The benzothiazepine diltiazem blocks ionic current through L-type Ca(2+) channels, as do the dihydropyridines (DHPs) and phenylalkylamines (PAs), but it has unique properties that distinguish it from these other drug classes. Wild-type L-type channels containing alpha(1CII) subunits, wild-type P/Q-type channels containing alpha(1A) subunits, and mutants of both channel types were transiently ex...

pharmacokinetic studies of diltiazem. CYP3A4, a key enzyme in the metabolism of diltiazem is mainly located in liver, but it is also expressed in the small intestine (Watkins et al., 1987; Pichard et al., 1990; Kolars et al., 1992). Thus, diltiazem could be metabolized in both the small intestine and the liver (Homsy et al., 1995a; Homsy et al., 1995b; Lefebvre et al., 1996). Lee et al. (1991) ...

Background—Topical nitrates lower anal sphincter pressure and heal anal fissures, but a majority of patients experience headache. The internal anal sphincter has a calcium dependent mechanism to maintain tone, and also receives an inhibitory extrinsic cholinergic innervation. It may therefore be possible to lower anal sphincter pressure using calcium channel blockers and cholinergic agonists wi...

BACKGROUND Calcium channel blockers are widely used in the treatment of post-transplant hypertension but have the potential for drug interaction with calcineurin inhibitors. Renal allograft outcomes when diltiazem is used with cyclosporine have been reported, but similar data with tacrolimus are not available. METHODS We performed a retrospective analysis of all our renal transplant recipient...

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...

Perioperative vasospasm during cardiovascular surgery is a challenging problem. Several vasodilator agents are frequently utilized for its prevention in surgical practice. Magnesium and diltiazem both have known potential vasorelaxant effects. We planned to compare the efficacy of diltiazem and magnesium in relieving phenylephrine-precontracted rat aortic rings. Ten young adult female Wistar al...

BACKGROUND The spectrum of cutaneous eruptions in association with calcium channel blockers is extensive, varying from exanthemas to severe adverse events. Reactions due to diltiazem occur more frequently than with other calcium channel blockers. Patch testing has been used as confirmatory testing in patients with extensive cutaneous reactions. Cross-reactivity among these drugs have not been e...

OBJECTIVES The study sought to assess the safety, feasibility, and effect of diltiazem as disease-modifying therapy for at-risk hypertrophic cardiomyopathy (HCM) mutation carriers. BACKGROUND HCM is caused by sarcomere mutations and characterized by left ventricular hypertrophy (LVH) with increased risk of heart failure and sudden death. HCM typically cannot be diagnosed early in life, althou...

Diltiazem, a calcium channel blocker was studied to observe its effects on the acetylcholine contractile responses of isolated frog rectus abdominis muscle. This response was modified in a dual manner i.e., initial potentiation, followed by inhibition. Diltiazem may not have anticholinesterase like mechanism, as it potentiated the responses to both acetylcholine and succinylcholine. Rectus musc...

Effects of MCI-176, 2-(2,5-dimethoxyphenylmethyl)-3-(2-dimethylaminoethyl)-6-isopropox y-4 (3H)-quinazolinone hydrochloride, on coronary and aortic blood flows, mean blood pressure and heart rate were investigated in comparison with those of diltiazem in anesthetized dogs. MCI-176, like diltiazem, dose-dependently increased coronary and aortic blood flows and decreased mean blood pressure. In p...