Name: | aliskiren |
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PubChem Compound ID: | 5493444 |
Molecular formula: | C30H53N3O6 |
Molecular weight: | 551.758 g/mol |
Synonyms: |
Aliskiren (USAN); SPP100; Aliskiren [INN]; 173334-57-1; D03208; Rasilez; Aliskiren; SPP 100; Rasilez (TN)
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Name: | aliskiren |
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Name (isomeric): | DB01258 |
Drug Type: | small molecule |
Synonyms: |
Rasilez; SPP 100
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Brand: | Rasilez, Tekturna |
Category: | Antihypertensive Agents |
CAS number: | 173334-57-1 |
Indication: | For the treatment of mild to moderate hypertension. It may be used alone or in combination with other antihypertensive agents. |
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Pharmacology: | Aliskiren is a nonpeptide renin inhibitor marketed under the trade name Tekturna by Novartis. |
Mechanism of Action: |
Renin is secreted by the kidney in response to decreases in blood volume and renal perfusion. Renin cleaves angiotensinogen to form the inactive decapeptide angiotensin I (Ang I). Ang I is converted to the active octapeptide angiotensin II (Ang II) by angiotensin-converting enzyme (ACE) and non-ACE pathways. Ang II is a powerful vasoconstrictor an...
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Absorption: | Rapidly absorbed following oral administration. Absolute bioavailability = 2.6% |
Protein binding: | 47-51% |
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. |
Route of elimination: | About one fourth of the absorbed dose appears in the urine as parent drug. |
Half Life: | 24-41 hours |
Toxicity: | The most likely manifestation of overdosage would be hypotension. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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