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Charles S Lieber - One of the best experts on this subject based on the ideXlab platform.
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effects of h2 receptor antagonists on gastric alcohol dehydrogenase activity
Digestive Diseases and Sciences, 1991Co-Authors: Joan Caballeria, Enrique Baraona, Ramon Deulofeu, Rolando Hernandezmunoz, Juan Rodes, Charles S LieberAbstract:Inhibition of gastric alcohol dehydrogenase (ADH) activity by Cimetidine results in elevated blood levels of ethanol after moderate consumption. To search for alternative H2-blockers lacking such an effect, we compared Cimetidine, ranitidine, nizatidine, and famotidine. They inhibited rat gastric ADH noncompetitively, with aKi for ethanol oxidation of 0.68 mM for Cimetidine, 0.5 mM for ranitidine, 1 mM for nizatidine, and 4.5 mM for famotidine. These concentrations are higher than therapeutic plasma levels, but intracellular concentrations in the gastric mucosa (assessed with [3H] Cimetidine and [14C]famotidine) were at least 10- and 2-fold greater than in the blood, respectively. These results suggests that, given at therapeutic dosesin vivo, the degree of inhibition by Cimetidine and ranitidine should be significant and comparable, that by nizatidine should be smaller, and that by famotidine should be negligible. These drugs also exerted either mixed or competitive inhibition of rat hepatic ADH, but the effects of Cimetidine and famotidine were observed at concentrations unlikely to occurin vivo. Thus, in alcoholics and in social drinkers who require treatment with H2-receptor antagonists, famotidine might be preferable to the other H2 blockers tested.
Alex Sparreboom - One of the best experts on this subject based on the ideXlab platform.
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conjunctive therapy of cisplatin with the oct2 inhibitor Cimetidine influence on antitumor efficacy and systemic clearance
Clinical Pharmacology & Therapeutics, 2013Co-Authors: Jason A Sprowl, L Van Doorn, L Van Gerven, P De Bruijn, Alice A Gibson, Ron H J Mathijssen, Alex SparreboomAbstract:The organic cation transporter 2 (OCT2) regulates uptake of cisplatin in proximal tubules, and inhibition of OCT2 protects against severe cisplatin-induced nephrotoxicity. However, it remains uncertain whether potent OCT2 inhibitors, such as Cimetidine, can influence the antitumor properties and/or disposition of cisplatin. Using an array of preclinical assays, we found that Cimetidine had no effect on the uptake and cytotoxicity of cisplatin in ovarian cancer cells with high OCT2 mRNA levels (IGROV-1 cells). Moreover, the antitumor efficacy of cisplatin in mice bearing luciferase-tagged IGROV-1 xenografts was unaffected by Cimetidine (P = 0.39). Data obtained in 18 patients receiving cisplatin (100 mg/m(2)) in a randomized crossover fashion with or without Cimetidine (800 mg × 2) revealed that Cimetidine did not alter exposure to unbound cisplatin, a marker of antitumor efficacy (4.37 vs. 4.38 µg·h/ml; P = 0.86). These results support the future clinical exploration of OCT2 inhibitors as specific modifiers of cisplatin-induced nephrotoxicity.
Joan Caballeria - One of the best experts on this subject based on the ideXlab platform.
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effects of h2 receptor antagonists on gastric alcohol dehydrogenase activity
Digestive Diseases and Sciences, 1991Co-Authors: Joan Caballeria, Enrique Baraona, Ramon Deulofeu, Rolando Hernandezmunoz, Juan Rodes, Charles S LieberAbstract:Inhibition of gastric alcohol dehydrogenase (ADH) activity by Cimetidine results in elevated blood levels of ethanol after moderate consumption. To search for alternative H2-blockers lacking such an effect, we compared Cimetidine, ranitidine, nizatidine, and famotidine. They inhibited rat gastric ADH noncompetitively, with aKi for ethanol oxidation of 0.68 mM for Cimetidine, 0.5 mM for ranitidine, 1 mM for nizatidine, and 4.5 mM for famotidine. These concentrations are higher than therapeutic plasma levels, but intracellular concentrations in the gastric mucosa (assessed with [3H] Cimetidine and [14C]famotidine) were at least 10- and 2-fold greater than in the blood, respectively. These results suggests that, given at therapeutic dosesin vivo, the degree of inhibition by Cimetidine and ranitidine should be significant and comparable, that by nizatidine should be smaller, and that by famotidine should be negligible. These drugs also exerted either mixed or competitive inhibition of rat hepatic ADH, but the effects of Cimetidine and famotidine were observed at concentrations unlikely to occurin vivo. Thus, in alcoholics and in social drinkers who require treatment with H2-receptor antagonists, famotidine might be preferable to the other H2 blockers tested.
Kenneth A Kudsk - One of the best experts on this subject based on the ideXlab platform.
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pneumonia and stress ulceration in severely injured patients a prospective evaluation of the effects of stress ulcer prophylaxis
Archives of Surgery, 1993Co-Authors: Timothy C Fabian, Bradley A Boucher, Martin A Croce, David A Kuhl, Stephen W Janning, Bridgett C Coffey, Kenneth A KudskAbstract:• Stress ulcer prophylaxis is a routine aspect of the care of critically injured patients. Recent reports have suggested that patients undergoing prophylaxis with histamine antagonists are predisposed to nosocomial pneumonia, and that treatment with sucralfate can prevent this problem. An open, prospective randomized trial of three regimens was conducted with 278 evaluable patients. The patients were assigned to one of three groups: the group receiving sucralfate, the group receiving a Cimetidine hydrochloride bolus, and the group undergoing continuous infusion with Cimetidine. Stress ulceration developed in 8% of patients in the sucralfate group, 13% of patients in the Cimetidine bolus group, and 12% of patients in the Cimetidine infusion group, while nosocomial pneumonia developed in 29% of patients in the sucralfate group, 32% of patients in the Cimetidine bolus group, and 23% of patients in the Cimetidine infusion group. Multivariate analysis of risk factors associated with pneumonia demonstrated independent significance for score on the Glasgow Coma Scale, Injury Severity Score, cord injury, shock, and head injury. Only spinal cord injury was associated with stress ulceration. We conclude that sucralfate and Cimetidine are both effective for stress ulcer prophylaxis and that there is no association of Cimetidine with nosocomial pneumonia. ( Arch Surg. 1993;128:185-192)
Enrique Baraona - One of the best experts on this subject based on the ideXlab platform.
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effects of h2 receptor antagonists on gastric alcohol dehydrogenase activity
Digestive Diseases and Sciences, 1991Co-Authors: Joan Caballeria, Enrique Baraona, Ramon Deulofeu, Rolando Hernandezmunoz, Juan Rodes, Charles S LieberAbstract:Inhibition of gastric alcohol dehydrogenase (ADH) activity by Cimetidine results in elevated blood levels of ethanol after moderate consumption. To search for alternative H2-blockers lacking such an effect, we compared Cimetidine, ranitidine, nizatidine, and famotidine. They inhibited rat gastric ADH noncompetitively, with aKi for ethanol oxidation of 0.68 mM for Cimetidine, 0.5 mM for ranitidine, 1 mM for nizatidine, and 4.5 mM for famotidine. These concentrations are higher than therapeutic plasma levels, but intracellular concentrations in the gastric mucosa (assessed with [3H] Cimetidine and [14C]famotidine) were at least 10- and 2-fold greater than in the blood, respectively. These results suggests that, given at therapeutic dosesin vivo, the degree of inhibition by Cimetidine and ranitidine should be significant and comparable, that by nizatidine should be smaller, and that by famotidine should be negligible. These drugs also exerted either mixed or competitive inhibition of rat hepatic ADH, but the effects of Cimetidine and famotidine were observed at concentrations unlikely to occurin vivo. Thus, in alcoholics and in social drinkers who require treatment with H2-receptor antagonists, famotidine might be preferable to the other H2 blockers tested.