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Irbesartan, sold under the brand name Aprovel among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease. [5] It is a reasonable initial treatment for high blood pressure. [5] It is taken by mouth. [5] Versions are available as the combination irbesartan/hydrochlorothiazide. [5] [6] [7] [8]
Irbesartan was developed by Sanofi Research and is longer acting than valsartan and losartan and it has an imidazolinone ring where a carbonyl group functions as a hydrogen bond acceptor instead of the hydroxymethyl group in losartan. Irbesartan is a non-competitive inhibitor. [4]
Angiotensin-converting-enzyme inhibitors (ACE inhibitors) are a class of medication used primarily for the treatment of high blood pressure and heart failure. [1] [2] This class of medicine works by causing relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart.
ATC code C09 Agents acting on the renin–angiotensin system is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products.
Antihypertensive agents comprise multiple classes of compounds that are intended to manage hypertension (high blood pressure). Antihypertensive therapy aims to maintain a blood pressure goal of <140/90 mmHg in all patients, as well as to prevent the progression or recurrence of cardiovascular diseases (CVD) in hypertensive patients with established CVD. [2]
They selectively block the activation of the AT 1 receptor, preventing the binding of angiotensin II compared to ACE inhibitors. [4] ARBs and the similar-attributed ACE inhibitors are both indicated as the first-line antihypertensives in patients developing hypertension along with left-sided heart failure. [5]
Reflecting the critical role of zinc, ACE can be inhibited by metal-chelating agents. [14] ACE in complex with inhibitor lisinopril, zinc cation shown in grey, chloride anions in yellow. Based on PyMOL rendering of PDB 1o86. The picture shows that lisinopril is a competitive inhibitor, since it and angiotensin I are similar structurally.
These results also indicate that the N-domain possess a broader selectivity than the C-domain. Another difference between the older ACE inhibitors and RXP 407 is the molecular size of the compound. The older ACE inhibitors had mostly been interacting with S 1 ’, S 2 ’ and S 1 subsites but RXP 407 interacts in addition with the S 2 subsite.