In this study, the effects of various hydrophilic (HPMC and Carbopol 971) and plastic (Ethylcellulose and Eudragit RL100) polymers on the release profile of diltiazem HCl from matrix tablets were evaluated in-vitro. For this purpose, tablets containing 60 mg of diltiazem HCl along with various amounts of the aforementioned polymers were prepared using the wet granulation technique. Tablets prep...

  In this study interaction of three types of calcium channel blockers nifedipine, diltiazem and verapamil on the effects of lead acetate on two types of pain (nociception and inflammation) induced by formalin in mice were examined. In order to study nociception, formalin test was selected because of greater resemblance to clinical pain. Lead acetate (50, 75, l00, 125 and 150 mg/kg) administere...

In the present study, we have characterized the presence and distribution of cGMP-gated cationic channels (CNG) in the rat urethra as well as its putative role in the mediation of the nitrergic relaxation. Previous studies have shown the inhibition of the sheep urethral nitrergic relaxations by the CNG's inhibitor L-cis-diltiazem [1]. Also in the rat urethra, L-cis-diltiazem (50 M) inhibited n...

An elderly woman, distraught over the recent death of her husband, was found dead of an apparent suicide. Qualitative screening detected only the presence of diltiazem, an antihypertensive, antianginal agent that was prescribed for a known heart ailment. Quantitation of diltiazem was carried out on available fluids and tissues with the following results: blood 6.7 mg/L, urine 5.4 mg/L, vitreous...

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...

[3H]Nitrendipine binding to drug receptor sites associated with calcium channels is allosterically regulated by a diverse group of calcium channel antagonists. Verapamil, D-600 (methoxyverapamil), tiapamil, lidoflazine, flunarizine, cinnarizine, and prenylamine all reduce [3H]nitrendipine binding affinity. By contrast, diltiazem, a benzothiazepine calcium channel antagonist, enhances [3H]nitren...

The effects of 9 calcium antagonists on ABCG2/BCRP-mediated resistance and transport were examined in HeLa and SN-38-resistant HeLa (HeLa/SN100) cells, overexpressing ABCG2/BCRP. Sensitivity to mitoxantrone, an ABCG2/BCRP substrate, in HeLa/SN100 cells was significantly reversed by the coexistence of the calcium antagonists, except for diltiazem a...

Diltiazem hydrochloride (Ia) is an important coronary vasodilator drug of the calcium channel-blocker type, used in therapy of heart disease and hypertension. The compound is (+)-5-[2-(dimethylamino)ethyl]-c&, 2,3dihydro3-hydroxy-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one acetate monohydrochloride. The drug and its tablet formulations are official in the USP [l] wherein they are estimated...

Results: Of the 352 patients, 173 (49.1%) achieved their goal diastolic blood pressure, in 133 (37.8%) the alternate drug failed, and 46 (13.1%) left the study for various reasons. Overall response rates were as follows: diltiazem, 63%; clonidine, 59%; prazosin, 47%; hydrochlorothiazide, 46%; atenolol, 41%; and captopril, 37%. The best response rate for patients in whom hydrochlorothiazide fail...