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Publication
Farmacocinética do ibuprofeno
| Name: | Description: | Size: | Format: | |
|---|---|---|---|---|
| PPG_19606 | 1.86 MB | Adobe PDF |
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Advisor(s)
Abstract(s)
O ibuprofeno é um anti-inflamatório não esteroide (AINE) da família dos derivados
arilpropiónicos usado no tratamento sintomático de artrite reumatoide, osteoartrite,
tendinite e bursite aguda principalmente em pacientes com intolerância gastrointestinal
a outros AINE.
A intensidade dos processos de absorção, distribuição, metabolização e excreção varia
com o tempo; por esta razão, a quantidade de fármaco no organismo, também varia ao
longo do tempo. O ibuprofeno apresenta um tempo de semivida relativamente curto e
que é diferente para os seus dois isómeros e uma cinética de absorção linear. É
rapidamente e extensamente absorvido no trato gastrointestinal apresentando uma
percentagem de ligação às proteínas plasmáticas superior a 98% com um volume de
distribuição até 0,2 L/kg. Acumula-se em quantidades apreciáveis nos tecidos
inflamados onde haja necessidade de atividade anti-inflamatória/analgésica; e é
excretado em 70 a 80% com a urina e fezes.
Os estudos farmacocinéticos da variação da concentração de um fármaco e dos seus
metabolitos ao longo do tempo e local permitem construir modelos apropriados para
interpretar a cinética de um fármaco bem como a sua eficácia e toxicidade.
No caso específico do ibuprofeno esses estudos permitiram concluir que a
farmacocinética do ibuprofeno é bem descrita por um modelo bicompartimental que
considere a conversão do R-ibuprofeno em S-ibuprofeno e um compartimento efeito
para ter em conta o desfasamento entre a concentração plasmática no sangue e a
resposta.
Nos estudos mais recentes, a farmacocinética do ibuprofeno tem vindo a ser modelada
usando modelos de base fisiológica que permitem quantificar a concentração da
molécula em órgãos alvo específicos.
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that belongs to the family of arylpropionic derivatives used in the symptomatic treatment of rheumatoid arthritis, osteoarthritis, acute tendonitis and bursitis in patients with gastrointestinal intolerance to other NSAIDs. The intensity of the absorption, distribution, metabolism and excretion varies with time; for this reason, the amount of drug molecule in the body also varies over time. Ibuprofen has a relatively short half-life and that is different for the two isomers and a linear absorption kinetics. It is rapidly and extensively absorbed in the gastrointestinal tract and 98% of the molecules bind to serum proteins. It has a distribution volume up to 0.2 L / kg and accumulates in significant quantities in the inflamed tissues where there is need for anti-inflammatory/analgesic activity; it is excreted in 70 to 80% with urine and feces. The analysis of the variation of the concentration of a drug and its metabolites over time and local allow building appropriate models to interpret the kinetics of a drug its efficacy and toxicity. In the specific case of ibuprofen these studies showed that the pharmacokinetics of ibuprofen is well described by a two-compartment model that considers the conversion of R-ibuprofen into S-ibuprofen and includes an effect compartment to take into account the time lag between plasma concentration in the blood and the response. In more recent studies, the pharmacokinetics of ibuprofen has been modeled using physiologically based models, these allow to quantify the concentration of the molecule in specific target organs.
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that belongs to the family of arylpropionic derivatives used in the symptomatic treatment of rheumatoid arthritis, osteoarthritis, acute tendonitis and bursitis in patients with gastrointestinal intolerance to other NSAIDs. The intensity of the absorption, distribution, metabolism and excretion varies with time; for this reason, the amount of drug molecule in the body also varies over time. Ibuprofen has a relatively short half-life and that is different for the two isomers and a linear absorption kinetics. It is rapidly and extensively absorbed in the gastrointestinal tract and 98% of the molecules bind to serum proteins. It has a distribution volume up to 0.2 L / kg and accumulates in significant quantities in the inflamed tissues where there is need for anti-inflammatory/analgesic activity; it is excreted in 70 to 80% with urine and feces. The analysis of the variation of the concentration of a drug and its metabolites over time and local allow building appropriate models to interpret the kinetics of a drug its efficacy and toxicity. In the specific case of ibuprofen these studies showed that the pharmacokinetics of ibuprofen is well described by a two-compartment model that considers the conversion of R-ibuprofen into S-ibuprofen and includes an effect compartment to take into account the time lag between plasma concentration in the blood and the response. In more recent studies, the pharmacokinetics of ibuprofen has been modeled using physiologically based models, these allow to quantify the concentration of the molecule in specific target organs.
Description
Projeto de Pós-Graduação/Dissertação apresentado à Universidade Fernando Pessoa como parte dos requisitos para obtenção do grau de Mestre em Ciências Farmacêuticas
Keywords
Ibuprofeno Farmacocinética Modelos farmacocinéticos compartimentais Modelos farmacocinéticos de base fisiológica Ibuprofen Pharmacokinetics Compartmental models Physiologically Based Pharmacokinetic models