II. 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

III. 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

IV. Pharmacokinetics

  1. Renally excreted (renal dose adjustment not necessary, but requires monitoring)
  2. Metabolized by CYP3A4 without inhibitory or induction effects

V. 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%)

VI. Monitoring: Check response 2 weeks after starting medication

  1. Serum Creatinine
  2. Serum electrolytes (esp. Serum Potassium)
  3. Blood Pressure response

VII. 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

VIII. Indications

  1. Second line antihypertensive for those unable to use ACE Inhibitors or Angiotensin Receptor Blockers

IX. Dosing

  1. Start: 150 mg orally daily
  2. Maximum: 300 mg daily

X. Adverse effects

  1. Headache (up to 6%)
  2. Gastrointestinal symptoms (up to 9%)
  3. Dizziness

Images: Related links to external sites (from Bing)

Related Studies (from Trip Database) Open in New Window

Cost: Medications

tekturna (on 1/5/2016 at Medicaid.Gov Survey of pharmacy drug pricing)
TEKTURNA 150 MG TABLET $4.83 each
TEKTURNA 300 MG TABLET $6.20 each
TEKTURNA HCT 150-12.5 MG TAB $4.87 each
TEKTURNA HCT 150-25 MG TABLET $4.82 each
TEKTURNA HCT 300-12.5 MG TAB $6.16 each
TEKTURNA HCT 300-25 MG TABLET $6.06 each

Ontology: 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)

Ontology: Tekturna (C1870961)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C446481
English Tekturna

Ontology: DIRECT RENIN INHIBITOR (C1950687)

Concepts Pharmacologic Substance (T121)
English DIRECT RENIN INHIBITOR, [CV806] DIRECT RENIN INHIBITOR