A closer look at new FDA actions: Novartis' Tekturna

Monica Holmberg, PharmD
Published Online: Saturday, September 1, 2007
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Novartis? Tekturna

For the first time in over 10 years, an antihypertensive medication of a new class has received approval from the FDA for the treatment of hypertension in adult patients.1 Novartis? Tekturna (aliskiren) is described as a direct renin inhibitor and is the first in this new class of antihypertensive medications to be approved.2

Approximately 25% of Americans are affected by hypertension.1,2 Worldwide, this value rises to almost 1 billion individuals, 70% of whom remain inadequately treated.2 Called the silent killer, hypertension often remains asymptomatic until major damage is already done to the body. Complications of hypertension can include increased risk of stroke, heart attack, kidney failure, heart failure, and death.1

Tekturna is a once-daily treatment and may be used either as monotherapy or in conjunction with other antihypertensive medications. Its use with high-dose angiotensin-converting enzyme (ACE) inhibitors has not been studied extensively. 3

Mechanism of Action

Tekturna?s direct inhibition of renin secretion from the kidney prevents the conversion of angiotensinogen to angiotensin I. Angiotensin I is a precursor to angiotensin II; without angiotensin I, the production of angiotensin II is not possible. Angiotensin II is a peptide responsible for raising blood pressure through catecholamine release, aldosterone secretion, and sodium reabsorption. Thus, preventing the formation of angiotensin II results in decreased blood pressure.3

Clinical Trials

Six randomized, double-blind, placebo-controlled clinical trials studied Tekturna?s safety and efficacy for 8 weeks in patients with mild-to-moderate hypertension. Doses ranged from 150 to 600 mg daily. At the studies? end, Tekturna was determined to be more effective than placebo. Doses of 150 or 300 mg daily were found to be the most reasonable; doses above 300 were not found to be any more effective than the 300-mg dose.

Some patients continued the study as open-label for up to a year. A significant difference in blood pressure was found in patients using Tekturna, compared with those using placebo; on discontinuing treatment with Tekturna, patients? blood pressure returned to baseline after a few weeks.3

Warnings

Tekturna carries a boxed warning against its use in pregnancy. When administered to a pregnant woman, drugs that work directly on the reninangiotensin system have been shown to cause harm or even death to the fetus. As a result, Tekturna should not be used during pregnancy, and patients should be educated to communicate with their health care provider if they are or plan to become pregnant.

Some patients using Tekturna experienced angioedema of the face, extremities, lips, tongue, glottis, and/or larynx. This reaction may occur at any time during treatment with Tekturna. Should angioedema occur, Tekturna should be discontinued immediately, and the patient should receive appropriate supportive care and monitoring.

Hypotension occurred rarely in patients using Tekturna alone or in addition to other antihypertensive medications; however, volume-depleted or salt-depleted patients may be at a greater risk for developing hypotension after initiating treatment with Tekturna. Monitoring and supervision may be appropriate for these patients.3

Precautions

Tekturna was not studied in patients with renal dysfunction, as defined as creatinine 1.7 mg/dL for women or 2.0 mg/dL for men and/or estimated glomerular filtration rate <30 mL/min. Tekturna was not found to cause hyperkalemia when administered alone; hyperkalemia was noted in patients using Tekturna in combination with an ACE inhibitor.

Tekturna is metabolized by CYP3A4. Tekturna levels were noted to be increased significantly when administered concomitantly with atorvastatin and ketoconazole and lowered when administered with irbesartan. Concomitant use of furosemide and Tekturna has resulted in decreased furosemide levels.3

Adverse Reactions

In clinical trials, the most common adverse reaction was diarrhea. Other reactions included cough and rash.1

References

1. Tekturna?the first new type of high blood pressure medicine in more than a decade?receives its first approval in the US [press release]. East Hanover, NJ: Novartis Pharmaceuticals Corp; March 6, 2007. Available at: www.pharma.us.novartis.com/newsroom/pressReleases/releaseDetail.jsp?PRID=2019. Accessed June 2007.

2. FDA approves new drug treatment for high blood pressure [press release]. Rockville, Md: FDA; March 6, 2007. Available at: www.fda.gov/bbs/topics/NEWS/2007/NEW01580.html. Accessed June 2007.

3. Tekturna [package insert]. East Hanover, NJ: Novartis Pharmaceuticals Corp; 2007. Available at: www.pharma.us.novartis.com/product/pi/pdf/tekturna.pdf. Accessed June 2007.



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