60-99-1COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2VRQVVMDWGGWHTJ-CQSZACIVSA-NMethotrimeprazine is a member of the class of phenothiazines that is 10H-phenothiazine substituted by a (2R)-3-(dimethylamino)-2-methylpropyl group and a methoxy group at positions 10 and 2 respectively. It has a role as an anticoronaviral agent, a non-narcotic analgesic, a phenothiazine antipsychotic drug, a serotonergic antagonist, a dopaminergic antagonist, a cholinergic antagonist and an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor. It is a tertiary amine and a member of phenothiazines. It derives from a hydride of a 10H-phenothiazine.
60-99-1DTXSID1023289CHEMBL1764CHEBI:6838DEA NFLIS-Drug Category -> Depressants and Tranquilizers
Pharmaceuticals -> Listed in ZINC15
Pharmaceuticals -> Antipsychotics
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
Pharmaceuticals
9.19
9.19
安全情報は参考情報です。供給元の安全データシート(SDS)、適用法令、専門家による評価に代わるものではありません。
Warning
H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]
P261, P264, P270, P271, P280, P301+P317, P302+P352, P304+P340, P317, P321, P330, P362+P364, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 40 reports by companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Methotrimeprazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, its binding to 5HT2 receptors may also play a role. Methotrimeprazine exerts its actions through a central adrenergic-blocking, a dopamine-blocking, a serotonin-blocking, and a anticholinergic blocking.
Drug-Induced Liver Injury Severity and Toxicity (DILIst)
LEVOMEPROMAZINE
DILI Positive
Oral,Intramuscular; Intravenous
DOI:10.1016/j.drudis.2019.09.022
N05AA02
N - Nervous system
QN - Nervous system
Methotrimeprazine is a phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604)
Hepatic. Methotrimeprazine is metabolized in the liver and degraded to a sulfoxid-, a glucuronid- and a demethyl-moiety.
Hepatic. Methotrimeprazine is metabolized in the liver and degraded to a sulfoxid-, a glucuronid- and a demethyl-moiety. Half Life: Approximately 20 hours.
Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS.
Use (kg) in Switzerland (2009): >100
For the treatment of psychosis, particular those of schizophrenia, and manic phases of bipolar disorder. As a potentiator of anesthetics: In general anesthesia where it can be used as both a pre- and post-operative sedative and analgesic. (L1857) As an anti-emetic: For the treatment of nausea and vomiting of central origin.(L1857) As a sedative: For the management of insomnia. (L1857)
定義ChEBI: A member of the class of phenothiazines that is 10H-phenothiazine substituted by a (2R)-3-(dimethylamino)-2-methylpropyl group and a methoxy group at positions 10 and 2 respectively.
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