Company:

Novartis

Antihypertensive agent (direct renin inhibitor)

Aliskiren 150mg, 300mg; tabs.

Treatment of hypertension, as monotherapy or combined with other antihypertensive agents.

Aliskiren is an orally active, nonpeptide, potent direct renin inhibitor that decreases plasma renin activity (PRA) and inhibits the conversion of angioten-sinogen to angiotensin I. Unlike ACE inhibitors and angiotensin receptor blockers, whose effects suppress the negative feed-back loop leading to a compensatory rise in plasma renin concentration, aliskiren blocks the effect of increased renin levels so that PRA, angiotensin I and angiotensin II are reduced.

Aliskiren may be administered with other antihypertensive agents, however it is not known whether additive effects are present when aliskiren is used with ACE inhibitors or beta blockers.

The efficacy of aliskiren was evaluated in six randomized, double-blind, placebo-controlled 8-week trials involving patients with mild-to-moderate hypertension. Approximately 2,730 patients were given doses of 75–600mg of aliskiren and 1,231 patients were given placebo. Patients taking aliskiren showed reasonable blood pressure lowering effect at 150–300mg with no further increase in effect at 600mg. A substantial portion of effect was observed within 2 weeks of treat-ment. Patients in these trials continued open-label aliskiren for up to one year. A persistent BP lowering effect was seen by a randomized withdrawal study (patients randomized to continue drug or placebo), which showed a statistically significant difference between patients kept on aliskiren and those given placebo.

Aliskiren was also evaluated in combination with other antihypertensives. In these studies, BP reductions when used in combination with hydrochlorothiazide or valsartan were greater than the reductions seen with either aliskiren, HCTZ, or valsartan monotherapy. Aliskiren 150mg, when administered with amlodipine 5mg provided additional BP reduction, however the combination was not statistically significantly better than amlodipine 10mg. Aliskiren has not been studied in combination with maximal doses of ACE inhibitors.

≥18yrs: initially 150mg once daily, may increase to 300mg once daily if BP not adequately controlled. May be given with other antihypertensives (see literature).

< 18yrs: not recommended.

Moderate to severe renal dysfunction. History of dialysis. Nephrotic syndrome. Renovascular hypertension. Correct salt/volume depletion before starting therapy or start under close supervision. Monitor for hyperkalemia in diabetics. Pregnancy (Cat.C in 1st trimester; Cat.D 2nd and 3rd trimesters); discontinue as soon as pregnancy detected. Nursing mothers: not recommended.

Decreases furosemide plasma levels; may have diminished effect. Potentiated by atorvastatin, ketoconazole. Antagonized by irbesartan. Caution with max doses of ACE inhibitors.

Diarrhea, hypotension, cough, rash, edema, elevated uric acid, gout, renal stones; rare: angioedema.

Tabs—30, 90

For more information call (888) 835-8876 or visit www.Tekturna.com

3/28/07