Stereochemistry | RACEMIC |
Molecular Formula | C33H34N4O6 |
Molecular Weight | 582.6463 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)OC(=O)C1=C(C)NC(N)=C(C1C2=CC(=CC=C2)[N+]([O-])=O)C(=O)OC3CN(C3)C(C4=CC=CC=C4)C5=CC=CC=C5
InChI
InChIKey=ZKFQEACEUNWPMT-UHFFFAOYSA-N
InChI=1S/C33H34N4O6/c1-20(2)42-32(38)27-21(3)35-31(34)29(28(27)24-15-10-16-25(17-24)37(40)41)33(39)43-26-18-36(19-26)30(22-11-6-4-7-12-22)23-13-8-5-9-14-23/h4-17,20,26,28,30,35H,18-19,34H2,1-3H3
Molecular Formula | C33H34N4O6 |
Molecular Weight | 582.6463 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
Azelnidipine (INN; marketed under the brand name CalBlock) is a dihydropyridine calcium channel blocker. It is sold in Japan by Daiichi-Sankyo pharmaceuticals, Inc. Azelnidipine is a new dihydropyridine calcium channel antagonist with selectivity for both L-type and T-type Ca channels. It has recently been approved in Japan for the treatment of patients with hypertension. Results from clinical trials showed that long-term treatment with azelnidipine effectively controls blood pressure (BP) in a cohort of 95 patients with mild-to-moderate hypertension. The antihypertensive efficacy of azelnidipine in patients with mild-to-moderate hypertension was shown to be similar to that of amlodipine or nitrendipine in a randomised double-blind study. Azelnidipine and amlodipine controlled 24-hour BP to a similar extent. Azelnidipine is generally well tolerated. Vasodilator adverse events such as headache and hot facial flushes account for most of the adverse events. Its use is not associated with reflex tachycardia.
CNS Activity
Originator
Approval Year
PubMed
Sample Use Guides
The normal dose for an adult is 8-16 mg of azelnidipine once daily, taken orally after breakfast. The maximum dosage is 16 mg/day. The initial dosage is to be 8 mg/day or less, to be adjusted as symptoms are monitored, up to 16 mg daily.
Route of Administration:
Oral