II. Indications
III. Contraindications
- Children under age 6 years old (or weight <20 kg)
- Pregnancy
- Lactation
IV. Mechanism
- Direct Renin Inhibitor
- Full effect at current dose within 2 weeks of starting
- Additive effect on Hypertension when combined with other agents
- However increased risk in combination - see precautions below
- Addiditive effect in combination with ACE Inhibitors, Angiotensin Receptor Blockers
- Additive effect in combination with Diuretics
- Possible additive effect in combination with Amlodipine
V. Precautions
- Risk of complications, especially in diabetes, when combined with ACE Inhibitors and Angiotensin Receptor Blockers
- Increased risk in combination of Cerebrovascular Accident, renal complications, Hyperkalemia, or Hypotension
VI. Pharmacokinetics
- Renally excreted (renal dose adjustment not necessary, but requires monitoring)
- Metabolized by CYP3A4 without inhibitory or induction effects
VII. Interactions
- Irbesartan (decreases Aliskiren by 50%)
- Atorvastatin (increases Aliskiren by 50%)
- Furosemide (Aliskaren decreases Furosemide efficacy by up to 50%)
- Ketoconazole (increases Aliskiren by 80%)
VIII. Monitoring: Check response 2 weeks after starting medication
- Serum Creatinine
- Serum Electrolytes (esp. Serum Potassium)
- Blood Pressure response
IX. Efficacy
- Similar effect on Blood Pressure as ACE Inhibitors and Angiotensin Receptor Blockers
- Unlike ACE Inhibitors and Angiotensin Receptor Blockers, no evidence that Direct Renin Inhibitors improve outcomes
- No significant benefit in Hypertension, Chronic Kidney Disease, Heart Failure
- Risk of hyptension, Hyperkalemia and increased Serum Creatinine
- (2016) Presc Lett 3(6):34
X. Indications
- Second line antihypertensive for those unable to use ACE Inhibitors or Angiotensin Receptor Blockers
XI. Dosing: Adults
- Start: 150 mg orally daily
- Maximum: 300 mg daily
- Capsules may be opened and mixed with dairy or soy-based pudding, milk, ice cream
XII. Dosing: Children (Age 6 to 17 years and weight >20 kg)
- Weight 20 to 50 kg
- Start 75 mg orally daily
- Maximum 150 mg/day
- Capsules may be opened and mixed with dairy or soy-based pudding, milk, ice cream
- Weight 50 kg
- Dose as adult (see above)
XIII. Adverse Effects
- Headache (up to 6%)
- Gastrointestinal symptoms including Diarrhea (up to 9%)
- Dizziness
- Hyperkalemia
XIV. Safety
- Pregnancy Category X
- Not safe in Lactation
XV. Drug Interactions
- Avoid with ACE Inhibitors or Angiotensin Receptor Blockers in Diabetes Mellitus or GFR <60 ml/min
- Risk of impaired Renal Function, Hypotension or Hyperkalemia
- Avoid with Cyclosporine or Itraconazole
- Avoid with NSAIDS and COX2 Inhibitors
- Risk of impaired Renal Function and reduced antihypertensive effect
- Avoid with Potassium Replacement or high Potassium food intake
XVI. Resources
XVII. References
- Gradman (2005) Circulation 111:1012-8 [PubMed]
- (2020) Med Lett Drugs Ther 62(1598): 73-80
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
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