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Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Tropisetron is a highly potent and selective 5-HT3 antagonist used as an antiemetic in cancer chemotherapy (Lee et al. 1993; Simpson et al. 2000). It is extensively metabolized by hydroxylation of the indole ring in the 5-, 6-, and 7-positions followed by conjugation in humans (Figure 3.40) (Fischer et al. 1992a; Kutz 1993). The major metabolic route is 6-hydrox-ylation, accounting for 45% of the urinary excretion, while 12% of the dose is excreted as 5-OH-tropisetron in urine. Oxidative N-demethylation and N-oxygenation at the tropinyl nitrogen also occur but to a minor extent, with trace levels of the corresponding metabolites detected (Fischer et al. 1992a).
Development of palliative medicine in the United Kingdom and Ireland
Published in Eduardo Bruera, Irene Higginson, Charles F von Gunten, Tatsuya Morita, Textbook of Palliative Medicine and Supportive Care, 2015
The effect of the setrons on the serotonin-mediated emetic pathways may lend itself to the management of chronic nausea. Ondansetron, a selective 5-HT3 antagonist, has been used in palliative care setting in patients not responding to conventional treatments. In 9 of 16 patients with advanced human immunodeficiency disease, the treatment was effective and well tolerated [27]. However, in a controlled study, the efficacy of ondansetron at relatively large doses was similar to that reported with placebo [18]. Tropisetron-containing combinations or tropisetron as a single agent are much more effective in the control of emesis in patients with advanced cancer than the conventional antiemetic combination of chlorpromazine plus dexamethasone 28*. Not being antidopaminergic, setrons are potentially useful when the risk of extrapyramidal reactions is high, such as in children or elderly people who have neurological diseases with an extrapyramidal component. They appear to have no effect on motion sickness [2].
Clinical pharmacology of opioids: adverse effects of opioids
Published in Nigel Sykes, Michael I Bennett, Chun-Su Yuan, Clinical Pain Management, 2008
Some authors have reported transdermal hyoscine hydrobromate (scopolamine)163 and ondansetron164 to be effective in this setting. In a randomized prospective trial, tropisetron, as a single agent or in combination, was more effective than chlorpromazine plus dexamethasone in the management of nausea and vomiting in advanced cancer patients on opioids.165 Also, haloperidol has been found to be effective in postoperative nausea and vomiting during epidural analgesia in a randomized controlled trial (RCT).166 On the other hand, another RCT has found no difference in the antiemetic efficacy of ondansentron, metoclopramide, and placebo in opioid-induced nausea and emesis in cancer patients,167 and there is a suggestion that morphine might reduce the antiemetic efficacy of serotonin antagonists in the setting of chemotherapy-induced nausea.168 Recently, olanzapine has been advocated for refractory nausea and vomiting.169
Comparison of effectiveness, cost and safety between moderate sedation and deep sedation under esophagogastroduodenoscopy in Chinese population: a quasi-experimental study
Published in Scandinavian Journal of Gastroenterology, 2022
Feng Hu, Long Zou, Hongxia Chang, Lin Tian, Fanrong Liu, Ya Lan, Fangxin Zhang, Xiao Liu
Before the procedure, patients were fasting and entered the endoscopy room for routine preparation of painless EGD. The venous access to the right upper limb was established, and electrocardiograph, respiration, HR, blood pressure (left upper limb), pulse oxygen saturation, and mental status were monitored. All patients were given tropisetron (2 mg) to prevent vomiting before sedation. During the procedure, the moderate sedation group was administered intravenously by an endoscopist specially trained in sedation in the absence of an anesthesiologist. The deep sedation was performed by a trained anesthesiologist. Up to the prescribed sedation depth, EGD was performed. Standard EGD was performed by two experienced endoscopists. The sedation level was assessed every 3 min to help adjust the titration infusion rate. The mandible was raised or mask oxygen inhalation was used when the respiration rate was less than 10 times/min and the SaO2 was less than 90%. Atropine was used when the HR was below 55 beats/min, and dopamine (1–2 mg) was intravenously injected when blood pressure was reduced by 30%. After the procedure, patients were admitted to the recovery room for observation and left the hospital until reaching the standard of discharge that was evaluated by the physician.