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Tekturna

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Tekturna, Aliskiren, Direct Renin Inhibitor

  • Indications
  1. Hypertension
  • Contraindications
  1. Children under age 6 years old (or weight <20 kg)
  2. Pregnancy
  3. Lactation
  • Mechanism
  1. Direct Renin Inhibitor
  2. Full effect at current dose within 2 weeks of starting
  3. Additive effect on Hypertension when combined with other agents
    1. However increased risk in combination - see precautions below
    2. Addiditive effect in combination with ACE Inhibitors, Angiotensin Receptor Blockers
    3. Additive effect in combination with Diuretics
    4. Possible additive effect in combination with Amlodipine
  • Precautions
  1. Risk of complications, especially in diabetes, when combined with ACE Inhibitors and Angiotensin Receptor Blockers
    1. Increased risk in combination of Cerebrovascular Accident, renal complications, Hyperkalemia, or Hypotension
  • Pharmacokinetics
  1. Renally excreted (renal dose adjustment not necessary, but requires monitoring)
  2. Metabolized by CYP3A4 without inhibitory or induction effects
  • Interactions
  1. Irbesartan (decreases Aliskiren by 50%)
  2. Atorvastatin (increases Aliskiren by 50%)
  3. Furosemide (Aliskaren decreases Furosemide efficacy by up to 50%)
  4. Ketoconazole (increases Aliskiren by 80%)
  • Monitoring
  • Check response 2 weeks after starting medication
  1. Serum Creatinine
  2. Serum Electrolytes (esp. Serum Potassium)
  3. Blood Pressure response
  • Efficacy
  1. Similar effect on Blood Pressure as ACE Inhibitors and Angiotensin Receptor Blockers
  2. Unlike ACE Inhibitors and Angiotensin Receptor Blockers, no evidence that Direct Renin Inhibitors improve outcomes
    1. No significant benefit in Hypertension, Chronic Kidney Disease, Heart Failure
    2. Risk of hyptension, Hyperkalemia and increased Serum Creatinine
    3. (2016) Presc Lett 3(6):34
  • Indications
  1. Second line Antihypertensive for those unable to use ACE Inhibitors or Angiotensin Receptor Blockers
  • Dosing
  • Adults
  1. Start: 150 mg orally daily
  2. Maximum: 300 mg daily
  3. Capsules may be opened and mixed with dairy or soy-based pudding, milk, ice cream
  • Dosing
  • Children (Age 6 to 17 years and weight >20 kg)
  1. Weight 20 to 50 kg
    1. Start 75 mg orally daily
    2. Maximum 150 mg/day
    3. Capsules may be opened and mixed with dairy or soy-based pudding, milk, ice cream
  2. Weight 50 kg
    1. Dose as adult (see above)
  • Adverse Effects
  1. Headache (up to 6%)
  2. Gastrointestinal symptoms including Diarrhea (up to 9%)
  3. Dizziness
  4. Hyperkalemia
  • Safety
  1. Pregnancy Category X
  2. Not safe in Lactation
  • Drug Interactions
  1. Avoid with ACE Inhibitors or Angiotensin Receptor Blockers in Diabetes Mellitus or GFR <60 ml/min
    1. Risk of impaired Renal Function, Hypotension or Hyperkalemia
  2. Avoid with Cyclosporine or Itraconazole
  3. Avoid with NSAIDS and COX2 Inhibitors
    1. Risk of impaired Renal Function and reduced Antihypertensive effect
  4. Avoid with Potassium Replacement or high Potassium food intake
  • Resources
  1. Aliskiren (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=f3fd2503-25ef-4660-a29a-f62c491e28fb
  • References
  1. Gradman (2005) Circulation 111:1012-8 [PubMed]
  2. (2020) Med Lett Drugs Ther 62(1598): 73-80
  3. Hamilton (2020) Tarascon Pocket Pharmacopoeia