO2 nanofibers integrated on the P-SSF against sonication, the optimum thickness of the TiO2 and PVDF layer was found to be 29 and 42 μm, respectively. At 10 L/m2 h flux, 40–90% of cimetidine was oxidized when the thickness of TiO2 layer increased from 10 to 29 μm; however, no further increase of cimetidine oxidation was observed as its thickness increased to 84 μm, maybe due to limited light penetration. At flux conditions of 10, 20, and 50 L/m2 h, the oxidation efficiencies for cimetidine were found to be 89, 64, and 47%, respectively. This was attributed to reduced contact time of cimetidine within the TiO2 layer. Further, the degradation efficacy of cimetidine was stably maintained for 72 h at a flux of 10 L/m2 h and a trans-filter pressure of 0.1–0.2 kPa. Overall, our results showed that it can potentially be employed in the treatment of effluents containing organic micropollutants

  3. Effect of sialoadenectomy and synthetic human urogastrone on healing of chronic gastric ulcers in rats

    DEFF Research Database (Denmark)

    Poulsen, Steen Seier; Nexø, Ebba

    1986-01-01

    The effect of extirpation of the submandibular glands, an exocrine organ for epidermal growth factor/urogastrone (EGF/URO), and the effect of oral administration of synthetic human (EGF/URO) on healing of chronic gastric ulcers in rats has been investigated. Removal of the submandibular glands...... delayed healing of chronic gastric ulcers when examined after 50, 100, and 200 days. Oral administration of synthetic human EGF/URO stimulated gastric ulcer healing when examined after 25 and 50 days of treatment. The effect of synthetic human EGF/URO was comparable with that of cimetidine. The combined...... administration of synthetic human EGF/URO and cimetidine further increased healing of gastric ulcers compared with administration of each substance. Neither synthetic human EGF/URO, nor removal of the submandibular glands had any influence on gastric acid secretion. This study showed that the submandibular...

  4. Effect of antisecretory agents and vagotomy on healing of "chronic" cysteamine-induced duodenal ulcers in rats

    DEFF Research Database (Denmark)

    Poulsen, Steen Seier

    1986-01-01

    Penetrated cysteamine-induced duodenal ulcers in rats have a very prolonged course of healing. In this study, it was investigated how much the healing of these ulcers is accelerated by some treatments. The treatments included omeprazole, cimetidine, and truncal vagotomy. In addition, the effect...... of omeprazole and cimetidine on gastric acid secretion was investigated in chronic gastric fistula rats. After 25 days of treatment, significantly more rats in the treated groups had healed ulcers than in the control group. There was little further improvement up to 100 days of treatment, and the difference...... between treated and untreated groups decreased. The morphology of healing ulcers in treated and untreated rats was also compared. In controls, there was a simultaneous regeneration of mucosa and the submucosal Brunner's glands from the edges of the ulcer, the slow proliferation rate of the latter probably...

  5. Evaluation of H2 receptor antagonists in chronic idiopathic urticaria

    Directory of Open Access Journals (Sweden)

    Minocha Y

    1995-01-01

    Full Text Available H1-antagonist (hydroxyzine hydrochloride in dosage of 10 mg-25 mg thrice a day failed to elicit satisfactory response in 60 out of 170 patients of chronic idiopathic urticaria. Additional administration of H2-antagonist (cimetidine in dosage of 200 mg four times a day, in patients not responding earlier to H1-antagonist alones exhibited moderate to good improvement of various parameters of urticaria in approximately 85% patients

  6. Successful treatment of florid cutaneous warts with intravenous cidofovir in an 11-year-old girl.

    OpenAIRE

    IRVINE, ALAN

    2008-01-01

    Cutaneous warts, commonly seen in children and the immunosuppressed are socially distressing and are often resistant to traditional treatments. Here, we report an 11-year-old girl with bilateral florid verrucous lesions on her hands, feet and chin, which were refractory to a number of standard treatments including cryotherapy, cantharidin preparations, topical salicylic acid, surgical debulking techniques, oral Cimetidine, and topical and intralesional Cidofovir. As the disfiguring lesions ha...

  7. Prophylaxis of anaphylactoid reactions to a polypeptidal plasma substitute by H1- plus H2-receptor antagonists: synopsis of three randomized controlled trials

    OpenAIRE

    Schöning, B.; Lorenz, Wilfried; Doenicke, A.

    1982-01-01

    To demonstrate the efficacy of a premedication with H1- + H2-receptor antagonists against histamine-release responses in anaesthesia and surgery 3 randomized controlled trials were conducted in patients, volunteers and experimental animals (dogs). Cutaneous anaphylactoid reactions following infusion of polygeline (Haemaccel) in orthopedic patients were successfully abolished by premedication with 0.1 mg/kg dimethpyrindene (Fenistil) and 5 mg/kg cimetidine (Tagamet). Chlorpheniramine (Piriton)...

  8. Duodenal mucosal architecture in non-specific and ulcer-associated duodenitis.

    OpenAIRE

    M. Hasan; Sircus, W; Ferguson, A.

    1981-01-01

    This study was done to determine the severity and extent of abnormalities of duodenal mucosal architecture in non-specific (non-ulcerative) and ulcer-associated duodenitis. The effect of successful treatment with cimetidine on these changes has also been assessed. A method of microdissection and measurement of villus height, crypt depth, and mitotic figure count per crypt was applied to endoscopic biopsies from the duodenum. Five groups of patients were studied: untreated ulcer-associated duo...

  9. Renal accumulation of [{sup 111}In]DOTATOC in rats: influence of inhibitors of the organic ion transport and diuretics

    Energy Technology Data Exchange (ETDEWEB)

    Stahl, A.R. [Technische Universitaet Muenchen, Klinikum rechts der Isar, Department of Nuclear Medicine, Munich (Germany); Universitaetsklinikum Essen, Department of Radiology, Essen (Germany); Wagner, B.; Heemann, U.; Lutz, J. [Technische Universitaet Muenchen, Klinikum rechts der Isar, Department of Nephrology, Munich (Germany); Poethko, T.; Perutka, M.; Wester, H.J.; Essler, M.; Schwaiger, M. [Technische Universitaet Muenchen, Klinikum rechts der Isar, Department of Nuclear Medicine, Munich (Germany)

    2007-12-15

    Radiation exposure to the kidney limits therapy with radiometal labelled DOTATOC. This study evaluates the organic anion and cation transport (inhibitors: probenecid and cimetidine/dexamethason) as well as diuresis (furosemide and mannitol) regarding renal uptake of [{sup 111}In]DOTATOC. One hundred eight male Fisher rats were injected with [{sup 111}In]DOTATOC via the tail vein. Prior to activity injection a total of 84 rats underwent injection with probenecid vs. sodium chloride 0.9% (48 rats), cimetidine vs. dexamethasone vs. sodium chloride 0.9% (18 rats), and furosemide vs. mannitol vs. sodium chloride 0.9% (18 rats). Rats were sacrificed at predetermined time points up to 48 h after activity injection. Kidneys, adrenal glands, pancreas, spleen, blood, liver, and muscle were harvested and injected activity per gram tissue was determined. Autoradiographic images of the kidneys were acquired in a total of 24 rats. Probenecid led to a reduction in renal uptake by up to 30% while not significantly changing the activity accumulation in the other organs investigated. This reduction was attributable to the renal cortex (ratio cortex/medulla 1.72 vs. 1.99; p = 0.006). Cimetidine and dexamethasone had no effect in any of the organs. Furosemide led to a 44% increase in renal activity accumulation attributable to enhanced renal medullary uptake (ratio cortex/medulla 1.44 versus 1.69; p = 0.006). Mannitol had no effect on renal activity uptake. Inhibition of the organic anion transport by probenecid may help reduce renal uptake regarding therapy with radiometal labelled DOTATOC. The enhancing effect of furosemide may be unfavourable for therapy. The results must be confirmed by human studies. (orig.)

  10. Evaluation of the acute toxicity, phytochemical constituents and anti - ulcer properties of methanolic leaf extract of Annona muricata in mice

    Directory of Open Access Journals (Sweden)

    Valentine Uneojo Omoja

    2014-02-01

    Full Text Available This study investigated the acute toxicity, phytochemical constituents and anti - ulcer properties of methanolic leaf extract of Annona muricata in mice. The anti - ulcer activity was evaluated using absolute ethanol-induced ulcer and aspirin-induced ulcer models in mice. An LD50 of 354.8 +/- 8 mg/kg body weight, bw of the extract was obtained on oral administration. Investigation of the phytochemical constituents of the plant extract revealed the presence of saponins, alkaloids and traces of tannins. All doses of the extract (50, 75 and 100 mg/kg used for the study significantly reduced (p<0.05 the mean number of ulcers in both ulcer models when compared to the untreated group A (10 ml/kg distil water. Optimum antiulcer activity of the extract against absolute ethanol-induced ulcer was noted at 50 mg/kg bw. At this 50 mg/kg, the mean number of ulcers and mean ulcer index of the extract was significantly lower (p<0.05 than that of Cimetidine at 100 mg/kg (3.60 +/- 0.51: 5.00 +/- 0.32; 1.5+/-0.05: 0.98+/-0.03, the treated control group whereas the protective index of the extract was higher than that of cimetidine (50.51 %: 24.24 %. The results obtained from this study strongly suggest that methanolic leaf extract of Annona muricata can be effectively used for the treatment of ulcer in low doses and can provide better therapeutic effect than cimetidine if used in ulcers caused by alcoholism and related agents. [J Intercult Ethnopharmacol 2014; 3(1.000: 37-43

  11. Evaluation of the transporter-mediated herb-drug interaction potential of DA-9801, a standardized dioscorea extract for diabetic neuropathy, in human in vitro and rat in vivo

    Science.gov (United States)

    2014-01-01

    Background Drug transporters play important roles in the absorption, distribution, and elimination of drugs and thereby, modulate drug efficacy and toxicity. With a growing use of poly pharmacy, concurrent administration of herbal extracts that modulate transporter activities with drugs can cause serious adverse reactions. Therefore, prediction and evaluation of drug-drug interaction potential is important in the clinic and in the drug development process. DA-9801, comprising a mixed extract of Dioscoreae rhizoma and Dioscorea nipponica Makino, is a new standardized extract currently being evaluated for diabetic peripheral neuropathy in a phase II clinical study. Method The inhibitory effects of DA-9801 on the transport functions of organic cation transporter (OCT)1, OCT2, organic anion transporter (OAT)1, OAT3, organic anion transporting polypeptide (OATP)1B1, OATP1B3, P-glycoprotein (P-gp), and breast cancer resistance protein (BCRP) were investigated in HEK293 or LLC-PK1 cells. The effects of DA-9801 on the pharmacokinetics of relevant substrate drugs of these transporters were also examined in vivo in rats. Results DA-9801 inhibited the in vitro transport activities of OCT1, OCT2, OAT3, and OATP1B1, with IC50 values of 106, 174, 48.1, and 273 μg/mL, respectively, while the other transporters were not inhibited by 300 μg/mL DA-9801. To investigate whether this inhibitory effect of DA-9801 on OCT1, OCT2, and OAT3 could change the pharmacokinetics of their substrates in vivo, we measured the pharmacokinetics of cimetidine, a substrate for OCT1, OCT2, and OAT3, and of furosemide, a substrate for OAT1 and OAT3, by co-administration of DA-9801 at a single oral dose of 1,000 mg/kg. Pre-dose of DA-9801 5 min or 2 h prior to cimetidine administration decreased the Cmax of cimetidine in rats. However, DA-9801 did not affect the elimination parameters such as half-life, clearance, or amount excreted in the urine, suggesting that it did not inhibit elimination

  12. The effect of intravenous omeprazole on the gastric and duodenal potential difference and pH in healthy subjects

    DEFF Research Database (Denmark)

    Rubinstein, E; Højgaard, L

    1993-01-01

    The effect of intravenous omeprazole (40 and 80 mg) on the gastric and duodenal potential difference (PD) and pH was investigated in 9 healthy volunteers. Gastric PD and pH increased significantly (p ... found in duodenal PD or pH. It has been claimed that gastric PD changes following acid secretion inhibition with cimetidine and glucagon might be due to changes in the parietal cell surface area. Omeprazole causes no changes in the parietal cell structure, and the changes in gastric PD following...

  13. Longitudinal study of influence of Helicobacter pylori on current risk of duodenal ulcer relapse. The Hvidovre Ulcer Project Group

    DEFF Research Database (Denmark)

    Clausen, M R; Franzmann, M B; Holst, C;

    1992-01-01

    Seventy-four patients with duodenal ulcer were followed up longitudinally for 2 years after initial ulcer healing. Endoscopy including biopsy of the antral mucosa was performed every 3rd month and whenever clinical symptoms of relapse occurred. The presence of Helicobacter pylori in the biopsy...... acid output, time of healing of the preceding ulcer, treatment of the present ulcer (cimetidine, antacids, or no treatment), or type and degree of gastritis. Thus, although H. pylori is prevalent in patients with duodenal ulcer disease, the present study indicates that H. pylori does not have a...... substantial note in the precipitation of active duodenal ulcer....

  14. Choledochoscope manometry about different drugs on the Sphincter of Oddi

    Institute of Scientific and Technical Information of China (English)

    Jing Kong; Shuo-Dong Wu; Xiao-Bo Zhang; Zhen-Sheng Li; Gang Shi; Wei Wang; Jun-Zhi Chen

    2008-01-01

    AIM: To assess the effects of H2-receptor blocking pharmacon, protease inhibitor, and gastro kinetic agents on the human Sphincter of Oddi (SO) motility by choledochoscope manometry.METHODS: One hundred and seventy-five patients with T tube installed after cholecystectomy and choledochotomy were assessed by choledochoscope manometry. They were randomly assigned into groups of H2-receptor blocking pharmacon, protease inhibitor, and gastro kinetic agents. The Sphincter of Oddi basal pressure (SOBP), amplitude (SOCA), frequency of contractions (SOF), duodenal pressure (DP), and common bile duct pressure (CBDP) were scored and analyzed.RESULTS: SOBP and SOCA were significantly decreased after Cimetidine administration, and no statistical difference was seen in the Famotidine group. In the Gabexate mesilate group, SOBP had decreased significantly. In the Ulinastatin group, SOCA decreased when Ulinastatin was given at the rate of 2500 U/min; when Ulinastatin administration was raised to 5000 U/ min, SOBP, SOF and SOCA all experienced a fall. SOBP and SOCA for Domperidone and SOCA for Mosapride groups all decreased distinctly after administration.CONCLUSION: The regular dosage of Cimetidine showed an inhibitory effect on the motility of SO, while Pamotidine had no obvious effects otherwise. Gabnexata mesilate, Ulinastatin and gastro kinetic agents also showed inhibitory effects on the SO motility.

  15. Influence of the histaminergic system on opiate-induced neurosecretion and behaviour.

    Science.gov (United States)

    Duka, T; Hoehe, M; Doenicke, A; Stephan, U; Matussek, N

    1987-01-01

    The influence of the histaminergic system on fentanyl (Fe)-induced growth hormone (GH) and prolactin (PRL) release as well as on Fe-induced increase of noradrenaline (NA) plasma levels has been studied in male volunteers. These volunteers received, according to a randomized block design, different pretreatments: the H1-antagonist dimethindene (Di) (0.1 mg/kg i.v.), or the H2-antagonist cimetidine (Ci)(5 mg/kg i.v.), or a combination of dimethindene and cimetidine (Di + Ci), or saline. The PRL increase caused by Fe (0.2 mg/70 kg) was not altered by pretreatment with the H1-antagonist Di, the H2-antagonist Ci, or the combination of both. The increase of NA plasma levels after Fe also was not modified by the histamine antagonists. In contrast, the maximum GH increase after Fe was blunted by the combination of Ci and Di, but not by either Ci or Di alone. These results suggest an involvement of the histaminergic system in opiate-induced GH-release.

  16. Bar-code technology applied to drug-use evaluation.

    Science.gov (United States)

    Zarowitz, B J; Petitta, A; Mlynarek, M; Touchette, M; Peters, M; Long, P; Patel, R

    1993-05-01

    Bar-code technology was used to determine: (1) patterns in histamine H2-receptor antagonist use and (2) the occurrence of adverse drug effects and drug interactions associated with the use of these agents in critically ill patients. Patients at Henry Ford Hospital (Detroit) receiving histamine H2-receptor antagonists over a two-month period were evaluated. Clinical information was collected in the intensive care units by using a bar-code system. The data-capture menu was based on drug-use-evaluation criteria for H2-receptor antagonists. Data collected in the scanning wands were uploaded into a computer database and were analyzed at the end of the study. Data were collected for 207 patients. Cimetidine was the predominant H2-receptor antagonist used, and the predominant indication was stress-ulcer prophylaxis. Dosing trends followed accepted guidelines for cimetidine dosage adjustment in renal and hepatic failure. Two drug interactions and six adverse drug reactions occurred. Pharmacists made 92 recommendations to the medical staff regarding modification in therapy, involving 32% of the patients. Data collection required an average of 10 minutes per day each for three pharmacists. H2-receptor antagonist use patterns were evaluated in intensive care units through the application of bar-code technology. The speed and efficiency of this automated tool facilitated collection of a large amount of data. PMID:8099468

  17. Thioperamide treats neonatal hypoxic-ischemic encephalopathy by postsynaptic H1 receptors*

    Institute of Scientific and Technical Information of China (English)

    Feiyong Jia; Lin Du; Yunpeng Hao; Shicheng Liu; Ning Li; Huiyi Jiang

    2013-01-01

    Thioperamide, a selective histamine H3 receptor antagonist, can increase histamine content in the brain, improve brain edema, and exert a neuroprotective effect. This study aimed to examine the mechanism of action of thioperamide during brain edema in a rat model of neonatal hypoxic- is-chemic encephalopathy. Our results showed that thioperamide significantly decreased brain water content and malondialdehyde levels, while significantly increased histamine levels and superoxide dismutase activity in the hippocampus. This evidence demonstrates that thioperamide could pre-vent oxidative damage and attenuate brain edema fol owing neonatal hypoxic-ischemic encepha-lopathy. We further observed that changes in the above indexes occurred after combined treatment of thioperamide with the H1 receptor antagonist, pyrilamine, and the H2 receptor antagonist, ci-metidine. Experimental findings indicated that pyrilamine reversed the effects of thioperamide;however, cimetidine had no significant influence on the effects of thioperamide. Our present findings suggest that thioperamide can increase brain histamine content and attenuate brain edema and oxidative damage by acting in combination with postsynaptic H1 receptors in a rat model of neo-natal hypoxic-ischemic encephalopathy.

  18. Neural histamine in the tuberomammillary nucleus regulates the onset of neurogenic pulmonary edema in rabbits

    Institute of Scientific and Technical Information of China (English)

    Rong Dong; Xiaohong Zhang; Lijuan Shi

    2009-01-01

    Objective:To explore the effect of neural histamine in the tuberomammillary nucleus(TM) on neurogenic pulmonary edema (NPE) onset in rabbits and the function of the rostral ventrolateral medulla(RVLM) in the neural histamine modulation of NPE.Methods:NPE was produced by the intracisternal injections of fibrinogen and thrombin.The contents of histamine in the TM and RVLM in rabbits were measured with high performance liquid chromatography(HPLC).Rabbits were placed on a stereotaxic frame and microinjection cannulae were inserted into the TM and RVLM using brain atlas coordinates.Animals were pretreated with R-α-methylhistamine(MeHA) in the TM and chlorphenamine Mmaleate/cimetidine in the RVLM prior to establishing the NPE model.Changes in the lung water ratio and mean arterial pressure(MAP) were recorded,and paraffin sections of lung tissue were observed by light microscope.Results:We found that the contents of histamine(HA) in the TM and RVLM increased significantly with the onset of NPE.Pretreatment with MeHA in the TM and chlorphenamine Mmaleate in the RVLM significantly decreased MAP,and the lung water ratio and histological characteristics of the NPE in the rabbit model.Pretreatment with cimetidine in the RVLM had no effect on NPE.Conculsion:The results suggest that neural histamine in the TM is involved in the onset of NPE,and this effect of neural histamine is mediated by H receptor in the RVLM.

  19. Pentadecapeptide BPC 157 and anaphylactoid reaction in rats and mice after intravenous dextran and white egg administration.

    Science.gov (United States)

    Duplancic, Bozidar; Stambolija, Vasilije; Holjevac, Jadranka; Zemba, Mladen; Balenovic, Igor; Drmic, Domagoj; Suran, Jelena; Radic, Bozo; Filipovic, Marinko; Blagaic, Alenka Boban; Brcic, Luka; Kolenc, Danijela; Grabarevic, Zeljko; Seiwerth, Sven; Sikiric, Predrag

    2014-03-15

    Anesthetized mice or rats received intravenously 6%, 10%, 20%, 40%, 60%, 80%, and 90% dextran and/or white egg (1ml/rat or 0.15ml/mouse) into their tails. Medication (/kg b.w., 5ml/kg) was given intraperitoneally (BPC 157 10µg, 1µg, 10ng, and 10pg/kg, chloropyramine 20mg/kg, and cimetidine 10mg/kg intraperitoneally, alone or in combination while controls received an equivolume of saline), immediately after challenge or, alternatively, at 5min after or 24 or 48h before challenge. The effect was assessed at 5, 10, 20 and 30min after dextran and/or white egg challenge. We commonly noted prominent edema involving the face, upper and lower lip, snout, paws and scrotum (presented with extreme cyanosis), poor respiration and the number of fatalities after dextran and/or white egg application. Contrary, BPC 157 regimens (10µg, 1µg, 10ng, and 10pg/kg) effectively, may both prevent anaphylactoid reactions that may arise from dextran and/or white egg application and furthermore, rescue already advanced reactions when given after the challenge. Chloropyramine and cimetidine given alone were only moderately effective. When given together with BPC 157, the observed effect correlates with the strong effect of BPC 157 given alone. PMID:24486708

  20. Delayed phase of hematoporphyrin-induced phototoxicity: modulation by complement, leukocytes, and antihistamines

    Energy Technology Data Exchange (ETDEWEB)

    Lim, H.W.; Young, L.; Hagan, M.; Gigli, I.

    1985-02-01

    The role of complement, leukocytes, and histamine was investigated in the delayed phase of hematoporphyrin-induced phototoxicity in guinea pigs. The phototoxic response was quantified by the accumulation of intravenously injected (/sup 125/I)bovine serum albumin in the skin. There was a greater than 6-fold increase in the vascular response at the completion of irradiation, which subsided partially to reach a plateau of twice the preirradiation level between 0.5 h and 12 h. At 18 h, the vascular responsiveness returned to the baseline value. The 7 h timepoint was selected in this study to evaluate the modulation of the delayed phase. In complement-depleted guinea pigs, as well as in leukopenic animals, the enhancement in the vascular response was significantly suppressed (p vs control, less than 0.0001 and 0.0022, respectively). Cimetidine, when administered prior to irradiation, significantly suppressed the phototoxic response (p vs control, 0.0365). The combination of diphenhydramine and cimetidine, administered 6 h after the induction of phototoxicity, also suppressed the vascular response (p vs control, less than 0.0001). These data indicate that the expression of the delayed phase of hematoporphyrin-induced phototoxicity, similar to the early phase, requires the presence of an intact complement system, leukocytes, and histamine.

  1. Evaluation of domperidone as a modifier of gamma-radiation-induced emesis. Report for January 1984-January 1986

    Energy Technology Data Exchange (ETDEWEB)

    Cordts, R.E.; Yochmowitz, M.G.; Hardy, K.A.

    1987-09-01

    The D2 antidopaminergic drug Domperidone was evaluated singly and in combination with synthetic adrenocorticoid and an H2 antihistamine for its ability to reduce the acute emetic effects of /sup 60/Co whole-body radiation. Random-source adult male dogs were fasted 12 hours, fed a standard meal, injected 44 minutes later and irradiated 47 minutes after that. Four groups of dogs were radiated after drug injections as follows: saline (Con), domperidone (Dom), cimetidine + thiethylperazine (Cim+Thi), and dexamethasone + domperidone + cimetidine (Dex+Dom+Cim). Drug quantities for dogs represented 10 mg Dom, 10 mg Thi, 20 mg Dex, and 300 mg Cim for an average human (70 ka, 1.8 m2). Subjects were exposed on an up-down schedule to determine the radiation necessary to produce vomiting in 50% (ED50) of each group. Emesis onset times, offset times, and number of episodes were recorded. The ED50 of Dex+Dom+Cim was higher than Con. Dom produced more emetic episodes than Con or Dex+Dom+Cim. This drug in combination with an adrenocorticoid and antihistamine significantly raised the emetic threshold while maintaining episodes at a low incidence.

  2. Postmarketing drug surveillance by record linkage in Tayside.

    Science.gov (United States)

    Crombie, I K; Brown, S V; Hamley, J G

    1984-09-01

    The feasibility of conducting postmarketing drug surveillance by record linkage in Tayside was assessed. The key feature of the method is that all hospital discharge data are already computerised by the area health board and may be accessed through the unique community health number (CHNo) which has been allocated to all Tayside residents. The 12 861 prescriptions for cimetidine dispensed in Tayside over a nine month period were collected and the CHNo identified for 76%. These corresponded to 3802 individuals and their discharge data, together with those for an equal number of controls matched by age, sex, and general practitioner were retrieved from the computer. The expected excess of those diseases for which cimetidine is prescribed (peptic ulcer and oesophagitis) was observed. Other drug-disease associations were observed but may have been due to confounding and emphasise the inadequacy of community based controls. The major advantages of record linkage are, firstly, the low cost of the method, the present study costing just over pounds 12 000, and, secondly, the duration of patient follow up which may may be extended for as many years as required simply by rerunning the computer programs. To assemble large patient cohorts the study would have to be extended to other area health boards that are currently developing similar computer systems. Record linkage may provide a cost effective method for the follow up of patients to identify serious adverse drug reactions, particularly those that take several years to develop.

  3. Effect of Two Histamine Receptor Antagonists on Hematology of Porcine Reproductive and Respiratory Syndrome%组胺受体拮抗剂对高致病性猪蓝耳病血液学的影响

    Institute of Scientific and Technical Information of China (English)

    刘芳; 高登慧; 欧德渊; 万文华; 向智龙; 禾采红; 黄露

    2011-01-01

    为探索组胺(HA)受体拮抗剂对高致病性蓝耳病(PRRS)病毒感染患猪血液学的影响,揭示内源性组胺在高致病性猪蓝耳病发生发展过程中的部分作用,通过人工使仔猪感染高致病性蓝耳病,并相应注射扑尔敏、西咪替丁后第5天采用RT-PCR方法检测仔猪血液中的PRRSV,第7天采用ETDA抗凝管颈静脉采血,全自动血液分析仪测定血液指标.结果表明,1)攻毒后第5天均扩出1条约1064 bp的特异性目的条带,表明攻毒成功;2)西咪替丁组、阳性组仔猪血液中白细胞总数、淋巴细胞数量、单核细胞数量极显著低于阴性组(P<0.01),而扑尔敏组均显著高于阳性组(P<0.05);3)阳性组仔猪血液中血红蛋白浓度、红细胞压积显著低于阴性组(P<0.05),西咪替丁组红细胞数显著高于阳性组;4)扑尔敏组、西咪替丁组仔猪血液中血小板含量、血小板压积极显著高于阴性组(P<0.0l),阳性组血小板含量极显著高于阴性组(P<0.01),阳性组血小板压积显著高于阴性组(P<0.05).说明,扑尔敏能抑制高致病性蓝耳病患猪血液中白细胞总数、白细胞中淋巴细胞数量和白细胞中单核细胞数量的下降,稳定红细胞相关指标的数量,具有增强机体免疫力的作用,但促进了血小板的升高,西咪替丁能维持高致病性蓝耳病患猪血液中红细胞相关指标的稳定.%The piglets artificially infected with porcine reproductive and respiratory syndrome were injected with two histamine receptor antagonists (Cimetidine and Chlorpheniramine) and then PRRSV in tested piglets was detected by RT-PCR after 5d and the blood indexes were determined by an automatic blood analyzer after 7 d to study the effect of histamine receptor antagonist on hematology of porcine reproductive and respiratory syndrome and to reveal the part effect of endogenous histamine on occurrence and development of porcine reproductive and respiratory syndrome. The

  4. H1 + H2-receptor antagonists for premedication in anaesthesia and surgery: a critical view based on randomized clinical trials with Haemaccel and various antiallergic drugs.

    Science.gov (United States)

    Lorenz, W; Doenicke, A; Schöning, B; Mamorski, J; Weber, D; Hinterlang, E; Schwarz, B; Neugebauer, E

    1980-04-01

    Histamine release by drugs used in anaesthesia and surgery has been often demonstrated in human volunteers, but only occassionally in patients. Three questions arose from these studies. (1) Is the incidence of histamine release high in patients during routine anaesthesia and surgery? (2) Can the clinical effects of histamine release in man be prevented by H1 + H2-receptor antagonists? (3) Are there any side-effects of such a premedication? These problems were investigated in patients and volunteers by randomized controlled clinical trials using only one of the histamine-liberating drugs in man, the plasma substitute Haemaccel. This drug was chosen because it causes a reproducible histamine release in man and because its mechanism of action in man is largely known. (1) Out of 600 orthopaedic patients 30 (5%) showed anaphylactoid reactions following Haemaccel infusion. 26 of these had a histamine release of more than 1 ng histamine/ml plasma. Using predictive values this gives an efficiency of the test by nearly 98%. (2) In volunteers the combination of an H1-plus H2-receptor antagonist (dimethypyrindene and cimetidine) completely prevented the clinical effects of histamine release by Haemaccel (9 allergoid and anaphylactoid reactions in the control group, none in the H1 + H2-group). The incidence of histamine release, however, remained unchanged. (3) The premedication was found to release histamine itself. Cimetidine was effective when given alone but especially in combination with chlorpheniramine (4 events out of 7 applications). The clinical side-effects of these premedication were mild since apparently the free histamine was largely blocked at the receptor sites. It is concluded that premedication with a combination of H1- and H2-receptor antagonists is indicated due to the high incidence of histamine release during anaesthesia and surgery induced by various drugs and treatments. Such premedication is effective but associated with mild side-effects. For this

  5. In vitro and in vivo invasiveness of different pulsed-field get electrophoresis types of Listeria monocytogenes

    DEFF Research Database (Denmark)

    Larsen, Charlotte Nexmann; Nørrung, Birgit; Sommer, Helle Mølgaard;

    2002-01-01

    The virulence of different pulsed-field gel electrophoresis (PFGE) types of Listeria monocytogenes was examined by monitoring their ability to invade Caco-2 cells. Strains belonging to seven different PFGE types originating from both foods and humans were included. No significant differences in...... virulent than others is supported by this study showing that certain PFGE types of L. monocytogenes commonly found in food are less invasive than others to Caco-2 cells. In contrast to the differences in invasion, identical intracellular growth rates between the different PFGE types were observed. In vivo...... studies of the actual ability of the strains to invade the liver and spleen of cimetidine-treated rats following an oral dose of 109 L. monocytogenes cells were performed for isolates of PFGE types 1, 2, 5, and 15. After 2 days, equal amounts of bacteria were observed in the liver and spleen of the rats...

  6. Signs of sympathetic denervation associated with a thoracic melanoma in a horse.

    Science.gov (United States)

    Murray, M J; Cavey, D M; Feldman, B F; Trostle, S S; White, N A

    1997-01-01

    Sympathetic denervation in a 20-year-old, gray, Thoroughbred-Percheron gelding was manifested by cutaneous hyperthermia and sweating over the right side of the body, demarcated by a line from the withers to the elbow and extending cranially. There was cutaneous hyperthermia over the right side of the head, but other signs of Horner's syndrome (sweating, ptosis, miosis, enophthalmos) were not present. The pattern of cutaneous hyperthermia and sweating was consistent with sympathetic denervation localized to the cervicothoracic ganglion, and thoracic radiographs revealed increased density in the craniodorsal thorax. Cytologic evaluation of a sample of pleural effusion revealed mesothelial cells containing melanin and cells suggestive of melanocytes or melanoblasts. Treatment with oral cimetidine and intrapleural cisplatin was not successful. A necropsy was not performed, but the clinical findings supported a diagnosis of thoracic melanoma involving the cervicothoracic ganglion. PMID:9298473

  7. High-frequency oscillation in the hippocampus of the behaving rat and its modulation by the histaminergic system.

    Science.gov (United States)

    Knoche, A; Yokoyama, H; Ponomarenko, A; Frisch, C; Huston, J; Haas, H L

    2003-01-01

    The histaminergic neurons located in the posterior hypothalamus modulate whole brain activity in a manner dependent on behavioral state. We have investigated their influence on high-frequency oscillation (200-Hz ripples) in the hippocampal CA1 region of freely moving rats. The occurrence of these ripples, assumed to be involved in memory trace formation, was markedly enhanced after injection of the H1-antagonists pyrilamine and ketotifen in a lateral ventricle, indicating a tonic activity of the histaminergic system. The H2- and H3-antagonists cimetidine and thioperamide were ineffective. We suggest a mediation of these effects through blocking the known histaminergic excitation of septal neurons. Histamine administered by the intracerebroventricular route had an inhibitory action on ripples. H1-receptor activation, which has been shown to inhibit learning and memory, thus shifts hippocampal activity away from high-frequency oscillation toward theta activity.

  8. Effect of restraint stress on nociceptive responses in rats: role of the histaminergic system.

    Science.gov (United States)

    Ibironke, G F; Mordi, N E

    2011-12-20

    Stress induced analgesia (SIA) is well known, but the reverse phenomenon, hyperalgesia is poorly documented. This study investigated the role of the histaminergic system in restraint stress hyperalgesia in rats, using thermal stimulation method (hot plate and tail flick tests). Paw licking and tail withdrawal latencies were taken before and after restraint for about one hour. Significant decreases (p<0.05) were obtained in these latencies after the restraint in both tests. Administration of H1 and H2 receptor blockers, chlorpheniramine and cimetidine respectively 30 mins before the restraint still resulted in significant reductions (p<0.05) in these latencies, connoting the persistence of hyperalgesia, showing that histamine H1 and H2 receptors did not participate in the mechanism of restraint stress hyperalgesia. We therefore suggest a histaminergic independent mechanism for restraint stress induced hyperalgesia.

  9. IS PEPTIC ULCER WITH HELICOBACTER INFEC¬TION THE CAUSE OF CHRONIC URTICARIA?

    Directory of Open Access Journals (Sweden)

    A. Farhoudi

    2000-01-01

    Full Text Available Helicobacter pylori, the most important cause of gastritis and peptic ulcer, has recently been associated with several extradigestive diseases. The aim of this study was to assess the prevalence of Helicobacter pylori infection and effects of bacterium eradication in 50 patients affected by idiopathic chronic urticaria. Helicobacter pylori was assessed by serology or biopsy and urease test or 13C urea breath test. Amoxicillin, bismuth subcitrate (Denol, metronidazole and cimetidine were given to infected patients for 2 weeks. The results of therapy were assessed by urea breath test six weeks after therapy. In response to treatment urticaria clinically regressed in 16 out of 24 patients (66.6%. Thus bacterium eradication was associated with a remission of urticaria symptoms, suggesting a possible role in the pathogenesis of this disorder.

  10. Efficacy and safety of herbal medicines in treating gastric ulcer: a review.

    Science.gov (United States)

    Bi, Wei-Ping; Man, Hui-Bin; Man, Mao-Qiang

    2014-12-01

    Gastric ulcer is a common disorder of the digestive system. Current therapeutic regimens largely rely on Western medicine. However, numerous studies have demonstrated that herbal medicines can effectively treat gastric ulcer in humans and various animal models via divergent mechanisms. This review updates the efficacy and safety of herbal medicines in treating gastric ulcer, and the mechanisms of their action in humans and animal models. Studies have demonstrated that the efficacy of herbal medicines is comparable or superior to that of drugs such as omeprazole or cimetidine in humans and animal models, and herbal medicines display fewer adverse effects. The mechanisms by which herbal medicines benefit gastric ulcer include stimulation of mucous cell proliferation, anti-oxidation, and inhibition of gastric acid secretion and H(+)/K(+)-ATPase activity. Some herbal medicines also exhibit antimicrobial properties. Utilization of herbal medicines could be a valuable alternative to treat gastric ulcer in humans effectively, with few adverse effects.

  11. Heterotopic mesenteric ossification after a ruptured abdominal aortic aneurism: case report with a review of literatures.

    Science.gov (United States)

    Honjo, Hiroaki; Kumagai, Youichi; Ishiguro, Toru; Imaizumi, Hideko; Ono, Tomojiro; Suzuki, Okihide; Ito, Tetsuya; Haga, Norihiro; Kuwabara, Kohki; Sobajima, Jun; Kumamoto, Kensuke; Ishibashi, Keiichiro; Baba, Hiroyuki; Sato, Osamu; Ishida, Hideyuki; Kuwano, Hiroyuki

    2014-01-01

    Heterotopic mesenteric ossification (HMO) is a rare disease that results in intra-abdominal ossification of unknown origin. An 88-year-old man developed an intestinal obstruction 2 weeks after undergoing an operation for a ruptured abdominal aortic aneurysm, resulting in intestinal obstructions those did not improved concervatively. During relaparotomy performed 30 days after the first operation, hard adhesions of the small intestine and mesentery were found; these adhesions were difficult to separate without damaging the serosa of the small intestine. We removed 240 cm of the small intestine and performed a jejuno-ileo anastomosis. Microscopically, trabecular bone tissue had increased irregularly in the fat tissue of the nodules with fibrosis, which were partially lined with osteoblasts. Accordingly, we histopathologically diagnosed the patient as having HMO. The patient was treated with NSAIDs and cimetidine to prevent the recurrence of HMO. No signs of recurrence have occurred as of one year after the second operation. PMID:25058788

  12. Specific cerebral heat shock proteins and histamine receptor cross-talking mechanisms promote distinct lead-dependent neurotoxic responses in teleosts

    International Nuclear Information System (INIS)

    Recent interests are beginning to be directed towards toxic neurobiological dysfunctions caused by lead (Pb) in aquatic vertebrates. In the present work, treatment with a maximum acceptable toxic concentration of this heavy metal was responsible for highly significant (p 2R) antagonist cimetidine (Cim), as shown by the very robust (p 3R) thioperamide (Thio), instead, blocked Pb-dependent up-regulatory trends of both chaperones in mostly hypothalamic areas. Moreover, intense neuronal damages of the above brain regions coincided with altered expressions of HSP70 and HSP90 when treated only with Cim. Overall these first results show that distinct HnR are able to exert a net neuroprotective role arising from their interaction with chaperones in fish exposed to Pb-dependent stressful conditions making this a potentially key interaction especially for T. pavo, aquatic species which plays an important ecological role towards the survival of other commercially vital fishes

  13. PFAPA (Periodic fever, aphtous stomatitis, pharingitis, cervical adenitis or Marshall’s syndrome in children

    Directory of Open Access Journals (Sweden)

    N N Kuzmina

    2005-01-01

    Full Text Available PFAPA (periodic fever, aphtous stomatitis, pharingitis, cervical adenitis or Marshall’s syndrome is one of the rare periodic fever conditions appearing in children. Its cause is unknown. This syndrome may continue for several years. During interictal period the child is quite well, grows and develops normally. The disease should be differentiated from Behcet’s disease, cyclic neutropenia, familial Mediterranean fever, familial Ireland fever, hyperimmunoglobulinemia D syndrome, systemic juvenile idiopathic arthritis, chronic tonsillitis, some infectious diseases. Many drugs are used for the treatment of PFAPA syndrome: antibiotics, non-steroidal anti-inflammatory drugs, chloroquin, antiviral drugs, glucocorticoids, cimetidin. Tonsillectomy is used quite often. Analysis of the literature data shows that best results may be achieved with tonsillectomy (sometimes in combination with ade- notomy. PFAPA in a child of 2 years age diagnosed for the first time in Russian pediatric rheumatology is described.

  14. Semitransparent peroral small bowel imaging

    Energy Technology Data Exchange (ETDEWEB)

    Emons, D.

    1981-10-01

    171 follow-through examinations of the small bowel performed in children and adolescents with a large contrast medium meal and the high voltage-low density barium technique (10 to 25 g BaSO/sub 4//100 ml, depending on age), are described. A ready made suspension, diluted with water, proved unsatisfactory. Coating properties and stability of the diluted, weak suspension were then greatly improved by hydroxyethylcellulose as a thickening agent and in addition by premedication of the patient with cimetidine. Pure cellulose solution instead of the last portion of barium prevented thickening in the ileum. The procedure has the well known advantages of a large contrast medium meal without the problem of overly dense superpositions.

  15. Equine gastric ulcer syndrome (egus: diagnosis and therapy

    Directory of Open Access Journals (Sweden)

    Mot, T.,

    2008-06-01

    Full Text Available Equine gastric ulcer syndrome is especially reported in racing horses, with a prevalence of 60-90% in adults and 25-50% in foals. The ethiology of equine gastric ulcer is polifactorial, represented by nutritional factors, stress generated by training and captivity, drugs (corticosteroids-prednisolone, dexametasone, nesteroidicanti-inflammatory drugs: flumixin-meglumine, fenilbutazone, duodenal refluence. The diagnosis is established on clinical signs and therapeutic response and it is confirmed by endoscopic exam. Therapeutically it is recommended to administer: antiacide (aluminiu hydroxide, magnesium hydroxide, inhibitors of H2 receptors(cimetidine, ranitidine, famotidine, inhibitors of protons pump (Omeprazol, Sucralphate. Diagnosis and therapeutic aspects in equine gastric ulcer syndrome are presented in this study.

  16. Effect of antihistamines, disodium cromoglycate (DSCG) or methysergide on post-irradiation cerebral blood flow and mean systemic arterial blood pressure in primates after 25 Gy, whole-body, gamma irradiation

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Forcino, C.D. [Armed Forces Radiobiology Research Inst., Bethesda, MD (United States)

    1995-06-01

    Exposure to ionizing radiation causes hypotension, cerebral ischemia and release of histamine (HA) and serotonin (5-HT). To investigate the relationship among these responses, rhesus monkeys (Macaca mulatta) received physiological saline (i.v.), disodium cromoglycate (DSCG), antihistamines (AH, mepyramine and cimetidine), or methysergide (METH), then were given 25 Gy whole-body irradiation. Monkeys receiving DSCG, AH or METH had higher post-irradiation mean arterial blood pressure (MBP) than saline-treated controls. Compared to levels in controls, post-irradiation hippocampal blood flow (rCBF) levels were higher in monkeys receiving DSCG, AH or METH. Treatment with the 5-HT{sub 2} receptor antagonist methysergide was the most effective in maintaining both rCBF and MBP after irradiation. Results support the hypothesis that the irradiation-induced cerebral ischemia and, to some extent, the hypotension is mediated by serotonin through 5-HT{sub 2} receptor sites. (author) 72 refs.

  17. Complete inhibition of food-stimulated gastric acid secretion by combined application of pirenzepine and ranitidine.

    Science.gov (United States)

    Londong, W; Londong, V; Ruthe, C; Weizert, P

    1981-07-01

    In a double-blind, placebo controlled and randomised secretory study the effectiveness of pirenzepine, ranitidine, and their combination was compared intraindividually in eight healthy subjects receiving intravenous bolus injections. Pirenzepine (0.15 mg/kg) plus ranitidine (0.6 mg/kg) suppressed peptone-stimulated gastric acid secretion from 69 +/- 11 to 2 +/- 0.4 mmol H+/3 h; the mean percentage inhibition was 97%. Postprandial gastrin was unaffected. There were only minor side-effects in a few experiments (reduction of salivation, brief blurring of vision), but no prolactin stimulation after ranitidine or ranitidine plus pirenzepine. The combined application of ranitidine and pirenzepine inhibited meal-stimulated acid secretion more effectively and produced fewer side-effects than the combination of cimetidine plus pirenzepine studied previously. PMID:6114900

  18. Vitamin D: Pharmacokinetics and Safety When Used in Conjunction with the Pharmaceutical Drugs Used in Cancer Patients: A Systematic Review

    International Nuclear Information System (INIS)

    Vitamin D has reported anti-cancer and anti-inflammatory properties modulated through gene transcription and non-genomic signaling cascades. The purpose of this review was to summarize the available research on interactions and pharmacokinetics between vitamin D and the pharmaceutical drugs used in patients with cancer. Hypercalcemia was the most frequently reported side effect that occurred in high dose calcitriol. The half-life of 25(OH)D3 and/or 1,25(OH)2D3 was found to be impacted by cimetidine; rosuvastatin; prednisone and possibly some chemotherapy drugs. No unusual adverse effects in cancer patients; beyond what is expected from high dose 1,25(OH)2D3 supplementation, were revealed through this review. While sufficient evidence is lacking, supplementation with 1,25(OH)2D3 during chemotherapy appears to have a low risk of interaction. Further interactions with vitamin D3 have not been studied

  19. Modeling and analysis of transport in the mammary glands

    Science.gov (United States)

    Quezada, Ana; Vafai, Kambiz

    2014-08-01

    The transport of three toxins moving from the blood stream into the ducts of the mammary glands is analyzed in this work. The model predictions are compared with experimental data from the literature. The utility of the model lies in its potential to improve our understanding of toxin transport as a pre-disposing factor to breast cancer. This work is based on a multi-layer transport model to analyze the toxins present in the breast milk. The breast milk in comparison with other sampling strategies allows us to understand the mass transport of toxins once inside the bloodstream of breastfeeding women. The multi-layer model presented describes the transport of caffeine, DDT and cimetidine. The analysis performed takes into account the unique transport mechanisms for each of the toxins. Our model predicts the movement of toxins and/or drugs within the mammary glands as well as their bioaccumulation in the tissues.

  20. Effect of antihistamines, disodium cromoglycate (DSCG) or methysergide on post-irradiation cerebral blood flow and mean systemic arterial blood pressure in primates after 25 Gy, whole-body, gamma irradiation

    International Nuclear Information System (INIS)

    Exposure to ionizing radiation causes hypotension, cerebral ischemia and release of histamine (HA) and serotonin (5-HT). To investigate the relationship among these responses, rhesus monkeys (Macaca mulatta) received physiological saline (i.v.), disodium cromoglycate (DSCG), antihistamines (AH, mepyramine and cimetidine), or methysergide (METH), then were given 25 Gy whole-body irradiation. Monkeys receiving DSCG, AH or METH had higher post-irradiation mean arterial blood pressure (MBP) than saline-treated controls. Compared to levels in controls, post-irradiation hippocampal blood flow (rCBF) levels were higher in monkeys receiving DSCG, AH or METH. Treatment with the 5-HT2 receptor antagonist methysergide was the most effective in maintaining both rCBF and MBP after irradiation. Results support the hypothesis that the irradiation-induced cerebral ischemia and, to some extent, the hypotension is mediated by serotonin through 5-HT2 receptor sites. (author) 72 refs

  1. Nerolidol, an antiulcer constituent from the essential oil of Baccharis dracunculifolia DC (Asteraceae).

    Science.gov (United States)

    Klopell, Fernando Canani; Lemos, Marivane; Sousa, João Paulo Barreto; Comunello, Eros; Maistro, Edson Luis; Bastos, Jairo Kennup; de Andrade, Sérgio Faloni

    2007-01-01

    In this study, the antiulcerogenic effect of essential oil from Baccharis dracunculifolia was evaluated using the model of acute gastric lesions induced by ethanol. The ulcerative lesion index (ULI) was significantly reduced by oral administration of the essential oil of B. dracunculifolia at doses of 50, 250 and 500 mg/kg which reduced the lesions by 42.79, 45.70 and 61.61%, respectively. The analysis of the chemical composition of the essential oil from B. dracunculifolia by GC showed that this was composed mainly of mono- and sesquiterpenes and the majority compound was nerolidol. Therefore, antiulcerogenic activity of nerolidol (50, 250 and 500 mg/kg) was investigated using ethanol-, indomethacin- and stress-induced ulcer models in rat. In the stress-induced ulcer model, a significant reduction of the ULI in animals treated with nerolidol (50, 250 and 500 mg/kg) and cimetidine (100 mg/kg) was observed, compared to the control group (p omeprazol (positive control), respectively. In indomethacin-ulcer the percentage of inhibition of ulcer was 34.69, 40.80, 51.02 and 46.93% in groups treated with 50, 250, 500 mg/kg of nerolidol and 100 mg/ kg of cimetidine (positive control), respectively. The results of this study show that nerolidol displays antiulcer activity, as it significantly inhibited the formation of ulcers induced in different animal models. However, further pharmacological and toxicological investigations, to delineate the mechanism(s) of action and the toxic effects, are required to allow the use of nerolidol for the treatment of gastric ulcer. PMID:17913068

  2. Bidirectional crosstalk between stress-induced gastric ulcer and depression under chronic stress.

    Directory of Open Access Journals (Sweden)

    Shuang Zhang

    Full Text Available Stress contributes to a variety of diseases and disorders such as depression and peptic ulcer. The present study aimed to investigate the correlation between stress ulcer and depression in pathogenesis and treatment by using chronic stress depression (CSD, chronic psychological stress ulcer (CPSU and water immersion restrain stress models in rats. Our data showed that the ulcer index of the animals after CSD exposure was significantly higher than that of controls. Depression-like behaviors were observed in rat after CPSU exposure. Fluoxetine hydrochloride significantly reduced the ulcer index of rats exposed to CPSU stress, while ranitidine inhibited depression-like behavior of the animals in CSD group. The ulcer index of rats administered with mifepristone after CPSU stress was markedly reduced compared to CPSU group, although there was no significant difference in the depression-like behavior between mifepristone-treated CSD group and naive controls. We also found that the rats exposed to CPSU or CSD stress displayed a lower level of corticosterone than naive controls, however, the acute stress (AS group showed an opposite result. Additionally, in order to study the relevance of H(2 receptors and depression, we treated the CSD group with cimetidine and famotidine respectively. The data showed that cimetidine inhibited depression-like behavior in CSD rats, and famotidine had no impact on depression. Overall our data suggested that the hypothalamic-pituitary-adrenal (HPA axis dysfunction may be the key role in triggering depression and stress ulcer. Acid-suppressing drugs and antidepressants could be used for treatment of depression and stress ulcer respectively. The occurrence of depression might be inhibited by blocking the central H(2 receptors.

  3. Formation of 4'-carboxyl acid metabolite of imrecoxib by rat liver microsomes

    Institute of Scientific and Technical Information of China (English)

    Hai-yan XU; Peng ZHANG; Ai-shen GONG; Yu-ming SUN; Feng-ming CHU; Zong-ru GUO; Da-fang ZHONG

    2006-01-01

    Aim:Imrecoxib is a novel and moderately selective COX-2 inhibitor.The aim of the present in vitro investigation was to study the formation of the major metabolite 4'-carboxylic acid imrecoxib (M2) and identify the enzyrne(s) involved in the reaction.Methods:The formation of M2 was studied in rat liver cytosol in the absence or presence of liver microsomes.The formed metabolite was identified and quantified by LC/MSn.In addition,to characterize the cytochrome P450 (CYP) isozymes involved in M2 formation,the effects of typical CYP inhibitors (such as ketoconazle,quinine,α-naphthoflavone, methylpyrazole,and cimetidine) on the formation rate of M2 were investigated.Results:The formation of M2 from 4'hydroxymethyl imrecoxib (M4) was completely dependent on rat liver microsomes and NADPH.Enzyme kinetic studies demonstrated that the formation rate of M2 conformed to monophasic Michaelis-Menten kinetics.Additional experiments showed that the formation of M2 was induced significantly by dexamethasone and lowered by ketoconazole strongly and concentration-dependently.By comparison.other CYP inhibitors.such as α-naphthoflavone,cimetidine,quinine,and methylpyrazole had no inhibitory effects on this metabolic pathway.Conclusion:These biotransformation studies of M4 and imrecoxib in rat liver at the subcellular level showed that the formation of M2 occurs in rat liver microsomes and is NADPH-dependent.The reaction was mainly catalyzed by CYP 3A in untreated rats and in dexamethasone-induced rats.Other CYP,such as CYP 1A,2C,2D,and 2E,seem unlikely to participate in this metabolic pathway.

  4. Role of rat liver cytochrome P450 3A and 2D in metabolism of imrecoxib

    Institute of Scientific and Technical Information of China (English)

    Hai-yan XU; Zhi-yong XIE; Peng ZHANG; Jin SUN; Feng-ming CHU; Zong-ru GUO; Da-fang ZHONG

    2006-01-01

    Aim: To investigate the in vitro metabolism of imrecoxib in rat liver microsomes and to identify the cytochrome P450 (CYP) forms involved in its metabolism. Methods: Liver microsomes of Wistar rats were prepared using an ultracentrifuge. The in vitro metabolism of imrecoxib was studied by incubation with rat liver microsomes. To characterize the CYP forms involved in the 4'-methyl hydroxylation of imrecoxib, the effects of typical CYP inducers (such as dexamethasone, isoniazid and (3-naphthoflavone) and of CYP inhibitors (such as ketoconazole, quinine, a-naphthoflavone, methylpyrazole, and cimetidine) on the formation rate of 4'-hydroxymethyl imrecoxib were investigated. Results: Imrecoxib wasmetabolized to 3 metabolites by rat liver microsomes: 4'-hydroxymethyl imrecoxib (M4), 4'-hydroxymethyl-5-hydoxyl imrecoxib (M3), and 4'-hydroxymethyl-5-carbonyl imrecoxib (M5). Over the imrecoxib concentration range studied (5-600 umol/L), the rate of 4'-methyl hydroxylation conformed to monophasic Michaelis-Menten kinetics. Dexamethasone significantly induced the formation of M4. Ketoconazole markedly lowered the metabolic rate of imrecoxib in a concentration-dependent manner. Moreover, a significant inhibitory effect of quinine on the formation of M4 was observed in microsomes obtained from control rats, isoniazid-induced rats, and (3-naphthoflavone-induced rats. In contrast, α-naphthoflavone, cimetidine, and methylpyrazole had no inhibitory effects on this metabolic pathway. Conclusion: Imrecoxib is metabolized via 4'-methyl hydroxylation in rat liver microsomes. The reaction is mainly catalyzed by CYP 3A. CYP 2D also played a role in control rats, in isoniazid-induced rats and in β-naphthoflavone-induced rats.

  5. Nuclear magnetic resonance-based metabolomics for prediction of gastric damage induced by indomethacin in rats

    Energy Technology Data Exchange (ETDEWEB)

    Um, So Young [Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration, 643 Yeonje-ri, Gangoe-myeon, Cheongwon-gun, Chungbuk (Korea, Republic of); Division of Life and Pharmaceutical Science and College of Pharmacy, Ewha Womans University, 52 Ewahyeodae-gil, Seodaemun-gu, Seoul (Korea, Republic of); Park, Jung Hyun [Division of Life and Pharmaceutical Science and College of Pharmacy, Ewha Womans University, 52 Ewahyeodae-gil, Seodaemun-gu, Seoul (Korea, Republic of); Chung, Myeon Woo [Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration, 643 Yeonje-ri, Gangoe-myeon, Cheongwon-gun, Chungbuk (Korea, Republic of); Kim, Kyu-Bong [College of Pharmacy, Dankook University, Dandae-ro, Cheonan, Chungnam (Korea, Republic of); Kim, Seon Hwa [Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration, 643 Yeonje-ri, Gangoe-myeon, Cheongwon-gun, Chungbuk (Korea, Republic of); Division of Life and Pharmaceutical Science and College of Pharmacy, Ewha Womans University, 52 Ewahyeodae-gil, Seodaemun-gu, Seoul (Korea, Republic of); College of Pharmacy, Dankook University, Dandae-ro, Cheonan, Chungnam (Korea, Republic of); Choi, Ki Hwan, E-mail: hyokwa11@korea.kr [Department of Pharmacology, National Institute of Toxicological Research, Korea Food and Drug Administration, 643 Yeonje-ri, Gangoe-myeon, Cheongwon-gun, Chungbuk (Korea, Republic of); Lee, Hwa Jeong, E-mail: hwalee@ewha.ac.kr [Division of Life and Pharmaceutical Science and College of Pharmacy, Ewha Womans University, 52 Ewahyeodae-gil, Seodaemun-gu, Seoul (Korea, Republic of)

    2012-04-13

    Highlights: Black-Right-Pointing-Pointer NMR based metabolomics - gastric damage by indomethacin. Black-Right-Pointing-Pointer Pattern recognition analysis was performed to biomarkers of gastric damage. Black-Right-Pointing-Pointer 2-Oxoglutarate, acetate, taurine and hippurate were selected as putative biomarkers. Black-Right-Pointing-Pointer The gastric damage induced by NSAIDs can be screened in the preclinical step of drug. - Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) have side effects including gastric erosions, ulceration and bleeding. In this study, pattern recognition analysis of the {sup 1}H-nuclear magnetic resonance (NMR) spectra of urine was performed to develop surrogate biomarkers related to the gastrointestinal (GI) damage induced by indomethacin in rats. Urine was collected for 5 h after oral administration of indomethacin (25 mg kg{sup -1}) or co-administration with cimetidine (100 mg kg{sup -1}), which protects against GI damage. The {sup 1}H-NMR urine spectra were divided into spectral bins (0.04 ppm) for global profiling, and 36 endogenous metabolites were assigned for targeted profiling. The level of gastric damage in each animal was also determined. Indomethacin caused severe gastric damage; however, indomethacin administered with cimetidine did not. Simultaneously, the patterns of changes in their endogenous metabolites were different. Multivariate data analyses were carried out to recognize the spectral pattern of endogenous metabolites related to indomethacin using partial least square-discrimination analysis. In targeted profiling, a few endogenous metabolites, 2-oxoglutarate, acetate, taurine and hippurate, were selected as putative biomarkers for the gastric damage induced by indomethacin. These metabolites changed depending on the degree of GI damage, although the same dose of indomethacin (10 mg kg{sup -1}) was administered to rats. The results of global and targeted profiling suggest that the gastric damage induced by

  6. Electrochemical Transformation of Trace Organic Contaminants in Latrine Wastewater.

    Science.gov (United States)

    Jasper, Justin T; Shafaat, Oliver S; Hoffmann, Michael R

    2016-09-20

    Solar-powered electrochemical systems have shown promise for onsite wastewater treatment in regions where basic infrastructure for conventional wastewater treatment is not available. To assess the applicability of these systems for trace organic contaminant treatment, test compound electrolysis rate constants were measured in authentic latrine wastewater using mixed-metal oxide anodes coupled with stainless steel cathodes. Complete removal of ranitidine and cimetidine was achieved within 30 min of electrolysis at an applied potential of 3.5 V (0.7 A L(-1)). Removal of acetaminophen, ciprofloxacin, trimethoprim, propranolol, and carbamazepine (>80%) was achieved within 3 h of electrolysis. Oxidation of ranitidine, cimetidine, and ciprofloxacin was primarily attributed to reaction with NH2Cl. Transformation of trimethoprim, propranolol, and carbamazepine was attributed to direct electron transfer and to reactions with surface-bound reactive chlorine species. Relative contributions of aqueous phase ·OH, ·Cl, ·Cl2(-), HOCl/OCl(-), and Cl2 were determined to be negligible based on measured second-order reaction rate constants, probe compound reaction rates, and experiments in buffered Cl(-) solutions. Electrical energy per order of removal (EEO) increased with increasing applied potentials and current densities. Test compound removal was most efficient at elevated Cl(-) concentrations present when treated wastewater is recycled for use as flushing water (i.e., ∼ 75 mM Cl(-); EEO = 0.2-6.9 kWh log(-1) m(-3)). Identified halogenated and oxygenated electrolysis products typically underwent further transformations to unidentifiable products within the 3 h treatment cycle. Identifiable halogenated byproduct formation and accumulation was minimized during electrolysis of wastewater containing 75 mM Cl(-). PMID:27564843

  7. Nuclear magnetic resonance-based metabolomics for prediction of gastric damage induced by indomethacin in rats

    International Nuclear Information System (INIS)

    Highlights: ► NMR based metabolomics – gastric damage by indomethacin. ► Pattern recognition analysis was performed to biomarkers of gastric damage. ► 2-Oxoglutarate, acetate, taurine and hippurate were selected as putative biomarkers. ► The gastric damage induced by NSAIDs can be screened in the preclinical step of drug. - Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) have side effects including gastric erosions, ulceration and bleeding. In this study, pattern recognition analysis of the 1H-nuclear magnetic resonance (NMR) spectra of urine was performed to develop surrogate biomarkers related to the gastrointestinal (GI) damage induced by indomethacin in rats. Urine was collected for 5 h after oral administration of indomethacin (25 mg kg−1) or co-administration with cimetidine (100 mg kg−1), which protects against GI damage. The 1H-NMR urine spectra were divided into spectral bins (0.04 ppm) for global profiling, and 36 endogenous metabolites were assigned for targeted profiling. The level of gastric damage in each animal was also determined. Indomethacin caused severe gastric damage; however, indomethacin administered with cimetidine did not. Simultaneously, the patterns of changes in their endogenous metabolites were different. Multivariate data analyses were carried out to recognize the spectral pattern of endogenous metabolites related to indomethacin using partial least square-discrimination analysis. In targeted profiling, a few endogenous metabolites, 2-oxoglutarate, acetate, taurine and hippurate, were selected as putative biomarkers for the gastric damage induced by indomethacin. These metabolites changed depending on the degree of GI damage, although the same dose of indomethacin (10 mg kg−1) was administered to rats. The results of global and targeted profiling suggest that the gastric damage induced by NSAIDs can be screened in the preclinical stage of drug development using a NMR based metabolomics approach.

  8. Envenenamento ofídico em crianças: frequência de reações precoces ao antiveneno em pacientes que receberam pré-tratamento com antagonistas H1 e H2 da histamina e hidrocortisona Snake envenomation in children: early reactions frequency at antivenom in patients pretreated with histamine antagonists HI and H2 and hydrocortisone

    Directory of Open Access Journals (Sweden)

    Fábio Bucarethi

    1994-10-01

    Full Text Available Foram estudadas 24 crianças, com idade entre 2 a 14 anos, de 1989 a 1993, vítimas de acidentes ofídicos, submetidas a pré-tratamento com antagonistas H1 (dextroclorfeniramina e H2 (cimetidine ou ranitidina da histamina e hidrocortisona, com objetivo de avaliar a frequência e o tipo de reações precoces (RP ao antiveneno (AV. Em nenhum paciente havia antecedente de atopia ou uso prévio de algum tipo de antiveneno ou antitoxina heteróloga. Das 24 crianças 15 receberam AV botrópico (RP em 5, 7 AV crotálico (RP em 5, 1 AV crotálico e AV botrópico-crotálico e 1 AV elapídico (RP. Foram observadas RP graves em 3 crianças, as 3 classificadas como acidente crotálico grave. A análise dos resultados sugere que o pré-tratamento realizado não ofereceu uma proteção segura quanto ao aparecimento de RP.Type and frequency of early reactions (ER were studied in 24 children aging 2-14 years victims of snake bites who received pretreatment with histamine antagonists H1 (dextrochlorfenirarnine and H2 (cimetidine or ranitidine and hydrocortisone from 1989 to 1993. None of them had atopy nor received any type of anti-venoms(AV and antitoxins before. Of 24 children, 15 received bothropic AV (ER in 5, 7 crotalic AV (ER in 5, 1 crotalic plus crotalic-bothropic AV, and 1 elapidic AV (ER in 1. In 3 children severe early reactions were observed and they were classified as severe crotalic accident. Results suggest that pre-treatment did not offer safety protection at the appearance of early reactions.

  9. Anti-ulcerogenic activity of aqueous extract of Carica papaya seed on indomethacin-induced peptic ulcer in male albino rats

    Institute of Scientific and Technical Information of China (English)

    Hussein O B Oloyede; Matthew C Adaja; Taofeek O Ajiboye; Musa O Salawu

    2015-01-01

    OBJECTIVE:Carica papaya is an important fruit with its seeds used in the treatment of ulcer in Nigeria. This study investigated the anti-ulcerogenic and antioxidant activities of aqueous extract of Carica papaya seed against indomethacin-induced peptic ulcer in male rats. METHODS:Thirty male rats were separated into 6 groups (A–F) of ifve rats each. For 14 d before ulcer induction with indomethacin, groups received once daily oral doses of vehicle (distil ed water), cimetidine 200 mg/kg body weight (BW), or aqueous extract of C. papaya seed at doses of 100, 150 or 200 mg/kg BW (groups A, B, C, D, E and F, respectively). Twenty-four hours after the last treatment, groups B, C, D, E and F were treated with 100 mg/kg BW of indomethacin to induce ulcer formation. RESULTS:Carica papaya seed extract signiifcantly (P<0.05) increased gastric pH and percentage of ulcer inhibition relative to indomethacin-induced ulcer rats. The extract signiifcantly (P<0.05) decreased gastric acidity, gastric acid output, gastric pepsin secretion, ulcer index and gastric secretion volume relative to group B. These results were similar to that achieved by pretreatment with cimetidine. Speciifc activities of superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase and glucose-6-phosphate dehydrogenase in the extract-treated groups (D, E and F) were increased signiifcantly over the group B (P<0.05). Pretreatment with the seed extract protected rats from the indomethacin-mediated decrease in enzyme function experienced by the group B. Similarly, indomethacin-mediated decrease in reduced glutathione level and indomethacin-mediated increase in malondialdehyde were reversed by Carica papaya extract. CONCLUSION:In this study, pretreatment with aqueous extract of Carica papaya seed exhibited anti-ulcerogenic and antioxidant effects, which may be due to the enhanced antioxidant enzymes.

  10. Antiulcerogenic activity of Carica papaya seed in rats.

    Science.gov (United States)

    Pinto, Lorraine Aparecida; Cordeiro, Kátia Wolff; Carrasco, Viviane; Carollo, Carlos Alexandre; Cardoso, Cláudia Andréa Lima; Argadoña, Eliana Janet Sanjinez; Freitas, Karine de Cássia

    2015-03-01

    The purpose of the present study was to evaluate the gastroprotective and healing effects of the methanolic extract of the seed of the papaya Carica papaya L. (MECP) in rats. Models of acute gastric ulcer induction by ethanol and indomethacin and of chronic ulcer by acetic acid were used. The gastric juice and mucus parameters were evaluated using the pylorus ligation model, and the involvement of sulfhydryl compounds (GSH) and nitric oxide in the gastroprotective effect was analyzed using the ethanol model. The toxicity was assessed through toxicity tests. No signs of toxicity were observed when the rats received a single dose of 2000 mg/kg of extract. The MECP in doses of 125, 250, and 500 mg/kg significantly reduced the gastric lesion with 56, 76, and 82 % inhibition, respectively, and a dose of 30 mg/kg lansoprazole showed 79 % inhibition in the ethanol model. MECP (125, 250, 500 mg/kg) and cimetidine (200 mg/kg) reduced the gastric lesion in the indomethacin model, with 62, 67, 81, and 85 % inhibition, respectively. The MECP (500 mg/kg) and cimetidine (200 mg/kg) treatments showed a reduction in ulcerative symptoms induced by acetic acid by 84 and 73 %, respectively. The antiulcerogenic activity seems to involve GSH because the inhibition dropped from 72 to 13 % in the presence of a GSH inhibitor. Moreover, the MECP showed systemic action, increasing the mucus production and decreasing gastric acidity. Treatments with MECP induce gastroprotection without signs of toxicity. This effect seems to involve sulfhydryl compounds, increased mucus, and reduced gastric acidity.

  11. Afferent signalling from the acid-challenged rat stomach is inhibited and gastric acid elimination is enhanced by lafutidine

    Directory of Open Access Journals (Sweden)

    Holzer Peter

    2009-06-01

    Full Text Available Abstract Background Lafutidine is a histamine H2 receptor antagonist, the gastroprotective effect of which is related to its antisecretory activity and its ability to activate a sensory neuron-dependent mechanism of defence. The present study investigated whether intragastric administration of lafutidine (10 and 30 mg/kg modifies vagal afferent signalling, mucosal injury, intragastric acidity and gastric emptying after gastric acid challenge. Methods Adult rats were treated with vehicle, lafutidine (10 – 30 mg/kg or cimetidine (10 mg/kg, and 30 min later their stomachs were exposed to exogenous HCl (0.25 M. During the period of 2 h post-HCl, intragastric pH, gastric volume, gastric acidity and extent of macroscopic gastric mucosal injury were determined and the activation of neurons in the brainstem was visualized by c-Fos immunocytochemistry. Results Gastric acid challenge enhanced the expression of c-Fos in the nucleus tractus solitarii but caused only minimal damage to the gastric mucosa. Lafutidine reduced the HCl-evoked expression of c-Fos in the NTS and elevated the intragastric pH following intragastric administration of excess HCl. Further analysis showed that the gastroprotective effect of lafutidine against excess acid was delayed and went in parallel with facilitation of gastric emptying, measured indirectly via gastric volume changes, and a reduction of gastric acidity. The H2 receptor antagonist cimetidine had similar but weaker effects. Conclusion These observations indicate that lafutidine inhibits the vagal afferent signalling of a gastric acid insult, which may reflect an inhibitory action on acid-induced gastric pain. The ability of lafutidine to decrease intragastric acidity following exposure to excess HCl cannot be explained by its antisecretory activity but appears to reflect dilution and/or emptying of the acid load into the duodenum. This profile of actions emphasizes the notion that H2 receptor antagonists can protect

  12. 苦参对大鼠细胞色素P4501A2体内代谢活性的影响%Effect of Sophora flavescens on the metabolic activity of CYP1A2 in rats

    Institute of Scientific and Technical Information of China (English)

    刘洁; 赵仁永; 李芹; 焦建杰; 汪云; 韩晓文; 娄建石

    2011-01-01

    Objective To study the effect of Sophora flavescens on the metabolic activity of cytochrome P4501 A2( CYP1A2) in rats with caffeine as probe. Methods The rats were randomly divided into four groups: blank control group, Sophora flavescens group ( test group) , phenobarbital group (induction control group) and cimetidine group (inhibition control group). Sophora flavescens were administered orally for five days at a dose of 100 mg ·kg-1 body weight for Sophora flavescens group and normal saline were administered orally for blank control group at the same volume as Sophora flavescens group. Sodium phenobarbital and cimetidine injection were administered intraperitoneally for five days at a dose of 50 mg · kg-1 body weight for phenobarbital group and cimetidine group, respectively. On the 6th day, all rats in each group were injected caffeine 2. 5 mg · kg-1, then venous blood samples were collected at a set of time - points. The plasma concentrations of the caffeine were determined by HPLC. Results In Sophora flavescens group, AUC, MRT and Cmux of caffeine were significantly lower than those of blank control group and cimetidine group ( P < 0. 05 ) and were significantly higher than those of phenobarbital group ( P < 0. 05), and CL was significantly higher than that of blank control group and cimetidine group (P < 0. 05 ) and was significantly lower than that of phenobarbital group ( P < 0. 05). Conclusion Sophora flavescens can significantly induce the metabolicactivity of CYP1A2 in rats, but the effect of induction is weaker than phenobarbital.%目的 以咖啡因作为探针药物,研究苦参对大鼠细胞色素P450 1A2.(CYP1 A2)体内代谢活性的影响.方法 将Wistar大鼠随机分为4组:空白对照组、苦参组(实验组)、苯巴比妥组(诱导剂阳性对照组)和西咪替丁组(抑制剂阳性对照组).苦参组,灌胃给予苦参溶液100 mg·kg-1;空白对照组,灌胃给予与苦参组体积相同的生理盐水;苯巴比妥组,腹

  13. 组胺H1和H2受体在新生大鼠离体延髓脑片呼吸节律性放电调节中的作用%Role of histamine H1 and H2 receptors in the modulation of respiratory rhythmical discharge in medulla oblongata slice preparation of neonatal rats

    Institute of Scientific and Technical Information of China (English)

    齐莹; 千智斌; 吴中海

    2008-01-01

    本研究探讨组胺H1和H2受体在新生大鼠基本节律性呼吸的发生和调节中的作用.以改良的Kreb's液恒温灌流新生Sprague-Dawley大鼠离体延髓脑片标本,稳定记录与之相连舌下神经根的呼吸节律性放电活动(respiratory-related rhythmical discharge activity, RRDA).实验分为5组:第1、2、3组分别单独给予组胺(histamine, HA)、 H1受体特异阻断剂pyrilamine和H2受体特异阻断剂cimetidine;第4组分别先后给予HA和HA+pyrilamine;第5组分别先后给予HA和HA+cimetidine,观察舌下神经根RRDA的变化.结果显示,单独给予HA后呼吸周期(respiratory cycle, RC)及呼气时程(expiratory time, TE)明显缩短,而吸气时程(inspiratory time, TI)及放电积分幅度(integral amplitude, IA)无明显变化;给予pyrilamine后RC、 TE明显延长,TI、 IA也无明显变化,且HA的作用可以被pyrilamine逆转;给予cimetidine后RC、 TE、 TI、 IA均无明显变化,且HA的作用不能被cimetidine逆转.结果提示,H1受体参与哺乳动物基本呼吸节律的产生和调节,H2受体对哺乳动物基本节律性呼吸的调控无明显影响.

  14. Prevalence of anti-ulcer drug use in a Chinese cohort

    Institute of Scientific and Technical Information of China (English)

    Tzeng-Ji Chen; Li-Fang Chou; Shinn-Jang Hwang

    2003-01-01

    AIM: To estimate the age-specific prevalence of anti-ulcer drug use and to calculate the usage of different anti-ulcer drugs over 5 years within the universal health insurance program in Taiwan area. METHODS: The National Health Insurance Research Database in Taipei supplied the cohort data sets of 200 000people. The ambulatory and inpatient claims of the cohort from 1997 to 2001 were analyzed. The anti-ulcer drugs included all drug items of the group A02B (drugs for treatment of peptic ulcer) in the Anatomical Therapeutic Chemical classification system (version 2000). The amount of drug usage was measured in unit of defined daily dose. RESULTS: Among bhe totally 13 034 393 visits wibh 56 672 631ambulatory prescription items, there were 398 150 (0.7 %)prescribed items of anti-ulcer drugs in 378 855 (2.9 %)visits. Among the 107 649 admissions with 5 762 312inpatient prescription items, there were 24 598 (0.4 %)prescribed items of anti-ulcer drugs in 11 548 (10.7 %)admissions. The annual prevalence of anti-ulcer drug use was 9.6 % in 1997, 11.6 % in 1998, 15.4 % in 1999, 14.5 %in 2000, and 15.9 % in 2001 respectively. The 5-year prevalence was 36.1%. The age-specific prevalence among the people younger than 20 years was 9.2 % in 2001 and 23.7 % during the 5-year period. Cimetidine not only was the most popular ingredient among anti-ulcer drugs (57 634cimetidine users in 70 729 all anti-ulcer drug users during the 5-year period) but also had the largest prescribed amount (42.3 % of DDDs for all anti-ulcer drug users during the 5-year period). The annually prescribed amount of anti-ulcer drugs had grown from 4.9 DDDs/1000 inhabitants/day in 1997 to 7.5 in 2001. This increase was largely attributed to H2-receptor antagonists and the expanding number of users. CONCLUSION: Prescribing of anti-ulcer drugs is indeed popular among the Chinese population in Taiwan area. The disproportionate use of anti-ulcer drugs by children demands further investigation.

  15. Structure-activity relationship analysis of cytotoxic cyanoguanidines: selection of CHS 828 as candidate drug

    Directory of Open Access Journals (Sweden)

    Gullbo Joachim

    2009-06-01

    Full Text Available Abstract Background N-(6-(4-chlorophenoxyhexyl-N'-cyano-N''-4-pyridyl guanidine (CHS 828 is the first candidate drug from a novel group of anti-tumour agents – the pyridyl cyanoguanidines, shown to be potent compounds interfering with cellular metabolism (inhibition of nicotinamide phosphoribosyl transferase and NF-κB signalling. Substituted cyanoguanidines are also found in anti-hypertensive agents such as the potassium channel opener pinacidil (N-cyano-N'-(4-pyridyl-N''-(1,2,2-trimethylpropylguanidine and histamine-II receptor antagonists (e.g. cimetidine, N-cyano-N'-methyl-N''-[2-[[(5-methylimidazol-4-yl]methyl]thio]ethylguanidine. In animal studies, CHS 828 has shown very promising activity, and phase I and II studies resulted in further development of a with a water soluble prodrug. Findings To study the structural requirements for cyanoguanidine cytotoxicity a set of 19 analogues were synthesized. The cytotoxic effects were then studied in ten cell lines selected for different origins and mechanisms of resistance, using the fluorometric microculture cytotoxicity assay (FMCA. The compounds showed varying cytotoxic activity even though the dose-response curves for some analogues were very shallow. Pinacidil and cimetidine were found to be non-toxic in all ten cell lines. Starting with cyanoguanidine as the crucial core it was shown that 4-pyridyl substitution was more efficient than was 3-pyridyl substitution. The 4-pyridyl cyanoguanidine moiety should be linked by an alkyl chain, optimally a hexyl, heptyl or octyl chain, to a bulky end group. The exact composition of this end group did not seem to be of crucial importance; when the end group was a mono-substituted phenyl ring it was shown that the preferred position was 4-substitution, followed by 3- and, finally, 2-substitution as the least active. Whether the substituent was a chloro, nitro or methoxy substituent seemed to be of minor importance. Finally, the activity patterns in the

  16. Development and evaluation of a gastro-retentive delivery system for improved antiulcer activity of ginger extract (Zingiber officinale).

    Science.gov (United States)

    Kumar Singh, Pramod; Pal Kaur, Indu

    2011-11-01

    Aim was to develop and optimize multiunit gastro-retentive floating beads (FBs) intended for localized and prolonged release of ginger for treating gastric ulcers. Protective effect of ginger extract (GE) against ulcer is well documented, but therapeutic use is compromised due to poor bioavailability and physicochemical properties. GE was only slightly soluble (3.19 ± 0.38 mg/ml) in simulated gastric fluid (SGF; pH 1.2). The solubility decreased in water to 0.69 ± 0.03 mg/ml and further by 26% in the presence of calcium carbonate (0.5% w/v). We prepared FBs of GE using calcium carbonate and sodium alginate in different proportions. Beads were evaluated for diameter, buoyancy, entrapment, and porosity. In vitro dissolution showed a Fickian release with a cumulative release of >80% at 24 h. Preclinical evaluation was done in cold-restraint stress induced gastric ulcers, in albino rats, in terms of (i) ulcer index, hemorrhagic streaks (l), mucus content, (ii) oxido-nitrosative stress, and (iii) histopathology. GE loaded FBs (200 mg/kg) were significantly better than free GE and better/equivalent to cimetidine (10 mg/kg). The system was evaluated for therapeutic effect (curative), i.e. after the induction of ulcers. Most of the natural phytochemical or antioxidants show pretreatment effectiveness. We, however, developed and established GE FBs for sustained curative effect. PMID:21401390

  17. Other antiandrogens.

    Science.gov (United States)

    Schmidt, J B

    1998-01-01

    Various substances of steroidal or nonsteroidal structure may serve as an alternative for the antiandrogenic treatment of acne. Compounds with antiandrogenic properties like cimetidine or ketoconazole are rarely administered for acne due to their weak effects. In contrast, spironolactone is an effective antiandrogen that shows good treatment effects in hirsutism and acne. Side effects occur frequently and are dose dependent. Isotretinoin--the most effective agent in acne therapy--has been under discussion for additional antiandrogenic properties for years. At present there is additional evidence for the antiandrogenic effects of isotretinoin. Regarding substances acting on both levels, androgen receptor binding and 5 alpha-reductase inhibition, the question is raised whether the term 'antiandrogen' should be amplified by including the 5 alpha-reductase inhibitors. This would pay tribute to the biological aspect of antiandrogenicity that takes into account not only the mode of action but also the effects of the substance. Under this aspect type 1 5 alpha-reductase inhibitors may gain attention in the future. PMID:9557251

  18. Update and future of systemic acne treatment.

    Science.gov (United States)

    Zouboulis, Christos C; Piquero-Martin, Jaime

    2003-01-01

    Systemic treatment is required in patients with moderate-to-severe acne, especially when acne scars start to occur. Antibiotics with anti-inflammatory properties, such as tetracyclines (oxytetracycline, tetracycline chloride, doxycycline, minocycline and limecycline) and macrolide antibiotics (erythromycin and azithromycin) are the agents of choice for papulopustular acne, even though the emerging resistant bacterial strains are minimizing their effect, especially regarding erythromycin. Systemic antibiotics should be administered during a period of 8-12 weeks. In severe papulopustular and in nodulocystic/conglobate acne, oral isotretinoin is the treatment of choice. Hormonal treatment represents an alternative regimen in female acne, whereas it is mandatory in resistant, severe pubertal or post-adolescent forms of the disease. Compounds with anti-androgenic properties include estrogens combined with progestins, such as ethinyl estradiol with cyproterone acetate, chlormadinone acetate, desogestrel, drospirenone, levonogestrel, norethindrone acetate, norgestimate, and other anti-androgens directly blocking the androgen receptor (flutamide) or inhibiting androgen activity at various levels, corticosteroids, spironolactone, cimetidine, and ketoconazole. After 3 months of treatment control of seborrhea and acne can be obtained. Low-dose corticosteroids (prednisone, prednisolone, or dexamethasone) are indicated in patients with adrenal hyperandrogenism or acne fulminans. New developments and future trends represent low-dose long-term isotretinoin regimens, new isotretinoin formulations (micronized isotretinoin), isotretinoin metabolites, combination treatments to reduce toxicity, insulin-sensitizing agents, 5alpha-reductase type 1 inhibitors, antisense oligonucleotide molecules, and, especially, new anti-inflammatory agents, such as lipoxygenase inhibitors. PMID:12566804

  19. Dehydration-induced vasopressin secretion in humans: involvement of the histaminergic system.

    Science.gov (United States)

    Kjaer, A; Knigge, U; Jørgensen, H; Warberg, J

    2000-12-01

    In rats, the hypothalamic neurotransmitter histamine participates in regulation of vasopressin secretion and seems to be of physiological importance, because blockade of the histaminergic system reduces dehydration-induced vasopressin secretion. We investigated whether histamine is also involved in regulation of vasopressin secretion during dehydration in humans. We found that 40 h of dehydration gradually increased plasma osmolality by 10 mosmol/kg and induced a fourfold increase in vasopressin levels. Pretreatment with the H(2)-receptor antagonists cimetidine or ranitidine significantly reduced the dehydration-induced increase in vasopressin levels approximately 40% after 34 and 37 h of dehydration, whereas this was not the case with the H(1)-receptor antagonist mepyramine. Dehydration reduced aldosterone secretion by approximately 50%. This effect of dehydration was reduced by both H(1)- and H(2)-receptor blockade after 16 and/or 34 h of dehydration. We conclude that vasopressin secretion in response to dehydration in humans is under the regulatory influence of histamine and that the effect seems to be mediated via H(2)-receptors. In addition, the regulation of aldosterone secretion during dehydration also seems to involve the histaminergic system via H(1) and H(2) receptors.

  20. Histaminergic system in co-cultures of hippocampus and posterior hypothalamus: a morphological and electrophysiological study in the rat.

    Science.gov (United States)

    Diewald, L; Heimrich, B; Büsselberg, D; Watanabe, T; Haas, H L

    1997-11-01

    Neurons of the tuberomammillary nucleus in the posterior hypothalamus diffusely project to most parts of the central nervous system, where their main transmitter, histamine, modulates the excitability of the target neurons. The development of a histaminergic hypothalamo-hippocampal pathway and its function were studied in organotypic co-cultures. Immunocytochemistry for histidine decarboxylase, the specific synthesizing enzyme, stained clusters of neurons in the hypothalamic tuberomammillary area. Immunolabelled varicose processes innervated the co-cultured hippocampus and established a few synaptic contacts on dendrites. Cultured tuberomammillary neurons displayed their typical membrane properties and were spontaneously active. In hippocampal pyramidal cells of the CA3 region the long-lasting afterhyperpolarization was reduced by histamine or impromidine and increased by the H2 antagonist cimetidine, but not by the H1 antagonist mepyramine. The membrane potential was depolarized in presence of an H2 agonist and hyperpolarized by an H2 antagonist. In single hippocampal cultures histamine antagonists did not affect afterhyperpolarization and membrane potential. Histaminergic neurons retain their main morphological and physiological characteristics in slice cultures and establish a functional connection with co-cultured target cells.

  1. Distribution of histaminergic neurons and their modulatory effects on oscillatory activity in the olfactory center of the terrestrial slug Limax.

    Science.gov (United States)

    Matsuo, Ryota; Fukata, Rena; Kumagai, Moeko; Kobayashi, Asuka; Kobayashi, Suguru; Matsuo, Yuko

    2016-01-01

    Terrestrial mollusks can form an odor aversion memory following the simultaneous presentation of a food odor and an aversive stimulus. The local field potential oscillation recorded on the surface of the procerebrum (PC; the higher olfactory center) exhibits a frequency change in response to the detection of a learned odor; such a change is thus considered to reflect the internal state of the brain during memory recall. Thus far, dopamine and serotonin have been demonstrated to change the oscillatory frequency. Other monoamines, however, have not yet been studied. In the present study, we investigated the possible involvement of histamine (HA). Immunohistochemical staining of HA and in situ hybridization against histidine decarboxylase revealed the location of the cell bodies of HAergic neurons in all ganglia of the brain. The majority of them were located at the medial aspect of the pedal ganglia, and the cerebral ganglia also contained numerous HAergic neurons in their posterior regions. The neuropil layers of the PC received HAergic innervation from the neurons in the cerebral ganglion, as well as from a few neurons located in the dorsomedial part of the cell mass layer of the PC. The HAergic fibers, however, innervated spatially limited regions of the PC, and seemed to affect a small fraction of the PC neurons. HA exerted accelerating effects on the LFP oscillation in a dose-dependent manner, and this effect was suppressed by an H2 blocker, cimetidine. Our results support the involvement of HA in the functioning of the PC. PMID:26105566

  2. The ABCG2 efflux transporter from rabbit placenta: Cloning and functional characterization.

    Science.gov (United States)

    Halwachs, Sandra; Kneuer, Carsten; Gohlsch, Katrin; Müller, Marian; Ritz, Vera; Honscha, Walther

    2016-02-01

    In human placenta, the ATP-binding cassette efflux transporter ABCG2 is highly expressed in syncytiotrophoblast cells and mediates cellular excretion of various drugs and toxins. Hence, physiological ABCG2 activity substantially contributes to the fetoprotective placenta barrier function during gestation. Developmental toxicity studies are often performed in rabbit. However, despite its toxicological relevance, there is no data so far on functional ABCG2 expression in this species. Therefore, we cloned ABCG2 from placenta tissues of chinchilla rabbit. Sequencing showed 84-86% amino acid sequence identity to the orthologues from man, rat and mouse. We transduced the rabbit ABCG2 clone (rbABCG2) in MDCKII cells and stable rbABCG2 gene and protein expression was shown by RT-PCR and Western blot analysis. The rbABCG2 efflux activity was demonstrated with the Hoechst H33342 assay using the specific ABCG2 inhibitor Ko143. We further tested the effect of established human ABCG2 (hABCG2) drug substrates including the antibiotic danofloxacin or the histamine H2-receptor antagonist cimetidine on H33342 accumulation in MDCKII-rbABCG2 or -hABCG2 cells. Human therapeutic plasma concentrations of all tested drugs caused a comparable competitive inhibition of H33342 excretion in both ABCG2 clones. Altogether, we first showed functional expression of the ABCG2 efflux transporter in rabbit placenta. Moreover, our data suggest a similar drug substrate spectrum of the rabbit and the human ABCG2 efflux transporter. PMID:26907376

  3. Photocatalytic applications of paper-like poly(vinylidene fluoride)-titanium dioxide hybrids fabricated using a combination of electrospinning and electrospraying.

    Science.gov (United States)

    Ramasundaram, Subramaniyan; Son, Aseom; Seid, Mingizem Gashaw; Shim, Sujin; Lee, Sang Hyup; Chung, Yun Chul; Lee, Changha; Lee, Jaesang; Hong, Seok Won

    2015-03-21

    A paper-like photocatalyst was fabricated by electrospraying an N,N'-dimethylformamide (DMF) dispersion of titanium dioxide (TiO2) nanoparticles (NPs) on a poly(vinylidene fluoride) nanofiber (PVDF NF) mat prepared by electrospinning. Morphological studies revealed that the TiO2 NPs uniformly deposited as clusters on the surface of the PVDF NF mat. The immobilized amount of TiO2 was found to be 2.08, 2.44, 3.80, and 4.73 mg per 45 cm(2) of PVDF-TiO2 hybrids for the electrospraying of 10, 20, 40, and 60 ml of TiO2-DMF, respectively. The hybrid photocatalysts were effective in degrading bisphenol A (BPA), 4-chlorophenol (4-CP), and cimetidine (CMT), which dissolved in both deionized water and secondary wastewater effluents, with activity being proportional to the quantity of TiO2 NPs immobilized. For the highest loading amount of TiO2, BPA, 4-CP, and CMT degraded completely within 100, 100, and 40 min of UV irradiation, respectively. Stable photo-oxidation of CMT was maintained through 10 repeated cycles. During these cycles, it was confirmed that there was no loss of TiO2 NPs by inductively coupled plasma optical emission spectrometry. Our results suggest that effective and stable PVDF-TiO2 hybrid photocatalysts can be fabricated on a large scale by combining electrospinning and electrospraying techniques.

  4. Influence of patient medication on diagnostic accuracy in nuclear medicine

    Energy Technology Data Exchange (ETDEWEB)

    Sampson, C.B. [Addenbrooke`s Hospital, Cambridge (United Kingdom). Dept. of Nuclear Medicine

    1997-12-31

    Full text. In recently years many reports have published of unusual or unexpected changes in the biodistribution of radiopharmaceuticals which do not correlate with normality or disease. Whilst many extraneous factors can alter tracer kinetics it has become apparent that concomitant patient medication can be such a factor. If the clinician is unaware that patient is on drug therapy difficulties arise in making a accurate diagnosis. Most drug/radio pharmaceutical effects are those in which the functional status of the organ is altered as a result of the pharmacological action of the drug. Examples here are narcotic analgesics such as methadone, pethidine and morphine which cause spasm of the biliary tract due to contraction of the sphincter of Oddi and an altered transit time of the technetium labelled tracer. Cytotoxic drugs such as cyclophosphamide and vincristine can markedly affect tumour uptake of 67-gallium so that litter or no activity is taken up by the tumour. Nifedipine, because of its powerful calcium channel blocking activity is known to affect the radiolabelling of white cells and red cells and to affect uptake of Tc-99 m MDP into bones. Other important and confusing effects are caused by phenothiazines, cimetidine and oral contraceptives. In recent years it has been reported that drugs such as cyclosporin, azathioprine and heparin and derivatives of heparin can markedly interfere with cell labelling procedures. This review will consider some of the clinical effects of drugs and will also address the reporting of instances of drug/radio pharmaceutical interactions

  5. Protective effect of tetrahydrocoptisine against ethanol-induced gastric ulcer in mice.

    Science.gov (United States)

    Li, Weifeng; Huang, Huimin; Niu, Xiaofeng; Fan, Ting; Mu, Qingli; Li, Huani

    2013-10-01

    Excessive alcohol consumption can lead to gastric ulcer and the present work was aimed to examine the protective effect of tetrahydrocoptisine (THC) in the model of ethanol-induced gastric ulcer in mice. Fasted mice treated with ethanol 75% (0.5ml/100g) were pre-treated with THC (10 or 20mg/kg, ip), cimetidine (100mg/kg, ip) or saline in different experimental sets for a period of 3days, and animals were euthanized 4h after ethanol ingestion. Gross and microscopic lesions, immunological and biochemical parameters were taken into consideration. The results showed that ethanol induced gastric damage, improving nitric oxide (NO) level, increased pro-inflammatory cytokine (TNF-α and IL-6) levels and myeloperoxidase (MPO) activity, as well as the expression of nuclear factor-κB (NF-κB) in the ethanol group. Pretreatment of THC at doses of 10 and 20mg/kg bodyweight significantly attenuated the gastric lesions as compared to the ethanol group. These results suggest that the gastroprotective activity of THC is attributed to reducing NO production and adjusting the pro-inflammatory cytokine, inhibited neutrophil accumulation and NF-κB expression.

  6. Protective effect of δ-amyrone against ethanol-induced gastric ulcer in mice.

    Science.gov (United States)

    Li, Weifeng; Yao, Huan; Niu, Xiaofeng; Wang, Yu; Zhang, Hailin; Li, Huani; Mu, Qingli

    2015-06-01

    The purpose of this study is to examine the protective effect of δ-amyrone on ethanol-induced gastric ulcer in mice. The mice intragastric administration 75% (0.5 mL/100g) ethanol was pretreated with δ-amyrone (4 and 8 mg/kg) and cimetidine (100 mg/kg) or vehicles in different experimental groups for a continuous three-day, and animals were euthanized 3h after ethanol ingestion. The gastric lesions were significantly attenuated by δ-amyrone (4 and 8 mg/kg) as compared to the ulcer control group. Pre-treatment with δ-amyrone prevented the myeloperoxidase (MPO) activity, production of nitric oxide (NO) in serum, expression of inducible nitric oxide synthase (iNOS) and nuclear factor kappa B (NF-κB) p65 protein expression. Analysis of cytokines in gastric tissue and serum of ethanol-induced mice showed the levels of tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) were decreased by δ-amyrone in response to NF-κB p65. These results suggested that δ-amyrone exerts its protective effect on experimental gastric ulcer by inhibiting NF-κB signaling pathways, which subsequently reduces overproduction of the inducible enzymes iNOS and suppresses the release of the inflammatory factors TNF-α, IL-6 and NO. Thus, δ-amyrone shows promise as a therapeutic agent in experimental gastric ulcer.

  7. Protective effect of tetrahydrocoptisine against ethanol-induced gastric ulcer in mice

    Energy Technology Data Exchange (ETDEWEB)

    Li, Weifeng, E-mail: liwf@mail.xjtu.edu.cn; Huang, Huimin; Niu, Xiaofeng, E-mail: niuxf@mail.xjtu.edu.cn; Fan, Ting; Mu, Qingli; Li, Huani

    2013-10-01

    Excessive alcohol consumption can lead to gastric ulcer and the present work was aimed to examine the protective effect of tetrahydrocoptisine (THC) in the model of ethanol-induced gastric ulcer in mice. Fasted mice treated with ethanol 75% (0.5 ml/100 g) were pre-treated with THC (10 or 20 mg/kg, ip), cimetidine (100 mg/kg, ip) or saline in different experimental sets for a period of 3 days, and animals were euthanized 4 h after ethanol ingestion. Gross and microscopic lesions, immunological and biochemical parameters were taken into consideration. The results showed that ethanol induced gastric damage, improving nitric oxide (NO) level, increased pro-inflammatory cytokine (TNF-α and IL-6) levels and myeloperoxidase (MPO) activity, as well as the expression of nuclear factor-κB (NF-κB) in the ethanol group. Pretreatment of THC at doses of 10 and 20 mg/kg bodyweight significantly attenuated the gastric lesions as compared to the ethanol group. These results suggest that the gastroprotective activity of THC is attributed to reducing NO production and adjusting the pro-inflammatory cytokine, inhibited neutrophil accumulation and NF-κB expression. - Highlights: • THC decreased ethanol-induced pro-inflammatory cytokine release. • THC inhibited the production of NO in serum and gastric tissue. • THC reduced NF-κB expression and MPO accumulation in ethanol-induced gastric tissue.

  8. Campylobacter pylori-associated gastritis: attempts to eradicate the bacteria by various antibiotics and anti-ulcer regimens.

    Science.gov (United States)

    Glupczynski, Y; Burette, A; Nyst, J F; De Prez, C; De Koster, E; Deltenre, M

    1988-01-01

    The efficacy of various antimicrobial and anti-ulcer agents on the eradication of Campylobacter pylori in patients with antral gastritis or duodenal ulcers was investigated by several open studies or double-blind, placebo-controlled protocols. Among the anti-ulcer agents, ranitidine, cimetidine or sucraflate had no effect on C. pylori. Colloidal bismuth subcitrate achieved clearance of C. pylori in 40% of treated patients at the end of therapy but a high relapse rate (14/16 patients) was observed after a 6-month follow-up period. The antibacterial agents doxycycline, minocycline, ofloxacin, clindamycin, paromomycin and nifuroxazide failed to eradicate C. pylori in most patients. By contrast, short term elimination of C. pylori could be achieved in more than 90% of patients treated with amoxycillin. However, relapse occurred as a rule in all amoxycillin-treated patients within one month after therapy. Overall, we observed no correlation between the in-vitro activity of the different antibacterial agents and their in vivo efficacy. Development of resistance during therapy does not seem to account for this discrepancy since it occurred only with ofloxacin. On the basis of these results, we conclude that long term eradication of C. pylori from the gastric antrum cannot be achieved after monotherapy either with antibiotics or with bismuth salts. PMID:2979039

  9. Fluorescence imaging for a noninvasive in vivo toxicity-test using a transgenic silkworm expressing green fluorescent protein.

    Science.gov (United States)

    Inagaki, Yoshinori; Matsumoto, Yasuhiko; Ishii, Masaki; Uchino, Keiro; Sezutsu, Hideki; Sekimizu, Kazuhisa

    2015-06-10

    In drug development, the toxicity of candidate chemicals must be carefully examined in an animal model. Here we developed a live imaging technique using silkworms for a noninvasive toxicity test applicable for drug screening. Injection of carbon tetrachloride, a tissue-injuring chemical, into transgenic silkworms expressing green fluorescent protein (GFP) induced leakage of GFP from the tissues into the hemolymph. The leakage of GFP was suppressed by pre-administration of either cimetidine, a cytochrome P450 inhibitor, or N-acetyl cysteine, a free-radical scavenger. The transgenic silkworm was made transparent by feeding a diet containing chemicals that inhibit uric acid deposition in the epithelial cells. In the transparent silkworms, GFP fluorescence in the fat body could be observed from outside the body. Injection of salicylic acid or iron sulfate, tissue-injuring chemicals, into the transparent silkworms decreased the fluorescence intensity of the GFP in the fat body. These findings suggest that the transparent GFP-expressing silkworm model is useful for evaluating the toxicity of chemicals that induce tissue injury.

  10. A Sensitive Medium-Throughput Method to Predict Intestinal Absorption in Humans Using Rat Intestinal Tissue Segments.

    Science.gov (United States)

    Da Silva, Laís Cristina; Da Silva, Taynara Lourenço; Antunes, Alisson Henrique; Rezende, Kênnia Rocha

    2015-09-01

    A range of in vitro, ex vivo, and in vivo approaches are currently used for drug development. Highly predictive human intestinal absorption models remain lagging behind the times because of numerous variables concerning permeability through gastrointestinal tract in humans. However, there is a clear need for a drug permeability model early in the drug development process that can balance the requirements for high throughput and effective predictive potential. The present study developed a medium throughput screening Snapwell (MTS-Snapwell) ex vivo model to provide an alternative method to classify drug permeability. Rat small intestine tissue segments were mounted in commercial Snapwell™ inserts. Unidirectional drug transport (A-B) was measured by collecting samples at different time points. Viability of intestinal tissue segments was measured by examining transepithelial electric resistance (TEER) and phenol red and caffeine transport. As a result, the apparent permeability (Papp; ×10(-6) cm/s) was determined for atenolol (10.7 ± 1.2), caffeine (17.6 ± 3.1), cimetidine (6.9 ± 0.1), metoprolol (12.6 ± 0.7), theophylline (15.3 ± 1.6) and, ranitidine (3.8 ± 0.4). All drugs were classified in high/low permeability according to Biopharmaceutics Classification System showing high correlation with human data (r = 0.89). These findings showed a high correlation with human data (r = 0.89), suggesting that this model has potential predictive capacity for paracellular and transcellular passively absorbed molecules.

  11. FACTORS AFFECTING PHARMACOKINETIC DISPOSITION OF DRUGS

    Directory of Open Access Journals (Sweden)

    Mehta Hiren R

    2011-05-01

    Full Text Available Absorption of drugs from the gastrointestinal tract is a complex process the variability of which is influenced by many physicochemical and physiologic factors. The two most important physicochemical factors that affect both the extent and the rate of absorption are lipophilicity and solubility. The rate and extent of absorption are governed by the solubility, permeability and stability of the drug, with solubility being a pH-dependent parameter for weak acids and bases. The gastrointestinal tract can be viewed as discrete sections with a variety of differential local pH environments ranging from the acidic stomach to the more basic small intestine. The multiple peaking, double peaking or secondary peaking phenomena can occur in the disposition of a variety of xenobiotics during drug development (the pre-clinical phase and in subsequent clinical studies and use. The physicochemical and physiological mechanisms underlying the occurrence of this phenomenon are often multi factorial and include but are not limited to solubility-limited absorption, modified-release formulations, complexation, enterohepatic recirculation, gastric emptying and the intestinal transit time, site-specific absorption, gastric secretion-enteral reabsorption. Double peak absorption has been described with several orally administered drugs such as cimetidine furosemide, piroxicam, ranitidine, talinolol, alprazolam and phenazopyridine.

  12. Review of therapeutic agents for burns pruritus and protocols for management in adult and paediatric patients using the GRADE classification

    Directory of Open Access Journals (Sweden)

    Goutos Ioannis

    2010-10-01

    Full Text Available To review the current evidence on therapeutic agents for burns pruritus and use the Grading of Recommendations, Assessment, Development and Evaluation (GRADE classification to propose therapeutic protocols for adult and paediatric patients. All published interventions for burns pruritus were analysed by a multidisciplinary panel of burns specialists following the GRADE classification to rate individual agents. Following the collation of results and panel discussion, consensus protocols are presented. Twenty-three studies appraising therapeutic agents in the burns literature were identified. The majority of these studies (16 out of 23 are of an observational nature, making an evidence-based approach to defining optimal therapy not feasible. Our multidisciplinary approach employing the GRADE classification recommends the use of antihistamines (cetirizine and cimetidine and gabapentin as the first-line pharmacological agents for both adult and paediatric patients. Ondansetron and loratadine are the second-line medications in our protocols. We additionally recommend a variety of non-pharmacological adjuncts for the perusal of clinicians in order to maximise symptomatic relief in patients troubled with postburn itch. Most studies in the subject area lack sufficient statistical power to dictate a ′gold standard′ treatment agent for burns itch. We encourage clinicians to employ the GRADE system in order to delineate the most appropriate therapeutic approach for burns pruritus until further research elucidates the most efficacious interventions. This widely adopted classification empowers burns clinicians to tailor therapeutic regimens according to current evidence, patient values, risks and resource considerations in different medical environments.

  13. Mechanisms of cardiovascular activity of Andrographis paniculata in the anaesthetized rat.

    Science.gov (United States)

    Zhang, C Y; Tan, B K

    1997-04-01

    The cardiovascular activities of crude water extract (WE) of Andrographis paniculata (Burm. f.) Nees (Acanthaceae), its three semi-purified ethyl acetate (FA), n-butanol (FB) and aqueous (FC) fractions, as well as andrographolide, a major plant constituent, were elucidated in anaesthetized Sprague-Dawley (SD) rats for the very first time. FA and andrographolide, which possesses multiple pharmacological activities, elicited no drop in mean arterial blood pressure (MAP), while WE, FB and FC produced a significant fall in MAP in a dose-dependent manner without significant decrease in heart rate. The ED50 values for WE, FB and FC were 11.4, 5.0 and 8.6 mg/kg-respectively. These suggested that the hypotensive substance(s) of the crude water extract was concentrated in FB. Pharmacological antagonist studies were consequently only tested in FB (5 mg/kg). The hypotensive action of FB was not mediated through effects on the beta-adrenoceptor, muscarinic cholinergic receptor and angiotensin-converting enzyme, for it was not affected by propranolol, atropine and captapril, respectively. However, it seems to work via alpha-adrenoceptors, autonomic ganglion and histaminergic receptors, since the hypotensive effect of FB was negated or attenuated in the presence of phentolamine, hexamethonium as well as pyrilamine and cimetidine. PMID:9174969

  14. Cardiovascular activity of 14-deoxy-11,12-didehydroandrographolide in the anaesthetised rat and isolated right atria.

    Science.gov (United States)

    Zhang, C; Kuroyangi, M; Tan, B K

    1998-12-01

    The cardiovascular activity of 14-deoxy-11,12-didehydroandrographolide (DDA) from Andrographis paniculata (Burm.f.) Nees (Acanthaceae) was elucidated in anaesthetised Sprague-Dawley (SD) rats and isolated rat right atria. In anaesthetised rats, DDA produced significant falls in mean arterial blood pressure (MAP) and heart rate in a dose-dependent manner with the maximum decrease of 37.6 +/- 2.6% and 18.1 +/- 4.8%, respectively. The ED50 value for MAP was 3.43 mmol kg-1. Pharmacological antagonist studies were done using this dose. The hypotensive action of DDA was not mediated through effects on the alpha-adrenoceptor, muscarinic cholinergic and histaminergic receptors, for it was not affected by phentolamine, atropine as well as pyrilamine and cimetidine. However, it seems to work via adrenoceptors, autonomic ganglia receptor and angiotensin-converting enzyme, since the hypotensive effect of DDA was negated or attenuated in the presence of propranolol, hexamethonium and captopril. In the isolated right atria, DDA caused negative chronotropic action and antagonised isoproterenol-induced positive chronotropic actions in a non-competitive and dose-dependent manner. These results further supported the bradycardia-inducing and beta-adrenoceptor antagonistic properties of DDA in vivo. PMID:9990649

  15. Proton-Coupled Organic Cation Antiporter Contributes to the Hepatic Uptake of Matrine.

    Science.gov (United States)

    Wu, Chunyong; Sun, Xiaomin; Feng, Chao; Liu, Xiaoying; Wang, Hufang; Feng, Fang; Zhang, Junying

    2016-03-01

    Matrine is the major bioactive alkaloid found in certain Sophora plants and has been used for the treatment of liver diseases and protection of liver function. The aim of this study was to investigate the human liver uptake mechanism of matrine by using HepG2 cells as the in vitro model. Matrine was transported into HepG2 cells in a time- and temperature-dependent manner. The cellular uptake was saturable and was significantly reduced by the metabolic inhibitors, such as sodium azide and rotenone. Furthermore, the uptake of matrine was found to be regulated by a protonophore (carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone) and pH, indicating that this influx transporter may be a proton-coupled antiporter. The uptake of matrine was sensitive to inhibition by the cationic drugs including pyrilamine, quinidine, verapamil, amantadine, diphenhydramine, and cimetidine but insensitive to other typical substrates or inhibitors of well-known organic cation transport systems. The present study reveals that, for the first time, in HepG2 cells, the existence of a proton-coupled organic cation antiporter that contributes substantially to the hepatic uptake of matrine.

  16. Crystal structure and theoretical study of IR and 1H and 13C NMR spectra of cordatin, a natural product with antiulcerogenic activity

    Science.gov (United States)

    Brasil, Davi S. B.; Alves, Cláudio N.; Guilhon, Giselle M. S. P.; Muller, Adolfo H.; Secco, Ricardo De S.; Peris, Gabriel; Llusar, Rosa

    Cordatin is a furan diterpenoid with a clerodane skeleton isolated from Croton palanostigma Klotzsch (Euphorbiaceae). This natural product shows significant antiulcerogenic activity, similar to cimetidine (Tagamet®), a compound used for the treatment of peptic ulcers. The crystal structure of cordatin was obtained by X-ray diffraction and its geometrical parameters were compared with theoretical calculations at the B3LYP theory level. The IR and NMR (1H and 13C chemical shifts and coupling constants) spectra were obtained and compared with the theoretical calculations. The B3LYP theory level, with the 6-31G(d,p) and 6-311G(d,p) basis set, provided IR absorption values close to the experimental data. Moreover, theoretical NMR parameters obtained in both gas phase and chloroform solvent at the B3PW91/DGDZVP, B3LYP/6-311+G(2d,p), and B3PW91/6-311+G(2d,p) levels showed good correlations with the experimental results.

  17. Successful treatment of florid cutaneous warts with intravenous cidofovir in an 11-year-old girl.

    Science.gov (United States)

    Cusack, Caitriona; Fitzgerald, Deborah; Clayton, Timothy M; Irvine, Alan D

    2008-01-01

    Cutaneous warts, commonly seen in children and the immunosuppressed are socially distressing and are often resistant to traditional treatments. Here, we report an 11-year-old girl with bilateral florid verrucous lesions on her hands, feet and chin, which were refractory to a number of standard treatments including cryotherapy, cantharidin preparations, topical salicylic acid, surgical debulking techniques, oral Cimetidine, and topical and intralesional Cidofovir. As the disfiguring lesions had a marked adverse effect on her quality of life, a trial of IV Cidofovir was instituted. We administered five cycles of IV Cidofovir with a 1-week interval between the first and second treatment, followed by 2-week intervals thereafter. This regime was well tolerated and we report dramatic resolution of the lesions with persistent clearance 6 months after completion of the fifth infusion. Resolution of recalcitrant warts with IV Cidofovir has been reported in a limited number of cases. Our experience supports its efficacy in this setting, and to the best of our knowledge this is the first report of successful treatment of cutaneous warts with IV Cidofovir in a pediatric case. PMID:18577053

  18. Treatment of molluscum contagiosum: a brief review and discussion of a case successfully treated with adapelene.

    Science.gov (United States)

    Scheinfeld, Noah

    2007-01-01

    Molluscum contagiosum occur in 2-8 percent of children. This infection is among the most common viral skin infections in children. Although the lesions will resolve spontaneously when puberty, there are several reasons to treat them. The lesions can be cosmetically unappealing. About 10 percent of those with this infection develop a pruritic eczematous eruption. In about 4 percent of children with molluscum, the lesions are numerous and recurrent with no other coexisting immunological problem. Patients who have atopic dermatitis may develop widespread involvement with molluscum. Treatment options include destruction, topical therapy, and oral therapy. Destructive treatment modalities include curettage, cryotherapy, expression or pricking with a sterile needle, electrodesiccation, photodynamic therapy, and laser ablation. Destructive therapy is poorly tolerated in children. Topical medical therapy includes salicylic acid, glycolic acid, tretinoin, tazortene, 5 percent sodium nitrite co-applied daily with 5 percent salicylic acid topical preparations, podofilox, liquefied phenol, tretinoin, cantharidin, and potassium hydroxide. Oral treatment of molluscum includes cimetidine. No therapy is universally effective. I report herein a case of generalized numerous and recurrent molluscum treated with minimal irritation with adapelene. PMID:18328209

  19. Immunomodulators in warts: Unexplored or ineffective?

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    Surabhi Sinha

    2015-01-01

    Full Text Available Cutaneous warts are known to be recurrent and often resistant to therapy. Resistant warts may reflect a localized or systemic cell mediated immune (CMI deficiency to HPV. Many modalities of treatment are in use; most of the provider-administered therapies are destructive and cause scarring, such as cryotherapy, chemical cauterisation, curettage, electrodessication and laser removal. Most patient-applied agents like podophyllotoxin have the risk of application-site reactions and recurrence. Thus immunotherapy is a promising modality which could lead to resolution of warts without any physical changes or scarring and in addition would augment the host response against the causative agent, thereby leading to complete resolution and decreased recurrences. Immunomodulators can be administered systemically, intralesionally or intradermally, and topically. A few agents have been tried and studied extensively such as cimetidine and interferons; others are new on the horizon, such as Echinacea, green tea catechins and quadrivalent HPV vaccine, and their efficacy is yet to be completely established. Though some like levamisole have shown no efficacy as monotherapy and are now used only in combination, other more recent agents require large and long term randomized placebo-controlled trials to clearly establish their efficacy or lack of it. In this review, we focus on the immunomodulators that have been used for the treatment of warts and the studies that have been conducted on them.

  20. Evolving role of immunotherapy in the treatment of refractory warts

    Directory of Open Access Journals (Sweden)

    Devinder M Thappa

    2016-01-01

    Full Text Available Cutaneous and genital warts are common dermatological conditions caused by the human papilloma virus (HPV. Although it is a benign condition, it causes disfigurement, has a tendency to koebnerize, and can be transmitted to others. This makes adequate and timely treatment important. There are several conventional treatments available with variable response. Topical and systemic immunotherapy has now found a significant place in the treatment of warts because of its nondestructive action, ease of use, and promising results. Through this review, we would like to present a brief overview of the various immunotherapeutic agents used. These include more established agents such as imiquimod, Mycobacterium w vaccine, bacillus Calmette-Guérin vaccine, measles, mumps, and rubella vaccine, Candida antigen, trichophyton antigen, tuberculin, zinc, cimetidine, levamisole, HPV vaccine, and autoimplantation therapy. Other agents such as contact immunotherapy which is sparsely used now than before and newer agents such as Corynebacterium parvum, sinecatechins, echinacea, propolis, glycyrrizinic acid, and Vitamin D have also been discussed. The mechanism of action of these agents, along with their dosage, mode of administration, duration of use, expected outcomes and comparative efficacy, evidence for their use, and expected side effects, if any, are reviewed.

  1. Effects of Flos carthami on CYP2D6 and on the Pharmacokinetics of Metoprolol in Rats

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    Gaofeng Liu

    2011-01-01

    Full Text Available Flos carthami is a traditional Chinese herbal medicine. Clinically, the Flos carthami Injection has been used concomitantly with other Western drugs and may be used concomitantly with β-blockers, such as metoprolol, to treat cerebrovascular and coronary heart diseases, in China. Metoprolol is a CYP2D6 substrate and is predominantly metabolized by this isozyme. However, we do not know whether there is an effect of Flos carthami on CYP2D6 and the consequences of such an effect. Concern is raised regarding the possible herb-drug interaction. In this report, the effects of Flos carthami on the activity of CYP2D6 in vivo and in vitro and on the pharmacokinetics of metoprolol, in rats, are investigated. To assess the inhibitory potency of Flos carthami, the concentration associated with 50% inhibition (IC50 of dextromethorphan metabolism was determined based on the concentration-inhibition curves. The inhibitory effect of Flos carthami on CYP2D6 was also compared with cimetidine in vitro. Flos carthami could significantly inhibit CYP2D6 in rats both in vitro and in vivo (P<.05 and could slow down the metabolic rate of metoprolol as suggested by prolonged t1/2 (67.45%, by increased Cmax (74.51% and AUC0−∞ (76.89%. These results suggest that CYP2D6 is a risk factor when Flos carthami is administered concomitantly with metoprolol or other CYP2D6 substrates.

  2. Adoptive chemoimmunotherapy using ex vivo activated memory T-cells and cyclophosphamide: tumor lysis syndrome of a metastatic soft tissue sarcoma.

    Science.gov (United States)

    Gold, J E; Malamud, S C; LaRosa, F; Osband, M E

    1993-09-01

    Adoptively transferred immune cells in combination with chemotherapeutic agents form the basis for adoptive chemoimmunotherapy (ACIT) of neoplastic disease. Autolymphocytes (ALT-cells) are ex vivo activated peripheral blood lymphocytes (PBL) from tumor-bearing hosts (TBH) that consist primarily of tumor-specific CD45RO+ (memory) T-cells. These ALT-cells combined with cimetidine (CIM) as autolymphocyte therapy (ALT), have previously been demonstrated to be a safe and active form of outpatient adoptive immunotherapy (AIT) in human TBH with metastatic renal cell cancer (RCC). We have previously described an effective ACIT protocol using ALT and cyclophosphamide (CY) for patients with relapsed and refractory non-RCC solid tumors. We now report a case of a patient with a metastatic gastric leiomyosarcoma to the liver, who developed a clinical picture consistent with a tumor-lysis syndrome (TLS), following salvage therapy for his tumor with ACIT using ALT and CY. TLS is a well-known complication resulting from the treatment of rapidly proliferating hematopoietic tumors such as Burkitt's lymphoma and acute lymphocytic leukemia. TLS has also been rarely described in chronic lymphocytic leukemia, as well as certain solid tumors such as breast cancer, small cell lung cancer, and medulloblastoma. However, there have been no previous reports of TLS occurring either secondary to immunotherapy or in sarcomas. The nature of these unusual findings is discussed. PMID:8342564

  3. Pharmacologic considerations for patients taking oral contraceptives.

    Science.gov (United States)

    Hassan, T

    1987-03-01

    This is a brief review of the theoretical and known drug reactions with oral contraceptives. There are at least 6 possible types of drug reactions that may affect the action of oral contraceptives, not including malabsorption related to changes in intestinal motility or flora. Ampicillin is an example of an antibiotic that may cause diarrhea, thereby reducing absorption of pill steroids. The steroids in orals are subject to enterohepatic circulation, which is in turn affected by the gut flora. Antibiotics known to suppress gut flora include: penicillins, cephalosporins, tetracyclines, sulfas, neomycin and erythromycin. Although controlled clinical trials of antibiotic intake with oral contraception have not shown significant interactions, anecdotal reports of pill failures have been published. The other important drug interaction affecting contraception by orals is enhanced hepatic degradation, as seen with rifampicin. Other drugs such as cimetidine, MAO-inhibitor antidepressants, chloramphenicol, influenza or BCG vaccine, isoniazid, warfarin, metronidazole and disulfiram may delay steroid metabolism and possibly increase side effects. When prescribing drugs it is important to realize that certain drugs decrease oral contraceptive concentrations: antibiotics anticonvulsants, griseofulvin, purgatives and rifampicin. PMID:3155374

  4. Macrolide antibacterials. Drug interactions of clinical significance.

    Science.gov (United States)

    von Rosensteil, N A; Adam, D

    1995-08-01

    Macrolide antibiotics can interact adversely with commonly used drugs, usually by altering metabolism due to complex formation and inhibition of cytochrome P-450 IIIA4 (CYP3A4) in the liver and enterocytes. In addition, pharmacokinetic drug interactions with macrolides can result from their antibiotic effect on microorganisms of the enteric flora, and through enhanced gastric emptying due to a motilin-like effect. Macrolides may be classified into 3 different groups according to their affinity for CYP3A4, and thus their propensity to cause pharmacokinetic drug interactions. Troleandomycin, erythromycin and its prodrugs decrease drug metabolism and may produce drug interactions (group 1). Others, including clarithromycin, flurithromycin, midecamycin, midecamycin acetate (miocamycin; ponsinomycin), josamycin and roxithromycin (group 2) rarely cause interactions. Azithromycin, dirithromycin, rikamycin and spiramycin (group 3) do not inactivate CYP3A4 and do not engender these adverse effects. Drug interactions with carbamazepine, cyclosporin, terfenadine, astemizole and theophylline represent the most frequently encountered interactions with macrolide antibiotics. If the combination of a macrolide and one of these compounds cannot be avoided, serum concentrations of concurrently administered drugs should be monitored and patients observed for signs of toxicity. Rare interactions and those of dubious clinical importance are those with alfentanil and sufentanil, antacids and cimetidine, oral anticoagulants, bromocriptine, clozapine, oral contraceptive steroids, digoxin, disopyramide, ergot alkaloids, felodipine, glibenclamide (glyburide), levodopa/carbidopa, lovastatin, methylprednisolone, phenazone (antipyrine), phenytoin, rifabutin and rifampicin (rifampin), triazolam and midazolam, valproic acid (sodium valproate) and zidovudine. PMID:7576262

  5. Hypothermic and antipyretic effects of ACTH (1-24) and alpha-melanotropin in guinea-pigs

    Science.gov (United States)

    Kandasamy, S. B.; Williams, B. A.

    1984-01-01

    Intracerebroventricular administration of adrenocorticotropin (ACTH 1-24) and alpha-melanotropin (alpha-MSH), peptides which occur naturally in brain induced dose-related hypothermia in guinea-pigs at room temperature (21 C) and also produced greater hypothermia at low (10 C) ambient temperature. However, when the experiments were repeated in a warm (30 C) environment, no effect on body temperature was observed. These results indicate that the peptides did not reduce the central set-point of temperature control. The hypothermia induced by ACTH and alpha-MSH was not mediated via histamine H1- or H2-receptors and serotonin since the H1-receptor antagonist, mepyramine, the H2-receptor antagonist, cimetidine, and the serotonin antagonist, methysergide, had no antagonistic effects. The peptides were antipyretic since they reduced pyrogen-induced-fever and hyperthermia due to prostaglandin E2, norepinephrine and dibutyryl cAMP, at a dose which did not affect normal body temperature. The powerful central effects of these peptides on normal body temperature, fever and hyperthermia, together with their presence of the brain regions important to temperature control, suggest that they participate in thermoregulation.

  6. Involvement of H1 and H2 receptors and soluble guanylate cyclase in histamine-induced relaxation of rat mesenteric collecting lymphatics

    Science.gov (United States)

    Kurtz, Kristine H.; Moor, Andrea N.; Souza-Smith, Flavia M.; Breslin, Jerome W.

    2014-01-01

    Objective This study investigated the roles of the H1 and H2 histamine receptors, nitric oxide (NO) synthase, and soluble guanylate (sGC) cyclase in histamine-induced modulation of rat mesenteric collecting lymphatic pumping. Methods Isolated rat mesenteric collecting lymphatics were treated with 1–100 μM histamine. Histamine receptors were blocked with either the H1 antagonist mepyramine or the H2 antagonist cimetidine. The role of NO/sGC signaling was tested using the arginine analog L-NAME, the sGC inhibitor ODQ, and sodium nitroprusside (SNP) as a positive control. Results Histamine applied at 100 μM decreased tone and contraction frequency (CF) of isolated rat mesenteric collecting lymphatics. Pharmacologic blockade of either H1 or H2 histamine receptors significantly inhibited the response to histamine. Pretreatment with ODQ, but not L-NAME, completely inhibited the histamine-induced decrease in tone. ODQ pretreatment also significantly inhibited SNP-induced lymphatic relaxation. Conclusions H1 and H2 histamine receptors are both involved in histamine-induced relaxation of rat mesenteric collecting lymphatics. NO synthesis does not appear to contribute to the histamine-induced response. However, sGC is critical for the histamine-induced decrease in tone and contributes to the drop in CF. PMID:24702851

  7. A new approach for trace analysis of guanidine compounds in surface water with resorcinarene-based ion chromatography columns.

    Science.gov (United States)

    Panahi, Tayyebeh; Weaver, Douglas J; Lamb, John D; Harrison, Roger G

    2016-02-01

    Trace levels of pharmaceuticals have been detected in surface water and may pose a health risk to humans and other organisms. New chromatographic materials will help identify and quantify these contaminants. We introduce a new ion chromatographic (IC) material designed to separate cationic pharmaceuticals and report its ability to separate a group of guanidine compounds. Guanidine moieties are strongly basic and protonated under acid conditions, and therefore can potentially be separated on the newly designed stationary phase and detected by ion exchange chromatography. The new column packing material is based on glutamic acids bonded to resorcinarene moieties that in turn are bound to divinylbenzene macroporous resin. Detection limits in the range of 5-30 μg L(-1) were achieved using integrated pulsed amperometric detection (IPAD) for guanidine (G), methylguanidine (MG), 1,1-dimethylbiguanide (DMG), agmatine (AGM), guanidinobenzoic acid (GBA) and cimetidine (CIM). Suppressed conductivity (CD) and UV-vis detection resulted in limits of detection similar to IPAD, in the range of 2-66 μg L(-1), but were not able to detect all of the analytes. Three water sources, river, lake, and marsh, were analyzed and despite matrix effects, sensitivity for guanidine compounds was in the 100 μg L(-1) range and apparent recoveries were 80-96%. The peak area precision was 0.01-2.89% for IPAD, CD and UV-vis detection. PMID:26649362

  8. Prokinetic Activity of Prunus persica (L. Batsch Flowers Extract and Its Possible Mechanism of Action in Rats

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    Wei Han

    2015-01-01

    Full Text Available The peach tree, Prunus persica (L. Batsch, is widely cultivated in China, and its flowers have been used for centuries in traditional Chinese medicine to treat gut motility disorders. But few studies have explored the pharmacological effect of Prunus persica (L. Batsch flowers on gastrointestinal motility. In this study, the activities of different extracts from Prunus persica (L. Batsch flowers on the smooth muscle contractions were evaluated using isolated colon model, and the ethyl acetate extract (EAE showed the strongest effects in vitro. EAE (10−8–10−5 g/mL caused a concentration-dependent stimulatory effect in rat colonic tissue. Additionally, ketotifen (100 µM, cimetidine (10 µM, and pyrilamine (1 µM produced a significant inhibition of contractions caused by EAE. Furthermore, immunofluorescence and toluidine blue staining revealed increased numbers of mast cells in the EAE group, and EAE increased histamine release from the colonic tissues. These data indicate that EAE has significant prokinetic activity and acts by a mechanism that mainly involves mast cell degranulation. Our study provides a pharmacological basis for the use of an extract of Prunus persica (L. Batsch flowers in the treatment of gut motility disorders.

  9. Simultaneous determination of moxifloxacin and H2 receptor antagonist in pharmaceutical dosage formulations by RP-HPLC: application to in vitro drug interactions

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    Najma Sultana

    2011-01-01

    Full Text Available Simultaneous determination of moxifloxacin (MOX and H2-antagonists was first time developed in bulk and formulations. Purospher STAR C18 (250 x 4.6 mm, 5 μm column was used. The mobile phase (methanol: water: ACN, 60:45:5 v/v/v, pH 2.7 was delivered at a flow rate of 1.0 mL min-1, eluent was monitored at 236, 270 and 310 nm for cimetidine, famotidine and ranitidine, respectively. The proposed method is specific, accurate (98-103%, precise (intra-day and inter-day variation 0.098-1.970% and linear (r>0.998. The LOD and LOQ were 0.006-0.018 and 0.019-0.005 μg mL-1, respectively. The statistical parameters were applied to verify the results. The method is applicable to routine analysis of formulations and interaction of MOX with H2-antagonist.

  10. Modeling uptake of selected pharmaceuticals and personal care products into food crops from biosolids-amended soil.

    Science.gov (United States)

    Prosser, Ryan S; Trapp, Stefan; Sibley, Paul K

    2014-10-01

    Biosolids contain a variety of pharmaceuticals and personal care products (PPCPs). Studies have observed the uptake of PPCPs into plants grown in biosolids-amended soils. This study examined the ability of Dynamic Plant Uptake (DPU) model and Biosolids-amended Soil Level IV (BASL4) model to predict the concentration of eight PPCPs in the tissue of plants grown in biosolids-amended soil under a number of exposure scenarios. Concentrations in edible tissue predicted by the models were compared to concentrations reported in the literature by calculating estimated human daily intake values for both sets of data and comparing them to an acceptable daily intake value. The equilibrium partitioning (EqP) portion of BASL4 overpredicted the concentrations of triclosan, triclocarban, and miconazole in root and shoot tissue by two to three orders of magnitude, while the dynamic carrot root (DCR) portion overpredicted by a single order of magnitude. DPU predicted concentrations of triclosan, triclocarban, miconazole, carbamazepine, and diphenhydramine in plant tissues that were within an order of magnitude of concentrations reported in the literature. The study also found that more empirical data are needed on the uptake of cimetidine, fluoxetine, and gemfibrozil, and other ionizable PPCPs, to confirm the utility of both models. All hazard quotient values calculated from literature data were below 1, with 95.7% of hazard quotient values being below 0.1, indicating that consumption of the chosen PPCPs in plant tissue poses de minimus risk to human health. PMID:25207852

  11. Antihistamines block radiation-induced increased intestinal blood flow in canines

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Doyle, T.F.; Donlon, M.A.; Gossett-Hagerman, C.J.

    1985-06-01

    Radiation-induced systemic hypotension is accompanied by increased intestinal blood flow (IBF) and an increased hematocrit (HCT) in dogs. Histamine infusion leads to increased IBF and intestinal edema with consequent secretion of fluid into the intestinal lumen. This study was performed to determine whether these effects could be diminished by prior administration of H1 and H2 histamine blockers. Dogs were given an iv infusion of mepyramine (0.5 mg/min) and cimetidine (0.25 mg/min) for 1 hr before and for 1 hr after radiation (H1 and H2 blockers, respectively). Mean systemic arterial blood pressure (MBP), IBF, and HCT were monitored for 2 hr. Systemic plasma histamine levels were determined simultaneously. Data obtained indicated that the H1 and H2 blockers, given simultaneously, were successful in blocking the increased IBF and the increased HCT seen after 100 Gy, whole-body, gamma radiation. However, the postradiation hypotension was only somewhat affected, with the MBP falling to a level 28% below the preradiation level. Plasma histamine levels reached a sharp peak, as much as 20% above baseline, at 4 min postradiation. These findings implicate histamine in the radiation-induced increase in IBF and HCT but not for the gradual decrease in postradiation blood pressure.

  12. Effect of disodium cromoglycate (DSCG) and antihistamines on post-irradiation cerebral blood flow and plasma levels of histamine and neurotensin

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Pautler, E.L.; Carraway, R.E.; Cochrane, D.E.; Hampton, J.D.

    1988-01-01

    In an attempt to elucidate mechanisms underlying the irradiation-induced decrease in regional cerebral blood flow (rCBF) in primates, hippocampal and visual cortical blood flows of rhesus monkeys were measured by hydrogen clearance, before and after exposure to 100-Gy, whole-body, gamma irradiation. Systemic blood pressures were monitored simultaneously. Systemic arterial plasma histamine and neurotensin levels were determined preirradiation and postirradiation. Compared to control animals, the irradiated monkeys exhibited an abrupt decline in systemic blood pressure to 23% of the preirradiation level within 10-min postirradiation, falling to 12% by 60 min. A decrease in hippocampal blood flow to 32% of the preirradiation level was noted at 10-min postirradiation, followed by a slight recovery to 43% at 30 min and a decline to 23% by 60 min. The cortical blood flow for the same animals showed a steady decrease to 29% of the preirradiation levels by 60-min postirradiation. Animals given the mast-cell stabilizer disodium cromoglycate and the antihistamines mepyramine and cimetidine before irradiation did not exhibit an abrupt decline in blood pressure but displayed a gradual decrease to a level 33% below preirradiation levels by 60 min postirradiation. Also, the treated, irradiated monkeys displayed rCBF values that were not significantly different from the nonirradiated controls. The plasma neurotensin levels in the irradiated animals, treated and untreated, indicated a nonsignificant postirradiation increase above control levels.

  13. Exposure to heavy charged particles affects thermoregulation in rats

    Energy Technology Data Exchange (ETDEWEB)

    Kandasamy, S.B.; Hunt, W.A.; Dalton, T.K.; Joseph, J.A.; Harris, A.H. [Armed Forces Radiobiology Research Institute, Bethesda, MD (United States); Rabin, B.M. [Armed Forces Radiobiology Research Institute, Bethesda, MD (United States)]|[Univ. of Maryland, Baltimore, MD (United States)

    1994-09-01

    Rats exposed to 0.1-5 Gy of heavy particles ({sup 56}Fe, {sup 40}Ar, {sup 20}Ne or {sup 4}He) showed dose-dependent changes in body temperature. Lower doses of all particles produced hyperthermia, and higher doses of {sup 20}Ne and {sup 56}Fe produced hypothermia. Of the four HZE particles, {sup 56}Fe particles were the most potent and {sup 4}He particles were the least potent in producing changes in thermoregulation. The {sup 20}Ne and {sup 40}Ar particles produced an intermediate level of change in body temperature. Significantly greater hyperthermia was produced by exposure to 1 Gy of {sup 20}Ne, {sup 40}Ar and {sup 56}Fe particles than by exposure to 1 Gy of {sup 60}Co {gamma} rays. Pretreating rats with the cyclo-oxygenase inhibitor indomethacin attenuated the hyperthermia produced by exposure to 1 Gy of {sup 56}Fe particles, indicating that prostaglandins mediate {sup 56}Fe-particle-induced hyperthermia. The hypothermia produced by exposure to 5 Gy of {sup 56}Fe particles is mediated by histamine and can be attenuated by treatment with the antihistamines mepyramine and cimetidine. 15 refs., 4 figs.

  14. Antihistamines block radiation-induced increased intestinal blood flow in canines

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Doyle, T.F.; Donlon, M.A.; Gossett-Hagerman, C.J.

    1985-01-01

    Radiation-induced systemic hypotension is accompanied by increased intestinal blood flow (IBF) and an increased hematocrit (HCT) in dogs. Histamine infusion leads to increased IBF and intestinal edema with consequent secretion of fluid into the intestinal lumen. This study was performed to determine whether these effects could be diminished by prior administration of H/sub 1/ and H/sub 2/ histamine blockers. Dogs were given an iv infusion of mepyramine (0.5 mg/min) and cimetidine (0.25 mg/min) for 1 hr before and for 1 hr after radiation (H sub 1 and H sub 2 blockers, respectively). Mean systemic arterial blood pressure (MBP), IBF, and HCT were monitored for 2 hr. Systematic plasma histamine levels were determined simultaneously. Data obtained indicated that the H sub 1 and H sub 2 blockers, given simultaneously, were successful in blocking the increased IBF and the increased HCT seen after 100 Gy, whole-body, gamma radiation. However, the postradiation hypotension was only somewhat affected, with the MBP falling to a level 28% below the preradiation level. Plasma histamine levels reached a sharp peak, as much as 20% above baseline, at 4 min postradiation. These findings implicate histamine in the radiation-induced increase in IBF and HCT but not for the gradual decrease in postradiation blood pressure. (Author)

  15. Renal transepithelial transport of nucleosides.

    Science.gov (United States)

    Nelson, J A; Vidale, E; Enigbokan, M

    1988-01-01

    Previous work from this and other laboratories has suggested that the mammalian kidney has unique mechanisms for handling purine nucleosides. For example, in humans and in mice, adenosine undergoes net renal reabsorption whereas deoxyadenosine is secreted [Kuttesch and Nelson: Cancer Chemother. Pharmacol. 8, 221 (1982)]. The relationships between these renal transport systems and classical renal organic cation and anion, carbohydrate, and cell membrane nucleoside transport carriers are not established. To investigate possible relationships between such carriers, we have tested effects of selected classical transport inhibitors on the renal clearances of adenosine, deoxyadenosine, 5'-deoxy-5-fluorouridine (5'-dFUR), and 5-fluorouracil in mice. The secretion of deoxyadenosine and 5'-dFUR, but not the reabsorption of adenosine or 5-fluorouracil, was prevented by the classical nucleoside transport inhibitors, dipyridamole and nitrobenzylthioinosine. Cimetidine, an inhibitor of the organic cation secretory system, also inhibited the secretion of 5'-dFUR, although it did not inhibit deoxyadenosine secretion in earlier studies [Nelson et al.: Biochem. Pharmacol. 32, 2323 (1983)]. The specific inhibitor of glucose renal reabsorption, phloridzin, failed to inhibit the reabsorption of adenosine or the secretion of deoxyadenosine. Failure of the nucleoside transport inhibitors and phloridzin to prevent adenosine reabsorption suggests that adenosine reabsorption may occur via a unique process. On the other hand, inhibition of the net secretion of deoxyadenosine and 5'-dFUR by dipyridamole and nitrobenzylthioinosine implies a role for the carrier that is sensitive to these compounds in the renal secretion (active transport) of these nucleosides.

  16. Effect of Flabellaria paniculata Cav. extracts on gastric ulcer in rats

    Directory of Open Access Journals (Sweden)

    Sofidiya Margaret O

    2012-10-01

    Full Text Available Abstract Background The leaves and root of Flabellaria paniculata (Malpighiaceae are frequently used in the treatment of wounds and ulcers in Nigerian folk medicine. The purpose of this study was to compare the effect of ethanolic extracts from the leaves (FPL and root (FPR of F. paniculata on gastric ulcers in rats. Methods The effect of FPL and FPR (100, 200 and 400 mg/kg was evaluated in ethanol and indomethacin gastric ulcer models. Control groups for FPL and FPR were orally treated with 3% Tween 20 and distilled water respectively. FPL was further investigated in pylorus ligation model. Misoprostol and cimetidine were used as reference. Results FPL significantly (P 50 of FPL was estimated to be 4570 mg/kg while that of FPR was 2754 mg/kg. The LD50 in intraperitoneal injection was estimated to be 1202.26 and 1380.38 mg/kg for FPL and FPR respectively. The phytochemical investigation showed that both extracts possess triterpenoids and saponin, while the presence of flavonoid was detected only in FPL. Conclusions The results of this study indicated that FPL and not FPR is effective against experimentally induced gastric ulcers. The presence of varied phytochemical constituents probably influenced the pharmacological differences between the two extracts.

  17. Oral dosing with papaya latex is an effective anthelmintic treatment for sheep infected with Haemonchus contortus

    Directory of Open Access Journals (Sweden)

    Donnan Alison A

    2011-03-01

    Full Text Available Abstract Background The cysteine proteinases in papaya latex have been shown to have potent anthelmintic properties in monogastric hosts such as rodents, pigs and humans, but this has not been demonstrated in ruminants. Methods In two experiments, sheep were infected concurrently with 5,000 infective larvae of Haemonchus contortus and 10,000 infective larvae of Trichostrongylus colubriformis and were then treated with the supernatant from a suspension of papaya latex from day 28 to day 32 post-infection. Faecal egg counts were monitored from a week before treatment until the end of the experiment and worm burdens were assessed on day 35 post-infection. Results We found that the soluble fraction of papaya latex had a potent in vivo effect on the abomasal nematode H. contortus, but not on the small intestinal nematode T. colubriformis. This effect was dose-dependent and at tolerated levels of gavage with papaya latex (117 μmol of active papaya latex supernatant for 4 days, the H. contortus worm burdens were reduced by 98%. Repeated treatment, daily for 4 days, was more effective than a single dose, but efficacy was not enhanced by concurrent treatment with the antacid cimetidine. Conclusions Our results provide support for the idea that cysteine proteinases derived from papaya latex may be developed into novel anthelmintics for the treatment of lumenal stages of gastro-intestinal nematode infections in sheep, particularly those parasitizing the abomasum.

  18. Investigating Photosensitized Properties of Natural Organic Matter and Effluent Organic Matter

    KAUST Repository

    Niu, Xi-Zhi

    2013-05-01

    The photosensitized processes significantly enhance photolysis of various chemicals in the aqueous system with dissolved organic matter (DOM) as sensitizer. The excitation of chromophores on the DOM molecule further generates reactive species as triplet states DOM, singlet oxygen, hydroxyl radical, carbonate radical etc. We investigated the photosensitization properties of Beaufort Fulvic Acid, Suwannee River Fulvic Acid, South Platte River Fulvic Acid, and Jeddah wastewater treatment plant effluent organic matter with a sunlight simulator. DOM photochemical properties were characterized by observing their performances in 3DOM*, singlet oxygen, hydroxyl radical production with indirect probing protocols. Sensitized degradation of 0.1 μM and 0.02 μM 2, 4, 6- Trimethylphenol exhibited higher pseudo-first-order rate constant than that of 10 μM. Pre-irradiated DOMs were found to be depressed in photochemical properties. Photolysis of 5 different contaminants: ibuprofen, bisphenol A, acetaminophen, cimetidine, and caffeine were found to be enhanced in the presence of sensitizers. The possible reaction pathways were revealed. Long time irradiance induced change in contaminants degradation kinetics in some DOM solutions, which was proposed to be due to the irradiation initiated indirect transformation of DOMs. Key Words: Photolysis Dissolved Organic Matter, Triplet State DOM, Singlet Oxygen, Hydroxyl Radical, Contaminants Degradation.

  19. Vitamin D: Pharmacokinetics and Safety When Used in Conjunction with the Pharmaceutical Drugs Used in Cancer Patients: A Systematic Review

    Energy Technology Data Exchange (ETDEWEB)

    Kennedy, Deborah A.; Cooley, Kieran; Skidmore, Becky; Fritz, Heidi; Campbell, Tara [Canadian College of Naturopathic Medicine, 1255 Sheppard Avenue East, Toronto, Ontario, M2K 1E2 (Canada); Seely, Dugald, E-mail: dseely@ccnm.edu [Canadian College of Naturopathic Medicine, 1255 Sheppard Avenue East, Toronto, Ontario, M2K 1E2 (Canada); Ottawa Integrative Cancer Centre, 29 Bayswater Avenue, Ottawa, Ontario, K1Y 2E5 (Canada)

    2013-03-11

    Vitamin D has reported anti-cancer and anti-inflammatory properties modulated through gene transcription and non-genomic signaling cascades. The purpose of this review was to summarize the available research on interactions and pharmacokinetics between vitamin D and the pharmaceutical drugs used in patients with cancer. Hypercalcemia was the most frequently reported side effect that occurred in high dose calcitriol. The half-life of 25(OH)D{sub 3} and/or 1,25(OH){sub 2}D{sub 3} was found to be impacted by cimetidine; rosuvastatin; prednisone and possibly some chemotherapy drugs. No unusual adverse effects in cancer patients; beyond what is expected from high dose 1,25(OH){sub 2}D{sub 3} supplementation, were revealed through this review. While sufficient evidence is lacking, supplementation with 1,25(OH){sub 2}D{sub 3} during chemotherapy appears to have a low risk of interaction. Further interactions with vitamin D{sub 3} have not been studied.

  20. Role of histamine H1-and H2-receptors in the cardiovascular system of the rabbit.

    Science.gov (United States)

    Sakai, K

    1980-01-01

    The effects of histamine were examined on the circulation of the blood-perfused heart, kidney, intestine, and hindlimb of rabbits. Single intrarterial injections of drugs were made into the perfusion system of the coronary, renal, mesenteric, or femoral vascular bed. In the hearts, histamine caused dose-dependent positive inotropic and chronotropic responses and vaso-constriction. 2-Methylhistamine, a relatively selective histamine H1-receptor agonist, produced vascular effects very similar to those of histamine, but had no cardiac actions at low and negative inotropic responses at high doses. 4-Methylhistamine, a relatively selective histamine H2-receptor agonist, induced slight vasodilatation and positive inotropic and chronotropic responses. In the renal, mesenteric, and femoral vascular beds, histamine and 2-methylhistamine caused vasoconstriction, while 4-methylhistamine induced slight vasodilatation. Mepyramine, a selective H1-receptor antagonist, blocked the vasoconstriction in response to histamine and 2-methylhistamine, but not the positive inotropic and chronotropic responses to histamine. The combined action of mepyramine and cimetidine (a selective H2-receptor antagonist) eliminated all cardiac and vascular effects of histamine. These results strongly support the view that in the cardiovascular system of the rabbit, H1-receptors mediate negative inotropic effects and vasoconstriction, whereas H2-receptors are responsible for positive inotropic and chronotropic effects and vasodilatation.

  1. Influence of patient medication on diagnostic accuracy in nuclear medicine

    International Nuclear Information System (INIS)

    Full text. In recently years many reports have published of unusual or unexpected changes in the biodistribution of radiopharmaceuticals which do not correlate with normality or disease. Whilst many extraneous factors can alter tracer kinetics it has become apparent that concomitant patient medication can be such a factor. If the clinician is unaware that patient is on drug therapy difficulties arise in making a accurate diagnosis. Most drug/radio pharmaceutical effects are those in which the functional status of the organ is altered as a result of the pharmacological action of the drug. Examples here are narcotic analgesics such as methadone, pethidine and morphine which cause spasm of the biliary tract due to contraction of the sphincter of Oddi and an altered transit time of the technetium labelled tracer. Cytotoxic drugs such as cyclophosphamide and vincristine can markedly affect tumour uptake of 67-gallium so that litter or no activity is taken up by the tumour. Nifedipine, because of its powerful calcium channel blocking activity is known to affect the radiolabelling of white cells and red cells and to affect uptake of Tc-99 m MDP into bones. Other important and confusing effects are caused by phenothiazines, cimetidine and oral contraceptives. In recent years it has been reported that drugs such as cyclosporin, azathioprine and heparin and derivatives of heparin can markedly interfere with cell labelling procedures. This review will consider some of the clinical effects of drugs and will also address the reporting of instances of drug/radio pharmaceutical interactions

  2. Histamine ameliorates spatial memory deficits induced by MK-801 infusion into ventral hippocampus as evaluated by radial maze task in rats

    Institute of Scientific and Technical Information of China (English)

    Li-sha XU; Li-xia YANG; Wei-wei HU; Xiao YU; Li MA; Lu-ying LIU; Er-qing WEI; Zhong CHEN

    2005-01-01

    Aim: To investigate the role of histamine in memory deficits induced by MK-801 infusion into the ventral hippocampus in rats. Methods: An 8-arm radial maze (4arms baited) was used to assess spatial memory. Results: Bilateral ventral intrahippocampal (ih) infusion of MK-801 (0.3 μg/site), an N-methyl-D-aspartate (NMDA) antagonist, impaired the retrieval process in both working memory and reference memory. Intrahippocampal injection of histamine (25 or 50 ng/site) or intraperitoneal (ip) injection of histidine (25, 50 or 100 mg/kg) markedly ameliorated the spatial memory deficits induced by MK-801. Both the histamine H1 antagonist pyrilamine (0.5 or 1.0 μg/site, ih) and the H2 antagonist cimetidine (2.5 μg/site,ih) abolished the ameliorating effect of histidine (100 mg/kg, ip) on reference memory deficits, but not that on working memory deficits induced by MK-801. Conclusion:The results indicate that histamine in the ventral hippocampus can ameliorate MK-801-induced spatial memory deficits, and that histamine's effect on reference memory is mediated by postsynaptic histamine H1 and H2 receptors.

  3. Facilitating effect of histamine on spatial memory deficits induced by dizocilpine as evaluated by 8-arm radial maze in SD rats%组胺对地佐环平诱发的SD大鼠八臂迷宫空间记忆障碍的改善作用

    Institute of Scientific and Technical Information of China (English)

    黄育文; 陈忠; 胡薇薇; 张力三; 吴炜; 应力阳; 魏尔清

    2003-01-01

    AIM: To investigate whether or not histamine is involved in spatial memory deficits induced by dizocilpine (MK 801) as evaluated by 8-arm radial maze of rats. METHODS: 8-Arm (4-arm baited) radial maze was used to measure spatial memory in rats. RESULTS: Bilaterally intrahippocampal (ih) injection of MK-801 (0.3 μg/site) impaired working memory and reference memory in rats. Both histamine (50, 100 ng/site, ih) and intraperitoneal (ip) injection of histidine (100, 200 mg/kg) markedly improved the spatial memory deficits induced by MK-801. On the other hand, the ameliorating effect of histidine (100 mg/kg, ip) was completely antagonized by αfluoromethylhistidine (α-FMH, 5 μg/site, ih), a potent and selective histidine decarboxylase (HDC) inhibitor, and H1-antagonist pyrilamine (1 μg/site, ih), but not by H2-antagonist cimetidine, even at a high dose (2.5 μg/site, ih).CONCLUSION: The hippocampal histamine plays an important role in the ameliorating effect on MK-801-induced spatial memory deficits, and its action is mediated through postsynaptic H1-receptor.

  4. Effect of Lanthanum on Acid Secretion from Isolated Mouse Stomach in Vitro

    Institute of Scientific and Technical Information of China (English)

    徐项桂; 夏洪涛; 芮光; 胡翠英; 袁福根

    2004-01-01

    To explore the effect and the mechanism of La3+ on gastric acid secretion (GAS) of isolated mouse stomach with perfused lumen, 12 cm H2O column intragastric pressure-provided, whole stomach preparations from mice were incubated in buffer at 37 ℃ in vitro, and perfusate was measured for pH with a pHS-3 type pH meter. The results show that La3+ (0.41~820×10-6 mol*L-1) significantly promotes GAS in a concentration-dependant manner. Proglutamine, a blocker of gastrin receptor, potently inhibits GAS, and it may block the promotive effect of La3+ on GAS, and this effect increases with the increase of proglutamin concentration. Cimetidine, a blocker of histamine H2 receptor, also potently inhibits GAS, and blocks the promotive effect of La3+ on GAS in the same manner with proglutamine. These results suggest that La3+ promotes GAS in isolated stomach possibly by stimulating the releases of gastrin from G cell and Histamine from ECL cell or by activating the gastrin receptors and Histamine H2 receptors on the parietal cell, thereby accelerating the acid secretion of parietal cells in stomach.

  5. Posterior hypothalamic receptors involved in the cardiovascular changes elicited by electrical stimulation of the rostral ventrolateral medulla.

    Science.gov (United States)

    Bachelard, H; Rivest, R; Marsden, C A

    1991-07-01

    The posterior hypothalamic receptors involved in the cardiovascular responses to electrical stimulation of the rostral ventrolateral medulla were investigated in urethane-anaesthetized rats. Electrical stimulation of the rostral ventrolateral medulla produced a significant increase in systolic blood pressure. This response was significantly attenuated by the prior administration of d,l-propranolol (20 micrograms), clonidine (8 micrograms), atropine (8 micrograms) or methysergide (10 micrograms) into the posterior hypothalamus, but not by cimetidine (11 micrograms), chlorpheniramine (12 micrograms), naloxone (10 micrograms) or a vasopressin V1 antagonist (100 ng). The effect of clonidine (8 micrograms) on the pressor response to stimulation of the rostral ventrolateral medulla was antagonized by idazoxan (66 micrograms). These results confirm that the cardiovascular changes elicited by stimulation of the rostral ventrolateral medulla area are, in part, centrally modulated by alpha 2 and beta-adrenoceptors in the posterior hypothalamus which exert respectively, inhibitory and stimulatory effect. Furthermore the results indicate the involvement of posterior hypothalamic cholinergic and serotonergic receptors in the pressor response produced by stimulation of the rostral ventrolateral medulla.

  6. Ussing chamber技术评价 P-糖蛋白及有机阳离子转运体对左氧氟沙星跨胃黏膜转运的影响%Evaluation of P-glycoprotein and organic cation transporter on the transport of levofloxacin by Ussing chamber

    Institute of Scientific and Technical Information of China (English)

    胡咏梅; 张珊珊; 张磊; 胡兴萍; 许建明

    2015-01-01

    目的:评价P-糖蛋白及有机阳离子转运体对左氧氟沙星跨胃黏膜转运的影响。方法用大鼠胃黏膜与Ussing chamber 技术建立胃黏膜体外模型,分为空白组及加入P-糖蛋白抑制剂(环孢素A)或有机阳离子转运体抑制剂(西咪替丁)的抑制剂组并进行双向转运实验,用高效液相色谱法对左氧氟沙星进行定量分析,计算其表观渗透系数( Papp )。结果加入环孢素 A 后,50μg· mL-1左氧氟沙星 Papp ( S -M )/Papp ( M -S )由2.20变为1.06(P<0.05);加入西咪替丁后,50μg · mL-1左氧氟沙星 Papp ( S -M)/Papp ( M-S)与空白组比较,差异无统计学意义。结论 P-糖蛋白参与左氧氟沙星跨胃黏膜转运过程,而有机阳离子转运体不参与左氧氟沙星跨胃黏膜转运过程。%Objective To evaluate the effect of P-glycoprotein (P-gp) and organic cation transporter ( OCTs) on the transport of levofloxacin by using a model in vitro.Methods A model in vitro was established by rat gastric mucosa combined with Ussing chamber.The concentrations of levofloxacin collected from the transport assay were determined by HPLC and the transport parameters such as apparent permeability coefficient [Papp(M-S) and Papp(S-M)] and the ratio of Papp(S -M) versus Papp(M -S) were calculated and compared when the levofloxacin was used solely and co -used with P -gp inhibitor cyclosporin A or OCTs inhibitor cimetidine.Results When cyclosporin A was added , the Papp(S-M)/Papp(M-S) of levofloxacin decreased from 2.20 to 1.06 ( P<0.05).There was no significant difference compared with the blank group while cimetidine was added.Conclusion The reasults indicated that P-glycoprotein might be involved in the transport of levofloxacin in this model in vitro, while the organic cation transporter probably not participated in.

  7. Photocatalytic applications of paper-like poly(vinylidene fluoride)–titanium dioxide hybrids fabricated using a combination of electrospinning and electrospraying

    Energy Technology Data Exchange (ETDEWEB)

    Ramasundaram, Subramaniyan; Son, Aseom; Seid, Mingizem Gashaw; Shim, Sujin; Lee, Sang Hyup; Chung, Yun Chul [Center for Water Resource Cycle Research, Korea Institute of Science and Technology, Hwarangno 14 gil,Seongbuk-gu, Seoul 136-791 (Korea, Republic of); Lee, Changha [Urban and Environmental Engineering, and KIST-UNIST-Ulsan Center for Convergent Materials (KUUC), Ulsan National Institute of Science and Technology, Ulsan 698-805 (Korea, Republic of); Lee, Jaesang [School of Civil, Environmental, and Architectural Engineering, Korea University, 145, Anam-ro, Seongbuk-gu, Seoul 136-701 (Korea, Republic of); Hong, Seok Won, E-mail: swhong@kist.re.kr [Center for Water Resource Cycle Research, Korea Institute of Science and Technology, Hwarangno 14 gil,Seongbuk-gu, Seoul 136-791 (Korea, Republic of); Energy and Environmental Engineering, Korea University of Science and Technology, Hwarangno 14 gil,Seongbuk-gu, Seoul 136-791 (Korea, Republic of)

    2015-03-21

    Highlights: • A PVDF–TiO{sub 2} photocatalyst was fabricated by electrospinning and electrospraying. • The TiO{sub 2} nanoparticles mainly formed clusters on the PVDF nanofiber mat surface. • The photo-degradation of aqueous organic pollutants was efficiently achieved. • The hybrid photocatalysts were robust, reusable, and stable in aqueous solution. - Abstract: A paper-like photocatalyst was fabricated by electrospraying an N,N′-dimethylformamide (DMF) dispersion of titanium dioxide (TiO{sub 2}) nanoparticles (NPs) on a poly(vinylidene fluoride) nanofiber (PVDF NF) mat prepared by electrospinning. Morphological studies revealed that the TiO{sub 2} NPs uniformly deposited as clusters on the surface of the PVDF NF mat. The immobilized amount of TiO{sub 2} was found to be 2.08, 2.44, 3.80, and 4.73 mg per 45 cm{sup 2} of PVDF–TiO{sub 2} hybrids for the electrospraying of 10, 20, 40, and 60 ml of TiO{sub 2}–DMF, respectively. The hybrid photocatalysts were effective in degrading bisphenol A (BPA), 4-chlorophenol (4-CP), and cimetidine (CMT), which dissolved in both deionized water and secondary wastewater effluents, with activity being proportional to the quantity of TiO{sub 2} NPs immobilized. For the highest loading amount of TiO{sub 2}, BPA, 4-CP, and CMT degraded completely within 100, 100, and 40 min of UV irradiation, respectively. Stable photo-oxidation of CMT was maintained through 10 repeated cycles. During these cycles, it was confirmed that there was no loss of TiO{sub 2} NPs by inductively coupled plasma optical emission spectrometry. Our results suggest that effective and stable PVDF–TiO{sub 2} hybrid photocatalysts can be fabricated on a large scale by combining electrospinning and electrospraying techniques.

  8. Gastroprotective activity of alkaloid extract and 2-phenylquinoline obtained from the bark of Galipea longiflora Krause (Rutaceae).

    Science.gov (United States)

    Zanatta, Francielle; Gandolfi, Renan Becker; Lemos, Marivane; Ticona, Juan Carlos; Gimenez, Alberto; Clasen, Bruna Kurz; Cechinel Filho, Valdir; de Andrade, Sérgio Faloni

    2009-07-15

    As part of our continuing search for bioactive natural products from plants, the present study was carried out in order to evaluate the gastroprotective properties of alkaloid extract and 2-phenylquinoline obtained from the bark of Galipea longiflora (Rutaceae). Anti-ulcer assays were performed using the following protocols in mice: nonsteroidal anti-inflammatory drug (NSAID)/bethanecol-induced ulcer, ethanol/HCl-induced ulcer, and stress-induced ulcer. The effects of the extract on gastric content volume, pH and total acidity were also evaluated, using the pylorus ligated model. Treatment using doses of 50, 125 and 250 mg/kg of G. longiflora alkaloid extract and positive controls (omeprazol or cimetidine) significantly diminished the lesion index, total lesion area, and percentage of lesion, in comparison with the negative control groups in all the models evaluated. Regarding the model of gastric secretion, a reduction in volume of gastric juice and total acidity was observed, as well as an increase in gastric pH. The main alkaloid of the plant, 2-phenylquinoline, was also evaluated in the ethanol-induced ulcer model. The results showed that at a dose of 50 mg/kg, it significantly inhibited ulcerative lesions. However, this effect was less than that of the alkaloid extract. All these results taken together show that G. longiflora displays gastroprotective activity, as evidenced by its significant inhibition of the formation of ulcers induced by different models. There are indications that mechanisms involved in anti-ulcer activity are related to a decrease in gastric secretion and an increase in gastric mucus content. Also, there is evidence of involvement of NO in the gastroprotector mechanisms. These effects may be attributed, at least in part, to the presence of some alkaloids, particularly 2-phenylquinoline. PMID:19497430

  9. Effect of acid secretion blockade on acute gastric mucosal lesions induced by Tityus serrulatus scorpion toxin in anaesthetized rats.

    Science.gov (United States)

    Melo, Júnio Rios; de Araújo, Gnana Keith Marques; da Luz, Magda Maria Profeta; da Conceição, Sérgio Alexandre; Lisboa, Felipe Assis; Moraes-Santos, Tasso; Cunha-Melo, José Renan

    2006-10-01

    Scorpion venom (TX) promotes gastric acid and pepsin secretion leading to acute gastric mucosal lesions (AGML), when injected in animals. The goal of the present study was to observe the effects of acid gastric secretion blockers over the incidence of TX-induced AGML in vivo. To verify this model, we used male albino rats, fasted 18-20 h (n=122) and anaesthetized with urethane (1.4 g/kg, i.p.). Their trachea and left femoral vein were both cannulated; the first to avoid airway obstructions during scorpion intoxication and the second for administration of saline, TX and acid blockers. Following the surgical procedure, the animals were divided in 10 groups of at least 10 animals each. Control groups were injected with NaCl 0.9% 1 ml/kg (n=10) or TX 375 microg/kg (n=32). Test groups (n=10, each) received atropine 5 mg/kg, cimetidine 10mg/kg, ranitidine 2.5mg/kg, ranitidine 5mg/kg, omeprazol 1 mg/kg, omeprazol 4 mg/kg, octreotide 80 and octreotide 100 microg/kg 10 min before the TX was injected. After 1h of intoxication, the stomach was resected for macroscopic study and the gastric secretion was collected for volume, pH and acid output assessment. We observed that all blockers were able to completely or partially prevent the TX-induced acid secretion as well as the AGML (p<0.05). Our data suggest the TX-induced AGML can be prevented by different class of acid blockers injected before the intoxication. PMID:16926041

  10. Investigation of biological activity of polar extracts isolated from Phlomis crinita Cav ssp. mauritanica Munby.

    Science.gov (United States)

    Limem-Ben Amor, Ilef; Skandrani, Ines; Boubaker, Jihed; Ben Sghaïer, Mohamed; Neffati, Aicha; Bhouri, Wissem; Bouhlel, Ines; Chouchane, Nabil; Kilani, Soumaya; Guedon, Emmanuel; Ghoul, Mohamed; Ghedira, Kamel; Chekir-Ghedira, Leila

    2009-01-01

    The lyophilized infusion, the methanol, the ethyl acetate, and the total oligomer flavonoid (TOF)-enriched extracts prepared from the dried leaves of Phlomis crinita Cav. ssp. mauritanica Munby were investigated for the contents of flavonoids, tannins, coumarines and steroids. Antibacterial activity was investigated toward five bacterial strains. An inhibitory effect was observed against Staphyllococcus aureus and Enterococcus feacalis, and the minimal inhibitory concentrations ranged from 2.5 to 5 mg/mL of extract. The tested extracts exhibit an important free radical scavenging activity toward the 1,1-diphenyl 2-picrylhydrazyl (DPPH) free radical; with IC(50) values of 30.5, 6, 32, and 31.5 microg/mL, respectively, in the presence of lyophilized infusion, the TOF, the methanol, and the ethyl acetate extracts. Genotoxic and antigenotoxic properties of the different extracts were studied by using the SOS chromotest with Escherichia coli PQ37. The lyophilized infusion and TOF extracts obtained from P. crinita ssp. mauritanica showed no genotoxicity, whereas methanol and ethyl acetate extracts are considered as marginally genotoxic. On the other hand, we showed that each extract inhibited the mutagenicity induced by aflatoxin B1 (AFB1) (10 microg/assay) and nifuroxazide (NF) (10 microg/assay). The ethyl acetate extract showed the strongest level of protection toward the genotoxicity induced by both directly and indirectly genotoxic NF and AFB1. These tests proved that the lyophilized infusion possesses an antiradical activity likewise, it showed no genotoxic effect; that is why we choose this extract to assess its antiulcerogenic activity by using an ethanol-induced ulcerogenesis model in the rat. This test demonstrates that 300 mg/kg of a P. crinita ssp. mauritanica lyophilized infusion was more effective than the reference compound, cimetidine. PMID:19514937

  11. Intestinal Oxidative State Can Alter Nutrient and Drug Bioavailability

    Directory of Open Access Journals (Sweden)

    Faria Ana

    2009-01-01

    Full Text Available Organic cations (OCs are substances of endogenous (e.g., dopamine, choline or exogenous (e.g., drugs like cimetidine origin that are positively charged at physiological ph. since many of these compounds can not pass the cell membrane freely, their transport in or out of cells must be mediated by specific transport systems. Transport by organic cation transporters (OCTs can be regulated rapidly by altering their trafficking and/or affinities in response to stimuli. However, for example, a specific disease could lead to modifications in the expression of OCTs. Chronic exposure to oxidative stress has been suggested to alter regulation and functional activity of proteins through several pathways. According to results from a previous work, oxidation-reduction pathways were thought to be involved in intestinal organic cation uptake modulation. The present work was performed in order to evaluate the influence of oxidative stressors, especially glutathione, on the intestinal organic cation absorption. For this purpose, the effect of compounds with different redox potential (glutathione, an endogenous antioxidant, and procyanidins, diet antioxidants was assessed on MPP+ (1-methyl-4-phenylpyridinium iodide uptake in an enterocyte cell line (Caco-2. Caco-2 cells were subcultured with two different media conditions (physiological: 5 mM glucose, referred as control cells; and high-glucose: 25 mM glucose, referred as HG cells. In HG cells, the uptake was significantly lower than in control cells. Redox changing interventions affected Mpp+ uptake, both in control and in high-glucose Caco-2 cells. Cellular glutathione levels could have an important impact on membrane transporter activity. The results indicate that modifications in the cellular oxidative state modulate MPP+ uptake by Caco-2 cells. Such modifications may reflect in changes of nutrient and drug bioavailability.

  12. Effect of oral coadministration of drugs on the disposition of (/sup 14/C)-celiprolol HCl in rats

    Energy Technology Data Exchange (ETDEWEB)

    Town, C.; Knipe, J.; Taft, C.; Tantillo, N.; Klunk, L.; Grebow, P.

    1986-03-01

    Celiprolol HCL (C) is a cardioselective ..beta..-blocker undergoing clinical trials as an antihypertensive agent. Studies with rats indicated that the oral coadministration of 2.5 mg/kg of chlorthalidone (CT) caused a 40% decrease in the urinary excretion of radioactivity from a 40 mg/kg dose of (/sup 14/C)-C(C). In order to further understand the nature of this interaction, groups of 6 rats were given 40 mg/kg of (C) alone and, one week later,/sub R.(C) pluse the drug to be tested. The vehicle was 0.5% Methocel. After each dosing, urine was collected for 96 hours from each rat and the amount of total radioactivity excreted was compared between treatments. The results showed that oral coadministration of 2.5 mg/kg hydrochlorothiazide, 2.5 mg/kg furosemide, 2.5 mg/kg indapamide, 5.0 mg/kg cimetidine, 10.0 mg/kg theophylline, and 1.0 mg/kg digoxin were without effect on the disposition of orally administered (C). Conversely, 2.5 mg/kg CT, 2.5 mg/kg acetazolamide (AZ) and 5.0 mg/kg hydralazine (H) caused a significant (p < 0.05) decrease in the urinary excretio of orally administered (C). CT and AZ are both potent inhibitors of carbonic anhydrase and their action on this enzyme may cause the effect on the disposition of (C). The action of H may be due to its pharmacologic action and warrants further study.

  13. Olfactory interference during inhibitory backward pairing in honey bees.

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    Matthieu Dacher

    Full Text Available BACKGROUND: Restrained worker honey bees are a valuable model for studying the behavioral and neural bases of olfactory plasticity. The proboscis extension response (PER; the proboscis is the mouthpart of honey bees is released in response to sucrose stimulation. If sucrose stimulation is preceded one or a few times by an odor (forward pairing, the bee will form a memory for this association, and subsequent presentations of the odor alone are sufficient to elicit the PER. However, backward pairing between the two stimuli (sucrose, then odor has not been studied to any great extent in bees, although the vertebrate literature indicates that it elicits a form of inhibitory plasticity. METHODOLOGY/PRINCIPAL FINDINGS: If hungry bees are fed with sucrose, they will release a long lasting PER; however, this PER can be interrupted if an odor is presented 15 seconds (but not 7 or 30 seconds after the sucrose (backward pairing. We refer to this previously unreported process as olfactory interference. Bees receiving this 15 second backward pairing show reduced performance after a subsequent single forward pairing (excitatory conditioning trial. Analysis of the results supported a relationship between olfactory interference and a form of backward pairing-induced inhibitory learning/memory. Injecting the drug cimetidine into the deutocerebrum impaired olfactory interference. CONCLUSIONS/SIGNIFICANCE: Olfactory interference depends on the associative link between odor and PER, rather than between odor and sucrose. Furthermore, pairing an odor with sucrose can lead either to association of this odor to PER or to the inhibition of PER by this odor. Olfactory interference may provide insight into processes that gate how excitatory and inhibitory memories for odor-PER associations are formed.

  14. Modulatory effects of taurine on jejunal contractility

    Directory of Open Access Journals (Sweden)

    Q.Y. Yao

    2014-12-01

    Full Text Available Taurine (2-aminoethanesulfonic acid is widely distributed in animal tissues and has diverse pharmacological effects. However, the role of taurine in modulating smooth muscle contractility is still controversial. We propose that taurine (5-80 mM can exert bidirectional modulation on the contractility of isolated rat jejunal segments. Different low and high contractile states were induced in isolated jejunal segments of rats to observe the effects of taurine and the associated mechanisms. Taurine induced stimulatory effects on the contractility of isolated rat jejunal segments at 3 different low contractile states, and inhibitory effects at 3 different high contractile states. Bidirectional modulation was not observed in the presence of verapamil or tetrodotoxin, suggesting that taurine-induced bidirectional modulation is Ca2+ dependent and requires the presence of the enteric nervous system. The stimulatory effects of taurine on the contractility of isolated jejunal segments was blocked by atropine but not by diphenhydramine or by cimetidine, suggesting that muscarinic-linked activation was involved in the stimulatory effects when isolated jejunal segments were in a low contractile state. The inhibitory effects of taurine on the contractility of isolated jejunal segments were blocked by propranolol and L-NG-nitroarginine but not by phentolamine, suggesting that adrenergic β receptors and a nitric oxide relaxing mechanism were involved when isolated jejunal segments were in high contractile states. No bidirectional effects of taurine on myosin phosphorylation were observed. The contractile states of jejunal segments determine taurine-induced stimulatory or inhibitory effects, which are associated with muscarinic receptors and adrenergic β receptors, and a nitric oxide associated relaxing mechanism.

  15. The relationship between Na+/H+ exchanger expression and tyrosinase activity in human melanocytes

    International Nuclear Information System (INIS)

    The activity of melanosome-associated tyrosinase in human melanocytes differs based on racial skin type. In melanocytes from Black skin, tyrosinase activity is high while in White melanocytes the activity of the enzyme is low. Recent studies suggest that low tyrosinase activity in White melanocytes may be due to an acidic pH environment within the melanosome. Because sodium/hydrogen (Na+/H+) exchangers (NHEs) are known to regulate intracellular pH, melanocytes were treated with NHE inhibitors to determine what effect this inhibition might have on tyrosinase activity. Treatment of Black melanocytes with ethyl-isopropyl amiloride (EIPA) caused a rapid dose-dependent inhibition of tyrosinase activity. This inhibition was not due to either direct enzyme inhibition or to a decrease in tyrosinase abundance. In contrast, treatment of White melanocytes with EIPA, cimetidine, or clonidine resulted in little inhibition of tyrosinase activity. Reverse transcriptase-polymerase chain reaction (RT-PCR) and Western blot analysis showed that both Black and White melanocytes expressed mRNA and protein for NHE-1, NHE-3, NHE-5, NHE-6, and NHE-7. Immunohistochemical analysis showed that NHE-7 and NHE-3 co-localized with the melanosomal protein, Tyrosinase Related Protein-1 (TRP-1). In addition, the vesicular proton pump, vesicular ATPase (V-ATPase), was found to be present in both White and Black melanosomes, indicating that organelles from both racial skin types are capable of being acidified. The results suggest that one or more NHEs may help regulate melanosome pH and tyrosinase activity in human melanocytes

  16. Comparison of airway responses in sheep of different age in precision-cut lung slices (PCLS.

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    Verena A Lambermont

    Full Text Available Animal models should display important characteristics of the human disease. Sheep have been considered particularly useful to study allergic airway responses to common natural antigens causing human asthma. A rationale of this study was to establish a model of ovine precision-cut lung slices (PCLS for the in vitro measurement of airway responses in newborn and adult animals. We hypothesized that differences in airway reactivity in sheep are present at different ages.Lambs were delivered spontaneously at term (147d and adult sheep lived till 18 months. Viability of PCLS was confirmed by the MTT-test. To study airway provocations cumulative concentration-response curves were performed with different allergic response mediators and biogenic amines. In addition, electric field stimulation, passive sensitization with house dust mite (HDM and mast cells staining were evaluated.PCLS from sheep were viable for at least three days. PCLS of newborn and adult sheep responded equally strong to methacholine and endothelin-1. The responses to serotonin, leukotriene D4 and U46619 differed with age. No airway contraction was evoked by histamine, except after cimetidine pretreatment. In response to EFS, airways in PCLS from adult and newborn sheep strongly contracted and these contractions were atropine sensitive. Passive sensitization with HDM evoked a weak early allergic response in PCLS from adult and newborn sheep, which notably was prolonged in airways from adult sheep. Only few mast cells were found in the lungs of non-sensitized sheep at both ages.PCLS from sheep lungs represent a useful tool to study pharmacological airway responses for at least three days. Sheep seem well suited to study mechanisms of cholinergic airway contraction. The notable differences between newborn and adult sheep demonstrate the importance of age in such studies.

  17. Anti-ulcer activity of Ipomoea batatas tubers (sweet potato

    Directory of Open Access Journals (Sweden)

    Vandana Panda

    2012-04-01

    Full Text Available Background: Peptic ulcers occur in that part of the gastrointestinal tract which is exposed to gastric acid and pepsin, i.e., the stomach and duodenum. Gastric and duodenal ulcers are common pathologies that may be induced by a variety of factors such as stress, smoking and noxious agents including non-steroidal anti-inflammatory drugs. Ipomoea batatas tubers (sweet potato contain ample amounts of antioxidants. It has been proven already by many scientific studies that antioxidants have ulcer healing properties. In reference to this, we tried assessing the ulcer healing effect of Ipomoea batatas tubers. Methods: The anti-ulcer activity of the tubers of Ipomoea batatas (sweet potato was studied in cold stress and aspirin-induced gastric ulcers in Wistar rats. Methanolic extracts of Ipomoea batatas tubers (TE at two doses, viz., 400 and 800 mg /kg were evaluated in cold stress and aspirin-induced gastric ulcer models using cimetidine and omeprazole respectively as standards. The standard drugs and the test drugs were administered orally for 7 days in the cold stressmodel and for 1 day in the aspirin-induced gastric ulcer model. Gastroprotective potential, status of the antioxidant enzymes {superoxide dismutase (SOD, catalase (CAT, glutathione peroxidase (GPx and glutathione reductase(GR} along with GSH, and lipid peroxidation were studied in both models. Results: The results of the present study showed that TE possessed gastroprotective activity as evidenced by its significant inhibition of mean ulcer score and ulcer index and a marked increase in GSH, SOD, CAT, GPx, and GR levels and reduction in lipid peroxidation in a dose dependant manner.Conclusion: The present experimental findings suggest that tubers of Ipomoea batatas may be useful for treating peptic ulcers.

  18. Homopterocarpin contributes to the restoration of gastric homeostasis by Pterocarpus erinaceus following indomethacin intoxication in rats

    Institute of Scientific and Technical Information of China (English)

    M Tolulope Olaleye; Afolabi C Akinmoladun; Olamide O Crown; Katty E Ahonsi; A O Adetuyi

    2013-01-01

    Objective:To investigate the restorative effect ofPterocarpus erinaceus (P. erinaceus) and homopterocarpin, an isoflavonoid isolated from it, on indomethacin-induced disruption in gastric homeostasis in rats.Methods:Adult rats were divided into five groups and fasted for48 h before treatment.Group1 received olive oil (vehicle), group2 received25 mg/kg indomethacin while groups3-5 received cimetidine (100 mg/kg), homopterocarpin (25 mg/kg) andP. erinaceus ethanolic stem bark extract (100 mg/kg) respectively.After1 h, all the groups except group 2 were administered25 mg/kg of indomethacin.One hour later, the rats were sacrificed and the ulcer index and other gastroprotective indices were evaluated.Results:Indomethacin caused significant injury to the stomach of the rats as reflected in the ulcer indices (9.0±1.4) as compared with that of control (2.0±0.0).Equally, there were significant increases in gastric acid concentration and malondialdehyde level in the stomachs of the ulcerated animals compared with the control.However mucus content, reduced gluthatione level and gastric pH were significantly reduced in the ulcerated animals compared with the control.Pretreatment with eitherPterocarpus bark extract or homopterocarpin reversed the effects of indomethacin on the evaluated parameters.Conclusions:These results indicate that both homopterocarpin and Pterocarpus extract offered gastroprotection against indomethacin-induced ulcer by antioxidativemechanism and the modulation of gastric homeostasis.The results also suggest that homopterocarpin might be responsible for, or contribute to the antiulcerogenic property ofP. erinaceus.

  19. Importance of the dentist in early diagnosis of pemphigus vulgaris

    Directory of Open Access Journals (Sweden)

    Thiago de Santana Santos

    2009-10-01

    Full Text Available The vulgar pemphigus is a chronic, rare, vesicle-bubble disease of autoimmune origin and with a possibility of following a dangerous clinical course when it is not diagnosed and treated in its initial stage. It usually affects people from 40 to 60 years old, being rare in children. In the majority of cases, oral manifestations are the first signs of the disease, so that dentists play an important rol in its early diagnosis. The authors present a case report of vulgar pemphigus in a 17 year-old patient, attended by the Bucco-Maxillo-Facial Surgery Service of the “Fundação de Beneficência Hospital de Cirurgia” in Aracaju-SE, Brazil. The patient was admitted with a complaint of the presence of numerous scattered painful ulcers in the mouth that had developed in approximately two months, and reported that at first, blisters that broke quickly appeared, leading to extremely painful ulcerations. Incisional biopsies were performed in the jugal mucosa and retromolar regions, and also a complete hemogram to discard the hypothesis of leukemia. In view of the clinical and histopathological findings, the final diagnosis of pemphigus vulgaris was made. Before receiving specialized treatment, the patient presented marked worsening of the clinical condition, with exacerbation of intraoral signs and symptoms and development of skin lesions around the body surface. The patient was hospitalized in the “Hospital Universitário da Universidade Federal de Sergipe” and treated with prednisone, cimetidine and nystatin, showing significant improvement of symptoms in approximately two weeks. At present, the patient is under the care of an interdisciplinary team that includes dermatologists and dentists.

  20. Mechanisms of histamine stimulated secretion in rabbit ileal mucosa.

    Science.gov (United States)

    Linaker, B D; McKay, J S; Higgs, N B; Turnberg, L A

    1981-11-01

    Histamine is present in high concentrations in the intestine and we investigated the possibility that it might have a role here in intestinal transport. When added to the basal side of rabbit ileal mucosa in vitro histamine (10(-4)M) induced a short-lived increase in electrical potential difference and short circuit current. It inhibited net chloride absorption but did not influence sodium transport. Alkali secretion, measured by a pH stat technique, was inhibited, suggesting that bicarbonate secretion was reduced. Both the electrical and ion flux responses to histamine were blocked by the H1 receptor blocker diphenhydramine, but not by the H2 receptor blocker cimetidine. The presence of specific H1 histamine receptors was further supported by shifts in the dose-response curve to histamine by four different concentrations of diphenhydramine. Calculation of a pA2 value from these "Schild' plots provided a figure of 7.85, which is similar to that for H1 receptors in other tissues. Aminoguanidine, a histaminase blocker, had no electrical effects alone but shifted the histamine dose response curve to the left. These studies indicate that histamine inhibits chloride absorption and alkali secretion, possibly by influencing a chloride/bicarbonate exchange process, through specific mucosal H1 receptors. Enhancement of histamine effects by a histaminase inhibitor suggests that histaminases are present in the intestinal mucosa and supports the possibility of a role for endogenous histamine in influencing ion transport. The observations indicate a mechanism by which absorption might be impaired in diseases in which histamine is liberated locally in the intestine. PMID:7308851

  1. Biliary excretion of acetaminophen-glutathione as an index of toxic activation of acetaminophen: effect of chemicals that alter acetaminophen hepatotoxicity

    Energy Technology Data Exchange (ETDEWEB)

    Madhu, C.; Gregus, Z.; Klaassen, C.D.

    1989-03-01

    Acetaminophen (AA) is converted, presumably by cytochrome P-450, to an electrophile which is conjugated with glutathione (GS). AA-GS is excreted into bile, therefore the biliary excretion rate of AA-GS may reflect the rate of activation of AA in vivo. In order to test this hypothesis, the effect of agents capable of altering the activation of AA including cytochrome P-450 inducers and inhibitors, cobaltous chloride which decreases the amount of P-450, prostaglandin synthetase inhibitors (indomethacin and naproxen), antioxidants (butylated hydroxyanisole, alpha-tocopherol, ascorbic acid and ascorbic acid palmitate) and other chemicals known to decrease AA hepatotoxicity (dimethylsulfoxide and cysteamine), on the biliary excretion of AA-GS was studied in hamsters, the species most sensitive to AA-induced hepatotoxicity. The biliary excretion of AA-GS increased linearly up to 1 mmol/kg of AA i.v., but at higher dosages exhibited saturation kinetics. Dosages above 0.5 mmol/kg lowered hepatic GS concentration. Of the cytochrome P-450 inducers, 3-methylcholanthrene and 2,3,7,8-tetrachlorodibenzo-p-dioxin, increased the biliary excretion of AA-GS (2.9- and 3.2-fold, respectively) whereas ethanol and isoniazid did not affect it, and pregnenolone-16 alpha-carbonitrile tended to decrease it (43%). Phenobarbital tended to increase the biliary excretion of AA-GS, but not in a statistically significant manner. Several cytochrome P-450 inhibitors (metyrapone, 8-methoxypsoralen, 2-(4,6-dichloro-biphenyloxy) ethylamine, alpha-naphthoflavone and cimetidine) decreased the biliary excretion of AA-GS, although SKF 525-A and piperonyl butoxide did not. Cobaltous chloride decreased dramatically the biliary excretion of AA-GS.

  2. Study of Total Alkaloids from Rhizoma Coptis Chinensis on Experimental Gastric Ulcers

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    Objective: To study the effects of total alkaloids (TA) extracted from Rhizoma Coptis Chinensis on experimental gastric ulcer models. Methods: Four kinds of experimental ulcer models were established respectively by water-immersion stress, intragastric ethanol, acetic acid erosion, and pylorus ligation. The anti-ulcer effects of TA were evaluated, and compared with that of berberine (Ber) and cimetidine(Cim). Results: TA showed significant inhibitory effects on ulcerative formation induced by water-immersion stress, intragastric ethanol, and pylorus l igation in dose-dependent manner, and showed therapeutic effect on acetic acid erosion-inducing ulcer, in comparison with the control group. The anti-ulcer activity of Ber was less than TA containing equal content of Ber. TA significantly reduced the free acidity, total acidity and total acid output, but didn't affect the gastric juice volume, gastric pepsin activity, adherent mucus quantity of stomach wall and free mucus dissolving in gastric juice. The suppressive activities of TA on gastric acid secretion didn't occur when it was administered into dodecadactylon at a dose of 360 mg/kg wt. Moreover,when compared with Cim, the inhibitory effect of TA on gastric acid secretion isn't proportional to the inhibitory effects on the formation of the 4 kinds of experimental ulcers. Conclusion: TA is a potent candidate in therapeutic drugs for treating gastric ulcer. Its anti-ulcer effective components and mechanism is not only related to Ber and inhibition of gastric acid, but also to other ingredients of TA and mechanism so far unknown.

  3. Histamine as a punisher in squirrel monkeys: effects of pentobarbital, chlordiazepoxide and H1- and H2-receptor antagonists on behavior and cardiovascular responses.

    Science.gov (United States)

    Goldberg, S R

    1980-09-01

    Squirrel monkeys pressed a key under a two-component, 30-response fixed-ratio schedule of food presentation. In both nonpunishment and punishment components, every 30th key-pressing response resulted in food presentation. In the punishment component, the 11th and 22nd response in each 30-response fixed-ratio also produced a 200msec i.v. injection of 30 to 100 microgram/kg of histamine; this resulted in about an 80% suppression of responding in the punishment component. A second group of squirrel monkeys, with arterial catheters for monitoring of blood pressure and heart rate, received automatic i.v. injections of 30 and 100 microgram/kg of histamine; key presses had no programmed consequences. Mean arterial blood pressure decreased by 5 to 20 min Hg and heart rate increased by 60 to 120 beats/min after each injection of histamine. As an effective punisher, histamine was functionally similar to other noxious stimuli such as electric shock. Behavior suppressed by histamine could be markedly increased by presession i.m. treatment with pentobarbital (3-5.6 mg/kg) or chlordiazepoxide (10-30 mg/kg). Presession i.m. treatment with 1 to 3 mg/kg of the H1-receptor antagonist, diphenhydramine, reversed the punishment effects of histamine but only enhanced the cardiovascular effects of histamine. In contrast, 10 to 30 mg/kg of the H2-receptor antagonist, cimetidine, failed to reverse the punishment effects of histamine but markedly attenuated the cardiovascular effects of histamine. Thus, histamine's suppression of responding appeared to be an H1 effect and did not appear to be related to its effects on blood pressure and heart rate. PMID:6105208

  4. Behavioural effects of histamine and its antagonists: a review.

    Science.gov (United States)

    White, J M; Rumbold, G R

    1988-01-01

    This review focuses on the behavioural effects of histamine and drugs which affect histaminergic function, particularly the H1- and H2-receptors antagonists. Research in this area has assumed considerable importance with increasing interest in the role of brain histamine, the clinical use of both H1 and H2 antagonists and evidence of nonmedical use of H1 antagonists. Results from a number of studies show that H1 and H2 antagonists have clear, but distinct subjective effects and that H1 antagonists have discriminative effects in animals. While H1 antagonists are reinforcers in certain conditions, histamine itself is a punisher. Moderate doses of H1 antagonists affect psychomotor performance in some situations, but the results are variable. The exceptions are terfenadine and astemizole, which do not seem to penetrate the blood-brain barrier readily. In studies of schedule-controlled behaviour, marked changes in response rate have been observed following administration of H1 antagonists, with the magnitude and direction dependent on the dose and the baseline behaviour. Histamine reduces avoidance responding, an effect mediated via H1-receptors. Changes in drinking and aggressive behaviour have also been observed following histamine administration and distinct roles for H1- and H2-receptors have been delineated. Separate H1- and H2-receptor mechanisms have also been suggested to account for changes in activity level. While the H2 antagonists do not always have strong behavioural effects when administered peripherally, there is evidence that cimetidine has a depressant effect on sexual function. These and other findings reveal an important role for histaminergic systems in a wide range of behaviour. PMID:3133686

  5. Effect of disodium cromoglycate (DSCG) and antihistamines on postirradiation cerebral blood flow and plasma levels of histamine and neurotensin

    Energy Technology Data Exchange (ETDEWEB)

    Cockerham, L.G.; Pautler, E.L.; Carraway, R.E.; Cochrane, D.E.; Hampton, J.D.

    1988-02-01

    In an attempt to elucidate mechanisms underlying the irradiation-induced decrease in regional cerebral blood flow (rCBF) in primates, hippocampal and visual cortical blood flows of rhesus monkeys were measured by hydrogen clearance, before and after exposure to 100 Gy, whole-body, gamma irradiation. Systemic blood pressures were monitored simultaneously. Systemic arterial plasma histamine and neurotensin levels were determined preirradiation and postirradiation. Compared to control animals, the irradiated monkeys exhibited an abrupt decline in systemic blood pressure to 23% of the preirradiation level within 10 min postirradiation, falling to 12% by 60 min. A decrease in hippocampal blood flow to 32% of the preirradiation level was noted at 10 min postirradiation, followed by a slight recovery to 43% at 30 min and a decline to 23% by 60 min. The cortical blood flow for the same animals showed a steady decrease to 29% of the preirradiation levels by 60 min postirradiation. Animals given the mast cell stabilizer disodium cromoglycate and the antihistamines mepyramine and cimetidine before irradiation did not exhibit an abrupt decline in blood pressure but displayed a gradual decrease to a level 33% below preirradiation levels by 60 min postirradiation. Also, the treated, irradiated monkeys displayed rCBF values that were not significantly different from the nonirradiated controls. The plasma neurotensin levels in the irradiated animals, treated and untreated, indicated a nonsignificant postirradiation increase above control levels. However, the postirradiation plasma histamine levels in both irradiated groups showed an increase of approximately 1600% above the preirradiation levels and the postirradiation control levels.

  6. Modulatory effects of taurine on jejunal contractility

    Energy Technology Data Exchange (ETDEWEB)

    Yao, Q.Y.; Chen, D.P.; Ye, D.M.; Diao, Y.P.; Lin, Y. [Dalian Medical University, Dalian, Liaoning (China)

    2014-10-14

    Taurine (2-aminoethanesulfonic acid) is widely distributed in animal tissues and has diverse pharmacological effects. However, the role of taurine in modulating smooth muscle contractility is still controversial. We propose that taurine (5-80 mM) can exert bidirectional modulation on the contractility of isolated rat jejunal segments. Different low and high contractile states were induced in isolated jejunal segments of rats to observe the effects of taurine and the associated mechanisms. Taurine induced stimulatory effects on the contractility of isolated rat jejunal segments at 3 different low contractile states, and inhibitory effects at 3 different high contractile states. Bidirectional modulation was not observed in the presence of verapamil or tetrodotoxin, suggesting that taurine-induced bidirectional modulation is Ca{sup 2+} dependent and requires the presence of the enteric nervous system. The stimulatory effects of taurine on the contractility of isolated jejunal segments was blocked by atropine but not by diphenhydramine or by cimetidine, suggesting that muscarinic-linked activation was involved in the stimulatory effects when isolated jejunal segments were in a low contractile state. The inhibitory effects of taurine on the contractility of isolated jejunal segments were blocked by propranolol and L-NG-nitroarginine but not by phentolamine, suggesting that adrenergic β receptors and a nitric oxide relaxing mechanism were involved when isolated jejunal segments were in high contractile states. No bidirectional effects of taurine on myosin phosphorylation were observed. The contractile states of jejunal segments determine taurine-induced stimulatory or inhibitory effects, which are associated with muscarinic receptors and adrenergic β receptors, and a nitric oxide associated relaxing mechanism.

  7. Microscopic colitis

    Institute of Scientific and Technical Information of China (English)

    Gianluca Ianiro; Giovanni Cammarota; Luca Valerio; Brigida Eleonora Annicchiarico; Alessandro Milani; Massimo Siciliano; Antonio Gasbarrini

    2012-01-01

    Microscopic colitis may be defined as a clinical syndrome,of unknown etiology,consisting of chronic watery diarrhea,with no alterations in the large bowel at the endoscopic and radiologic evaluation.Therefore,a definitive diagnosis is only possible by histological analysis.The epidemiological impact of this disease has become increasingly clear in the last years,with most data coming from Western countries.Microscopic colitis includes two histological subtypes [collagenous colitis (CC) and lymphocytic colitis (LC)] with no differences in clinical presentation and management.Collagenous colitis is characterized by a thickening of the subepithelial collagen layer that is absent in LC.The main feature of LC is an increase of the density of intra-epitll lial lymphocytes in the surface epithelium.A number of pathogenetic theories have been proposed over the years,involving the role of luminal agents,autoimmunity,eosinophils,genetics (human leukocyte antigen),biliary acids,infections,alterations of pericryptal fibroblasts,and drug intake; drugs like ticlopidine,carbamazepine or ranitidine are especially associated with the development of LC,while CC is more frequently linked to cimetidine,non-steroidal antiinflammatory drugs and lansoprazole.Microscopic colitis typically presents as chronic or intermittent watery diarrhea,that may be accompanied by symptoms such as abdominal pain,weight loss and incontinence.Recent evidence has added new pharmacological options for the treatment of microscopic colitis:the role of steroidal therapy,especially oral budesonide,has gained relevance,as well as immunosuppressive agents such as azathioprine and 6-mercaptopurine.The use of anti-tumor necrosis factor-α agents,infliximab and adalimumab,constitutes a new,interesting tool for the treatment of microscopic colitis,but larger,adequately designed studies are needed to confirm existing data.

  8. Anti-ulcerogenic effect of cavidine against ethanol-induced acute gastric ulcer in mice and possible underlying mechanism.

    Science.gov (United States)

    Li, Weifeng; Wang, Xiumei; Zhang, Hailin; He, Zehong; Zhi, Wenbing; Liu, Fang; Wang, Yu; Niu, Xiaofeng

    2016-09-01

    Cavidine, a major alkaloid compound isolated from Corydalis impatiens, has various pharmacological effects but its effect on gastric ulcer has not been previously explored. The current study aimed to investigate the possible anti-ulcerogenic potential of cavidine in the model of ethanol-induced gastric ulcer. Mice received cavidine (1, 5 or 10mg/kg, ig), cimetidine (CMD, 100mg/kg, ig) or vehicle at 12h and 1h before absolute ethanol administration (0.5mL/100g), and animals were euthanized 3h after ethanol ingestion. Gross and histological gastric lesions, biochemical, immunological and Western blot parameters were taken into consideration. The results showed that ethanol administration produced apparent mucosal injuries with morphological and histological damage, whereas cavidine pre-treatment reduced the gastric injuries. Cavidine pre-treatment also ameliorated the contents of malonaldehyde (MDA) and myeloperoxidase (MPO) activity, and increased the mucosa levels of glutathione (GSH), superoxide dismutase (SOD) and prostaglandin E2 (PGE2), relative to the model group. Also cavidine was able to decrease the levels of interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α), inhibit the up-regulation of cyclo-oxygenase-2 (COX-2) expression and activation of Nuclear factor-kappa B (NF-κB) pathway. Taken together, these results indicated that cavidine exerts a gastroprotective effect against gastric ulceration, and the underlying mechanism might be associated with the stimulation of PGE2, reduction of oxidative stress, suppression of NF-κB expression and subsequent reduced COX-2 and pro-inflammatory cytokines. PMID:27380619

  9. Syzygium aromaticum water extract attenuates ethanol‑induced gastric injury through antioxidant effects in rats.

    Science.gov (United States)

    Jin, Seong Eun; Lee, Mee-Young; Shin, In-Sik; Jeon, Woo-Young; Ha, Hyekyung

    2016-07-01

    The aim of the present study was to investigate whether Syzygium aromaticum water extract (SAWE) has a protective effect against ethanol‑induced gastric injury in rats. Acute gastric injury was induced via intragastric administration of absolute ethanol at a dose of 5 ml/kg. SAWE (250 or 500 mg/kg/day) or cimetidine (100 mg/kg/day), which was used as a positive control, were administered to the rats 2 h prior to ethanol administration for 3 days. All rats were sacrificed 24 h following the final ethanol administration. To examine whether SAWE has a gastroprotective effect, assays were performed to assess the contents of malondialdehyde (MDA) and glutathione (GSH), the activities of catalase, glutathione‑S‑transferase and superoxide dismutase, and an immune-linked immunosorbent assay was performed for prostaglandin E2 (PGE2) production in gastric tissues by hematoxylin and eosin and periodic acid-Schiff staining. Histological assessment of the gastric wall was performed. Compared with ethanol treatment alone, treatment with SAWE at a dose of 250 mg/kg/day significantly decreased the gastric MDA content and increased the GSH content, catalase activity, and production of gastric PGE2. Histological assessment showed that SAWE attenuated inflammatory cell infiltration and the loss of epithelial cells. These findings suggested that SAWE protected against ethanol‑induced gastric mucosal injury in the rats. These effects appeared to be associated with antioxidant activity, activation of the production of PGE2, suppression of inflammatory cell infiltration and loss of epithelial cells in the gastric mucosa. Collectively, SAWE may be beneficial in the prevention of gastric disease associated to oxidative stress. PMID:27177078

  10. Effects of pirarubicin, an antitumor antibiotic, on the cardiovascular system.

    Science.gov (United States)

    Hirano, S; Agata, N; Hara, Y; Iguchi, H; Shirai, M; Tone, H; Urakawa, N

    1991-01-01

    In the present study we examined the effects of pirarubicin [(2"R)-4'-O-tetrahydropyranyladriamycin, THP] on a cardiovascular system. An injection of THP (0.39-3.13 mg/kg, i.v.) reduced the mean blood pressure and caused an increase in the respiratory air rate in anesthetized rats. At 1.5 x 10(-6)-1.5 x 10(-5) M, THP markedly relaxed a contraction induced by 10(-7) M norepinephrine in rat aorta with endothelium but not in that without endothelium. At a dose of 0.02-0.5 mg, THP produced an increase in the contractile force and the perfusion flow of isolated perfused guinea pig hearts. At a higher concentration (4.5 x 10(-5)-1.5 x 10(-4) M), it produced a slight increase in the contractile force of the left atria in guinea pigs. This positive inotropic action of THP was inhibited by diphenhydramine (10(-6)-5 x 10(-5) M), chlorpheniramine (3 x 10(-7)-3 x 10(-5) M), and tripelennamine (3 x 10(-7)-3 x 10(-5) M) but not by propranolol (10(-6) M), cimetidine (10(-5) M), diltiazem (10(-6) M), or ryanodine (10(-8) M). THP given i.v. at 2.5 mg/kg elevated the plasma histamine level in anesthetized dogs. From these data, we conclude that THP mainly relaxed the rat aorta in the presence of endothelium and that at higher concentrations, it increased the contractile force in the cardiac muscle, probably mediated through the release of histamine.

  11. Human-health pharmaceutical compounds in Lake Mead, Nevada and Arizona, and Las Vegas Wash, Nevada, October 2000-August 2001

    Science.gov (United States)

    Boyd, Robert A.; Furlong, Edward T.

    2002-01-01

    The U.S. Geological Survey and the National Park Service conducted a reconnaissance study to investigate the occurrence of selected human-health pharmaceutical compounds in water samples collected from Lake Mead on the Colorado River and Las Vegas Wash, a waterway used to transport treated wastewater from the Las Vegas metropolitan area to Lake Mead. Current research indicates many of these compounds can bioaccumulate and may adversely affect aquatic organisms by disrupting physiological processes, impairing reproductive functions, increasing cancer rates, contributing to the development of antibiotic-resistant strains of bacteria, and acting in undesirable ways when mixed with other substances. These compounds may be present in effluent because a high percentage of prescription and non-prescription drugs used for human-health purposes are excreted from the body as a mixture of parent compounds and degraded metabolite compounds; also, they can be released to the environment when unused products are discarded by way of toilets, sinks, and trash in landfills. Thirteen of 33 targeted compounds were detected in at least one water sample collected between October 2000 and August 2001. All concentrations were less than or equal to 0.20 micrograms per liter. The most frequently detected compounds in samples from Las Vegas Wash were caffeine, carbamazepine (used to treat epilepsy), cotinine (a metabolite of nicotine), and dehydronifedipine (a metabolite of the antianginal Procardia). Less frequently detected compounds in samples collected from Las Vegas Wash were antibiotics (clarithromycin, erythromycin, sulfamethoxazole, and trimethoprim), acetaminophen (an analgesic and anti-inflammatory), cimetidine (used to treat ulcers), codeine (a narcotic and analgesic), diltiazem (an antihypertensive), and 1,7-dimethylxanthine (a metabolite of caffeine). Fewer compounds were detected in samples collected from Lake Mead than from Las Vegas Wash. Caffeine was detected in all samples

  12. 药物联合治疗膀胱疼痛综合征/间质性膀胱炎的疗效及影响因素%Efficacy and prognositic factors of combined medical therapy for painful bladder syndrome/ interstitial cystitis

    Institute of Scientific and Technical Information of China (English)

    张宁; 张鹏; 王飚; 张小东; 杨勇

    2009-01-01

    史者、妇科手术或尿道手术史者疗效不佳.%Objective To evaluate the efficacy and prognostic factors of combined medical thera-py with amitriptyline, cimetidine and intravesical resiniferatoxin post-hydrodistention for patients with painful bladder syndrome/interstitial cystitis (PBS/IC). Methods Twenty-nine patients with PBS/ IC according to NIDDK criteria were enrolled. There were 6 males and 23 females with average age of 52±14 years and average duration of symptoms of 3.7±1.9 years before diagnosis. The patients were divided into 2 groups. Non-concomitant disease group included 10 cases without concomitant disease and 7 cases with unrelated diseases such as hypertension and diabetes mellitus. Concomitant disease group included 5 cases with history of bladder neck incision, 3 cases with history of transurethral re-section of the prostate, 2 cases with history of gynecologic disease and 2 cases with history of gyneco-logic operation. Patients of concomitant disease group still had the painful bladder syndrome after 3 months when the primary disease had been cured. All patients were treated with amitriptyline (25 mg twice a day), cimetidine (800 mg per day) and intravesical resiniferatoxin (1-2 times) post-hydrodis-tention. The primary assessment index was O'Leary-Sant score. The secondary assessment index was pelvic pain score, mean voiding times per day and mean volume of each micturating. The data of pa-tients before treatment and after follow-up≥9 months were collected to evaluate the efficacy and prog-nostic factors of the combined treatment. Results The mean follow-up for all patients was 9.2±6.0 months. Patients were followed up at month 1 and month 6 after discharge. Then, patients would be followed up at each 6 months interval. The overall remission rate was 65.5% (19/29). Complete re-mission rate was 41.4% (12/29). Partial remission was 24. 1% (7/29). Non-remission rate was 34.5% (10/29). For all patients, the pre-treatment mean voiding

  13. Determination of the antiepileptics vigabatrin and gabapentin in dosage forms and biological fluids using Hantzsch reaction.

    Science.gov (United States)

    al-Zehouri, J; al-Madi, S; Belal, F

    2001-02-01

    A selective and sensitive method was developed for the determination of the anticonvulsants vigabatrin (I) (CAS 60643-86-9) and gabapentin (II) (CAS 60142-96-3). The method is based on the condensation of the drugs through their amino groups with acetylacetone and formaldehyde according to Hantzsch reaction yeilding the highly fluorescent dihydropyridine derivatives. The yellowish-orange color was also measured spectrophotometrically at 410 nm and 415 nm for I and II, respectively. The absorbance-concentration plots were rectilinear over the ranges 10-70 micrograms/ml and 20-140 micrograms/ml for I and II, respectively. As for the fluorescence-concentration plots, they were linear over the ranges 0.5-10 micrograms/ml and 2.5-20 micrograms/ml with minimum detection limits (S/N = 2) of 0.05 microgram/ml (approximately 2.1 x 10(-8) mol/l) and 0.1 microgram/ml (approximately 5.8 x 10(-7) mol/l) for I and II, respectively. The spectrophotometric method was applied to the determination of I and II in their tablets. The percentage recoveries +/- SD (n = 6) were 99.45 +/- 0.13 and 98.05 +/- 0.53, respectively. The spectrofluorimetric method was successfully applied to the determination of I and II in spiked human urine and plasma. The % recoveries +/- SD (n = 5) were 98.77 +/- 0.29 and 98.39 +/- 0.53 for urine and 99.32 +/- 0.74 and 98.90 +/- 0.96 for plasma, for I and II, respectively. No interference was encountered with the co-administered drugs: valproic acid (CAS 99-66-1), diphenylhydantoin (CAS 57-41-0), phenobarbital (CAS 50-06-6), carbamazepine (CAS 298-46-4), clonazepam (CAS 1622-61-3), clobazam (CAS 22316-47-8) or cimetidine (CAS 51481-61-9). A proposal of the reaction pathway is suggested. The advantages of the proposed methods over existing method are discussed. PMID:11258050

  14. Relato de um caso de latrodectismo ocorrido em Manaus, Amazonas, Brasil Report of a case of latrodectism occurred in Manaus, Amazonas, Brazil

    Directory of Open Access Journals (Sweden)

    Alcidéa R. B. de Souza

    1998-02-01

    Full Text Available Em 02/07/1995, foi atendido no Instituto de Medicina Tropical do Amazonas, paciente masculino, 11 anos, acidentado em Manaus, por picada na região retroauricular direita, clínicamente compatível com aquele causado por Latrodectus. Observavam-se abalos musculares, febre, calafrios e sudorese intensa. Instituída terapêutica com neostigmine precedido de atropina, gluconato de cálcio, cimetidina, diazepam e hidrocortisona. No terceiro dia apresentava-se melhorado, consciente, orientado e com diminuição importante do edema palpebral. A despeito de uma melhora progressiva diária, no quinto dia surgiu eritema máculo-pápulo-vesiculoso. Em 14/07/1995 teve alta, assintomático. O caso relatado é o primeiro descrito na região Amazônica, ocorrido na periferia de Manaus e pode ter sido uma consequência da expansão urbana das duas últimas décadas.In July 2, 1995 arrived at the Instituto de Medicina Tropical do Amazonas an eleven-year-old male with complaining of spider bite on his right retroauricular region, presenting typical findings of latrodectism. The accident was reported as having ocurred in the suburbs of Manaus. The patient was given neostigmine preceded by atropin, calcium gluconate, cimetidin, diazepan and hidrocortisone. Within three days the patient showed improvement, and was aware, orientated and with significant palpebral oedem reduction. Muscle spasms are still present, as well as fever, shivering, and intense sweating. In spite of a daily progressive improvement, at the fifth day appeared a spotted papular erythem. The patient was discharged without simptoms after the13th day. This is the first such reported case which took place in Amazonian region, it might have been happened a consequence of the urban sprawl wich has characterized the growth of the city of Manaus, in the last twenty years. It is not possible at this point to evaluate the epidemiolgical resounds of the event, but in any case, it seems plausible to

  15. Resistance to Qian soup ZhuSheKa interface sp6 joint foot acupoint treatment of chronic urticaria nucleic acid bacteria polysaccharide 30 cases curative effects%抗荨湯联合足三里穴位注射卡介菌多糖核酸治疗慢性荨麻疹30例疗效观察

    Institute of Scientific and Technical Information of China (English)

    胡建农

    2011-01-01

    Objective: To observe Qian soup (bachelor since resistance points to ZhuSheKa sp6 joint foot fungus polysaccharide nucleic acid injection interface. Brand name: ji Sue, zhejiang million horses pharmaceutcal Co. Production. The curative effect of treating chronic urticaria. Methods Selected 60 cases were randomly divided into two groups: treatment group of 30 cases Qian soup to fight ZhuSheKa interface sp6 joint foot fungus polysaccharide acupuncture treatment of nucleic acid injection, four weeks. 30 cases in oral chlorobenzene that sensitivity to 4mg, three times/d, cimetidine 0. 2 g, 2 times a/d; Two groups of course are for 1 month, 2 months after the completion of course judge curative effect, and were followed up for half a year. Results The treatment group and control group 70% , 90% efficiency was statistically significant difference (P<0. OS ) -Conclusion Qian resistance points ZhuSheKa sp6 joint foot soup of nucleic acid injection dielectric bacteria polysaccharide treatment of chronic nettle has good curative effect, and clinical application.%目的:观察抗荨汤联合足三里穴位注射卡介菌多糖核酸注射液治疗慢性荨麻疹的疗效.方法:将入选的60例患者随机分为两组,各30例,治疗组予抗荨汤联合足三里穴位注射卡介菌多糖核酸注射液治疗,隔日1次;对照组予口服氯苯那敏4mg,3次/d,西咪替丁0.2g,2次/d;两组疗程均为1个月,疗程结束后2个月时判定疗效,并随访半年.结果:治疗组有效率90%,对照组70%,差异有统计学意义(P<0.05).结论:抗荨汤联合足三里穴位注射卡介菌多糖核酸注射液治疗慢性荨麻疗效好,值得临床选用.

  16. H1 and H2 receptors in the locus ceruleus are involved in the intracerebroventricular histamine-induced carotid sinus baroreceptor reflex resetting in rats

    Institute of Scientific and Technical Information of China (English)

    Guo-Qing WANG; Wan-Ping SUN; Yong-Jin ZHU; Rong ZOU; Xi-Ping ZHOU

    2006-01-01

    Objective To investigate the role of H1 and H2 receptors in the locus ceruleus (LC) in carotid sinus baroreceptor reflex (CSR) resetting induced by intracerebroventricular (i.c.v.) injection of histamine (HA). Methods The left and right carotid sinus regions were isolated from the systemic circulation in 18 male Sprague-Dawley rats anesthetized with pentobarbital sodium. The intracarotid sinus pressure (ISP) was altered in a stepwise manner in vivo. ISP-mean arterial pressure (MAP) relationship curve and its characteristic parameters were constructed by fitting to the logistic function with five parameters. The changes in CSR performance induced by i.c.v. HA and the effects of pretreatment with H1 or H2 receptors selective antagonist, chlorpheniramine (CHL) or cimetidine (CIM) into the LC, on the responses of CSR to HA were examined. Results I.c.v. HA (100 ng in 5 μl) significantly shifted the ISP-MAP relationship curve upwards (P < 0.05) and obviously decreased the value of the reflex parameters such as MAP range and maximum gain (P < 0.05), but increased the threshold pressure, saturation pressure and ISP at maximum gain (P < 0.05). The pretreatment with CHL (0.5 μg in 1 μl) or CIM (1.5 μg in 1 μl) into the LC could obviously attenuate the changes mentioned above in CSR performance induced by HA, but the alleviative effect of CIM was less remarkable than that ofCHL (P < 0.05). Respective microinjection of CHL or CIM alone into the LC with the corresponding dose and volume did not change CSR performance significantly (P > 0.05). Conclusion Intracerebroventricular administration of HA results in a rapid resetting of CSR and a decrease in reflex sensitivity, and the responses of CSR to HA may be mediated, at least in part, by H1 and H2 receptors activities in the LC, especially by H1 receptors. Moreover, the effects of the central HA on CSR might be related to a histaminergic descending pathway from the hypothalamus to LC.

  17. In vivo electrophysiological investigations into the role of histamine in the dentate gyrus of the rat.

    Science.gov (United States)

    Manahan-Vaughan, D; Reymann, K G; Brown, R E

    1998-06-01

    Drugs acting at the three known classes of histamine receptors were injected intracerebroventricularly into the rat. The effects of these drugs upon synaptic potentials recorded from the dentate gyrus of the freely-moving rat were determined. Population spikes and field excitatory postsynaptic potentials were recorded from the granule cell layer of the dentate gyrus following stimulation of the perforant path. Drugs, dissolved in 0.9% NaCl were applied into the lateral cerebral ventricle in a volume of 5 microl over a period of 6 min. The histamine H1 receptor antagonist mepyramine (0.4 or 0.8 microg) had no significant effect on population spikes or field excitatory postsynaptic potentials. In contrast the H2 receptor antagonist cimetidine (3.25, 6.5 or 13 microg) showed a biphasic effect. At the lower doses (3.25 or 6.5 microg) a small (15%) depression of the field excitatory postsynaptic potentials and population spikes was observed beginning about 1 h following the infusion. At the highest dose tested (13 microg) a marked increase of the population spike was observed beginning immediately following the infusion and lasting for 90 min. Application of the H3 receptor agonist R-alpha-methylhistamine (0.2 microg) depressed the field excitatory postsynaptic potentials (15% at 4 h post-injection) and even more strongly the population spike (50%). Surprisingly, at higher doses (0.4 and 0.8 microg) no effect was seen. The H3 receptor antagonist thioperamide (0.41 and 0.82 microg) did not cause an increase in synaptic potentials but rather at the highest dose a small depression occurred at later time points (2-4 h following the infusion). At the lower dose (0.41 microg) thioperamide blocked the effect of R-alpha-methylhistamine (0.2 microg). These results show that the histaminergic system modulates information flow through the dentate gyrus in a complex manner involving both histamine H2 and H1 receptors.

  18. Randomized crossover study comparing the phosphate-binding efficacy of calcium ketoglutarate versus calcium carbonate in patients on chronic hemodialysis.

    Science.gov (United States)

    Bro, S; Rasmussen, R A; Handberg, J; Olgaard, K; Feldt-Rasmussen, B

    1998-02-01

    The objective of the study was to evaluate the phosphate-binding efficacy, side effects, and cost of therapy of calcium ketoglutarate granulate as compared with calcium carbonate tablets in patients on chronic hemodialysis. The study design used was a randomized, crossover open trial, and the main outcome measurements were plasma ionized calcium levels, plasma phosphate levels, plasma intact parathyroid hormone (PTH) levels, requirements for supplemental aluminum-aminoacetate therapy, patient tolerance, and cost of therapy. Nineteen patients on chronic hemodialysis were treated with a dialysate calcium concentration of 1.25 mmol/L and a fixed alfacalcidol dose for at least 2 months. All had previously tolerated therapy with calcium carbonate. Of the 19 patients included, 10 completed both treatment arms. After 12 weeks of therapy, the mean (+/-SEM) plasma ionized calcium level was significantly lower in the ketoglutarate arm compared with the calcium carbonate arm (4.8+/-0.1 mg/dL v 5.2+/-0.1 mg/dL; P = 0.004), whereas the mean plasma phosphate (4.5+/-0.3 mg/dL v 5.1+/-0.1 mg/dL) and PTH levels (266+/-125 pg/mL v 301+/-148 pg/mL) did not differ significantly between the two treatment arms. Supplemental aluminum-aminoacetate was not required during calcium ketoglutarate treatment, while two patients needed this supplement when treated with calcium carbonate. Five of 17 (29%) patients were withdrawn from calcium ketoglutarate therapy within 1 to 2 weeks due to intolerance (anorexia, vomiting, diarrhea, general uneasiness), whereas the remaining 12 patients did not experience any side effects at all. The five patients with calcium ketoglutarate intolerance all had pre-existing gastrointestinal symptoms; four of them had received treatment with cimetidine or omeprazol before inclusion into the study. Calculations based on median doses after 12 weeks showed that the cost of the therapy in Denmark was 10 times higher for calcium ketoglutarate compared with calcium

  19. A mechanism for the inhibition of neural progenitor cell proliferation by cocaine.

    Directory of Open Access Journals (Sweden)

    Chun-Ting Lee

    2008-06-01

    Full Text Available BACKGROUND: Prenatal exposure of the developing brain to cocaine causes morphological and behavioral abnormalities. Recent studies indicate that cocaine-induced proliferation inhibition and/or apoptosis in neural progenitor cells may play a pivotal role in causing these abnormalities. To understand the molecular mechanism through which cocaine inhibits cell proliferation in neural progenitors, we sought to identify the molecules that are responsible for mediating the effect of cocaine on cell cycle regulation. METHODS AND FINDINGS: Microarray analysis followed by quantitative real-time reverse transcription PCR was used to screen cocaine-responsive and cell cycle-related genes in a neural progenitor cell line where cocaine exposure caused a robust anti-proliferative effect by interfering with the G1-to-S transition. Cyclin A2, among genes related to the G1-to-S cell cycle transition, was most strongly down-regulated by cocaine. Down-regulation of cyclin A was also found in cocaine-treated human primary neural and A2B5+ progenitor cells, as well as in rat fetal brains exposed to cocaine in utero. Reversing cyclin A down-regulation by gene transfer counteracted the proliferation inhibition caused by cocaine. Further, we found that cocaine-induced accumulation of reactive oxygen species, which involves N-oxidation of cocaine via cytochrome P450, promotes cyclin A down-regulation by causing an endoplasmic reticulum (ER stress response, as indicated by increased phosphorylation of eIF2alpha and expression of ATF4. In the developing rat brain, the P450 inhibitor cimetidine counteracted cocaine-induced inhibition of neural progenitor cell proliferation as well as down-regulation of cyclin A. CONCLUSIONS: Our results demonstrate that down-regulation of cyclin A underlies cocaine-induced proliferation inhibition in neural progenitors. The down-regulation of cyclin A is initiated by N-oxidative metabolism of cocaine and consequent ER stress. Inhibition of

  20. Ethanol oxidation and the inhibition by drugs in human liver, stomach and small intestine: Quantitative assessment with numerical organ modeling of alcohol dehydrogenase isozymes.

    Science.gov (United States)

    Chi, Yu-Chou; Lee, Shou-Lun; Lai, Ching-Long; Lee, Yung-Pin; Lee, Shiao-Pieng; Chiang, Chien-Ping; Yin, Shih-Jiun

    2016-10-25

    Alcohol dehydrogenase (ADH) is the principal enzyme responsible for metabolism of ethanol. Human ADH constitutes a complex isozyme family with striking variations in kinetic function and tissue distribution. Liver and gastrointestinal tract are the major sites for first-pass metabolism (FPM). Their relative contributions to alcohol FPM and degrees of the inhibitions by aspirin and its metabolite salicylate, acetaminophen and cimetidine remain controversial. To address this issue, mathematical organ modeling of ethanol-oxidizing activities in target tissues and that of the ethanol-drug interactions were constructed by linear combination of the corresponding numerical rate equations of tissue constituent ADH isozymes with the documented isozyme protein contents, kinetic parameters for ethanol oxidation and the drug inhibitions of ADH isozymes/allozymes that were determined in 0.1 M sodium phosphate at pH 7.5 and 25 °C containing 0.5 mM NAD(+). The organ simulations reveal that the ADH activities in mucosae of the stomach, duodenum and jejunum with ADH1C*1/*1 genotype are less than 1%, respectively, that of the ADH1B*1/*1-ADH1C*1/*1 liver at 1-200 mM ethanol, indicating that liver is major site of the FPM. The apparent hepatic KM and Vmax for ethanol oxidation are simulated to be 0.093 ± 0.019 mM and 4.0 ± 0.1 mmol/min, respectively. At 95% clearance in liver, the logarithmic average sinusoidal ethanol concentration is determined to be 0.80 mM in accordance with the flow-limited gradient perfusion model. The organ simulations indicate that higher therapeutic acetaminophen (0.5 mM) inhibits 16% of ADH1B*1/*1 hepatic ADH activity at 2-20 mM ethanol and that therapeutic salicylate (1.5 mM) inhibits 30-31% of the ADH1B*2/*2 activity, suggesting potential significant inhibitions of ethanol FPM in these allelotypes. The result provides systematic evaluations and predictions by computer simulation on potential ethanol FPM in target tissues and hepatic

  1. Effects of histamine and its antagonists on murine T-cells and bone marrow-derived dendritic cells

    Directory of Open Access Journals (Sweden)

    Hu XF

    2015-08-01

    Full Text Available Xiufen Hu,1,* Mohammad Ishraq Zafar,2,* Feng Gao2 1Department of Paediatrics, Tongji Hospital, 2Department of Endocrinology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, People’s Republic of China *These authors contributed equally to this work Abstract: We determined the effects of histamine and its antagonists on the surface marker expression of dendritic cells (DCs and the influence of lipopolysaccharide (LPS, histamine, and histamine receptor antagonists on DCs and T-cells. The bone marrow was extracted from the femurs and tibiae of 6- to 8-week-old female Balb/c mice and cultured in medium containing penicillin, streptomycin, L-glutamine, fetal calf serum, or granulocyte macrophage colony-stimulating factor (GM-CSF alone or with interleukin (IL-4. The cells received three different doses of LPS and histamine, plus three different doses of descarboethoxyloratadine (DCL. We assayed the supernatant for various cytokines. The spleen cells of DO11.10 mice were examined by flow cytometry, which included labeling and sorting CD4+ T-cells, as well as coculture of DCs and T-cells with ovalbumin (OVA323–339 peptide. Histamine or histamine plus DCL did not affect the expression of major histocompatibility complex class II, CD11c, CD11b, CD86, and CD80. However, GM-CSF increased the expression of all markers except CD80. Histamine increased interferon-γ production in GM-CSF + IL-4-cultured cells; it also enhanced IL-10 production, but suppressed IL-12 production in LPS-stimulated DCs with no DCL. Cimetidine inhibited IL-10 production and restored IL-12 secretion in LPS-treated DCs. LPS increased IL-10 and decreased IL-12 levels. GM-CSF + IL-4-generated DCs had a stronger stimulatory effect on DO11.10 T-cell proliferation than GM-CSF-generated DCs. Inducible costimulator ligand expression was higher in GM-CSF + IL-4- than in GM-CSF-generated DC groups after 2 days of coculture, but decreased 4 days

  2. Serious drug interactions.

    Science.gov (United States)

    Aronson, J

    1993-10-01

    Of the many varieties of drug interactions, which occur when the disposition or actions of one drug are changed by another, only a few are serious or potentially fatal. A representative outline of some of these illustrates the problem. Precipitant drugs are those which produce the interaction, and object drugs are those whose effects are changed. The interactions which are usually significant are those which alter the metabolism, involve renal excretion, or change the effects of the object drug, especially when the object drug has a low therapeutic index (cardiovascular drugs, anticoagulants, drugs acting on the brain, hypoglycemic drugs, hormones, and cytotoxic drugs). Warfarin toxicity, for example, is produced by aspirin, phenylbutazone, and azapropazone. The dosage requirements of warfarin are reduced by chloramphenicol, ciprofloxacin and other quinolones, erythromycin and some of the other macrolides, metronidazole and other imidazoles, tetracyclines, amiodarone, cimetidine (but not ranitidine), and fibrates. Potassium-depleting drugs can potentiate the action of digoxin, and the elimination of digoxin can be reduced by amiodarone, propafenone, quinidine, and verapamil. Combined oral contraceptives can lose effectiveness through the interaction of carbamazepine, griseofulvin, phenytoin, or rifampicin, which increase estrogen metabolism. In addition, broad-spectrum antibiotics such as ampicillin or tetracyclines also reduce contraceptive effectiveness by altering gut absorption. Even a single drink of an alcoholic beverage may be dangerous to people taking antidepressants, antihistamines, antipsychotic drugs, benzodiazepines, or lithium. Antihistamines suffer inhibited metabolism in the liver if taken in conjunction with the antifungal imidazoles and some of the macrolide antibiotics. Cardiotoxicity of antihistamines is also enhanced by drugs with similar cardiotoxic effects. Lithium potentiation is enhanced by the new serotonin-reuptake inhibitors, and lithium

  3. Gynaecomastia: management in a developing country

    International Nuclear Information System (INIS)

    Gynaecomastia is a benign enlargement of male breast. It is common in the general population, resulting from various pathophysiological mechanisms. The aim of this study was to describe the presentation and outcome of treatment for gynaecomastia at a University Hospital in Pakistan. Methods: A three year retrospective study was carried out of one hundred men with gynaecomastia. Patients were evaluated in detail clinically and by appropriate investigations. They were counselled and kept on hormonal therapy for three months. Surgery was considered for patients with long standing gynaecomastia, failed medical therapy and for cosmetic reasons. Post operative complications and patient's satisfaction was assessed. Results: Most (90%) cases were idiopathic. Other causes were liver cirrhosis in 4 cases, testicular tumour in two, thyrotoxicosis in one and drug induced (use of cimetidine and Kushta) in two. Carcinoma of the breast was diagnosed in one patient. Most of the patients had bilateral, non tender lump in the breast. Three cases of idiopathic gynaecomastia resolved on danazol. Eighty-eight cases underwent surgical treatment. The mean age of patients who underwent surgery (n=88) was 30.5+-9.59 years. Most of the patients belonged to 21-30 years age group. Major indications for surgery were failure of medical treatment (45.5%) and cosmetic reasons (34.0%). Mean operating time for subcutaneous mastectomy was 42.2 +- 3.70 (36-48) minutes. Mean hospital stay after subcutaneous mastectomy was 5.2+- 2.44 (2-10) days. The only postoperative complication noted was wound infection (24%). Seventy-two (81.8%) were satisfied with the results of their surgical treatment. Conclusion: Gynaecomastia is the common condition affecting male breasts and most common cause of gynaecomastia is idiopathic. Secondary gynaecomastia may regress in size by treating the primary cause. Idiopathic gynaecomastia do not respond to danazol so they needed surgical treatment. Subcutaneous mastectomy

  4. Efecto del OLEOZON® frente a lesiones gástricas inducidas por indometacina en ratas (Effect of OLEOZON® on gastric lesions induced by indomethacin in rats

    Directory of Open Access Journals (Sweden)

    González Alvarez Ricardo

    2007-03-01

    indomethacin. In the second experiment gastric lesions were induced by indomethacin and thereafter treated with Oleozon in the same range of doses. Gastric lesions were evaluated determining the ulceration index. Cimetidine was used as areference antiulcer drug. The results demonstrated that the pretreatment with Oleozon did not prevent gastric damageinduced by indomethacin and therefore did not exert cytoprotective effect. In contrast, the treatment with Oleozon induced reversionof gastric lesions induced previously by indomethacin. These results support the potential therapeutic effectiveness of Oleozon as antiulcer drug in this experimental model.

  5. Scintigraphic assessment of Barrett's esophagus

    International Nuclear Information System (INIS)

    Barrett's (B) esophagus is defined by the presence of columnar epithelium above the gastroesophageal junction. Patients with 5cm histologically proven B were evaluated for mucosal labeling (ML), esophageal motility (EM), gastroesophageal reflux (GER), and gastric emptying (GE) of solids and liquids with and without iv metaclopramide (MCP). ML, after premedication with cimetidine, was evaluated 20 and 40 min after injection of Tc-99m04 with ANT and RAO views. Eight of 11 B and 0 of 2 controls (C) labeled esophageal mucosa. EM was assessed in the supine position over one min after a 15 ml swallow Tc-99mSc-H2O. The normal pattern shows sequential, aboral, discreet peaks with no retrograde movement over one min in three computer derived regions over the esophagus. Five of 16 B and 1 of 6 C demonstrated abnormal pattern. GER was assessed in the supine position by serially increasing extrinsic binder pressures from 0 to 100 Torr after ingestion of 300 ml of Tc-99mSc-orange juice (OJ). GER was present in 13 of 15 B and 0 of 11 C. Reflux ranged from 5.1% to 30% at 100 Torr. Hiatal hernia (HH) was identified in 14 of 16 B by endoscopy and in 10 of 16 by scintigraphy. GE was evaluated after a liquid meal of 300 ml Tc-99mSc-OJ and a solid meal of Tc-99mSc-egg salad sandwich. The supine subject was imaged anteriorly for 30 min (liquid) or 60 min (solid). GE was assessed an additional 10 min after MCP. Clearance time (50%) for solid Ge was calculated from extrapolated linear fits of decay corrected data. There was no significant difference in liquid or solid GE between B and C. The authors conclude the following: 1) ML detects B with lower sensitivity than previously reported; 2) EM disorders are frequently found in B; 3) GER is frequently identified in B; 4) HH can be identified by nuclear technique; and 5) B shows normal GE and responds to MCP

  6. Scintigraphic assessment of Barrett's esophagus

    Energy Technology Data Exchange (ETDEWEB)

    Kotler, J.A.; Sampliner, R.E.; Kogan, F.J.; Henry, R.E.; Mason, B.F.

    1984-01-01

    Barrett's (B) esophagus is defined by the presence of columnar epithelium above the gastroesophageal junction. Patients with 5cm histologically proven B were evaluated for mucosal labeling (ML), esophageal motility (EM), gastroesophageal reflux (GER), and gastric emptying (GE) of solids and liquids with and without iv metaclopramide (MCP). ML, after premedication with cimetidine, was evaluated 20 and 40 min after injection of Tc-99m04 with ANT and RAO views. Eight of 11 B and 0 of 2 controls (C) labeled esophageal mucosa. EM was assessed in the supine position over one min after a 15 ml swallow Tc-99mSc-H2O. The normal pattern shows sequential, aboral, discreet peaks with no retrograde movement over one min in three computer derived regions over the esophagus. Five of 16 B and 1 of 6 C demonstrated abnormal pattern. GER was assessed in the supine position by serially increasing extrinsic binder pressures from 0 to 100 Torr after ingestion of 300 ml of Tc-99mSc-orange juice (OJ). GER was present in 13 of 15 B and 0 of 11 C. Reflux ranged from 5.1% to 30% at 100 Torr. Hiatal hernia (HH) was identified in 14 of 16 B by endoscopy and in 10 of 16 by scintigraphy. GE was evaluated after a liquid meal of 300 ml Tc-99mSc-OJ and a solid meal of Tc-99mSc-egg salad sandwich. The supine subject was imaged anteriorly for 30 min (liquid) or 60 min (solid). GE was assessed an additional 10 min after MCP. Clearance time (50%) for solid Ge was calculated from extrapolated linear fits of decay corrected data. There was no significant difference in liquid or solid GE between B and C. The authors conclude the following: 1) ML detects B with lower sensitivity than previously reported; 2) EM disorders are frequently found in B; 3) GER is frequently identified in B; 4) HH can be identified by nuclear technique; and 5) B shows normal GE and responds to MCP.

  7. Effects of Different Adjuvant on the Immune Responses to Recombi-nant Protein L2E7E6 of Human Papillomavirus Type 16 in Mice%不同佐剂对人乳头瘤病毒16型L2E7E6蛋白免疫效果的影响

    Institute of Scientific and Technical Information of China (English)

    任皎; 赵莉; 高孟; 姜云水; 郝明强; 谭文杰; 田厚文; 阮力

    2013-01-01

      Objective: To investigate the effects of CpG, freund adjuvant, poly I:C, levamisole and cimetidine on the immune responses to recombinant protein L2E7E6 of human papillomavirus type 16 in mice. Methods: C57BL/6 mice were immunized with recombinant protein L2E7E6 combined with or without CpG, freund adjuvant, poly I:C, levamisole or cimetidine through intramuscular. Then the humoral and cellular immune responses were detected by ELISA and ELISPOT respectively, and the effects of tumor growth regression were measured by using the TC-1 tumor bearing mice model. Results: All of groups mice immunized with the recombinant protein L2E7E6 combined with or without adjuvant could elicit high specific IgG antibodies titer against L2, E7 and E6 proteins (IgG1 antibodies were predominant), among which those with freund adjuvant could secret higher IgG and IgG1 antibodies against E6 antigen and higher IgG1 antibody against E7 antigen respectively(P<0.05), and those with CpG could secret higher Th1-associated IgG2a antibodies against E7 antigen(P<0.05), however those with cimeti⁃dine could secret lower IgG antibody against E7 antigen(P<0.05). Furthermore, the mice vaccinated with the re⁃combinant protein combined with CpG could elicit stronger T cell immune responses to peptides E7 and E6 re⁃spectively, and eliminate the established TC-1 tumors in 70% vaccinated mice. In addition, those mice vaccinated with freund adjuvant and poly I:C were able to elicit moderate cellular immune responses to peptide E7 and de⁃layed tumor appearance in tumor-bearing mice. Conclusion: Accompanied with CpG, freund adjuvant or poly I:C, the recombinant protein could be enhanced on the cellular immune response and the effects of tumor growth re⁃gression in immunized mice, and it could have better effects with the CpG, which will provide the basis to devel⁃ op the L2E7E6 protein as one promising candidate vaccine.%  目的:研究CpG佐剂、弗氏佐剂、聚肌胞苷酸佐剂

  8. Organic anion transporter 3- and organic anion transporting polypeptides 1B1- and 1B3-mediated transport of catalposide

    Directory of Open Access Journals (Sweden)

    Jeong HU

    2015-01-01

    Full Text Available Hyeon-Uk Jeong,1 Mihwa Kwon,2 Yongnam Lee,3 Ji Seok Yoo,3 Dae Hee Shin,3 Im-Sook Song,2 Hye Suk Lee1 1College of Pharmacy, The Catholic University of Korea, Bucheon 420-743, Korea; 2College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 702-701, Korea; 3Central R&D Institute, Yungjin Pharm Co., Ltd., Suwon 443-270, Korea Abstract: We investigated the in vitro transport characteristics of catalposide in HEK293 cells overexpressing organic anion transporter 1 (OAT1, OAT3, organic anion transporting polypeptide 1B1 (OATP1B1, OATP1B3, organic cation transporter 1 (OCT1, OCT2, P-glycoprotein (P-gp, and breast cancer resistance protein (BCRP. The transport mechanism of catalposide was investigated in HEK293 and LLC-PK1 cells overexpressing the relevant transporters. The uptake of catalposide was 319-, 13.6-, and 9.3-fold greater in HEK293 cells overexpressing OAT3, OATP1B1, and OATP1B3 transporters, respectively, than in HEK293 control cells. The increased uptake of catalposide via the OAT3, OATP1B1, and OATP1B3 transporters was decreased to basal levels in the presence of representative inhibitors such as probenecid, furosemide, and cimetidine (for OAT3 and cyclosporin A, gemfibrozil, and rifampin (for OATP1B1 and OATP1B3. The concentration-dependent OAT3-mediated uptake of catalposide revealed the following kinetic parameters: Michaelis constant (Km =41.5 µM, maximum uptake rate (Vmax =46.2 pmol/minute, and intrinsic clearance (CLint =1.11 µL/minute. OATP1B1- and OATP1B3-mediated catalposide uptake also showed concentration dependency, with low CLint values of 0.035 and 0.034 µL/minute, respectively. However, the OCT1, OCT2, OAT1, P-gp, and BCRP transporters were apparently not involved in the uptake of catalposide into cells. In addition, catalposide inhibited the transport activities of OAT3, OATP1B1, and OATP1B3 with half-maximal inhibitory concentration values of 83, 200, and 235 µ

  9. 输液性静脉炎发生的原因及药物治疗进展%Causes of infusion phlebitis and advances in drug treatment

    Institute of Scientific and Technical Information of China (English)

    张峥; 朱全刚; 毛燕君

    2012-01-01

    Infusion phlebitis (IP) is the most common complication in the treatment of intravenous infusion, which not only increases the suffering of patients and health care costs, prolongs hospitalization, but also is a common cause of medical dispute. The occurrence of IP is related to drug factors, such as antineoplastic agents, antibiotics, sedative-hypnotics,etc, as well as infusion osmotic pressure and infusion pH value. Non-drug factors include paniculate pollution, catheter material and indwelling needle, etc. The mechanism involved may be associated with the E-selectin and intercellular adhesion molecule-1. Main emphasis should be paid to the prevention of IP. Prior intravenous administration of 200 mg cimetidine is effective in preventing vinorelbine-induced IP. Local applications of 25 % magnesium sulfate solution and anisodamine solution can also reduce the occurrence of IP. Partial hermetization, local application and physical therapy are the main treatment of IP. Drugs commonly used for the treatment of IP include nitroglycerin patch, heparin sodium ointment, multi-sulfonic acid mucopolysac-charide cream, piroxicam gel, Sanqi cream, diclofenac gel, tablets, etc.%输液性静脉炎(infusion phlebitis,IP)是静脉输液治疗中最常见的并发症,不仅增加病人的痛苦及医疗费用,延长住院时间,同时也是医患纠纷的常见原因.该病症的发生有药物因素,如抗肿瘤药、抗生素、镇静催眠药等可能诱发IP,输液渗透压以及输液pH值也与IP的发生有关.非药物因素有微粒污染、导管材质和静脉留置针等.IP的发生机制可能与E-选择素和细胞间黏附分子-1有关.IP应以预防为主,事先静脉注射西咪替丁200mg可有效预防长春瑞滨引起的IP.局部外敷25%硫酸镁溶液和山莨菪碱溶液也可减少IP的发生率.IP的治疗可采用局部封闭、局部外敷及物理疗法,常用药物包括硝酸甘油贴膜、肝素钠软膏、多磺酸黏多糖软膏、吡罗昔

  10. 左氧氟沙星在人胃黏膜上皮细胞中的摄取特征%Study on the uptake of levofloxacin by gastric epithelial system cells

    Institute of Scientific and Technical Information of China (English)

    胡兴萍; 胡咏梅; 张磊; 张珊珊; 许建明

    2014-01-01

    Objective To investigate the uptake mechanisms of levoflox-acin by gastric epithelial system ( GES-1 ) cells.Methods The uptake of levofloxacin in GES-1 cells were determined by HPLC and coomassie brilliant blue.The influences of incubated time ,extracellular levofloxacin concentrations, pH, temperature, inhibitors of transporters on the uptake of levofloxacin by GES -1 cells were tested.Results The uptake of levofloxacin by GES-1 cells was increased sharply at 1-5 minutes then was increased moderately at 7.5 -15.0 minutes and reached a steady state after the start of the incubation.The accumulation of levofloxacin increased with the extracellar levels ,but which was not linearly.The up-take of levofloxacin reached a maximum when temperature was 37 ℃and pH was 7.4.The increase in levofloxacin accumulation by cyclosporin A and verapamil in GES -1 cells was by 2.81% -13.23%, 2.07% -10.28%, respectively ( P >0.05 ).Effect of the cimetidine was not same that the two drugs.Conclusion Levofloxacin enters into GES -1 cells in carrier-mediated transport manner.P-gp might be involved in the process of uptake of levofloxacin in GES -1 cells.%目的:研究左氧氟沙星在人胃黏膜上皮细胞(GES-1)中的摄取特征。方法 GES-1细胞与左氧氟沙星孵育后用高效液相色谱法和考马斯亮蓝法研究其在细胞内的药物摄取量,同时考察时间、药物浓度、温度、pH值和转运体抑制剂(环孢素A、维拉帕米和西咪替丁)对左氧氟沙星在GES-1细胞中摄取的影响。结果在GES-1细胞内,左氧氟沙星摄取量,在1~5 min明显增加,在7.5~15.0 min缓慢增加并达到稳态;摄取量随着细胞外左氧氟沙星浓度的增加而增加,但不呈线性增加。在37℃、pH 7.4时,摄取量最大。环孢素A和维拉帕米能增加细胞内药物摄取量,分别较对照组增加了2.81%~13.23%,2.07%~10.28%,但差异无统计学意义( P>0.05);西咪替丁对此均

  11. A role for inositol 1,4,5-trisphosphate in the initiation of agonist-induced contractions of dog tracheal smooth muscle.

    Science.gov (United States)

    Hashimoto, T; Hirata, M; Ito, Y

    1985-09-01

    cimetidine (10-5M), nor prostaglandin F2 alpha. (PGF2 alpha. 1O-7 M) showed any effect on the contents of PI-P2 or PA in the lipid fraction of the smooth muscle cells. 8 These results indicate that in muscle cells of the dog trachea, Ins-P3 may play the role ofintracellular second messenger in the initiation of ACh or 5-HT-induced contraction, but not in the case of histamine or PGF2 alpha-induced contraction.

  12. Study on the Curative Effect of Esomeprazole Combined with Xylitol Infu-sion in the Treatment of Gastrointestinal Hemorrhage%埃索美拉唑联合木糖醇注射液治疗消化道出血疗效分析

    Institute of Scientific and Technical Information of China (English)

    张慧

    2015-01-01

    目的:分析消化道出血行埃索美拉唑与木糖醇注射液联合治疗的效果。方法回顾性分析2013年2月-2015年2月该院收治的消化道出血130例患者临床资料,按数字表法分为观察组和对照组,每组65例。对照组行西咪替丁治疗,观察组行埃索美拉唑与木糖醇注射液联合治疗,比较两组疗效。结果观察组总有效率96.92%显著比对照组70.77%高,且平均止血时间(1.50±0.02)d比对照组(3.65±2.36)d少,平均治疗时间(10.02±8.10)d比对照组(25.15±12.50)d少,比较差异均有统计学意义(P<0.05)。结论消化道出血患者行埃索美拉唑与木糖醇注射液联合治疗的效果显著,可有效止血。%Objective To analyze the effect of Esomeprazole combined Xylitol infusion in the treatment of gastrointestinal hemor-rhage. Methods The clinical data of 130 patients with gastrointestinal hemorrhage treated in our hospital between February 2013 and February 2015 were reviewed, and were randomly divided into an observation group and a control group, each with 65 cases. Patients in the control group received Cimetidine for treatment, whereas those in the observation group were given Esomeprazole and Xylitol infusion combined for treatment. The curative effect was compared between the two groups. Results The total rate treatment effectiveness in the observation group was 96.92%, significantly higher than that in the control group, which was 70.77%; And the mean time to hemostasis (1.50 ± 0.02) d d less than in the control group (3.65 ± 2.36), the mean duration of treatment (10.02 ± 8.10) d less than in the control group (25.15 ± 12.50) d, differences were statistically significant (P<0.05). Conclusion The combined therapy of Esomeprazole and Xylitol infusion is with significant curative effect for treating gastrointesti-nal bleeding, which can effectively stop the hemorrhage.

  13. Application of Combined Bacillus Subtilis and Enterococcus Faecium Granules with Multivitamines-Live in Treatment of Henoch Purpura in Children%枯草杆菌二联活菌颗粒在儿童腹型过敏性紫癜中的应用

    Institute of Scientific and Technical Information of China (English)

    左满凤; 艾柳; 舒琼璋; 董晶

    2012-01-01

    Objective:To observe the adjunctive effect of the viable organism praeparatum Combined Bacillus Subtilis and Enterococcus Faecium Granules with Multivitamines-Live(Medilae-Vita) in the treatment of henoch purpura in children. Methods: Together 139 children with henoch purpura as research subjects were divided into observation group and control group by random number table method. In the control group, children were treated with cimetidine, vitamin C, calcium, glucocorticosteroid; and antibiotics therapy was given to those who had combined infection. The observation group were given Medilac-Vita in addition to the same treatment as the control group. Aged 4~6 years, 1 g each time; aged - 12 years, 1. 5 g each time; all three times a day, 7 days as a course of treatment. The symptom changes of digestive tube ( stomachache, emesia, hemafecia), levels of salivary secretary IgA ( sIgA) and clinical effect after treatment in I week of the two groups were observed. Results: The extinction time of digestive tube symptoms in observation group was less than that of the control group (P0.05). The total effective rate in observation group was 95.71% , while that of the control group was 81.82% , there was significant difference in the two groups (x2 = 4. 978, P<0. 05). Conclusions: Viable organism praeparatum Medilac-Vila can enhance the immunity of mucous membrane. In the treatment of henoch purpura in children, it can relieve digestive tube symptoms quickly, prevent alimentary tract hemorrhage, and shorten the course of treatment%目的:观察枯草杆菌二联活菌颗粒在儿童腹型过敏性紫癜(HSP)治疗中的辅助作用.方法:将139例腹型HSP住院患儿中完成研究的125例纳入研究对象,采用随机数字表法随机分为观察组70例和对照组55例.对照组给予西咪替丁、维生素C、钙剂及糖皮质激素等综合治疗,合并感染者给予抗生素治疗,观察组在对照组治疗基础上加服枯草杆菌二联活菌颗粒,年龄4

  14. 孤束核胆碱能与组胺能系统对颈动脉窦压力感受器反射调节的交互作用%Involvement of cross interaction between central cholinergic and histaminergic systems in the nucleus tractus solitarius in regulating carotid sinus baroreceptor reflex

    Institute of Scientific and Technical Information of China (English)

    胡力旬; 张国兴; 张玉英; 赵红芬; 于康英; 王国卿

    2013-01-01

    脑胆碱能系统与组胺能系统影响颈动脉窦压力感受器反射(carotid sinus baroreceptor reflex,CSR)活动,然而二者是否在孤束核(nucleus tractus solitarius,NTS)水平相互作用,跨转调节CSR,尚不清楚.本文在麻醉Sprague-Dawley (SD)大鼠孤离的一侧颈动脉窦区,通过窦内逐级加压引发CSR和动脉血压变化,经Logistic五参数曲线拟合,求得窦内压(intracarotid sinus pressure,ISP)-平均动脉压(mean arterial pressure,MAP)关系曲线及其特征参数,观察预先在NTS微量注射各选择性胆碱能受体拮抗剂[M1受体拮抗剂哌仑西平(pirenzepine,PRZ)、M2受体拮抗剂美索曲明(methoctramine,MTR)或N1受体拮抗剂六烃季胺(hexamethonium,HEX)]对侧脑室微量注射(intracerebroventricular injection,i.c.v.)组胺(histamine,HA)所致CSR变化的影响,以及预先在NTS微量注射组胺能H1受体拮抗剂氯苯吡胺(chlorpheniramine,CHL)或H2受体拮抗剂西咪替丁(cimetidine,CIM)对i.c.v.拟胆碱药毒扁豆碱(physostigmine,PHY)所致CSR变化的影响,以期解析中枢两大系统对CSR是否具有跨转调节机制.结果显示:(1)单独NTS内注射所给剂量的各选择性胆碱能受体拮抗剂或组胺能受体拮抗剂对CSR均无明显作用(P>0.05),也不引起动脉血压水平明显变动;(2)预先NTS内注射PRZ或MTR可部分翻转i.c.v.HA所致的CSR重调定,表现为ISP-MAP关系曲线在高窦压区明显左下移位(P<0.05),ISP-Gain关系曲线在中窦压区显著上移(P<0.05),反射参数平均动脉压变动范围和最大增益加大(P<0.05),最大增益时的窦内压值与饱和压减少(P<0.05),上述效应中PRZ的作用不如MTR的显著(P<0.05),但HEX对i.c.v.HA所致的CSR变化无明显作用(P>0.05);(3)预先NTS内注射CHL或CIM对i.c.v.PHY所致CSR变化的影响,类似于NTS内注射PRZ或MTR对i.c.v.HA所致CSR变化的作用,且CHL的效应强于CIM (P< 0.05).上述结果表明:侧脑室注射HA所致的CSR重调定机制

  15. Anestesia para correção intra-útero de mielomeningocele: relato de caso Anestesia para corrección intra-útero de mielomeningocele: relato de caso Anesthesia for intrauterine myelomeningocele correction: case report

    Directory of Open Access Journals (Sweden)

    Angélica de Fátima de Assunção Braga

    2005-06-01

    mantenida arriba de 100 mmHg, con efedrina en bolus (5 mg, coloides y cristalóides. El líquido amniótico perdido fue sustituido por solución fisiológica entibiada. Después de la corrección del defecto fetal, se procedió al encerramiento uterino y de la membrana amniótica en dos planos, con hilo de vicryl y cola de fibrina. Se siguió la disminución gradativa de la concentración del isoflurano, y para el mantenimiento del relajamiento uterino se utilizó sulfato de magnesio (4 g/20minutos, seguido de infusión continuada (2 g/hora. Al final de la cirugía se inyectó morfina (2 mg por el catéter peridural para la analgesia postoperatoria. CONCLUSIONES: La anestesia para cirugía fetal envuelve dos seres, madre y feto, y el manoseo anestésico requiere: seguridad materno-fetal, anestesia e inmovilidad fetal, relajamiento uterino, prevención del trabajo de alumbramiento prematuro y analgesia postoperatoria.BACKGROUND AND OBJECTIVES: Fetal surgery is the treatment of choices for prenatal malformations that are not adequately corrected after birth and aims at treating or preventing the progression of the abnormalities. This report describes a case of anesthesia for intrauterine correction of a myelomeningocele. CASE REPORT: Pregnant patient, 19 years old, 23 weeks of gestational age, without previous anesthetic history, physical status ASA I, submitted to intrauterine fetal surgery under general anesthesia associated to continuous epidural continuous anesthesia. The patient was premedicated with rectal indomethacin (50 mg, intravenous metoclopramide (10 mg and cimetidine (50 mg, in addition to intravenous midazolam (2 mg. The patient received 0.25% bupivacaine with epinephrine (25 mg associated to fentanyl (100 µg epidurally, followed by cephalic catheter insertion for postoperative analgesia. The uterus was left-displace with a Crawford's wedge. Rapid sequence anesthesia was induced with fentanyl, propofol and rocuronium, and was maintained with 2.5% - 3