Antiemetics serotonin antagonists

Short-term toxicities of adjuvant chemotherapy are generally well tolerated, especially with the availability of serotonin-antagonist and substance P/neurokinin 1-antagonist antiemetics and colony-stimulating factors. 

Some synthetic TA primarily act as selective serotonin antagonist and are thus considered and used as antiemetics, including bemesetron, granisetron, tropisetron and scopolamine (Fig. 1) [36, 37],... 

Bemesetron is a synthetic ester of tropine and dichlorobenzoylic acid (Fig. 1). In contrast to TA introduced above, bemesetron primarily acts as a selective serotonin antagonist on the 5-HT3R in the CNS and GIT. Therefore, it was tested as an injectable antiemetic drug for cancer chemotherapy to treat vomiting and nausea but is not in clinical use [36, 37, 58],... 

B. Premedicate with antiemetics, including a serotonin antagonist. 

This discussion will be limited to the neural serotonin 5-HT3 receptors which came to the forefront with the advent of antiemetic agents exhibiting 5-HT3 antagonist properties. At the present time, there is no evidence that 5-HT, and 5-HT2 receptors play an important role in vomiting [64],... 

Greenshaw AJ, Silverstone PH. (1997). The non-antiemetic uses of serotonin 5-HT3 receptor antagonists. Clinical pharmacology and therapeutic applications. Drugs. 53(1) 20-39. 

Several different types of serotonin receptor (for example, S-HTi / 5-HT2A/ 5-HT2C/ 5-HTib/id) have been associated with the motor side effects of the SSRIs which may arise should these drugs be administered in conjunction with a monoamine oxidase inhibitor. The 5-HT3 receptor is an example of a non-selective cation charmel receptor which is permeable to both sodium and potassium ions and, because both calcium and magnesium ions can modulate its activity, the 5-HT3 receptor resembles the glutamate-NMDA receptor. Antagonists of the 5-HT3 receptor, such as ondansetron, are effective antiemetics and are particularly useful when... 

Neurokinin 1 (NKiJ-receptor antagonists have antiemetic properties that are mediated through central blockade in the area postrema. Aprepitant (an oral formulation) is a highly selective Nl -receptor antagonist that crosses the blood-brain barrier and occupies brain NKj receptors. It has no affinity for serotonin, dopamine, or corticosteroid receptors. Fosaprepitant is an intravenous formulation that is converted within 30 minutes after infusion to aprepitant. 

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