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TekturnaAka: Aliskiren, Direct renin inhibitor

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  1. 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. Addiditive effect in combination with ACE Inhibitors, Angiotensin Receptor Blockers
      2. Additive effect in combination with Diuretics
      3. Possible additive effect in combination with Amlodipine
  2. Pharmacokinetics
    1. Renally excreted (renal dose adjustment not necessary, but requires monitoring)
    2. Metabolized by CYP3A4 without inhibitory or induction effects
  3. 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%)
  4. Monitoring: Check response 2 weeks after starting medication
    1. Serum Creatinine
    2. Serum electrolytes (esp. Serum Potassium)
    3. Blood Pressure response
  5. Efficacy
    1. Similar effect on Blood Pressure as ACE Inhibitors and Angiotensin Receptor Blockers
  6. Indications
    1. Hypertension
  7. Dosing
    1. Start: 150 mg orally daily
    2. Maximum: 300 mg daily
  8. Adverse effects
    1. Headache (up to 6%)
    2. Gastrointestinal symptoms (up to 9%)
    3. Dizziness
  9. References
    1. Gradman (2005) Circulation 111:1012

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