Using a high-throughput functional screen, the atypical L-type Ca2+ channel blocker diltiazem was discovered to be an agonist at the human ghrelin (GHSR1a) receptor. In cellular proliferation, Ca2+ mobilization, and bioluminescence resonance energy transfer (BRET-2) assays, diltiazem was a partial agonist at GHSR1a receptors, with 50 to 80% relative efficacy compared with the GHSR1a peptide ago...

A 78-year-old woman was found dead in her basement. Qualitative screening of available postmortem specimens detected the presence of diltiazem and pentoxifylline. Quantitations were carried out by gas chromatography using nitrogen-phosphorus detection and confirmed by gas chromatography-mass spectrometry with the following results: blood, 0.59 mg/dL diltiazem and 0.63 mg/dL pentoxifylline; urin...

The short-term effects of intravenously administered diltiazem on pulmonary and systemic hemodynamics were evaluated in patients with hypoxic pulmonary hypertension. Twelve patients were randomly assigned to two groups in a double-blind fashion. One group (eight patients) received diltiazem, and the other group (four patients) received a placebo. Three increasing doses of diltiazem (0.2, 0.3, a...

Diltiazem, a calcium channel blocker, is mainly metabolized via demethylation or deacetylation in humans. Diltiazem demethylation is catalyzed by cytochrome P450 2D6 and 3A4. Although it was previously reported that the area under the curve ratio of deacetyldiltiazem to diltiazem after oral dosing with diltiazem in rats was sevenfold higher than in humans, the molecular mechanisms underlying th...

The purpose of this study was to investigate the possible effects of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, simvastatin, on the pharmacokinetics of diltiazem and its main metabolite, desacetyldiltiazem, in rats. HMG-CoA reductase inhibitors and diltiazem are sometimes prescribed as a combination therapy for the prevention or treatment of cardiovascular diseases. The eff...

Effect of honey on plasma concentration of diltiazem after oral and intravenous administration in rabbits, has been studied. For oral study, single dose of diltiazem (5 mg/kg, p.o.) along with saline was administered to New Zealand white rabbits (n=8). Blood samples were collected at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6 and 8 hr after drug administration from marginal ear vein. After a washou...

The effect of pretreatment with graded concentration of diltiazem on the inotropic responses to amrinone were studied on isolated atria of rabbit. The responses to amrinone were modified by diltiazem in a biphasic manner; initial potentiation followed by inhibition. The potentiation is proposed to be due to synergistic rise in cytosolic calcium ion concentration by diltiazem and amrinone. The i...

An in vivo study has been carried out to evaluate the synergism of diltiazem and nifedipine on the antihypertensive activity and the effect of ketotifen fumerate and potassium nitrate on this phenomenon of synergism in rabbit. It has been found that the lowering of blood pressure by concurrent administration of diltiazem and nifedipine was not equal to the sum of lowering of blood pressure by i...

Background & Aims: Hypertension, hyperuricaemia and nephrotoxicity are some common side-effects of Cyclosporine A (CsA) treatment in renal transplant recipients. Previous studies suggest that Calcium Channel Blockers (CCB) can increase serum level of CsA and may improve graft function in patients receiving CsA. The aim of this study was to evaluate the effects of Diltiazem and Amlodipine on cyc...

BACKGROUND Diltiazem, a calcium channel blocker, has been shown to be safe and effective in the treatment of patients in atrial fibrillation and/or atrial flutter. However, there have been no pharmacokinetic/pharmacodynamic studies of diltiazem in these patients. METHODS AND RESULTS The pharmacokinetics and pharmacodynamics of intravenous diltiazem were determined in 32 patients with atrial f...