C09CA02 - Eprosartan

Probably not porphyrinogenic

PNP

Mono.Rationale

Eprosartan is not metabolized by CYP enzymes, and is found not to be an inhibitor of CYP, there are no indications that eprosartan has potential for CYP induction.

Mono.ChemicalDescription

Angiotensin II receptor antagonist

Mono.TherapeuticCharacteristics

Eprosartan is used in the treatment of essential hypertension. It is administered orally.

Mono.MetabolismAndPharmacokinetics

Eprosartan is not metabolized by CYP, but is eliminated by biliary and renal excretion, primarily as unchanged compound. Less than 2 per cent is excreted as a glucuronide (drugbank). Eprosartan has been shown not to inhibit human cytochrome P450 enzymes CYP1A, 2A6, 2C9/8, 2C19, 2D6, 2E and 3A in vitro in concentrations up to 100µM. This concentration is approximately 15- fold higher than the mean maximum plasma concentration after administration of eprosatran 1200 mg a day for 7 days (SPC, Taavitsainen 2000). In an in vivo drug-drug interaction study eprosartan did not alter the plasma concentration of CYP substrates (Blum 1999). It has an elimination half-life of 5-9 hours (SPC).

Mono.IpnetDrugReports

Uneventful use reported in 1 patient with acute porphyria.

Mono.SimilarDrugs

Mono.ExploreAlternatives C09C / C09CA or Mono.GoBack.

Mono.References

#	Citation details	PubMed ID
1.	A review of eprosartan pharmacokinetic and pharmacodynamic drug interaction studies. Blum RA, Kazierad DJ, Tenero DM. Pharmacotherapy. 1999 Apr; 19(4 Pt 2):79S-85S.	10213526
2.	In vitro inhibition screening of human hepatic P450 enzymes by five angiotensin-II receptor antagonists. Taavitsainen P, Kiukaanniemi K, Pelkonen O. Eur J Clin Pharmacol. 2000 May; 56(2):135-40.	10877007
3.	Drug Interactions with Angiotensin Receptor Blockers: Role of Human Cytochromes P450. Yang R, Luo Z, et al. Curr Drug Metab. 2016; 17(7):681-91.	27216792
Drug reference publications
4.	DrugBank. Eprosartan. Access Date: 2018-August-30
Summary of Product Characteristics
5.	The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Teveten. (Last edition: February 2018)