II. Mechanism
- Direct renin inhibitor
- Full effect at current dose within 2 weeks of starting
- Additive effect on Hypertension when combined with other agents
- However increased risk in combination - see precautions below
- Addiditive effect in combination with ACE Inhibitors, Angiotensin Receptor Blockers
- Additive effect in combination with Diuretics
- Possible additive effect in combination with Amlodipine
III. Precautions
- Risk of complications, especially in diabetes, when combined with ACE Inhibitors and Angiotensin Receptor Blockers
- Increased risk in combination of Cerebrovascular Accident, renal complications, Hyperkalemia, or Hypotension
IV. Pharmacokinetics
- Renally excreted (renal dose adjustment not necessary, but requires monitoring)
- Metabolized by CYP3A4 without inhibitory or induction effects
V. Interactions
- Irbesartan (decreases Aliskiren by 50%)
- Atorvastatin (increases Aliskiren by 50%)
- Furosemide (Aliskaren decreases Furosemide efficacy by up to 50%)
- Ketoconazole (increases Aliskiren by 80%)
VI. Monitoring: Check response 2 weeks after starting medication
- Serum Creatinine
- Serum electrolytes (esp. Serum Potassium)
- Blood Pressure response
VII. Efficacy
- Similar effect on Blood Pressure as ACE Inhibitors and Angiotensin Receptor Blockers
- Unlike ACE Inhibitors and Angiotensin Receptor Blockers, no evidence that Direct renin inhibitors improve outcomes
- No significant benefit in Hypertension, Chronic Kidney Disease, Heart Failure
- Risk of hyptension, Hyperkalemia and increased Serum Creatinine
- (2016) Presc Lett 3(6):34
VIII. Indications
- Second line antihypertensive for those unable to use ACE Inhibitors or Angiotensin Receptor Blockers
IX. Dosing
- Start: 150 mg orally daily
- Maximum: 300 mg daily
XI. References
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| tekturna (on 3/22/2017 at Medicaid.Gov Survey of 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 | |
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 |
