ALISKIREN

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

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 150–300 mg once daily

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: 1–3 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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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