Last update April 28, 2024

Bis(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide fumarate (2:1)

Likely Compatibility

Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.

Aliskiren is a direct renin inhibitor used to control hypertension. Oral administration once daily.

At the time of the last update, we found no published data on its excretion in breast milk.

Its pharmacokinetic data (large volume of distribution (Novartis 2015, EMA 2012) and high molecular weight) make it unlikely to pass into breast milk in clinically significant quantities.

Its low oral bioavailability means that there is little or no passage into infant plasma from ingested breast milk, except in premature infants and in the immediate neonatal period, where there may be greater intestinal absorption.

Until more data on this drug in relation to breastfeeding are known, safer alternatives are preferable, especially in the neonatal period and in case of prematurity.

Alternatives

  • Captopril (Safe substance and/or breastfeeding is the best option.)
  • Enalapril (Safe substance and/or breastfeeding is the best option.)
  • Methyldopa (Safe substance and/or breastfeeding is the best option.)
  • Metoprolol (Safe substance and/or breastfeeding is the best option.)

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Bis(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide fumarate (2:1) is Aliskiren Fumarate in Chemical name.

Is written in other languages:

Groups

Bis(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide fumarate (2:1) belongs to these groups or families:

Tradenames

Main tradenames from several countries containing Bis(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide fumarate (2:1) in its composition:

  • Rasilez
  • Rasilez (Расилез)
  • Rasilez (锐思力)
  • Rasilez HCT™. Contains other elements than Bis(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide fumarate (2:1) in its composition
  • Rasilles
  • Rasilles HCT™. Contains other elements than Bis(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide fumarate (2:1) in its composition
  • Riprazo
  • Tekturna
  • Valturna

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 2 - 2.5 %
Molecular weight 1.220 daltons
Protein Binding 47 - 51 %
VD 1.93 l/Kg
pKa 14.56 -
Tmax 1 - 5 hours
34 - 41 hours

References

  1. Novartis. Aliskiren. Drug Summary. 2015 Full text (in our servers)
  2. EMEA. Aliskireno. Ficha técnica. 2012 Full text (in our servers)
  3. Waldmeier F, Glaenzel U, Wirz B, Oberer L, Schmid D, Seiberling M, Valencia J, Riviere GJ, End P, Vaidyanathan S. Absorption, distribution, metabolism, and elimination of the direct renin inhibitor aliskiren in healthy volunteers. Drug Metab Dispos. 2007 Abstract
  4. Vaidyanathan S, Jermany J, Yeh C, Bizot MN, Camisasca R. Aliskiren, a novel orally effective renin inhibitor, exhibits similar pharmacokinetics and pharmacodynamics in Japanese and Caucasian subjects. Br J Clin Pharmacol. 2006 Abstract Full text (link to original source)

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