Therapeutic tolerance, hemodynamic effects, and oral dose kinetics of dilazep dihydrochloride in hypertensive patients.

The oral dose metabolism of dilazep dihydrochloride [tetrahydro-1H-1,4-diazepine-1,4(5H)-dipropanol 3,4,5-trimethoxybenzoate] was examined in six hypertensive patients receiving a single oral dose of 600 mg of dilazep (3-3.8 mg/kg BW). Blood was collected at 0.

Calcium entry blocking activity of adenosine potentiating compounds in guinea pig taenia coli.

Calcium entry blocking activities of adenosine and its potentiating drugs, dilazep, lidoflazine and dipyridamole, were studied in potassium (100 mM)-depolarized guinea pig taenia coli, and compared with nifedipine, verapamil and diltiazem. The potency ratio of calcium entry blocking effect of nifedipine, diltiazem, lidoflazine and dilazep to verapamil was 158.5, 1/1.

Calcium entry blocking activity of dilazep and other adenosine potentiating compounds in guinea-pig atria.

In potassium-depolarized guinea-pig left atria treated with isoproterenol, calcium entry blocking activities of adenosine and its potentiating compounds, dipyridamole, lidoflazine and dilazep were studied and compared to verapamil and diltiazem. pA2 values for various drugs were calculated using concentration-response curves for calcium (parallel shift to the right). The order of potency for the calcium entry blocking effect was: verapamil greater than diltiazem greater than adenosine greater than lidoflazine = dilazep greater than dipyridamole.

Calcium entry blocking activity of dilazep in dog coronary artery.

Calcium entry blocking activities of adenosine and its potentiating compounds (dipyridamole, lidoflazine and dilazep) were studied in potassium (100 mmol/l) depolarized, dog, large coronary artery strips, in comparison to nifedipine, verapamil and diltiazem. Apparent pA2 values were calculated by using concentration-response curves for calcium before and 30 min after the addition of each dilator drug. The order of potency (using both pA2 and IC50 values) for the calcium entry blocking effect was: nifedipine greater than verapamil greater than diltiazem greater than lidoflazine greater than dilazep.