CAS NO 138402 11 6 (IRBESARTÁN)
Irbesartán, identified by CAS No. 138402-11-6 , is a well-established angiotensin II receptor blocker that plays a central role in the management of hypertension and related complications. Its effectiveness, safety profile, and organ-protective properties have made it a prominent option in clinical practice for over two decades.
Chemical Properties and Structure
Irbesartán is a non-peptide, orally active compound. It is a white, crystalline powder with moderate solubility in aqueous solutions. Its structure enables highly selective binding to the angiotensin II AT1 receptor, which is central to its pharmacological effects.
Mechanism of Action
Irbesartán acts by selectively blocking the angiotensin II type 1 (AT1) receptors found predominantly in vascular smooth muscle and the adrenal gland. Normally, angiotensin II binds to these receptors, causing vasoconstriction and stimulating the release of aldosterone, both of which raise blood pressure. By blocking these receptors, irbesartán causes blood vessels to relax and inhibits aldosterone secretion, thereby lowering blood pressure and relieving the cardiac workload.
It binds to the AT1 receptor with over 8,000 times greater affinity compared to the AT2 receptor, which means its effect is highly targeted, reducing the risk of off-target adverse effects.
Medical Uses
Irbesartán is primarily used for the following indications:
- Treatment of essential hypertension in adults, offering effective 24-hour blood pressure control with once-daily dosing.
- Delay of progression in diabetic nephropathy, particularly in patients with type 2 diabetes, hypertension, and signs of kidney damage such as microalbuminuria or proteinuria.
- It is often prescribed as monotherapy but also works well in combination with other antihypertensive agents, notably thiazide diuretics such as hydrochlorothiazide, for patients inadequately controlled with a single agent.
Pharmacological Benefits
Irbesartán is valued not only for its antihypertensive properties but also for beneficial effects that extend beyond blood pressure control:
- Proven reduction in left ventricular mass (hypertrophy), supporting healthier cardiac structure and function over time.
- Renoprotective effects, including reduced progression of diabetic kidney disease, are well documented both in early and later stages.
- Improvement in endothelial function, reduction of oxidative stress, and anti-inflammatory effects add to its value in cardiovascular and renal risk reduction.
Dosage and Administration
The usual starting dose is 150 mg once daily, which can be increased to 300 mg for patients requiring greater blood pressure reduction. The antihypertensive effect is apparent within two weeks and typically reaches its peak after 2-6 weeks of therapy. When used in combination with hydrochlorothiazide, it offers additive blood pressure reduction through complementary mechanisms.
Safety Profile and Adverse Effects
Irbesartán’s side effect profile resembles a placebo in most studies, with the most common adverse effects including dizziness, fatigue, and mild gastrointestinal symptoms. Potassium levels may increase, especially when combined with other agents that affect the renin-angiotensin system. The medication is generally well tolerated and is considered safe for long-term use.
However, precautions are necessary in certain populations:
- It is not recommended during pregnancy or while breastfeeding.
- Renal function and potassium levels should be monitored in patients with kidney impairment or those taking potassium-sparing diuretics.
Advancements and Clinical Experience
Irbesartán’s efficacy and safety have been confirmed in numerous large-scale, randomized clinical trials. Its place in hypertension and diabetic nephropathy management is supported by global treatment guidelines. Long-term adherence is high due to convenient dosing and favorable tolerability, contributing to its lasting popularity in clinical practice.
Research and Future Directions
Ongoing research explores further cardiovascular and renal benefits, expanding its use in complex patient groups and investigating synergistic effects with other medications. There is particular interest in its protective effects on heart structure and function, prevention of arrhythmias, and benefits in early kidney disease even in normotensive patients.
Conclusion
Irbesartán (CAS No. 138402-11-6) stands out as a versatile and reliable treatment for hypertension and diabetic nephropathy, with enduring clinical value attributed to its targeted action, robust efficacy, safety, and additional organ-protective properties.
URL: For more information, visit Verdant Pharma : CAS NO 138402 11 6 (IRBESARTÁN)
