a-LIS-ki-ren

Therapeutic Classification: antihypertensives

Pharmacologic Classification:

• Hypertension.

• Inhibition of renin results in decreased formation of angiotensin II, a powerful vasoconstrictor.

• Decreased BP.

Absorption: Poorly absorbed (bioavailability 2.5%).

Distribution: Unknown.

Metabolism/Excretion: 2% excreted unchanged in urine, remainder is probably metabolized (CYP3A4 enzyme system).

Half-life: 24 hr.

(antihypertensive effect)

Contraindicated in:

• Hypersensitivity
• Concurrent use with cyclosporine or itraconazole
• Concurrent use with ACE inhibitors or angiotensin receptor blockers (ARBs) in patients with diabetes or moderate-to-severe renal impairment (CCr <60 mL/min)
• OB: Pregnancy
• Lactation: Lactation
• Pedi: Children <2 yr.

Use Cautiously in:

• Salt or volume depletion (↑ risk of hypotension and acute renal failure; correct before use)
• Concurrent use with ACE inhibitors or ARBs
• Renal artery stenosis, severe HF, post-MI, or use of NSAIDs (↑ risk of acute renal failure)
• Severe renal impairment
• Pedi: Children 2–6 yr or <20 kg (safety and effectiveness not established).

CV: hypotension.

GI: abdominal pain, diarrhea (↑ in females and elderly), dyspepsia, reflux.

GU: acute renal failure.

Resp: cough.
Misc: ANGIOEDEMA.

Drug-Drug:

• ↑risk of hyperkalemia, renal impairment, and hypotension with concurrent use of ACE inhibitors or ARBs; concurrent use contraindicated in patients with diabetes or moderate-to-severe renal impairment (CCr <60 mL/min).
• Blood levels are ↑ by atorvastatin, itraconazole, ketoconazole, verapamil, and cyclosporine; avoid concurrent use with cyclosporine or itraconazole.
• May ↓ effects of furosemide.
• Antihypertensive effects may be ↑ by other antihypertensives, diuretics, and nitrates.
• ↑risk of hyperkalemia with concurrent use of ACE inhibitors, ARBspotassium supplements, potassium-sparing diuretics, or potassium-containing salt substitutes.
• NSAIDs and selective COX-2 inhibitors may blunt the antihypertensive effect and ↑ the risk of renal dysfunction.

Drug-Food:

• High fat meals significantly ↓ absorption.

• PO (Adults): 150 mg once daily initially; may ↑ to 300 mg once daily.
• PO (Children 6 yr and 50 kg): 150 mg once daily initially; may ↑ to 300 mg once daily.
• PO (Children 6 yr and 20–50 kg): 75 mg once daily initially; may ↑ to 150 mg once daily.

(Generic available)

• Tablets: 150 mg; 300 mg;

• Monitor BP and pulse frequently during initial dose adjustment and periodically during therapy. Notify health care professional of significant changes. If an excessive fall in BP occurs, place patient in a supine position and administer IV 0.9% NaCl, if necessary. A transient hypotensive response does not limit further therapy.
• Monitor frequency of prescription refills to determine adherence.

• Monitor renal function and serum potassium periodically during therapy, especially in patients with ↓ renal function or those taking ARBs, ACE inhibitors or NSAIDs, including selective COX-2 inhibitors. May cause ↑ in BUN, serum creatinine, potassium, uric acid, and creatine kinase.
  • May cause small ↓ in hemoglobin and hematocrit.

• Correct volume or sodium depletion prior to initiating therapy.
• PO: Administer at the same time each day without regard to meals.

• Instruct patient to take aliskiren as directed at the same time each day, even if feeling better. Advise patient to eat meals with similar nutrients when taking doses of aliskiren; high fat meals decrease absorption. Take missed doses as soon as remembered, but not if almost time for next dose. Do not double doses. Do not share medication with others, even with same condition; may be harmful.
• May cause dizziness. Caution patient to lie down and notify health care professional. Also, avoid driving and other activities requiring alertness until response to aliskiren is known. Dehydration, excessive perspiration, vomiting or diarrhea may increase risk.
• Instruct patient to avoid using potassium supplements or salt substitutes containing potassium during therapy.
• Advise patient to report signs and symptoms of angioedema (swelling of face, extremities, eyes, lips, or tongue; chest tightness; difficulty swallowing or breathing; rash; hives; itching; dizziness; vomiting) to health care professional immediately.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. If pregnancy is detected, discontinue aliskiren as soon as possible. If pregnancy occurs during therapy, serial ultrasound exams may be used to assess the intra-amniotic environment. Oligohydramnios may not appear until after the fetus has sustained irreversible injury. Closely monitor infants with histories of in utero exposure to aliskiren for hypotension, oliguria, and hyperkalemia; may require exchange transfusions.

• Decrease in BP without appearance of side effects. Antihypertensive effect is 90% attained by 2 wk.

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