Diltiazem: Ten Years of Clinical Experience in the Treatment of Hypertension

Abstract

Diltiazem hydrochloride is a benzothiazepine derivative calcium-channel blocker with proven antianginal and antihypertensive capabilities. Its primary mechanism of action is vasodilatation, which results in diminished vascular resistance and improved perfusion to various vascular beds and target organs. The antihypertensive efficacy of diltiazem in various demographic groups has been studied and compared with diuretics, beta-blockers, angiotensin-converting enzyme inhibitors, and other calcium-channel blockers. These studies have shown that the antihypertensive effect of diltiazem is similar to that of the other therapies. Diltiazem does not adversely affect electrolytes or carbohydrate or lipid metabolism, and it may have beneficial effects on the heart and kidneys. Diltiazem reduces myocardial hypertrophy and exerts antianginal effects on the heart through coronary vasodilation and reduction in the blood pressure double product. Diltiazem improves renal perfusion and attenuates proteinuria. These effects may be helpful in limiting the progression of renal injury. Overall, the efficacy and tolerability of diltiazem, as well as its salutary effects on the heart and kidneys, make it an important therapeutic consideration for patients with hypertensive disease.

Altered diltiazem metabolism in the neonatal rabbit following intra-uterine chronic exposure to diltiazem

“…Diltiazem (DTZ) is now established as a rst-line therapy for the management of hypertension (Weir 1995). As a consequence, its use for the treatment of hypertension occurring during pregnancy has been postulated (Holbrook et al 1988), especially in those clinical cases resistant to traditional therapy.…”

Effects of Ticlopidine on the Pharmacokinetics of Diltiazem and Its Main Metabolite, Desacetyldiltiazem, in Rats

“…Diltiazem is a calcium channel blocker that is widely used for the treatment of angina, supraventricular arrhythmias and hypertension (Chaffman and Brogden, 1985;Yeung et al, 1993;Weir, 1995). Diltiazem undergoes extensive and complex phase I metabolism including desacetylation, N-demethylation, and O-demethylation.…”

Effects of ischemia–reperfusion on the absorption and esterase metabolism of diltiazem in rat intestine

“…The health care costs entailed by such cases are tremendous (Goettler et al, 1997;Lagnaoui et al, 2000) and are avoidable. Diltiazem (DTZ) is a calcium-channel blocker widely prescribed to treat hypertension, chest pain (angina) and supraventricular arrhythmias (Chaffman and Brogden, 1985;Weir, 1995). DTZ is subject to extensive intestinal metabolism by different CYP450 isoforms and esterases, and this reduces the amount of intact drug in portal blood by over 50% of the dose (Lee et al, 1991;Lefebvre et al, 1996;Molden et al, 2000;Iwao et al, 2004), before hepatic metabolism (Fig.…”