aliskiren
Pharmacologic class: Direct renin inhibitor
Pregnancy risk category C (first trimester), D (second and third trimesters)
FDA Box Warning
• Drugs that act directly on the reninangiotensin system can cause injury and death to a developing fetus.
• Discontinue drug as soon as possible when pregnancy is detected.
Action
Decreases plasma renin activity and inhibits conversion of angiotensinogen to angiotensin
Availability
Tablets: 150 mg, 300 mg
Indications and dosages
➣ Hypertension (alone or in combination with other antihypertensives)
Adults: Initially, 150 mg P.O. once daily; may increase to 300 mg if blood pressure isn't adequately controlled
Contraindications
• Concurrent use of angiotensin receptor blockers (ARBs) or ACE inhibitors in patients with diabetes
Precautions
Use cautiously in:
• patients with severe renal dysfunction, nephrotic syndrome, renovascular hypertension, or history of dialysis
• angioedema (laryngeal edema)
• concurrent use of ACE inhibitors or ARBs in patients with renal impairment (GFR less than 60 ml/minute; avoid use)
• concurrent use of NSAIDs including selective COX-2 inhibitors, potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium, or other drugs that increase potassium levels
• females of childbearing age
• pregnant or breastfeeding patients
• children (safety and efficacy not established).
Administration
• Give consistently with or without food, but not with high-fat foods.
Adverse reactions
CNS: headache, fatigue
CV: dizziness, hypotension
EENT: nasopharyngitis
GI: diarrhea, gastroesophageal reflux
Musculoskeletal: back pain
Respiratory: upper respiratory tract infection, cough
Skin: rash
Other: edema, angioedema
Interactions
Drug-drug. ACE inhibitors, ARBs: increased risk of renal impairment, hypotension, and hyperkalemia
Cyclosporine, itraconazole: significantly increased aliskiren level
NSAIDs (including selective COX-2 inhibitors): increased risk of deterioration of renal function, including possible acute renal failure, and increased aliskiren antihypertensive effect
Drug-diagnostic tests. BUN, creatine kinase, potassium, serum creatinine, serum uric acid: increased values
Hematocrit, hemoglobin: decreased values
Drug-food. High-fat meals: decreased drug absorption
Patient monitoring
• Stay alert for signs and symptoms of renal dysfunction, especially in patients receiving NSAIDs.
☞ Monitor patient for signs and symptoms of angioedema; discontinue drug if signs and symptoms are present.
Patient teaching
• Instruct patient to take drug consistently with or without food, but not with high-fat foods.
• Instruct patient not to stop drug suddenly because doing so could result in uncontrolled high blood pressure.
• Advise female to tell prescriber if she's pregnant or breastfeeding before taking drug.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.