palonosetron hydrochloride basic information
nausea and vomiting drug adverse effects references
product name: palonosetron hydrochloride
synonyms: palonosetron hcl;palonosetron hydrochloride;(3as)-2-(3s)-1-azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1h-benz[de]isoquinolin-1-one monohydrochloride;(3as)-2-(3s)-1-azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1h-benz[de]isoquinolin-1-one hydrochloride;aloxi;onicit;rs-25259-197;(s,s)-palonosetron hydrochloride
cas: 135729-62-3
mf: c19h25cln2o
mw: 332.87
einecs:
product categories: selective 5-ht3 receptor antagonist;chiral reagents;heterocycles;intermediates & fine chemicals;pharmaceuticals
mol file: 135729-62-3.mol
palonosetron hydrochloride structure
palonosetron hydrochloride chemical properties
melting point >290°c
storage temp. refrigerator
cas database reference 135729-62-3(cas database reference)
safety information
msds information
palonosetron hydrochloride usage and synthesis
nausea and vomiting drug palonosetron hydrochloride is a drug to inhibit nausea and vomiting, which is a new type highly selective, high-affinity 5-ht3 receptor antagonist that can block the vomiting reflex center peripheral neurons presynaptic 5-ht. receptor excitement directly affects the central nervous system in 5-ht. impulse receptor excitement generated by the role of vagal afferent nerve after area, blocking the vagus nerve endings in the gut, preventing signals to 5-ht. receptor trigger zone can reduce the incidence of nausea and vomiting. central clinically for the treatment of acute severe emetogenic chemotherapy induced delayed nausea and vomiting. because of its high curative effect, little side effect, long half-life (about 40 h), small dosage, and so on, it has attracted much attention.
with 1,2,3,4-tetrahydro-1-naphthoic acid as the starting material, the split, amination, reduction, cyclization, salt of palonosetron hydrochloride granisetron.
clinical studies showed that palonosetron can be used safely with corticosteroids, analgesics, antiemetics, antispasmodics and anticholinergic drugsas the starting material, the split, amination, reduction, cyclization, salt of palonosetron hydrochloride granisetron.
murine tumor model studies indicate that palonosetron does not inhibit the five kinds of chemotherapy drugs studied (cisplatin, cyclophosphamide, cytarabine, doxorubicin and mitomycin c) anti-cancer activity.
adverse effects the most common adverse effects are headache, which occurs in 4–11% of patients, and constipation in up to 6% of patients. in less than 1% of patients, other gastrointestinal disorders occur, as well as sleeplessness, first-and second-degree atrioventricular block, muscle pain and shortness of breath. palonosetron is similarly well tolerated as other setrons, and slightly less than placebo.
references #
chemical properties white solid
uses serotonin 5-ht3 receptor antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (cinv). antiemetic.
uses palonosetron hcl is a 5-ht3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting
uses specifically inhibits cells of the adrenal cortex and their production of hormones for adrenocortical tumor therapy, causes cns damage, but no bone marrow depression.
definition chebi: a hydrochloride obtained by combining palonosetron with one molar equivalent of hydrogen chloride; an antiemetic used in combination with netupitant (under the trade name akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.
uses palonosetron is a potent, selective antagonist of the serotonin (5-ht) receptor 5-ht3 (pki = 10.4 in rat cortex) that minimally effects a wide range of other neuronal receptors. it is orally bioavailable and potently inhibits emesis induced by chemotherapeutic drugs, like cisplatin , but not by apomorphine , which acts by dopamine receptor antagonism. palonosetron is remarkable for its long duration of action, related to its high receptor-binding affinity and long half-life. it is effective in managing chemotherapy-induced nausea and vomiting.[cayman chemical]
palonosetron hydrochloride preparation products and raw materials