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Eprosartan for the treatment of hypertension
1Hypertension unit, Hospital 12 de Octubre, 28041 Madrid, Spain. Luis_M_Ruilope@teleline.es
Insights
Eprosartan, an angiotensin II receptor blocker, effectively lowers blood pressure with fewer side effects than ACE inhibitors. This antihypertensive agent is safe and well-tolerated for long-term use.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
Background:
- Antihypertensive agents reduce cardiovascular risks like stroke and heart failure.
- Ideal agents control all hypertension grades with minimal side effects.
- Angiotensin II (AII) receptor antagonists offer an alternative to ACE inhibitors, blocking AII Type 1 (AT(1)) receptors.
Purpose of the Study:
- To evaluate eprosartan, a novel AII receptor antagonist, for its efficacy and safety in hypertension management.
- To compare eprosartan's pharmacological profile and side effects with existing antihypertensive drugs, particularly ACE inhibitors.
Main Methods:
- Clinical trials assessed eprosartan's blood pressure-lowering efficacy against enalapril, an ACE inhibitor.
- Side effect profiles, including cough incidence, were compared.
- Eprosartan's unique non-biphenyl, non-tetrazole, non-peptide structure and dual action (postsynaptic and presynaptic AT(1) receptor antagonism) were highlighted.
Main Results:
- Eprosartan demonstrated comparable blood pressure reduction to enalapril.
- Eprosartan exhibited a significantly lower incidence of side effects, notably cough.
- Its lack of cytochrome P450 metabolism suggests a low potential for drug interactions.
Conclusions:
- Eprosartan is a safe, effective, and well-tolerated antihypertensive agent for monotherapy or combination treatment.
- Its distinct pharmacological profile and favorable side effect profile make it a valuable option for managing hypertension.
- Eprosartan offers a beneficial alternative, especially for patients prone to ACE inhibitor-related side effects or those on multiple medications.
Abstract:
Antihypertensive agents are proven to reduce the cardiovascular risk of stroke, coronary heart disease and cardiac failure. The ideal antihypertensive agent should control all grades of hypertension and have a placebo-like side effect profile. Angiotensin II (AII) receptor antagonists are a relatively new class of antihypertensive agent that block AII Type 1 (AT(1)) receptors, and reduce the pressor effects of AII in the vasculature. By this mechanism, they induce similar pharmacological effects compared with angiotensin-converting enzyme (ACE) inhibitors, resulting in a lowering of blood pressure. However, AII receptor blockers differ from ACE inhibitors with respect to side effects, and induce less cough, a side effect which may be related to bradykinin or other mediators such as substance P. Within the class of AII blockers, eprosartan differs from other currently available agents in terms of chemical structure, as it is a non-biphenyl, non-tetrazole, non-peptide antagonist with a dual pharmacological mode of action. Eprosartan acts at vascular AT(1) receptors (postsynaptically) and at presynaptic AT(1) receptors, where it inhibits sympathetically stimulated noradrenaline release. Its lack of metabolism by cytochrome P450 enzymes confers a low potential for metabolic drug interactions and may be of importance when treating elderly patients and those on multiple drugs. In clinical trials, eprosartan has been demonstrated to be at least as effective in reducing blood pressure as the ACE inhibitor enalapril, and has significantly lower side effects. Eprosartan is safe, effective and well-tolerated in long-term treatment, either as a monotherapy or in combination with other antihypertensive drugs such as hydrochlorothiazide.