Tekturna- For high BP: The first direct renin inhibitor

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Company:

Novartis

Pharmacologic class:

Antihypertensive agent (direct renin inhibitor)

Active ingredient:

Aliskiren 150 mg, 300 mg; tabs.

Indication:

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

Pharmacology:

Aliskiren is an orally active, nonpeptide, potent direct renin inhibitor that decreases plasma renin activity (PRA) and inhibits the conversion of angiotensinogen to angiotensin I. Unlike ACE inhibitors and angiotensin receptor blockers, whose effects suppress the negative feedback 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.

Clinical trials:

The efficacy of aliskiren was evaluated in six randomized, double-blind, placebo-controlled eight-week trials involving patients with mild-to-moderate hypertension. Approximately 2,730 patients were given doses of 75-600 mg of aliskiren and 1,231 patients were given placebo. Patients taking aliskiren showed reasonable BP-lowering effect at 150-300 mg, with no further increase in effect at 600 mg. A substantial portion of effect was observed within two weeks of treatment. 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, hydrochlorothiazide, or valsartan monotherapy. Aliskiren 150 mg, when administered with amlodipine 5 mg; provided additional BP reduction; however the combination was not statistically significantly better than amlodipine 10 mg. Aliskiren has not been studied in combination with maximal doses of ACE inhibitors.

Adults:

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

Children:

<18 years: not recommended.

Precautions:

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 first trimester; Cat. D second and third trimesters); discontinue when pregnancy detected. Nursing mothers: not recommended.

Interactions:

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

Adverse reactions:

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

How supplied:

Tabs—30, 90.

For more information, call 888.835.8876 or visit www.Tekturna.com

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