Hypertension-otherwise known as the silent killer-is one of the most confusing diseases for researchers. Although many of the risk factors for its etiology are known and researchers have reached several treatments for hypertension, it’s a mystery why some patients still stay resistant and uncontrolled even when using several treatment protocols. It’s alarming that with all the classes present for management of hypertension 7 out of 10 patients are still uncontrolled, according to the recent studies. Thus researchers are always seeking new ways to treat hypertension.
Treatment of hypertension differs mainly on the stage of the disease-on how high the blood pressure is- and usually patients are given a multi-regimen which means they are given several antihypertensive drugs along with lifestyle modifications in order to try to keep BP within an appropriate range.
Many classes of drugs are available for management of hypertension, the most used ones are:
• Beta blockers:
Blocking beta receptors which causes relaxation of small arteries, thus allowing easier flow of blood.
• Ca channel blockers:
Blocking ca channels in the heart and blood vessels, decreasing total peripheral resistance by vasodilatations of the blood vessels
• ACE ( angiotensin converting enzyme) inhibitors :
They are RAAS (renin angiotensin aldosteron system)blockers preventing conversion of angiotensin 1 into angiotensin 2 , thus inhibiting the vasoconstrictor effect of angiotensin2 on the blood vessels.
• ARBs ( angiotensin receptor blockers):
Also act as RAAS blockers and by blocking AT1 receptors stimulate vascular smooth muscle relaxation.
Since 1957 the researchers have known that the best way for hypertension management is blocking the RAAS system through blocking the source which is the renin itself, but they couldn’t manufacture the molecule due to low bio-availability and the very high cost of synthesis, finally in 2006 Novartis Pharmaceuticals launched Aliskrien (market name Rasilez®) in the US and UK, and was considered as a new era and a new class for hypertension management. The launch of this new product in the Middle East was in 2009.
The exact mechanism of Aliskiren is by blocking the renin enzyme in the RAAS system by 70-80% thus decreasing the amount of renin in the blood circulation and the local tissues, renin can be considered as the pro-molecule of angiotensin 2 thus when blocking the renin this leads to a decrease in angiotensin 2 concentration ,and angiotensin2 can be regarded as one of the major causes of vasoconstriction causing an increase in BP. Aliskiren also reduces the plasma renin activity which is linked to increased risk of myocardial infarction, CV morbidity and mortality, according to the recent publications.
Rasilez® is giving the patients very good results in terms of efficacy and blood pressure control versus the current molecules and also better safety and tolerability profiles, and also less side effects compared to others as ACE inhibitors which are known by causing dry cough and calcium channel blockers which causes peripheral edema
Up till now, it is the only molecule that has shown efficacy with almost all patient profiles including obese, diabetics, metabolic syndrome, elderly and even renal impairment patients. It also overcomes the well known problem of patients forgetting taking their medications when having a chronic disease, as it has the longest T ½ ( half life ) up to 41 hours inside the human body , meaning that if the patient skips 2 or even 3 doses ,there is a great chance that his/her blood pressure will still be controlled.
It also should be mentioned that as with any new medication more studies are still needed on a larger scope of patients to establish the preliminarily finding regarding Rasilez®. Finally we can say that Rasilez® is considered as a breakthrough, making a whole new generation and it can be regarded as the new hope for hypertension management.