Cardiovascular Medicine Book



Aka: Tekturna, Aliskiren, Direct renin inhibitor
  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. 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
  2. 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
  3. Pharmacokinetics
    1. Renally excreted (renal dose adjustment not necessary, but requires monitoring)
    2. Metabolized by CYP3A4 without inhibitory or induction effects
  4. 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%)
  5. Monitoring: Check response 2 weeks after starting medication
    1. Serum Creatinine
    2. Serum Electrolytes (esp. Serum Potassium)
    3. Blood Pressure response
  6. 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
  7. Indications
    1. Second line antihypertensive for those unable to use ACE Inhibitors or Angiotensin Receptor Blockers
  8. Dosing
    1. Start: 150 mg orally daily
    2. Maximum: 300 mg daily
  9. Adverse effects
    1. Headache (up to 6%)
    2. Gastrointestinal symptoms (up to 9%)
    3. Dizziness
  10. References
    1. Gradman (2005) Circulation 111:1012-8 [PubMed]
Medication Costs
tekturna (on 3/22/2017 at Medicaid.Gov Pharmacy Drug pricing)
TEKTURNA 150 MG TABLET $5.26 each
TEKTURNA 300 MG TABLET $6.67 each
TEKTURNA HCT 150-12.5 MG TAB $5.28 each
TEKTURNA HCT 150-25 MG TABLET $5.31 each
TEKTURNA HCT 300-12.5 MG TAB $6.66 each
TEKTURNA HCT 300-25 MG TABLET $6.67 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

aliskiren (C1120110)

Definition (NCI) An orally active nonpeptide renin inhibitor with antihypertensive activity. Aliskiren selectively binds to the S3 sub-pocket of renin, an enzyme in the renin-angiotensin-aldosterone system (RAAS) that is responsible for converting angiotensinogen to angiotensin I (AT I). By inhibiting the activity of renin, the conversion to AT I is prevented, which in turn prevents the conversion of AT I to AT II. This prevents arterial vasoconstriction by AT II and inhibits the production of aldosterone by AT II. As aldosterone causes re-uptake of sodium and water and eventually an increase in extracellular volume, aliskiren is able to prevent the effects that contribute to an increase in blood pressure.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C446481
SnomedCT 427002003, 426725002
English Aliskiren (product), Aliskiren, Aliskiren (substance), aliskiren (medication), ALISKIREN, aliskiren [Chemical/Ingredient], aliskiren, (2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methylnonamide
Spanish aliskireno (producto), aliskireno, aliskireno (sustancia), aliskiren, aliskiren (producto), aliskiren (sustancia)
Derived from the NIH UMLS (Unified Medical Language System)

Tekturna (C1870961)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C446481
English Tekturna
Derived from the NIH UMLS (Unified Medical Language System)


Concepts Pharmacologic Substance (T121)
Derived from the NIH UMLS (Unified Medical Language System)

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