This study investigated the protective effects of carvedilol alone and coadministered with prednisolone and diltiazem on doxorubicin (DOX) and 5-fluorouracil (5-FU)-induced toxicity. Each of 2 pools of 70 female rats were randomly allotted into 10 groups of 7 animals each and treated as follows: Group 1: normal saline (10 mL/kg); Group 2: normal saline and DOX (40 mg/kg)/5-FU (20 mg/kg) alone; ...

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ACE inhibitors are considered first line of treatment in patients with many forms of chronic kidney disease (CKD). Other antihypertensives such as calcium channel blockers achieve similar therapeutic effectiveness in attenuating hypertension-related renal damage progression. Our objective was to explore the value of positron emission tomography (PET) imaging of renal AT1 receptor (AT1R) to guid...

BACKGROUND Silent myocardial ischemia is an adverse prognostic marker in patients with coronary disease; however, controlled data on the effect of treatment are sparse and contradictory, and the relations among the occurrence of ST segment depression, drug efficacy, and heart rate are unclear. METHODS AND RESULTS Sixty patients with stable coronary artery disease, a positive treadmill exercis...

The inhibitory effects of six commonly used calcium channel blockers on three major cytochrome P-450 activities were examined and characterized in human liver microsomes. All six compounds reversibly inhibited CYP2D6 (bufuralol 1'-hydroxylation) and CYP2C9 (tolbutamide methyl hydroxylation) activities. The IC(50) values for the inhibition of CYP2D6 and CYP2C9 for nicardipine were 3 to 9 microM,...

Calcium influx blockers, diltiazem, nicardipine, nifedipine, niludipine, and nimodipine, which possess coronary vasodilator activity, greatly enhanced the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human K562 myelogenous leukemia. The extent of enhancement was different among the drugs, and up to a 50- to 70-fold inc...

Health technology The study focused on the use of two conduit vasodilators in the prevention of arterial conduit spasm after coronary bypass grafting (CABG). Patients received a 24-hour intravenous infusion of either nitroglycerin (0.1 microgram.kg-1.min-1) or diltiazem (0.1 mg/kg during 20 minutes and then 0.1 mg.kg-1.min-1), followed by 6 months of treatment with a daily dose of isosorbide mo...

The effects of nicardipine and nifedipine on the urinary excretion of urate were examined in rats and compared with those of diltiazem. Test drugs were administered to urethane-anesthetized oxonate-loaded rats by continuous i.v. infusion. Diltiazem (10 micrograms/rat/min), nicardipine (0.3 microgram/rat/min) and nifedipine (1.0 microgram/rat/min) caused similar reductions of systemic blood pres...

The objective of this in vitro study was to investigate both the intestinal metabolism and transport of diltiazem (DTZ) and its major metabolites in rat jejunum. Metabolism experiments were performed with everted sacs, whereas sheets mounted in a symmetrical twin chamber system were used in transport studies. DTZ was rapidly desacetylated by the rat jejunum to the principle metabolite desacetyl...

The enhancement of oral bioavailability of poorly water soluble drugs remains one of the most challenging aspects. Utilization of cyclodextrins attracted the attention of many researchers for the enhancement of the dissolution rate. The complexation of diltiazem hydrochloride with βcyclodextrin (CD) was investigated by phase solubility. Phase solubility study was performed to determine stiochio...