Mahesh R, Perumal R Venkatesha, Pandi P V
Pharmacy Group, Birla Institute of Technology & Science, Pilani, India.
Pharmazie. 2005 Feb;60(2):83-96.
The development of serotonin 5-HT3 receptor antagonists dramatically improved the treatment of chemotherapy-induced nausea and vomiting. Ondansetron, a serotonin 5-HT3 receptor antagonist in combination with dexamethasone is widely used to treat chemotherapy-induced nausea and vomiting. This treatment regimen is effective against acute nausea and vomiting, but fails to control delayed nausea and vomiting. Metoclopramide along with other antiemetics are used to treat delayed nausea and vomiting. The high doses of metoclopramide needed may produce extra pyramidal side effects. The recent developments of 5-HT3 and dopamine D2 dual receptor antagonists have been found to exhibit a broad spectrum of activity against peripherally and centrally acting stimuli, but are not much effective against delayed emesis associated with chemotherapy. In various animal models, neurokinin NK1 receptor antagonists showed promising results against acute and delayed emesis, but the clinical trials revealed that triple therapy (NK1 receptor antagonist, 5-HT3 receptor antagonist and dexamethasone) is superior than standard therapy (5-HT3 receptor antagonist & dexamethasone) or NK1 receptor antagonist alone, in controlling acute as well as delayed nausea and vomiting. Ginger, which is used traditionally for controlling emesis induced by various stimuli, also showed good activity against chemotherapy-induced nausea and vomiting in animal models. Non-pharmacological methods such as acupressure and acustimulation are good adjunct methods in treating nausea and vomiting. Since many mediators are involved in emesis induced by chemotherapy, cocktail treatment is proven to be more efficacious than a single drug, but increases treatment costs. So there is a need of further research in this field to get economically useful methods for the treatment of acute and delayed chemotherapy-induced nausea and vomiting.
5-羟色胺5-HT3受体拮抗剂的研发显著改善了化疗引起的恶心和呕吐的治疗。昂丹司琼,一种5-羟色胺5-HT3受体拮抗剂,与地塞米松联合广泛用于治疗化疗引起的恶心和呕吐。这种治疗方案对急性恶心和呕吐有效,但无法控制延迟性恶心和呕吐。甲氧氯普胺与其他止吐药一起用于治疗延迟性恶心和呕吐。所需的高剂量甲氧氯普胺可能会产生锥体外系副作用。最近发现5-HT3和多巴胺D2双受体拮抗剂对周围和中枢作用的刺激具有广泛的活性,但对化疗相关的延迟性呕吐效果不佳。在各种动物模型中,神经激肽NK1受体拮抗剂对急性和延迟性呕吐显示出有希望的结果,但临床试验表明,三联疗法(NK1受体拮抗剂、5-HT3受体拮抗剂和地塞米松)在控制急性和延迟性恶心和呕吐方面优于标准疗法(5-HT3受体拮抗剂和地塞米松)或单独使用NK1受体拮抗剂。生姜传统上用于控制各种刺激引起的呕吐,在动物模型中对化疗引起的恶心和呕吐也显示出良好的活性。非药物方法如指压和穴位刺激是治疗恶心和呕吐的良好辅助方法。由于许多介质参与化疗引起的呕吐,联合治疗被证明比单一药物更有效,但会增加治疗成本。因此,该领域需要进一步研究,以获得经济有效的方法来治疗急性和延迟性化疗引起的恶心和呕吐。