Eprosartan

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{{DrugProjectFormSinglePage |authorTag=João André Alves Silva, M.D. [1] |genericName=eprosartan mesylate |aOrAn=an |drugClass=angiotensin II receptor blocker |indication=hypertension |hasBlackBoxWarning=Yes |adverseReactions=abdominal pain, myalgia, dizziness, upper respiratory infection and fatigue |blackBoxWarningTitle=WARNING: FETAL TOXICITY |blackBoxWarningBody=Condition Name: See full prescribing information for complete boxed warning.

When pregnancy is detected, discontinue eprosartan as soon as possible.
Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus.

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(Description) |clinicalTrials=======Central Nervous System======

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|postmarketing=(Description) |drugInteractions=* Digoxin - concomitant administration of eprosartan and digoxin had no effect on single oral-dose digoxin pharmacokinetics.

Warfarin - concomitant administration of eprosartan and warfarin had no effect on steady-state prothrombin time ratios (INR) in healthy volunteers.
Glyburide - concomitant administration of eprosartan and glyburide in diabetic patients did not affect 24-hour plasma glucose profiles.
Ranitidine - eprosartan pharmacokinetics were not affected by concomitant administration of ranitidine.
Eprosartan did not inhibit human cytochrome P450 enzymes CYP1A, 2A6, 2C9/8, 2C19, 2D6, 2E and 3A in vitro.
Eprosartan is not metabolized by the cytochrome P450 system.
Ketoconazole and fluconazole - Eprosartan steady-state concentrations were not affected by concomitant administration of ketoconazole or fluconazole, potent inhibitors of CYP3A and 2C9, respectively.

|useInPregnancyFDA=(Description) |useInPregnancyAUS=(Description) |useInLaborDelivery=(Description) |useInNursing=(Description) |useInPed=* Eprosartan pharmacokinetics have not been investigated in patients younger than 18 years of age. |useInGeri=* Following single oral dose administration of eprosartan to healthy elderly men (aged 68 to 78 years), AUC, Cmax, and Tmax eprosartan values increased, on average by approximately twofold, compared to healthy young men (aged 20 to 39 years) who received the same dose.

The extent of plasma protein binding was not influenced by age.

|useInGender=* There was no difference in the pharmacokinetics and plasma protein binding between men and women following single oral dose administration of eprosartan. |useInRace=* A pooled population pharmacokinetic analysis of 442 Caucasian and 29 non-Caucasian hypertensive patients showed that oral clearance and steady-state volume of distribution were not influenced by race. |useInRenalImpair=* Following administration of 600 mg once daily, there was a 70-90% increase in AUC, and a 30-50% increase in Cmax in moderate or severe renal impairment. The unbound eprosartan fractions increased by 35% and 59% in patients with moderate and severe renal impairment, respectively. No initial dosing adjustment is generally necessary in patients with moderate or severe renal impairment, with maximum dose not exceeding 600 mg daily.

Eprosartan was poorly removed by hemodialysis (CLHD<1 L/hr).

|useInHepaticImpair=* Eprosartan AUC (but not Cmax) values increased, on average, by approximately 40% in men with decreased hepatic function compared to healthy men after a single 100 mg oral dose of eprosartan. Hepatic disease was defined as a documented clinical history of chronic hepatic abnormality diagnosed by liver biopsy, liver/spleen scan or clinical laboratory tests.

The extent of eprosartan plasma protein binding was not influenced by hepatic dysfunction.
No dosage adjustment is necessary for patients with hepatic impairment.

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Template:Px
Eprosartan
Systematic (IUPAC) name
4-({2-Butyl-5-[2-carboxy-2-(thiophen-2-ylmethyl)eth-1-en-1-yl]-1H-imidazol-1-yl}methyl)benzoic acid
Identifiers
CAS number	133040-01-4
ATC code	C09CA02
PubChem	5281037
DrugBank	DB00876
Chemical data
Formula	Template:OrganicBox atom Template:OrganicBox atom Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox atom Template:OrganicBox Template:OrganicBox atom Template:OrganicBox Template:OrganicBox Template:OrganicBox atom Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox
Mol. mass	Eprosartan mesylate: 520.625 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	15% (Eprosartan mesylate)
Metabolism	not metabolized
Half life	5 to 9 hours
Excretion	Renal 10%, biliary 90%
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	Oral

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