RESUMO
Omacetaxine mepesuccinate is a drug approved in 2014 by FDA for the use in CML therapy in patients resistant to at least two thymidine kinase inhibitors (TKIs). It possesses unique mechanism of anticancer activity that is principally different from mechanism of activity of TKIs. Omacetaxine mepesuccinate inhibits protein translation through prevention of the initial elongation step of protein synthesis and its use benefits CML patients possessing the BCR-ABL oncogene. Because of the superior activity of Omacetaxine in patients who became resistant to therapy with TKIs, FDA decided on the accelerated approval of this drug taking its consideration not only its activity as such but also a favorable benefit-to-risk profile in patients included into clinical studies.
Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Mepesuccinato de Omacetaxina/uso terapêutico , Leucemia Mielogênica Crônica BCR-ABL Positiva/tratamento farmacológico , Inibidores da Síntese de Proteínas/uso terapêutico , Resistencia a Medicamentos Antineoplásicos , Humanos , Inibidores de Proteínas QuinasesRESUMO
WHAT IS KNOWN AND OBJECTIVE: Morphine is used routinely in clinical practice to manage moderate to severe pain, whereas levomepromazine is commonly used at low doses to manage intractable nausea and vomiting. While it has been reported that an injection combination of morphine sulphate (0·5 mg/mL) and levomepromazine (0·1 mg/mL) was physically compatible, data on the chemical stability of combinations of these drugs has not been reported. Thus, a method was required for the assessment of the stability of morphine sulphate/levomepromazine hydrochloride combinations. METHODS: A high-performance liquid chromatography (HPLC) method was developed to assess the stability of the combinations. The injections were stored at 4 °C in the dark at room temperature under natural light and at 37 °C under artificial lighting. RESULTS AND DISCUSSION: Morphine sulphate was stable under all storage conditions, but the degree of degradation of levomepromazine hydrochloride increased as the storage temperature increased. The disappearance of levomepromazine hydrochloride was correlated with the appearance of a sulphoxide degradant. WHAT IS NEW CONCLUSION: The injection combinations of morphine sulphate and levomepromazine hydrochloride were shown in the current study to have a limited storage life with respect to their levomepromazine hydrochloride content.
Assuntos
Analgésicos não Narcóticos/química , Analgésicos Opioides/química , Metotrimeprazina/química , Morfina/química , Analgésicos não Narcóticos/administração & dosagem , Analgésicos Opioides/administração & dosagem , Cromatografia Líquida de Alta Pressão , Combinação de Medicamentos , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Humanos , Injeções , Luz , Metotrimeprazina/administração & dosagem , Morfina/administração & dosagem , Cuidados Paliativos/métodos , Sulfóxidos/química , TemperaturaRESUMO
Seeds of Monodora myristica and M. tenuifolia were extracted with hexane and the extracts were subjected to column chromatography, LC-MS and NMR analysis. In addition to masses of previously isolated compounds, other masses corresponding to unidentified compounds from the plants were detected. Using 2 D NMR techniques, one of the fractions from M. tenuifolia was characterised as a novel 13-(2-butylcyclopropyl)-6,9-dodecadienoic acid. However, none of the compounds detected in LC-MS corresponded to the ones previously identified by GC-MS.