Molecule

Drug Groups

approved; investigational

Description

Aliskiren is a renin inhibitor. It was approved by the U.S. Food and Drug Administration in 2007 for the treatment of hypertension.

Indication

For the treatment of mild to moderate hypertension. It may be used alone or in combination with other antihypertensive agents.

Pharmacology

Aliskiren is a nonpeptide renin inhibitor marketed under the trade name Tekturna by Novartis.

Toxicity

The most likely manifestation of overdosage would be hypotension.

Affected Organisms

Biotransformation

Approximately 80% of the drug in plasma following oral administration is unchanged. Cytochrome P450 (CYP) 3A4 oxidation produces two major metabolites that account for approximately 5% of the drug in plasma. Aliskiren is eliminated primarily through the biliary/fecal route as unchanged drug and, to a lesser extent, via oxidative metabolism via CYP3A4. Only 0.6% of the oral dose is recovered in urine.

Absorption

Rapidly absorbed following oral administration. Absolute bioavailability = 2.6%

Half Life

24-41 hours

Protein Binding

47-51%

Elimination

About one fourth of the absorbed dose appears in the urine as parent drug.

References

External Links