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Aliskiren

Pronouncation: (a-LIS-KYE-ren)
Class: Renin-angiotensin antagonist

Trade Names:
Tekturna
- Tablets 150 mg
- Tablets 300 mg

Pharmacology

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Direct renin inhibitor, decreasing plasma renin activity and inhibiting conversion of angiotensinogen to angiotensin I.

All agents that inhibit the renin-angiotensin system suppress the negative feedback loop, leading to a compensatory rise in plasma renin concentration. Aliskiren blocks the clinical effect of increased renin levels.

Pharmacokinetics

Absorption

Bioavailability about 2.5%. Following oral administration, C _max is reached within 1 to 3 h. High-fat meal decreases AUC and C _max 71% and 85%, respectively. Steady-state blood levels reached in about 7 to 8 days. Accumulation t _½ about 24 h.

Metabolism

Major enzyme responsible for aliskiren metabolism appears to be CYP3A4.

Elimination

About 25% of the absorbed dose of the parent drug appears to be excreted in the urine.

Hepatic or renal function impairment

Adjustment of the starting dose is not required.

Indications and Usage

Treatment of hypertension, either alone or in combination with other antihypertensive agents.

Contraindications

Standard considerations.

Dosage and Administration

Adults

PO Initial dose is 150 mg once daily. The daily dose may be increased to 300 mg in patients whose BP is not adequately controlled.

General Advice

May be taken without respect to meals.

Storage/Stability

Store at 59° to 86°F. Protect from moisture.

Drug Interactions

ACE inhibitors (eg, captopril)

Risk of hyperkalemia may be increased.

Atorvastatin

Aliskiren C _max and AUC may be increased about 50%.

Furosemide

Blood concentrations may be reduced by aliskiren, decreasing furosemide efficacy.

Irbesartan

Aliskiren C _max may be reduced up to 50%.

Ketoconazole

Aliskiren plasma concentrations may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Dermatologic

Rash (1%)

GI

Diarrhea (2%).

Lab Tests

Elevated BUN or serum creatinine (less than 7%); increased creatine kinase (1%).

Respiratory

Increased cough (1%).

Miscellaneous

Angioedema (0.06%).

Precautions

Warnings

Use during the second and third trimesters can cause injury and death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.

Pregnancy

Category C (first trimester); Category D (second and third trimesters).

Lactation

Undetermined.

Children

Safety and efficacy not established.

Amniotic fluid

In rare instances, when no alternative therapy was available, use in pregnancy has been associated with amniotic fluid deficiency.

Angioedema

Angioedema of the face, extremities, lips, tongue, glottis, and larynx has been reported and may occur any time during treatment.

Hypotension

Rarely, excessive fall in BP may occur.

In-utero exposure

Closely observe infants for hypotension, oliguria, and hyperkalemia.

Overdosage

Symptoms

Possible hypotension.

Patient Information

Inform female patients of childbearing potential of the risk associated with aliskiren exposure during the second and third trimesters of pregnancy.
Advise patient to immediately report swelling of the face, extremities, eyes, lips, or tongue, or difficulty in swallowing or breathing to health care provider and not to take another dose until doing so.