DROPERIDOL
- Product Name
- DROPERIDOL
- CAS No.
- 548-73-2
- Chemical Name
- DROPERIDOL
- Synonyms
- R 474;r4749;Dridol;Halkan;Inoval;R 4749;Inappin;Inapsin;Innovan;Innovar
- CBNumber
- CB9145418
- Molecular Formula
- C22H22FN3O2
- Formula Weight
- 379.43
- MOL File
- 548-73-2.mol
DROPERIDOL Property
- Melting point:
- 148-149°C
- Density
- 1.2154 (estimate)
- storage temp.
- 2-8°C
- solubility
- Practically insoluble in water, freely soluble in dimethylformamide and in methylene chloride, sparingly soluble in ethanol (96 per cent).
- pka
- 7.64(at 25℃)
- color
- Pale Yellow to Pale Beige
- Water Solubility
- 4.1mg/L(30 ºC)
- CAS DataBase Reference
- 548-73-2(CAS DataBase Reference)
- EPA Substance Registry System
- 2H-Benzimidazol-2-one, 1-[1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydro-4-pyridinyl]-1,3-dihydro- (548-73-2)
Safety
- Hazard Codes
- Xn
- Risk Statements
- 22
- Safety Statements
- 36
- RIDADR
- 3249
- WGK Germany
- 3
- RTECS
- DE2100000
- HazardClass
- 6.1(b)
- PackingGroup
- III
- HS Code
- 2933995800
- Hazardous Substances Data
- 548-73-2(Hazardous Substances Data)
- Toxicity
- LD50 oral in rat: 750mg/kg
N-Bromosuccinimide Price
- Product number
- PHR2585
- Product name
- Droperidol
- Packaging
- 500MG
- Price
- $267
- Updated
- 2024/03/01
- Product number
- D1414
- Product name
- Droperidol
- Packaging
- 1g
- Price
- $157
- Updated
- 2024/03/01
- Product number
- 1229001
- Product name
- Droperidol
- Purity
- United States Pharmacopeia (USP) Reference Standard
- Packaging
- 250mg
- Price
- $436
- Updated
- 2024/03/01
- Product number
- BP675
- Product name
- Droperidol
- Purity
- British Pharmacopoeia (BP) Reference Standard
- Packaging
- 100MG
- Price
- $221
- Updated
- 2023/06/20
- Product number
- 18884
- Product name
- Droperidol
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $32
- Updated
- 2024/03/01
DROPERIDOL Chemical Properties,Usage,Production
Description
D roperidol is a butyrophenone that has potent antidopaminergic (D2) activity and mild α2-blocking actions. It produces sedation and anxiolysis and is an effective antiemetic. A dverse effects include vasodilatation and hypotension, and at higher doses, dystonic reactions can occur. D roperidol was used for premedication and in neuroleptanaesthesia until reports of death from long QT syndrome led to its withdrawal in 2001. It has recently been reintroduced and licenced at lower doses for prevention of postoperative nausea and vomiting. D roperidol has an onset of 3–10 min after i.v. injection and duration of action of 6–12h. It undergoes hepatic metabolism, but approximately 10% of the drug is excreted unchanged in the urine.
Chemical Properties
Pale Yellow Solid
Originator
Dehydrobenzperidol,Janssen,W. Germany,1963
Uses
A D1, D2 dopamine receptor antagonist; butyrophenone antipsychotic and anti-emetic.
Uses
H2 antihistamine
Uses
A D1DR and D2DR inhibitor.
Uses
The neuroleptic droperidol possesses antipsychotic, sedative, and antishock action. It potentiates the action of drugs for narcosis. In psychiatric practice, droperidol is used for psychomotor excitement and hallucinations. The principal use of this drug lies in anesthesiology for neuroleptanalgesia in combination with fentanyl. It is used in premedication as well as in surgical operations and post-operational circumstances.
Definition
ChEBI: An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeo .
Manufacturing Process
A mixture of 10 parts of γ-chloro-4-fluorobutyrophenone, 5.5 parts of 1- (1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone, 4 parts of sodium carbonate, and 0.1 part of potassium iodide in 176 parts of 4-methyl-2- pentanone is stirred and refluxed for 64 hours. The cooled reaction mixture is filtered and the solvent is evaporated from the filtrate to leave an oily residue which is dissolved in toluene. The toluene solution is filtered and the solvent is evaporated. The resultant residue is recrystallized from a mixture of 32 parts of ethyl acetate and 32 parts of diisopropyl ether to give 1-[1-[(4-fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl]-2-benzimidazolinone hydrate melting at about 145°-146.5°C.
brand name
Inapsine (Akorn);Dehydrobenzperidol;Diaperidol;Inopsin.
Therapeutic Function
Tranquilizer
General Description
Droperidol, 1-{1-[3-(p-fluorobenzoyl)propyl]-1,2, 3,6-tetrahydro-4-pyridyl}-2-benzimidazolinone(Inapsine), may be used alone as a preanestheticneuroleptic or as an antiemetic. Because of its very shortactingand highly sedating properties, its most frequent useis in combination (Innovar) with the narcotic agent fentanyl(Sublimaze) preanesthetically.
General Description
Droperidol, 1-1-[3-(p-fluorobenzoyl)propyl]-1,2,[3,6-tetrahydro-4-pyridyl]-2-benzimidazolinone(Inapsine). Centrally acting acetylcholinesteraseinhibitors may increase the risk of antipsychotic-relatedEPS. CNS depressants may produce additive sedativeeffects (benzodiazepines, barbiturates, antipsychotics,ethanol, opiates, and other sedative medications).Droperidol in combination with certain forms of inhalationanesthetics may produce peripheral vasodilatation and hypotension.Metoclopramide may increase the risk of EPSproduced by droperidol.
Biochem/physiol Actions
D1, D2 dopamine receptor antagonist; butyrophenone antipsychotic and anti-emetic.
Synthesis
Droperidol, 1-[1-[3-(p-fluorobenzoyl)propyl]-1,2,3,6,4-piridyl]-2-benzymidazolinone (6.3.11), is synthesized from 1-benzyl-3-carbethoxypiperidin-4-one (3.1.47), which is reacted with o-phenylendiamine. Evidently, the first derivative that is formed under the reaction conditions, 1,5-benzdiazepine, rearranges into 1-(1-benzyl-1,2,3,6- tetrahydro-4-piridyl)-2-benzymidazolone (6.3.9). Debenzylation of the resulting product with hydrogen over a palladium catalyst into 1-(1,2,3,6-tetrahydro-4-piridyl)-2-benzimidazolon (6.3.10) and subsequent alkylation of this using 4??-chloro-4-fluorobutyrophenone (6.3.4) yields droperidol (6.3.11) [47¨C49].
Drug interactions
Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect; effects of
thiopental enhanced.
Analgesics: increased risk of ventricular arrhythmias
with methadone; increased risk of convulsions with
tramadol; enhanced hypotensive and sedative effects
with opioids.
Anti-arrhythmics increased risk of ventricular
arrhythmias with anti-arrhythmics that prolong
the QT interval, e.g. procainamide, disopyramide,
dronedarone and amiodarone - avoid.
Antibacterials: increased risk of ventricular
arrhythmias with moxifloxacin and macrolides -
avoid; increased risk of ventricular arrhythmias with
delamanid.
Antidepressants: increased risk of ventricular
arrhythmias with fluoxetine, fluvoxamine, sertraline
or tricyclics - avoid; possible increased risk of
convulsions with vortioxetine.
Antiepileptics: convulsive threshold lowered.
Antimalarials: avoid with artemether/lumefantrine
and piperaquine with artenimol; increased risk
of ventricular arrhythmias with chloroquine,
hydroxychloroquine or quinine - avoid.
Antipsychotics: increased risk of ventricular
arrhythmias with amisulpride, pimozide, sulpiride,
phenothiazines that prolong QT interval or
haloperidol - avoid; possibly increased risk of
ventricular arrhythmias with risperidone.
Antivirals: concentration possibly increased with ritonavir
Anxiolytics and hypnotics: increased sedative effects.
Atomoxetine: increased risk of ventricular
arrhythmias.
Beta-blockers: enhanced hypotensive effect;
increased risk of ventricular arrhythmias with sotalol
- avoid.
Cytotoxics: increased risk of ventricular arrhythmias
with arsenic trioxide and possibly ceritinib.
Desferrioxamine: avoid concomitant use.
Diuretics: enhanced hypotensive effect.
Hormone antagonists: increased risk of ventricular
arrhythmias with tamoxifen - avoid.
Lithium: increased risk of extrapyramidal side effects
and possibly neurotoxicity.
Pentamidine: increased risk of ventricular
arrhythmias - avoid.
Tacrolimus: increased risk of ventricular arrhythmias
- avoid.
Metabolism
Extensively metabolised in the liver, and undergoes oxidation, dealkylation, demethylation and hydroxylation by cytochrome P450 isoenzymes 1A2 and 3A4, and to a lesser extent by 2C19. The metabolites are inactive. About 75% of a dose is excreted in the urine, with 1% being excreted unchanged; 11% appears in the faeces.
DROPERIDOL Preparation Products And Raw materials
Raw materials
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View Lastest Price from DROPERIDOL manufacturers
- Product
- DROPERIDOL 548-73-2
- Price
- US $1.10/g
- Min. Order
- 1g
- Purity
- 99.9%
- Supply Ability
- 100 Tons min
- Release date
- 2021-07-23
- Product
- DROPERIDOL 548-73-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-10
- Product
- DROPERIDOL 548-73-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-08