Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?
The Korean Journal of Pain
;
: 73-79, 2018.
Artigo
em Inglês
| WPRIM
| ID: wpr-742182
ABSTRACT
All drugs have both favorable therapeutic and untoward adverse effects. Conventional opioid analgesics possess both analgesia and adverse reactions, such as nausea, vomiting, and respiratory depression. The opioid ligand binds to µ opioid receptor and non-selectively activates two intracellular signaling pathways the G protein pathway induce analgesia, while the β-arrestin pathway is responsible for the opioid-related adverse reactions. An ideal opioid should activate the G protein pathway while deactivating the β-arrestin pathway. Oliceridine (TRV130) has a novel characteristic mechanism on the action of the µ receptor G protein pathway selective (µ-GPS) modulation. Even though adverse reactions (ADRs) are significantly attenuated, while the analgesic effect is augmented, the some residual ADRs persist. Consequently, a G protein biased µ opioid ligand, oliceridine, improves the therapeutic index owing to increased analgesia with decreased adverse events. This review article provides a brief history, mechanism of action, pharmacokinetics, pharmacodynamics, and ADRs of oliceridine.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Insuficiência Respiratória
/
Vômito
/
Farmacocinética
/
Viés
/
Camundongos Knockout
/
Receptores Opioides
/
Receptores Opioides mu
/
Proteínas de Ligação ao GTP
/
Peptídeos e Proteínas de Sinalização Intracelular
/
Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos
Limite:
Animais
Idioma:
Inglês
Revista:
The Korean Journal of Pain
Ano de publicação:
2018
Tipo de documento:
Artigo
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