EPROSARTAN Chemical Properties

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

CAS DataBase Reference

133040-01-4

Safety Information

Hazardous Substances Data

133040-01-4(Hazardous Substances Data)

EPROSARTAN Usage And Synthesis

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.

Chemical Properties

Light-Yellow Solid

Originator

SmithKline Beecham (UK)

Uses

Prototype of the imidazoleacrylic acid angiotensin II receptor antagonists. Antihypertensive

Uses

Eprosartan is a prototype of the imidazoleacrylic acid angiotensin II receptor antagonists. Eprosartan is an antihypertensive.

Uses

Eprosartan (E590100) impurity.

Definition

ChEBI: A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.

brand name

Teveten

Clinical Use

Angiotensin-II antagonist
Hypertension

Drug interactions

Potentially hazardous interactions with other drugs Anaesthetics: enhanced hypotensive effect.
Analgesics: antagonism of hypotensive effect and increased risk of renal impairment with NSAIDs; hyperkalaemia with ketorolac and other NSAIDs.
Antihypertensives: increased risk of hyperkalaemia hypotension and renal impairment with ACE inhibitors and aliskiren.
Ciclosporin: increased risk of hyperkalaemia and nephrotoxicity.
Diuretics: enhanced hypotensive effect; hyperkalaemia with potassium-sparing diuretics.
Epoetin: increased risk of hyperkalaemia; antagonism of hypotensive effect.
Lithium: reduced excretion, possibility of enhanced lithium toxicity.
Potassium salts: increased risk of hyperkalaemia.
Tacrolimus: increased risk of hyperkalaemia and nephrotoxicity.

Metabolism

Following oral and intravenous dosing with [14C] eprosartan in human subjects, eprosartan was the only drug-related compound found in the plasma and faeces. In the urine, approximately 20% of the radioactivity excreted was an acyl glucuronide of eprosartan with the remaining 80% being unchanged eprosartan
Eprosartan is eliminated by both biliary and renal excretion. Following intravenous [14C] eprosartan, about 61% of radioactivity is recovered in the faeces and about 37% in the urine. Following an oral dose of [14C] eprosartan, about 90% of radioactivity is recovered in the faeces and about 7% in the urine.

EPROSARTAN(133040-01-4)Related Product Information

• SB 206328
• CINITAPRIDE HYDROGEN TARTRATE
• 4-(2-BUTYL-5-FORMYLIMIDAZOL-1-YLMETHYL)BENZOIC ACID
• Tacrolimus
• Losartan potassium
• Pregabalin
• Irbesartan
• Valsartan
• Eprosartan mesylate
• Olmesartan Medoxomil
• Tasosartan
• 4-Bromomethylbenzoic acid
• SB 201972
• 3-(2-THIENYL)PROPIONIC ACID
• Methyl (E)-3-[2-Butyl-1-[(4-Carbomethoxyphenyl)methyl]imidazol-5-yl]-2-(2-thienylmethyl)-2-propenoate
• Epalrestat iMpurity
• 4-(Hydroxymethyl)benzoic acid
• α-Methylcinnamaldehyde