Key result
Telmisartan, eprosartan, and olmesartan avoid CYP-mediated interactions and dosage adjustments compared with losartan.
Why the study?
Angiotensin receptor blockers used to treat hypertension can cause side effects that are sometimes associated with pharmacokinetic alterations, and the cytochrome P450 enzyme system plays an important role in clinically relevant drug-drug and food-drug interactions.
Eprosartan, telmisartan, and olmesartan do not undergo cytochrome P450 metabolism and require no dosage adjustments when co-administered with other drugs in patients with hypertension, unlike losartan which relies heavily on CYP2C9 and CYP3A4.
Answers are grounded in this paper and cite their sources.
May guide ARB choice in polypharmacy hypertension; leaves open prospective outcome trials confirming interaction-free profiles.
BACKGROUND: Angiotensin receptor blockers (ARBs) are the most recent class of agents for the treatment of hypertension. However, ARBs may cause a low incidence of headache, upper respiratory infection, back pain, muscle cramps, fatigue, dizziness, and many other side effects. In some cases, such toxicity is associated with pharmacokinetic alterations. METHODS: The cytochrome P450 (CYP) enzyme system plays an important role in a lot of clinically important pharmacokinetic drug interactions. To identify relevant studies on drug-drug and food-drug pharmacokinetic interactions with the ARBs, a literature search of Google Scholar was performed from January 1994 to June 2015, with the following keywords: 'losartan', 'valsartan,' 'candesartan,' 'irbesartan,' 'telmisartan,' 'eprosartan,' 'olmesartan,' and 'azilsartan', combined with the keyword 'pharmacokinetic interactions' and 'CYP'. RESULTS: Based on the literatures published, it has been demonstrated that pharmacokinetic interactions of losartan with other agents are mainly via CYP2C9- and CYP3A4-mediated, the role played by CYP enzyme system in the metabolism of valsartan, candesartan, irbesartan, and azilsartan appears modest, and cytochrome P450 system has no influence on the metabolism of telmisartan, eprosartan, olmesartan. Therefore, according to these pharmacokinetic findings, no dosage adjustment is recommended when eprosartan, telmisartan and olmesartan are combined with other pharmacological agents in patients with hypertension. CONCLUSION: This review summarize the available data on cytochrome P450 - related drug-drug interactions reported in the literature for the eight ARBs. Knowledge of the pharmacokinetic properties of the ARBs should allow the avoidance of the majority of drug interactions without compromising therapeutic benefits.
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Yang et al. (2016) conducted a review in Hypertension. Angiotensin receptor blockers (losartan, valsartan, candesartan, irbesartan, telmisartan, eprosartan, olmesartan, azilsartan) was evaluated on Cytochrome P450-mediated pharmacokinetic drug-drug and food-drug interactions. Among eight reviewed ARBs, losartan interacts mainly via CYP2C9 and CYP3A4, whereas telmisartan, eprosartan, and olmesartan have no CYP-mediated interactions and require no dosage adjustments.
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