Azeliren
Azeliren Uses, Dosage, Side Effects, Food Interaction and all others data.
Azeliren is a dihydropyridine calcium channel blocker. It is marketed by Daiichi-Sankyo pharmaceuticals, Inc. in Japan. It has a gradual onset of action and produces a long-lasting decrease in blood pressure, with only a small increase in heart rate, unlike some other calcium channel blockers . It is currently being studied for post-ischemic stroke management .
Azeliren is a vasodilator that induces a gradual decrease in blood pressure in hypertensive patients. Unlike other members of its drug class, azelnidipine does not induce reflex tachycardia due to vasodilation. This is likely due to the fact that it elicits a gradual fall in blood pressure
It also exhibits a prolonged hypotensive effect and has been shown to have a strong anti-arteriosclerotic action in vessels due to its high affinity for vascular tissue and antioxidative activity .
| Trade Name | Azeliren |
| Generic | Azelnidipine |
| Azelnidipine Other Names | Azelnidipine |
| Weight | 16mg, 8mg |
| Type | Tablet |
| Formula | C33H34N4O6 |
| Weight | Average: 582.657 Monoisotopic: 582.247834831 |
| Protein binding | Azelnidipine is widely bound to human plasma proteins (90%–91%) [L3183]. |
| Groups | Investigational |
| Therapeutic Class | |
| Manufacturer | La Renon Healthcare Pvt Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
For the treatment of hypertension.
How Azeliren works
Azeliren inhibits trans-membrane Ca2+ influx through the voltage-dependent channels of smooth muscles in vascular walls. Ca2+ channels are classified into various categories, including L-type, T-type, N-type, P/Q-type, and R-type Ca2+ channels. The L-type Ca2+ channels . Normally, calcium induces smooth muscle contraction, contributing to hypertension. When calcium channels are blocked, the vascular smooth muscle does not contract, resulting in relaxation of vascular smooth muscle walls and decreased blood pressure.
Toxicity
As with any calcium channel blocker toxicity, bradycardia and hypotension may result from overdose. The treatment of patients with bradycardia and hypotension begins with supportive therapy and atropine, however, patients with severe toxicity do not have an adequate response and must be managed more aggressively.
Calcium plays an imperative role in myocardial contractility, automaticity and vascular tone. Administration of exogenous calcium is of benefit in cases of toxicity .
Volume of Distribution
In a Chinese study examining the pharmacokinetics of the drug, the volume of distribution was found to be 1749 +/- 964 .
Elimination Route
Oral ingestion of azelnidipine demonstrates rapid and dose-dependent absorption .
Half Life
16 –28 hours .
Elimination Route
In one study, following a single 4mg oral dose of 14C-labeled azelnidipine in humans, about 26% of the drug was thought to br excreted in the urine and 63% in the feces during the 1 week period post administration .
Innovators Monograph
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