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1.
Artigo em Inglês | MEDLINE | ID: mdl-29867775

RESUMO

Thyroid cancer metastasizes in 4% of cases. Approximately two-thirds of these patients are refractory to radioactive iodine-131 (RAI) therapy and have a poor 10-year survival prognosis. Treatment with tyrosine kinase inhibitors (TKIs) may be administered in selected RAI-refractory patients. However, these agents are often associated with adverse events, including vomiting. We report the case of a patient affected by RAI-refractory thyroid cancer with lung and intracranial metastases undergoing treatment with the antiangiogenic TKI lenvatinib, and with teriparatide replacement therapy for postsurgical hypoparathyroidism. Due to lenvatinib-related vomiting, which did not respond to therapy, conventional oral calcium supplementation failed to maintain normal serum calcium levels and the patient had repeated episodes of hypocalcemia. Subcutaneous teriparatide injections restored serum calcium levels, and thus lenvatinib therapy could be continued. This experience indicates that hormone replacement with teriparatide is a feasible option for cancer patients affected by hypoparathyroidism not treatable with oral calcium supplementation.

2.
Eur J Med Chem ; 92: 672-81, 2015 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-25618014

RESUMO

This paper reports the synthesis and cardiac activity of new ß-blockers derived from (Z/E)-indeno[1,2-c]pyrazol-4(1H)-one oximes (5a,b). The latter compounds were allowed to react with epichlorohydrin, followed by reacting the oxiranyl derivatives formed (6a,b) with some aliphatic amines to give the target compounds (Z/E)-1-phenyl-1H-indeno[1,2-c]pyrazol-4-one O-((2-hydroxy-3-(substituted amino)propyl)oxime (7a-c) and (Z/E)-1-methyl-1H-indeno[1,2-c]pyrazol-4-one O-((2-hydroxy-3-(substituted amino)propyl)oxime (8a-c). These final products 7a-c and 8a-c were evaluated for their ability to modulate the cardiac performance of a prototype mammalian heart. The results showed that, out of these molecules tested, 7b elicits a more potent depressant effect on contractility and relaxation, and competitively antagonizes ß1-adrenergic receptors.


Assuntos
Antagonistas de Receptores Adrenérgicos beta 1/síntese química , Antagonistas de Receptores Adrenérgicos beta 1/farmacologia , Ésteres/farmacologia , Oximas/síntese química , Oximas/farmacologia , Pirazóis/farmacologia , Receptores Adrenérgicos beta 1/metabolismo , Antagonistas de Receptores Adrenérgicos beta 1/química , Animais , Relação Dose-Resposta a Droga , Ésteres/síntese química , Ésteres/química , Masculino , Estrutura Molecular , Oximas/química , Pirazóis/síntese química , Pirazóis/química , Ratos , Ratos Wistar , Relação Estrutura-Atividade
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