Pharmacodynamic interaction between intravenous nitroglycerin and oral sacubitril/valsartan (LCZ696) in healthy subjects.

Purpose: Sacubitril/valsartan (LCZ696) and nitroglycerin share the second messenger cGMP and lower blood pressure. Given the potential for co-administration of both drugs in patients with heart failure, this study was designed to investigate the potential for a pharmacodynamic drug interaction affec...

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Publicado en:European Journal of Clinical Pharmacology Vol. 74; no. 9; pp. 1121 - 1131
Autores principales: Schuehly, Uwe, Ayalasomayajula, Surya, Buchbjerg, Jeppe, Pal, Parasar, Golor, Georg, Prescott, Margaret F., Sunkara, Gangadhar, Hinder, Markus, Langenickel, Thomas H.
Formato: research tables/charts randomized controlled trial Journal Article
Publicado: Springer Nature Sep2018
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Sep2018
      vid: 74
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      pub: Springer Nature
      place: New York, New York
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        10.1007/s00228-018-2509-2
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        atl: Pharmacodynamic interaction between intravenous nitroglycerin and oral sacubitril/valsartan (LCZ696) in healthy subjects.
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          Schuehly, Uwe
          Ayalasomayajula, Surya
          Buchbjerg, Jeppe
          Pal, Parasar
          Golor, Georg
          Prescott, Margaret F.
          Sunkara, Gangadhar
          Hinder, Markus
          Langenickel, Thomas H.
        affil: Translational Medicine, Novartis Institutes for Biomedical Research, Basel, Switzerland
      sug:
        subj:
          Drug Interactions
          Nitroglycerin Administration and Dosage
          Valsartan Administration and Dosage
          Valsartan Pharmacodynamics
          Nitroglycerin Pharmacodynamics
          Heart Failure Drug Therapy
          Blood Pressure Drug Effects
          Human
          Randomized Controlled Trials
          Double-Blind Studies
          Crossover Design
          Blood Pressure Determination
          Heart Rate
          Valsartan Pharmacokinetics
          Systolic Pressure Drug Effects
          Diastolic Pressure Drug Effects
          Confidence Intervals
          Nucleotides Blood
          Administration, Intravenous
          Administration, Oral
          Drug Combinations
      ab: Purpose: Sacubitril/valsartan (LCZ696) and nitroglycerin share the second messenger cGMP and lower blood pressure. Given the potential for co-administration of both drugs in patients with heart failure, this study was designed to investigate the potential for a pharmacodynamic drug interaction affecting blood pressure.Methods: In this double-blind, placebo-controlled, randomised, crossover study, 40 healthy subjects received sacubitril/valsartan 200 mg bid (97/103 mg bid) or placebo for 5 days. Two hours after the morning dose of sacubitril/valsartan or placebo on day 5, subjects received intravenous nitroglycerin infusion at increasing doses up to 40 μg/min or placebo. Serial measurements of blood pressure (BP), heart rate, biomarkers and sacubitril/valsartan pharmacokinetics were conducted.Results: Administration of nitroglycerin alone led to a dose- and time-dependent decrease in supine systolic BP (SBP) and diastolic BP (DBP) which was similar when nitroglycerin was co-administered with sacubitril/valsartan. At the highest dose of nitroglycerin, the mean (95% CI) decrease from baseline of SBP/DBP was 19.54 (− 21.99, − 17.09)/12.38 (− 13.85, − 10.92) mmHg for nitroglycerin alone compared to 22.63 (− 25.06, − 20.21)/12.94 (− 14.38, − 11.49) mmHg when co-administered with sacubitril/valsartan. Co-administration of sacubitril/valsartan and nitroglycerin did not result in further plasma cGMP increase compared to sacubitril/valsartan alone. The co-administration of nitroglycerin and sacubitril/valsartan was safe and well tolerated and did not impact the pharmacokinetics of sacubitril/valsartan.Conclusions: The results from this study demonstrate no pharmacodynamic drug interaction between nitroglycerin and sacubitril/valsartan in healthy subjects, suggesting that no change of dose selection and escalation recommendations or clinical monitoring during nitroglycerin administration is required.
      pubtype: Academic Journal
      doctype:
        research
        tables/charts
        randomized controlled trial
        Journal Article
      ougenre: Article
    language: English
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