Description
Isradipine is a long-acting calcium blocker effective in the treatment of essential
hypertension. The advantages of isradipine as compared with other dihydropyridine
calcium antagonists include a "gentle" onset and fewer contraindications. It can be taken
by patients with diabetes mellitus, chronic obstructive airway diseases, gout, congestive
heart failure or ischemic heart disease.
Chemical Properties
Yellow Solid
Originator
Sandoz (Switzerland)
Uses
nonsedating H1-antihistamine
Uses
Dihydropyridine calcium channel blocker. Antihypertensive; antianginal
Uses
Isradipine is a L-type calcium channel blocker, Isradipine has anti-atherosclerotic effects in animals and improves endothelium-mediated nitric oxide (NO)-dependent vasodilation in vitro. Additional studies indicate that Isradipine may provide a neuroprotective effect in a rat model of focal ischemia and that Isradipine produces a dose-dependent sparing of dopamine neuronal fibers and cell bodies.
Definition
ChEBI: Isradipine is an isopropyl ester, a methyl ester, a dihydropyridine and a benzoxadiazole.
brand name
Dynacirc (Reliant);Prescal.
General Description
Isradipine, 4-(4-benzofuranazyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylic acid methyl 1-methylethyl ester (DynaCirc), is another second-generationdihydropyridine-type channel blocker. This drug, like theother second-generation analogs, is more selective for vascularsmooth muscle than for myocardial tissue. It is effectivein the treatment of stable angina, reducing the frequencyof anginal attacks and the need to use nitroglycerin.
Biological Activity
Potent and selective L-type voltage-gated Ca 2+ channel blocker. EC 50 and pA 2 values are 1.4 nM and 10.3 for relaxation of depolarization- and Ca 2+ -induced contractions of rabbit aorta respectively; EC 25 = 0.45 nM for reduction in rate of spontaneously beating guinea pig right atria. Long-acting antihypertensive agent in vivo , exerting primary effects on vascular tissue with secondary negative chronotropic action.
Biochem/physiol Actions
L-type calcium channel blocker (also referred to as dihydropyridine-type calcium channel blocker); antihypertensive.
References
1) Bracht et al. (2001), Isradipine improves endothelium-dependent vasodilation in normotensive coronary artery disease patients with hypercholesterolemia; J. Hyperten., 19 899
2) Chandra et al. (1999), Use of diffusion-weighted MRI and neurological deficit scores to demonstrate beneficial effects of isradipine in a rat model of focal ischemia ; Pharmacology, 58 292
3) Merck 14:5240
