Pharmacokinetics and pharmacodynamics of a nitric oxide-releasing derivative of enalapril in male conscious beagles (2005)
- Authors:
- Autor USP: NUCCI, GILBERTO DE - ICB
- Unidade: ICB
- Assunto: FARMACOLOGIA
- Language: Português
- Abstract: Objetivo: Enalapril, a nonsulphydryl angiotensin-converting enzyme (ACE) inhibitor, is a prodrug which has been used in the treatment of essential hypertension, congestive heart failure, myocardial infarction and diabetic nephropathy. The addition of an exogenous NO donor could improve the pharmacological activity of the drug. Then, this study investigates the pharmacokinetic and pharmacodynamic parameters of a nitric oxide-releasing derivative of enalapril (NCX 899) in beagles. Métodos e Resultados: The dogs received both nitro-enalapril (2.42 mg/kg, i.v., n=5) and enalapril maleate (2 mg/kg, i.v., n=5). The plasma concentrations of the analytes and their metabolites were quantified by reversed phase liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS). Additionally ECA inhibitory activity was tested by fluorimetry in dog serum. The nitro-enalapril group had values for the area under curve (AUC0-24h) of 23.15 ± 10.64, 201.28 ± 21.57 and 5313 ± 544.05 µgh/l for nitro-enalapril, enalapril and enalaprilat, respectively. The enalapril maleate group had values for AUC0-24h of 553.0 ± 156.1 and 4551.19 ± 965.2 µgh/l for enalapril and enalaprilat, respectively. The analysis did not show any significant difference of the enalaprilat values for AUC0-24h for both drugs. Nitro-enalapril was as effective as enalapril maleate in inhibiting the angiotensin-converting enzyme, as assessed ex-vivo in dog serum. Conclusões: Our results showed that NCX 899 could act inthe modulation of the arterial hypertension. This new compound presents an interesting therapeutic potential as showed in the ACE inhibitory activity in dog serum, indicating a therapeutic effect due to its potential nitric oxide-releasing properties.
- Imprenta:
- Publisher: Federação de Sociedades de Biologia Experimental
- Publisher place: Águas de Lindóia, São Paulo
- Date published: 2005
- Source:
- Título do periódico: Resumos
- Conference titles: Reunião Anual da Federação de Sociedades de Biologia Experimental, FeSBE
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ABNT
OKUYAMA, C. E. et al. Pharmacokinetics and pharmacodynamics of a nitric oxide-releasing derivative of enalapril in male conscious beagles. 2005, Anais.. Águas de Lindóia, São Paulo: Federação de Sociedades de Biologia Experimental, 2005. . Acesso em: 25 abr. 2024. -
APA
Okuyama, C. E., Mendes, G. D., Rezende, V. M., Lagos, R. M., Barrientos-Astigarraga, R. E., & De Nucci, G. (2005). Pharmacokinetics and pharmacodynamics of a nitric oxide-releasing derivative of enalapril in male conscious beagles. In Resumos. Águas de Lindóia, São Paulo: Federação de Sociedades de Biologia Experimental. -
NLM
Okuyama CE, Mendes GD, Rezende VM, Lagos RM, Barrientos-Astigarraga RE, De Nucci G. Pharmacokinetics and pharmacodynamics of a nitric oxide-releasing derivative of enalapril in male conscious beagles. Resumos. 2005 ;[citado 2024 abr. 25 ] -
Vancouver
Okuyama CE, Mendes GD, Rezende VM, Lagos RM, Barrientos-Astigarraga RE, De Nucci G. Pharmacokinetics and pharmacodynamics of a nitric oxide-releasing derivative of enalapril in male conscious beagles. Resumos. 2005 ;[citado 2024 abr. 25 ] - Role of adenosine A(3) receptors on the bradycardia induced by swin training
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