ALISKIREN (a-lis'ki-ren)
Tekturna Classifications: renin angiotensin system antagonist; direct renin inhibitor; antihypertensive agent; Therapeutic:direct renin inhibitor; antihypertensive agent Pregnancy Category: C first trimester; D second and third trimester
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Availability
150 mg, 300 mg tablets
Action
A direct renin inhibitor that reduces plasma renin activity and inhibits the conversion of angiotensinogen to angiotensin
I (Ang I) and subsequent production of angiotensin II (Ang II).
Therapeutic Effect
Lowers blood pressure by decreasing vasoconstriction and aldosterone production, thus reducing sodium reabsorption and fluid
retention.
Uses
Treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents.
Contraindications
Hypersensitivity to aliskiren; hyperkalemia; hypercalcemia; dehydration; pregnancy (category C first trimester; category
D second and third trimester); lactation; children <18 y.
Cautious Use
Cautious use in patients with Clcr <30 mL/min; older adults; history of angioedema; respiratory disorders; history of airway surgery; diabetes mellitus.
Route & Dosage
Hypertension Adult: PO 150300 mg once daily
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Administration
Oral
- Give consistently with regard to meals.
- Store at 15°30° C (59°86° F) and protect from light.
Adverse Effects (≥1%)
CNS: Headache, dizziness. GI: Diarrhea. Metabolic: Hyperkalemia.
Skin: Angioedema, rash.
Interactions
Drug: Enhances effects of other
ANTIHYPERTENSIVe AGENTS.
Atorvastatin and
ketoconazole increase the
plasma level of aliskiren, while
irbesartan decreases its
plasma level. Aliskiren decreases the
plasma level of
furosemide.
Pharmacokinetics
Absorption: 2.5%.
Peak: 13 h.
Metabolism: <10% via liver.
Elimination: Primarily in stool.
Half-Life: 24 h.
Assessment & Drug Effects
- Monitor for hypotension after the initiation of therapy and following dosage increase.
- Monitor for angioedema, which may occur any time during treatment. Withhold drug and immediately report to physician.
Patient & Family Education
- Full therapeutic effect is usually obtained by 2 wk of therapy.
- Report immediately any of the following: swelling about the face, lips, tongue; difficulty breathing or swallowing; swelling
of hands or feet.
- High fat meals interfere with the absorption of this drug. Do not take drug following a high fat meal.
- Lab tests: periodic serum potassium.