Aliskiren

Definition

An orally active nonpeptide renin inhibitor with antihypertensive activity. Aliskiren selectively binds to the S3 sub-pocket of renin, an enzyme in the renin-angiotensin-aldosterone system (RAAS) that is responsible for converting angiotensinogen to angiotensin I (AT I). By inhibiting the activity of renin, the conversion to AT I is prevented, which in turn prevents the conversion of AT I to AT II. This prevents arterial vasoconstriction by AT II and inhibits the production of aldosterone by AT II. As aldosterone causes re-uptake of sodium and water and eventually an increase in extracellular volume, aliskiren is able to prevent the effects that contribute to an increase in blood pressure.

Also known as (2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methylnonamide, ALISKIREN, CGP 60536, SPP100, Tekturna — per NCIT

Also identified as

• ATC C09XA02 per RXNORM
• NCIT NCIT:C65222 per NCIT
• SCTID 426725002 per RXNORM
• SCTID 427002003 per RXNORM
• UNII 502FWN4Q32 per RXNORM

Indications