Tropisetron
- 89565-68-4
- 105826-92-4 ( monohydrochloride )
A04AA03
Antiemetic
Selective blockade of central 5 -HT3 receptors
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Tropisetron is a 5 -HT3 antagonist and is used mainly as an antiemetic, but is now also in pain therapy use.
Areas of application
Tropisetron is used as a remedy for vomiting, nausea and nausea. This is particularly true in the context of chemotherapy and radiotherapy, where it can also be used preventively. It is also used for the prophylaxis of postoperative nausea and vomiting. This was a superiority of ondansetron, another 5 - HT3 antagonist, compared with tropisetron in comparison to costs and prophylactic effect in high-risk patients occupied.
Several studies have shown a significant reduction in pain in a subset of patients with fibromyalgia syndrome. The effect persists in these patients at relatively long time without taking must be made permanent. In another part of the patient, however, no effect is observed.
An analgesic effect was also observed in some rheumatic diseases and myofascial syndromes. The effect should be involved in these diseases comparable to that of local anesthetics such as lidocaine or prilocaine. This also antiinflammatory effect was observed.
It can be administered orally and intravenously.
Mechanism of Action
Tropisetron blocked the action of the neurotransmitter substance serotonin to its receptors in the nervous system. The analgesic effect is probably due to stimulation of the nociceptors, which results in preventing the activation of 5-HT3 receptors.
Tropisetron is metabolized by the enzyme CYP2D6.
Side effects
The most common side effects include headache, constipation, and diarrhea. More rarely occur hypertension, tremors, hives, trouble breathing.
Interactions
Administered concomitantly with agents such as antiarrhythmics, antibiotics and some drugs from the group of antidepressants can cause a prolonged Herzmuskeleregung. Rifampicin and phenobarbital reduce the effect of tropisetron.