Tekturna, Aliskiren, Direct renin inhibitor

  • 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
  • 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
  1. Start: 150 mg orally daily
  2. Maximum: 300 mg daily
  • Adverse effects
  1. Headache (up to 6%)
  2. Gastrointestinal symptoms (up to 9%)
  3. Dizziness