5-HT3 Receptor Antagonists in Antiemetic Therapy

2003 ◽  
pp. 22-32 ◽  
Author(s):  
J. Donnerer ◽  
E. Beubler

2016 ◽  
Vol 4 (1) ◽  
pp. 46-51 ◽  
Author(s):  
Florence Van Ryckeghem

AbstractChemotherapy-induced nausea and vomiting (CINV) remains one of the most disturbing side effects of cancer treatment. Research in antiemetic therapy has progressed gradually since the early eighties, and the development of antiemetic agents continues. This review focuses on the current management of CINV based on the most recent guidelines, and adherence to the latter is examined more carefully. Setrons (5HT3 receptor antagonists), corticosteroids, and NK-1 receptor antagonists are the cornerstones of antiemetic therapy. Corticosteroids are one of the oldest agents in the prevention of CINV. They are highly effective, increase the effect of other antiemetic agents, and are cost-effective. The latest developed 5HT3 receptor antagonist palonosetron led to an update of the guidelines of CINV. Other types include benzodiazepines, cannabinoids, and olanzapine. Various factors contribute to the overall risk of developing CINV, such as patient characteristics, emetogenic potency of the chemotherapeutic agents, and correct prevention of CINV. Current guidelines determine which is the right preventive regimen for each cancer patient at risk for experiencing CINV. Adherence to these guidelines and implementation in daily practice seem to be below the optimal level. In Belgium, authorities use the guidelines as a base for reimbursement and this has increased the level of implementation.



1990 ◽  
Vol 68 (2) ◽  
pp. 314-324 ◽  
Author(s):  
G. J. Sanger

Three major areas of medicine are identified in which there is a need for new antiemetic drugs. These are the nausea and vomiting arising from gastrointestinal motility disturbances (functional dyspepsia, diabetic neuropathy, classical migraine), the sickness evoked by abnormal motion, and the severe emesis experienced by cancer patients as a result of certain cytotoxic therapies. For gastrointestinal-related nausea, selective stimulants of gut motility are suggested to form the basis for a new type of antiemetic therapy. In motion sickness, there has been progress in the understanding of the illness, but little advance in the development of new drugs that selectively prevent this type of sickness. In cancer chemo- and radio-therapy, the discovery that selective 5-HT3 (5-HT, 5-hydroxytryptamine) receptor antagonists can prevent severe cytotoxic-evoked emesis now promises to radically change the type of antiemetic therapy given to these patients. This type of antiemetic compound and the pharmacology of the new 5-HT3 receptor antagonists are, therefore, discussed in detail.Key words: emesis, gastric motility, 5-hydroxytryptamine, 5-HT3 receptors.





2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Junichi Nishimura ◽  
Akiko Hasegawa ◽  
Toshihiro Kudo ◽  
Tomoyuki Otsuka ◽  
Masayoshi Yasui ◽  
...  

AbstractOlanzapine has exhibited efficacy as an antiemetic agent when used with 5-HT3 receptor antagonists, dexamethasone, and NK1 receptor antagonists for patients receiving highly emetogenic chemotherapy. In addition, several studies have reported the efficacy or safety of olanzapine in patients receiving moderately emetogenic chemotherapy, including carboplatin, irinotecan, and oxaliplatin. However, no reports of olanzapine use have focused on patients receiving oxaliplatin-based chemotherapy. Therefore, we analyzed the safety of antiemetic therapy using olanzapine, palonosetron, aprepitant, and dexamethasone in colorectal cancer patients undergoing oxaliplatin-based chemotherapy. This study was a prospective phase II single-institution study of 40 patients (median age 60 years, 23 patients were male). The primary endpoint was the incidence of adverse events, and the exploratory endpoints were the rate of chemotherapy-induced nausea and vomiting. Almost all patients (90%) had a performance status of 0. All patients received the scheduled antiemetic therapy. The most common adverse event was somnolence (n = 7 patients, 17.5%). All adverse events were grade 1. Thirty-six patients were included in the exploratory analysis of efficacy. No patients experienced vomiting during the first 120 h after chemotherapy, and complete response and complete control were both 86.1%. The rate of total control was 55.6% during the same time period. Olanzapine use with 5-HT3 receptor antagonists, dexamethasone, and NK1 receptor antagonists was safe for colorectal cancer patients receiving oxaliplatin-based chemotherapy.



1996 ◽  
Vol 26 (9) ◽  
pp. 1092-1097 ◽  
Author(s):  
F. E. R. SIMONS ◽  
T. G. FRASER ◽  
J. D. REGGIN ◽  
K. J. SIMONS


2011 ◽  
Vol 44 (17) ◽  
pp. 53
Author(s):  
MIRIAM E. TUCKER


VASA ◽  
2016 ◽  
Vol 45 (3) ◽  
pp. 201-212 ◽  
Author(s):  
Birgit Linnemann ◽  
Matthias Erbe

Abstract. The primary goal of therapy is to reduce the frequency and intensity of Raynaud’s attacks and to minimize the related morbidity rather than to cure the underlying condition. Treatment strategies depend on whether Raynaud’s phenomenon (RP) is primary or secondary. All patients should be instructed about general measures to maintain body warmth and to avoid triggers of RP attacks. Pharmacologic intervention can be useful for patients with severe and frequent RP episodes that impair the patient’s quality of life. Calcium channel blockers are currently the most prescribed and studied medications for this purpose. There has been limited evidence for the efficacy of alpha-1-adrenergic receptor antagonists, angiotensin receptor blockers, topical nitrates or fluoxetine to treat RP. The intravenously administered prostacyclin analogue iloprost can reduce the frequency and severity of RP attacks and is considered a second-line therapy in patients with markedly impaired quality of life, critical digital ischaemia and skin ulcers who are at risk for substantial tissue loss and amputation. Phosphodiesterase inhibitors (e.g., sildenafil) can also improve RP symptoms and ulcer healing whereas endothelin-1 receptor antagonists (e.g., bosentan) are mainly considered treatment options in secondary prevention for patients with digital skin ulcers related to systemic sclerosis. However, their use in clinical practice has been limited by their high cost. Antiplatelet therapy with low-dose aspirin is recommended for all patients who suffer from secondary RP due to ischaemia caused by structural vessel damage. Anticoagulant therapy can be considered during the acute phase of digital ischaemia in patients with suspected vascular occlusive disease attributed to the occurrence of new thromboses. In patients with critical digital ischaemia, consideration should be given to hospitalisation, optimisation of medical treatment in accordance with the underlying disease and evaluation for a secondary, possibly reversible process that is causing or aggravating the clinical symptoms.





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