| Item |
Information |
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Drug Groups
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approved; investigational |
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Description
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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 |
| • |
Humans and other mammals |
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| 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 |
| • |
Gradman AH, Schmieder RE, Lins RL, Nussberger J, Chiang Y, Bedigian MP: Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation. 2005 Mar 1;111(8):1012-8. Epub 2005 Feb 21.
[Pubmed]
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| • |
Staessen JA, Li Y, Richart T: Oral renin inhibitors. Lancet. 2006 Oct 21;368(9545):1449-56.
[Pubmed]
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| • |
Vaidyanathan S, Jarugula V, Dieterich HA, Howard D, Dole WP: Clinical pharmacokinetics and pharmacodynamics of aliskiren. Clin Pharmacokinet. 2008;47(8):515-31.
[Pubmed]
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| External Links |
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