Prediction of the extent and time course of drug-drug interactions (DDIs) between the mechanism-based inhibitor diltiazem (DTZ) and the CYP3A4 substrate midazolam (MDZ) is confounded by time- and concentration-dependent clearance of the inhibitor. Semiphysiologically based pharmacokinetic (PBPK) models were developed for DTZ and MDZ with the major metabolite of DTZ, N-desmethyldiltiazem (nd-DTZ...

The antihypertensive agent diltiazem (DTZ) impairs hepatic drug metabolism by inhibition of cytochrome P450 (CYP). The accumulation of DTZ metabolites in serum occurs during prolonged therapy and leads to decreased DTZ elimination. Thus, DTZ metabolites may contribute to CYP inhibition. This study assessed the role of human CYPs in microsomal DTZ oxidation and the capacity of DTZ metabolites to...

BACKGROUND The aim of this study was to compare the effect of topical glycerol trinitrate ointment (GTN) with topical diltiazem hydrochloride ointment (DTZ) in the treatment of chronic anal fissure. METHOD Prospectively, 102 patients were treated randomly with either GTN ointment (0.2%) or DTZ ointment (2%) couple of times daily for 12 weeks. RESULTS Forty-five patients (88.2%) in group DTZ...

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...

Diltiazem (DTZ) N-demethylation occurs by cytochrome P-450 (CYP) 3A based on the following observations: 1) a single enzyme Michaelis-Menten model of metabolite formation, 2) high correlations of DTZ N-demethylation activity to other CYP3A activities, 3) inhibition of DTZ N-demethylation activity by triacetyloleandomycin, and 4) DTZ N-demethylation activity by expressed CYP3A enzymes only. The ...

Article history: Received on: 02/03/2015 Revised on: 12/04/2015 Accepted on: 03/05/2015 Available online: 27/07/2015 The aim of this study is to investigative the stability of poly(ethylene oxide) (PEO) matrix tablets containing diltiazem hydrochloride (DTZ) after five-year storage at room temperature. DTZ matrix tablets containing different molecular weights (MW) of PEO and electrolytes (sodiu...

OBJECTIVE To assess and compare the effectiveness of topical 0.2% glycerl trinitrate (GTN) and topical 2% diltiazem (DTZ), in the management of chronic anal fissure. STUDY DESIGN Comparative, descriptive study. PLACE AND DURATION OF STUDY Department of Surgery, Liaquat University of Medical and Health Sciences, Jamshoro/Hyderabad from September 2004 to August 2005. METHODOLOGY Patients wi...

The effects of Ginkgo biloba leaf extract (GBE), one of the most widely used herbal dietary supplements in Japan, on the pharmacokinetics of diltiazem (DTZ), a typical probe of cytochrome P450 (CYP) 3A, were examined in rats. The simultaneous addition of GBE to small intestine and liver microsomes inhibited the formation of N-demethyl DTZ (MA), an active metabolite of DTZ produced by CYP3A, in ...

Objective: This study aimed to assess the enhanced anticancer effect of Temozolomide (TMZ) through a synergistic combination with Diltiazem (DTZ) in neuroblastoma cell line (SH-SY5Y).
 Material and Methods: The SH-SY5Y was cultured DMEM medium. TMZ DTZ stock solutions were prepared diluted obtain different concentrations. XTT assay performed evaluate viability. Cells treated alone or for 2...