ABSTRACT
A partir da síntese da serotonina, em 1951, iniciou-se a investigaçäo farmacológica dos receptores serotoninérgicos. A estimulaçäo dos mais variados tipos de receptores gera múltiplas respostas funcionais verificadas em nível de sistema nervoso central, terminaçöes nervosas serotoninérgicos em nível metabólico e fisiopatológico
Subject(s)
Humans , Animals , Rats , In Vitro Techniques , Receptors, Serotonin/drug effects , Receptors, Serotonin/metabolism , Receptors, Serotonin/physiology , Serotonin/metabolism , Enterochromaffin Cells/metabolism , Selective Serotonin Reuptake Inhibitors/pharmacology , Raphe Nuclei , Raphe Nuclei/metabolism , Serotonin Antagonists/pharmacokinetics , Serotonin Antagonists/pharmacology , Serotonin Receptor Agonists/pharmacology , Serotonin/pharmacology , VasoconstrictionABSTRACT
The antiemetic effect of tropisetron was studied in 97 cancer patients (67 men, 30 women) receiving cisplatin in doses of 75 mg/m² or higher. On 279 chemotherapy cycles studied (max 6 per patient) 5 mg of tropisetron was admonistered once a day i.v. on day 1 and p.o. on day 2 to 6. Efficacy preventing vomiting and nausea was measured in 24 hour period as: complete control 0 episodes, major control 1 to 2 episodes, minor control 3 to 4 episodes and no control 5 or more episodes. Satisfactory vomiting control (complete and major) was 69 percent, 63 percent, 82 percent,88 percent, 96 percent and 96 percent in days 1 to 6 of cycle 1. Satisfactory nausea control (complete and major) for the same day was 70, 66, 72, 85 92 and 97 percent. Similar data was obtained for the subsequeny cycles. Complete vomiting control was obtained in 47, 35, 56, 72, 81 and 84 percent and for nausea in 42, 39, 48, 64, 81 and 87 percent. 19 patients presented adverse effects (19,6 percent). Only 2 headache episodes had a definitive relation with antiemetic drug. 12 patients discontinued the medication; 6 due to drug inefficacy, 2 to illness unrelated to the drug, 1 to lack of collaboration, and 3 due to other reasons. We conclude that tropisetron allows satisfactory control of acute and delayed vomiting in a high percentage of patients treated with high doses of cisplatin. The drug does not have significant secondary effects. Tropisetron administration in only 1 daily dose implies an evident advantage and a treatment cost reduction