Pharmacokinetic, pharmacodynamic and clinical evaluation of aliskiren for hypertension treatment

Expert Opin Drug Metab Toxicol. 2011 Jan;7(1):115-28. doi: 10.1517/17425255.2011.538681. Epub 2010 Nov 24.

Abstract

Importance of the field: Aliskiren, a drug which inhibits the initial and rate-limiting step of the renin angiotensin aldosterone system (RAAS), recently approved for the treatment of hypertension, may become a reasonable therapeutic choice in a broad number of clinical conditions sharing an increased cardiovascular risk, where the inhibition of the RAAS has been shown to be beneficial.

Areas covered in this review: The present review summarizes the pharmacokinetic and pharmacodynamic properties of aliskiren along with the clinical trials that took into account the effects of aliskiren on blood pressure control and on a number of renal and cardiovascular end points. The specific effects of aliskiren on different populations (e.g., elderly hypertensives, patients with diabetes and hypertension, patients with hypertension and renal impairment) are discussed.

What the reader will gain: The review discusses the most recent discoveries of the cardiovascular and renal effects of aliskiren, including a comprehensive discussion of the ongoing trials and of the areas of remaining uncertainty.

Take home message: Aliskiren is a promising drug that may become a convenient choice in several clinical conditions. The full spectrum of the beneficial effects of aliskiren will be fully elucidated when the results of the large ongoing trials become available.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amides / adverse effects
  • Amides / pharmacokinetics*
  • Antihypertensive Agents / pharmacokinetics*
  • Cardiovascular Diseases / chemically induced
  • Clinical Trials as Topic
  • Diabetes Mellitus / drug therapy
  • Drug Evaluation*
  • Drug Therapy, Combination
  • Drug-Related Side Effects and Adverse Reactions
  • Fumarates / adverse effects
  • Fumarates / pharmacokinetics*
  • Humans
  • Hypertension / drug therapy*
  • Kidney Diseases / chemically induced
  • Kidney Diseases / drug therapy
  • Renin / blood
  • Renin-Angiotensin System

Substances

  • Amides
  • Antihypertensive Agents
  • Fumarates
  • aliskiren
  • Renin