Aliskiren
 | |
| Clinical data | |
|---|---|
| Pregnancy category |
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| Routes of administration | Oral |
| ATC code | |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | Low (approximately 2.5%) |
| Metabolism | Hepatic, CYP3A4-mediated |
| Elimination half-life | 24 hours |
| Excretion | Renal |
| Identifiers | |
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| CAS Number | |
| PubChem CID | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| Chemical and physical data | |
| Formula | C30H53N3O6 |
| Molar mass | 551.758 g/mol |
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Overview
Aliskiren (INN) is a first in class renin inhibitor co-developed by the Swiss pharmaceutical companies Novartis and Speedel.[1][2] It was approved by the U.S. Food and Drug Administration in 2007 for the treatment of hypertension.[3] The trade name for aliskiren is Tekturna in the USA, and Rasilez in the UK.
Adverse effects
- Angioedema
- Hyperkalemia (particularly when used with ACE inhibitors in diabetic patients)
- Hypotension (particularly in volume-depleted patients)
- Diarrhea and other GI symptoms
- Rash, elevated uric acid, gout, and renal stones.
A rare adverse event was allergic swelling of the face, lips or tongue and difficulty breathing, side effects that are common with other drugs for hypertension that act directly on the renin-angiotensin system. [4]
Contraindications
As with ACE inhibitors, renin inhibitors should not be used in pregnancy, specifically the second and third trimesters, during which they will interfere with fetal kidney development and lead to oligohydramnios.
Aliskiren has not yet been evaluated in patients with significantly impaired renal function.
Drug Interactions
Minor substrate of CYP3A4:
- Reduces furosemide blood concentration.
- Atorvastatin or ketoconazole may increase blood concentration.
References
- ↑ Gradman A, Schmieder R, Lins R, Nussberger J, Chiang Y, Bedigian M (2005). "Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients". Circulation. 111 (8): 1012–8. PMID 15723979.
- ↑ Straessen JA, Li Y, and Richart T (2006). "Oral Renin Inhibitors". Lancet. 368 (9545): 1449–56. PMID 17055947.
- ↑ "First Hypertension Drug to Inhibit Kidney Enzyme Approved". CBC. March 6, 2007.
- ↑ "FDA approves renin inhibitor aliskiren for hypertension". RxDrug News. 2007.
External links
- Template:PDFlink at the U.S. Food and Drug Administration website
- Aliskiren at KEGG Ligand Database
- aliskiren at the US National Library of Medicine Medical Subject Headings (MeSH)
- Speedel [3]
- Pages with script errors
- CS1 maint: Multiple names: authors list
- E number from Wikidata
- ECHA InfoCard ID from Wikidata
- Chemical articles with unknown parameter in Infobox drug
- Articles without EBI source
- Chemical pages without ChemSpiderID
- Chemical pages without DrugBank identifier
- Articles without KEGG source
- Articles without InChI source
- Articles without UNII source
- Articles containing unverified chemical infoboxes
- Antihypertensive agents
- Renin inhibitors
- Drugs