Aliskiren

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.

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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

1. ^ 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.
2. ^ Straessen JA, Li Y, and Richart T (2006). "Oral Renin Inhibitors". Lancet 368 (9545): 1449-56. PMID 17055947.
3. ^ "First Hypertension Drug to Inhibit Kidney Enzyme Approved", CBC, March 6, 2007. Retrieved on 2007-03-14. 
4. ^ FDA approves renin inhibitor aliskiren for hypertension. RxDrug News (2007). Retrieved on 2007-12-02.