Chemical Properties
Light-Yellow Solid
Uses
Eprosartan (E590100) impurity.
Uses
Eprosartan is a prototype of the imidazoleacrylic acid angiotensin II receptor antagonists. Eprosartan is an antihypertensive.
Uses
Prototype of the imidazoleacrylic acid angiotensin II receptor antagonists. Antihypertensive
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.
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.
Originator
SmithKline Beecham (UK)
Clinical Use
Angiotensin-II antagonistHypertension
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 eprosartanEprosartan 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.
