A influência da piperina na biodisponibilidade de fármacos: uma abordagem molecular

Oliveira, Rogério de; Filho, Edilson Beserra de Alencar; Vasconcellos, Mário L. A. A.

doi:10.1590/s0100-40422014000100013

Cited by 3 publications

(2 citation statements)

References 18 publications

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“…However, its infamous drug-drug and drug-food interaction profile, resulting from its significant protein binding and large interindividual variability, presents a challenge in dosing regimen and safety. In addition, piperine has been shown to interact with several drugs at different levels, 27,33,39,44,45 but its effect on the pharmacokinetics and pharmacodynamics of warfarin has not been investigated yet.…”

Section: Discussionmentioning

confidence: 99%

<p>Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats</p>

Zayed¹,

Babaresh²,

Darweesh³

et al. 2020

JEP

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Introduction: Piperine, the bioactive compound of black pepper, and warfarin are metabolized by cytochrome P450 enzymes and are both highly plasma protein-bound compounds. In this study, we evaluated the effect of co-administered piperine on the pharmacokinetics and anticoagulation of warfarin in rats. Methods: We studied four Sprague-Dawley rat groups: a negative control group receiving only oral warfarin, a test group receiving warfarin plus piperine, a positive control group receiving warfarin plus sulfaphenazole (CYP2C inhibitor), and another positive control group receiving warfarin plus ketoconazole (CYP3A inhibitor). We also analyzed plasma concentrations of warfarin and its major metabolite, 7-hydoxywarfarin. Blood clotting time, calculated as international normalized ratio (INR), was also measured. Results: Our results showed that although co-administration of piperine produced a nonsignificant decrease in warfarin concentrations, it resulted in significantly lower 7-hydroxywarfarin metabolite concentrations. Piperine significantly decreased, by sixfold, AUC 0-∞ , by eightfold, C max , but significantly increased, by fivefold, CL/F and, by sixfold, Vd/F of 7-hydroxywarfarin. The INR values were consistent with the decrease in warfarin concentration in the presence of piperine and showed a significant decrease at 24 h after warfarin dose. Conclusion:We conclude that piperine could be a potent inhibitor of cytochrome P450 metabolism of warfarin in vivo and, contrary to the expectation, may reduce the plasma concentration and anticoagulation of warfarin. This interaction could have a clinical significance and should be investigated in patients.

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Section: Discussionmentioning

confidence: 99%

<p>Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats</p>

Zayed¹,

Babaresh²,

Darweesh³

et al. 2020

JEP

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“…1 Ele e outros compostos relacionados podem ser determinados e caracterizados por diversos métodos de análises. [7][8][9][10][11][12][13][14]…”

Section: Aspectos Geraisunclassified

Avanços Químicos No Planejamento E Desenvolvimento De Derivados Do Paracetamol

et al. 2018

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CHEMICAL ADVANCES ON DESIGN AND DEVELOPMENT OF PARACETAMOL DERIVATIVES. Acetaminophen or paracetamol is a widely used analgesic and antipyretic drug and appears to be safe if used at normal therapeutic doses, but in large doses produce liver and / or kidney damage in humans and experimental animals. Prostaglandin endoperoxide synthase (PGES) and cytochrome P-450 are the key enzymes in humans as they are responsible for the analgesic and toxicity effects of paracetamol, respectively. At present, the development of new derivatives still has few impacts on clinical applications of safe compounds. Thus, in this work are discussed, a series of approaches on the design and development of acetaminophen derivatives. Some efforts were realized in our own research group.

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Pain Management in Dogs With Osteoarthrosis: A Case Report

Furtado

Sobral

2022

Environ. Smoke

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A doença articular degenerativa (DAD) ou osteoartrose (OA) é uma enfermidade comum entre os cães e caracteriza-se por ser progressiva, minimamente inflamatória e com alterações neoproliferativas não neoplásicas, que proporciona disfunção considerável em todas as estruturas articulares com sua posterior falência. Os animais afetados apresentam claudicação, relutância em se movimentar após repouso e dificuldade em realizar certas atividades, sendo estes os sinais comuns mais precoces. A decorrência dessas doenças pode ser agravada pela: obesidade, predisposição genética, idade ou traumatismos. Seu diagnóstico é feito com base na anamnese, histórico do paciente, exame físico e radiográfico. Os tratamentos de OA pode ser cirúrgico ou conservativo dependendo do caso, e tem como objetivo o alívio do desconforto e retardo do desenvolvimento das alterações degenerativas e é impossível reverter às alterações patológicas já existentes.

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A influência da piperina na biodisponibilidade de fármacos: uma abordagem molecular

Cited by 3 publications

References 18 publications

<p>Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats</p>

<p>Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats</p>

Avanços Químicos No Planejamento E Desenvolvimento De Derivados Do Paracetamol

Pain Management in Dogs With Osteoarthrosis: A Case Report

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