Tekturna (aliskiren)
Potential health benefits on cancers and research finds   2007
Novartis' Tekturna (aliskiren) tablets was approved on March 6, 2007 for
the treatment of high blood pressure, or hypertension. Tekturna, a new
molecular entity (NME), is the first high blood pressure drug approved by
FDA that inhibits renin, a kidney enzyme associated with the regulation of
blood pressure. Tekturna acts at the beginning of the blood pressure
regulation process, while other available high blood pressure medications
act at later stages.

High blood pressure is often considered as the silent killer, because it
usually has no symptoms until it causes major damage to the body organs,
such as stroke, heart attack, kidney failure, heart failure and death.

The effectiveness of Tekturna in lowering blood pressure has been
demonstrated in six placebo-controlled eight-week clinical trials, which
studied more than 2,000 patients with mild to moderate hypertension. The
effect was maintained for up to one year. Tekturna was effective across all
demographic subgroups, [1,4] but African American patients tended to have
smaller reductions in blood pressure than Caucasians and Asians, as is
generally true for drugs that affect the renin-angiotensin system, a
component of blood pressure regulation.

Tekturna by itself demonstrates effective blood lowering in a number of
studies. Tekturna can also be used in combination with a thiazide diuretic
(hydrochlorothiazide), an angiotensin-converting enzyme inhibitor (ramipril)
or a calcium channel blocker (amlodipine), a diuretic, further reductions in
blood pressure were achieved. [3]

What are the side effects and drug interaction of Tekturna?

Aliskiren is a novel, orally active direct renin inhibitor that lowers blood
pressure alone and in combination with existing antihypertensive agents. As
aliskiren does not affect cytochrome P450 enzyme activities, is minimally
metabolised, and is not extensively protein bound, the potential for drug
interactions is predicted to be low. [5]

In studies of healthy male volunteers aged 18-45 years, mean AUC and t1/2
for aliskiren were not significantly changed by the intake of lovastatin,
atenolol or celecoxib.

Aliskiren mean Cmax was not affected by either lovastatin or atenolol,
although a non-significant 36% increase was observed with celecoxib.
Modest, non-significant increases in aliskiren systemic availability followed
coadministration with cimetidine.

Tekturna was evaluated for safety in more than 6,460 patients, including
1,740 who were treated longer than six months, and more than 1,250 for
over one year. Side effects were usually mild and brief. The most common
side effect experienced by patients taking Tekturna was diarrhea. Diarrhea
was reported by approximately 2 percent of patients on the higher of the
two approved doses, compared with approximately 1 percent on placebo.
Rarely, patients taking Tekturna developed an allergic reaction with swelling
of the face, lips or tongue and difficulty breathing, as has been seen with
other drugs for high blood pressure that act directly on the
renin-angiotensin system.

The most commonly reported adverse events were headache, dizziness
and gastrointestinal symptoms (all mild in severity), which were similar in
frequency during antihypertensive drug treatment alone and in combination
with aliskiren except for an increase in dizziness during treatment with the
combination of aliskiren and hydrochlorothiazide. [5]

Tekturna and other drugs that act directly on the renin-angiotensin system
should not be used during pregnancy because they can cause injury and
even death to the developing fetus. [1]

According to Brown MJ's review article, of currently available
antihypertensive drugs, only the beta-blockers suppress renin secretion,
unfortunately they also reduce heart rate and cardiac output. [2] While,
calcium channel blockers and diuretics cause a modest activation of the
renin system secondary to the fall in renal afferent arteriolar pressure and
reduction in filtered sodium load. [2] Aliskiren is the first orally available
direct inhibitor that blocks the renin system at its rate limiting step and is
shown to reduce angiotensin I and II and plasma renin activity. [1-2]

[1] FDA Approves New Drug Treatment for High Blood Pressure FDA News
March 6, 2007. [2] Brown MJ. Direct renin inhibition a new way of targeting
the renin system. J Renin Angiotensin Aldosterone Syst. 2006
Jan;7(2):S8-S11. [3] Schmieder RE. Aliskiren: a clinical profile. J Renin
Angiotensin Aldosterone Syst. 2006 Jan;7 Suppl 2:S16-20. [4]
Vaidyanathan S, Jermany J, Yeh C, Bizot MN, Camisasca R. Aliskiren, a
novel orally effective renin inhibitor, exhibits similar pharmacokinetics and
pharmacodynamics in Japanese and Caucasian subjects. Br J Clin
Pharmacol. 2006 Dec;62(6):690-8. [5] Vaidyanathan S, et al, Lack of
pharmacokinetic interactions of aliskiren, a novel direct renin inhibitor for
the treatment of hypertension, with the antihypertensives amlodipine,
valsartan, hydrochlorothiazide (HCTZ) and ramipril in healthy volunteers.
Dieterle W, Corynen S, Vaidyanathan S, Mann J. Pharmacokinetic
interactions of the oral renin inhibitor aliskiren with lovastatin, atenolol,
celecoxib and cimetidine. Int J Clin Pharmacol Ther. 2005
Nov;43(11):527-35.
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