130-61-0CSc1ccc2c(c1)N(CCC1CCCCN1C)c1ccccc1S2.ClNZFNXWQNBYZDAQ-UHFFFAOYSA-NThioridazine hydrochloride is a hydrochloride. It has a role as a geroprotector and a first generation antipsychotic. It contains a thioridazine.
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
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 (98%): Harmful if swallowed [Warning Acute toxicity, oral]
P261, P264, P264+P265, P270, P271, P273, P280, P301+P317, P302+P352, P304+P340, P305+P351+P338, P319, P321, P330, P332+P317, P337+P317, P362+P364, P391, P403+P233, P405, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 49 reports by companies from 11 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
An airway must be established and maintained. Adequate oxygenation and ventilation must be ensured. Cardiovascular monitoring should commence immediately and should include continuous electrocardiographic monitoring to detect possible arrhythmias. Treatment may include one or more of the following therapeutic interventions: correction of electrolyte abnormalities and acid-base balance, lidocaine, phenytoin, isoproterenol, ventricular pacing, and defibrillation. Disopyramide, procainamide, and quinidine may produce additive QT-prolonging effects when administered to patients with acute overdosage of Mellaril and should be avoided. Caution must be exercised when administering lidocaine, as it may increase the risk of developing seizures. Treatment of hypotension may require intravenous fluids and vasopressors. Phenylephrine, levarterenol, or metaraminol are the appropriate pressor agents for use in the management of refractory hypotension. Gastric lavage and repeated doses of activated charcoal should be considered. Induction of emesis is less preferable to gastric lavage because of the risk of dystonia and the potential for aspiration of vomitus. Acute extrapyramidal symptoms may be treated with diphenhydramine hydrochloride or benztropine mesylate. Forced diuresis, hemoperfusion, hemodialysis and manipulation of urine pH are of unlikely benefit in the treatment of phenothiazine overdose due to their large volume of distribution and extensive plasma protein binding. (L1712)
THIORIDAZINE HYDROCHLORIDE
Phenothiazines [CS]; Phenothiazine [EPC]
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.
使用Thioridazine hydrochloride has been used as an intercalating agent for analyzing the integrity of double-stranded DNA (dsDNA) using square-wave voltammetry (SWV) techniques. Thioridazine hydrochloride has also been used as a positive control for the inhibition of hepatic enzyme cytochrome P4502D6 (CYP2D6) in human liver microsomes.
Thioridazine hydrochloride,10-[2-(1-methyl-2-piperidyl)ethyl]-2-(methylthio)phenothiazine monohydrochloride (Mellaril), is amember of the piperidine subgroup of the phenothiazines.The drug has a relatively low tendency to produce EPS. Thedrug has high anticholinergic activity, and this activity in thestriatum, counterbalancing a striatal DA block, may be responsiblefor the low EPS. It also has been suggested thatthere may be increased DA receptor selectivity, which may be responsible. The drug has sedative and hypotensive activityin common with chlorpromazine and less antiemeticactivity. At high doses, pigmentary retinopathy has been observed.Its major metabolites include N-demethylated, ringhydroxylated,and S-oxidized products. Thioridazine isprominently converted to the active metabolite mesoridazine(discussed next), which probably contributes to the antipsychoticactivity of thioridazine.
現在のフィルター条件では反応記録がありません。
読み込み中…
130-61-0DTXSID9049401CHEMBL1200916CHEBI:48566化学的特性Pale Yellow Solid
Thioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks alpha-adrenergic effect, depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.
LD<sub>50</sub>=956-1034 mg/kg (Orally in rats); Agitation, blurred vision, coma, confusion, constipation, difficulty breathing, dilated or constricted pupils, diminished flow of urine, dry mouth, dry skin, excessively high or low body temperature, extremely low blood pressure, fluid in the lungs, heart abnormalities, inability to urinate, intestinal blockage, nasal congestion, restlessness, sedation, seizures, shock
Drug Induced Liver Injury Rank (DILIrank 2.0)
Thioridazine hydrochloride
vLess-DILI-concern
5
Adverse reactions
DOI:10.1016/j.drudis.2016.02.015