Acute Porphyria Drugs

C09CA02 - Eprosartan

Propably not porphyrinogenic
PNP

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.
Chemical description
Angiotensin II receptor antagonist
Therapeutic characteristics
Eprosartan is used in the treatment of essential hypertension. It is administered orally.
Metabolism and pharmacokinetics
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).
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
Similar drugs
Explore alternative drugs in similar therapeutic classes C09C / C09CA or go back.
References
# Citation details PMID
*Scientific articles
1. A review of eprosartan pharmacokinetic and pharmacodynamic drug interaction studies.
Blum RA, Kazierad DJ, et al. Pharmacotherapy. 1999 Apr;19(4 Pt 2):79S-85S.
*Other sources
2.
Eur J Clin Pharmacol. 2000 May;56(2):135-40.
3. Curr Drug Metab Current drug metabolism. , 2016, Vol.17(7), p.681-691
4. DrugBank. Eprosartan.
5. The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Teveten. (Last edition:
Feb.2018).
6. Yang, Ruirui; Luo, Zhiqiang; et at. Drug Interactions with Angiotensin Receptor Blockers: Role of Human Cytochromes P450.
7. In vitro inhibition screening of human hepatic P450 enzymes by five angiotensin-II receptor antagonists.
Taavitsainen P, Kiukaanniemi K et al.

Tradenames

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