Aliskiren Hemifumarate

Name: Aliskiren Hemifumarate

Introduction

Nonpeptide renin inhibitor.1 2 3 4 5 6 7 8 9 10

Uses for Aliskiren Hemifumarate

Hypertension

Management of hypertension (alone or in combination with other antihypertensive agents);1 3 4 5 6 7 8 9 11 15 34 35 may be used in fixed combination with amlodipine with or without hydrochlorothiazide when such combined therapy is indicated.34 35

Most experience with combination therapy to date has been with diuretics, an angiotensin II receptor antagonist (valsartan), or a calcium-channel blocking agent (amlodipine); concomitant use of aliskiren with any of these drugs at maximum recommended dosages produces a greater BP response than does use of each drug alone.1 34 Triple combination of aliskiren, amlodipine, and hydrochlorothiazide produces greater BP reductions compared with dual combinations of these drugs.35

Not known whether effects of aliskiren and ACE inhibitors or aliskiren and β-adrenergic blocking agents are additive.1 Whether aliskiren further improves BP control in patients receiving maximum dosages of an ACE inhibitor not established.1

Use in combination with an ACE inhibitor or angiotensin II receptor antagonist is contraindicated in diabetic patients and is not recommended in patients with moderate or severe renal impairment (GFR <60 mL/minute).1 (See Use in Combination with ACE Inhibitors or Angiotensin II Receptor Antagonists under Cautions.)

Stability

Storage

Oral

Tablets

Aliskiren: Original container at 25°C (may be exposed to 15–30°C); protect from moisture.1

Aliskiren/amlodipine and aliskiren/amlodipine/hydrochlorothiazide fixed combinations: Original container at 25ºC (may be exposed to 15–30ºC); protect from heat and moisture.34 35

Actions

  • Binds with high affinity to plasma renin.9

  • Inhibits conversion of angiotensinogen to angiotensin I and reduces plasma renin activity (PRA) and concentrations of angiotensin I, angiotensin II, and aldosterone.1 2 3 4 6 8 9 10

  • May suppress feedback inhibition of renin secretion leading to a compensatory increase in plasma renin concentrations; however, PRA does not appear to increase, unlike therapy with ACE inhibitors or angiotensin II receptor antagonists.1 9 10

  • Not known whether aliskiren affects other renin-angiotensin-aldosterone (RAA) system components (e.g., ACE, non-ACE pathways).1

Advice to Patients

  • Importance of reading the manufacturer's patient information before initiating therapy and each time the prescription is refilled.1

  • When aliskiren is used in fixed combination with amlodipine with or without hydrochlorothiazide, advise patients of important precautionary information about the concomitant agent(s).34 35

  • Advise patients to take the drug once daily at same time every day, establishing a routine pattern with regard to food.1 11 34 35 Advise patients that high-fat meals substantially decrease oral absorption of the drug.1

  • Importance of advising patient that if a dose of aliskiren is missed to take it as soon as it is remembered.1 If it is almost time for the next dose, omit the missed dose and administer the next dose at the regularly scheduled time.1

  • Risk of angioedema, including laryngeal edema; importance of discontinuing the drug and immediately reporting suggestive manifestations (e.g., edema of face, extremities, eyes, lips, or tongue; swallowing or breathing with difficulty) to a clinician.1

  • Risk of fetal and neonatal morbidity and death when administered to pregnant women.1

  • Importance of women informing clinicians immediately if they are or plan to become pregnant or plan to breast-feed.1 Advise women to discontinue aliskiren if they become pregnant.1

  • Risk of hypotension, lightheadedness, or syncope, especially during initial therapy or with volume depletion secondary to inadequate fluid intake, excessive perspiration, diarrhea, or vomiting.1 Importance of informing clinician if lightheadedness occurs.1 If syncope occurs, importance of discontinuing therapy until clinician has been consulted.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1 Importance of not using potassium supplements or potassium-containing salt substitutes without consulting clinician.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

(web3)