EPROSARTAN
- CAS NO.:133040-01-4
- Empirical Formula: C23H24N2O4S
- Molecular Weight: 424.51
- MDL number: MFCD00897872
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-04-23 13:52:06
What is EPROSARTAN?
Absorption
Absolute bioavailability following a single 300 mg oral dose of eprosartan is approximately 13%. Administering eprosartan with food delays absorption.
Toxicity
There was no mortality in rats and mice receiving oral doses of up to 3000 mg eprosartan/kg and in dogs receiving oral doses of up to 1000 mg eprosartan/kg.
Description
Teveten was launched in Germany for the treatment of hypertension. There are several ways in which it has been prepared, the shortest of which is four steps; beginning with displacement of 2-butyl-4-chloroimidazole-5-carboxaldehyde with methyl 4-(bromomethyl)benzoate. Teveten is an angiotensin Ⅱ antagonist selective for the AT, subtype receptor. It is a potent, highly selective, competitve antagonist with no agonist activity. Duration of action is similar to Enalapril (greater than 12 hr) but Teveten had a faster onset. While it is orally active, it rapidly dissociates from the receptor. This is contrary to its prolonged duration of action, which presumably results from slow removal from compartments within tissue, cells or matrix around the AT, receptor. It is not bound by BSA.
The Uses of EPROSARTAN
Eprosartan (E590100) impurity.
Indications
For the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors).
Background
Eprosartan is an angiotensin II receptor antagonist used to treat hypertension. It performs 2 actions on the renin angiotensin system. By preventing the binding of angiotensin II to AT1, vascular smooth muscle relaxes and vasodilation occurs. By inhibiting norepinephrine production, blood pressure is further reduced.
What are the applications of Application
Eprosartan is a prototype of the imidazoleacrylic acid angiotensin II receptor antagonist
Pharmacokinetics
Angiotensin II, the principal pressor agent of the renin-angiotensin system, is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme [kininase II]. It is responsible for effects such as vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Eprosartan selectively blocks the binding of angiotensin II to the AT1 receptor, which in turn leads to multiple effects including vasodilation, a reduction in the secretion of vasopressin, and reduction in the production and secretion of aldosterone. The resulting effect is a decrease in blood pressure.
Metabolism
Eprosartan is not metabolized by the cytochrome P450 system. It is mainly eliminated as unchanged drug. Less than 2% of an oral dose is excreted in the urine as a glucuronide.
Properties of EPROSARTAN
Melting point: | 250-253°C |
storage temp. | Sealed in dry,2-8°C |
solubility | Dichloromethane (Slightly), Methanol (Slightly) |
form | Solid |
color | Pale Yellow to Light Yellow |
Safety information for EPROSARTAN
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for EPROSARTAN
Abamectin manufacturer
KARPSCHEM LABORATORIES PVT. LTD.
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