Herbesser R 100/Herbesser R 200 Mechanism of Action

Calcium antagonist.
Pharmacology: The therapeutic benefits achieved with diltiazem HCl eg, improvement of myocardial ischemia and hypotensive effect are believed to be related to its ability to dilate vessels by inhibiting the influx of calcium ion into smooth muscle cells of the coronary and peripheral blood vessels, etc.
Action on Myocardial Ischemia:
Improving action on the balance of myocardial oxygen demand and supply:
To increase coronary blood flow into the myocardial ischemic region by dilating the collateral channels and the large coronary artery (dogs).
To inhibit coronary artery spasms (monkeys, humans).
To decrease myocardial oxygen consumption without decreasing afterload and heart rate due to peripheral vasodilator (dogs).
Action on Myocardial Protection: To retain cardiac function and myocardial energy metabolism and reduce the infarct size by inhibiting excess calcium ion influx into cells under myocardial ischemia (rats).
Action on Blood Pressure:
To lower elevated blood pressure gradually although it hardly affects normal blood pressure (rats, humans). To suppress the elevation of blood pressure induced by exercise load (humans).
To lower blood pressure without decreasing cerebral and renal blood flow (dogs, humans).
To suppress myocardial and vascular hypertrophy while lowering blood pressure (rats).
Action on Sinus Rhythm and Cardiac Conduction System: To prolong slightly spontaneous sinus rhythm intervals and A-H conduction time. Not to affect the H-V conduction time (dogs, humans).
Pharmacokinetics: Blood Concentration: When 1 capsule of Herbesser R 100 was administered to healthy adult men at a single oral dosage, its plasma concentration reached the peak about 14 hrs after the administration. The half-life was about 7 hrs.
Metabolism: In case of oral administration to healthy adult men, diltiazem HCl was mainly metabolised by oxidative deamination, oxidative demethylation, deacetylation and conjugation.
Clinical Studies: Clinical Efficacy: The usefulness of Herbesser R 100/R 200 in the treatment of essential hypertension, angina pectoris and variant angina pectoris was demonstrated by clinical studies including double-blind comparative clinical trials using Herbesser R 100/R 200 as a control. See Table 1.

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