Tìm theo
Droperidol
Các tên gọi khác (8 ) :
  • 1-(1-(3-(P-Fluorobenzoyl)propyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
  • 1-(1-(4-(P-Fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
  • 1-{1-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1,2,3,6-tetrahydro-pyridin-4-yl}-1,3-dihydro-benzoimidazol-2-one
  • 1-{1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydro-4-pyridinyl}-2,3-dihydro-1H-benzo[D]imidazol-2-one
  • Droperidol
  • Dropéridol
  • Droperidolo
  • Droperidolum
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 548-73-2
ATC: N05AD08
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C22H22FN3O2
PTK: 379.4274
A butyrophenone with general properties similar to those of haloperidol. It is used 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 surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H22FN3O2
Phân tử khối
379.4274
Monoisotopic mass
379.169605168
InChI
InChI=1S/C22H22FN3O2/c23-17-9-7-16(8-10-17)21(27)6-3-13-25-14-11-18(12-15-25)26-20-5-2-1-4-19(20)24-22(26)28/h1-2,4-5,7-11H,3,6,12-15H2,(H,24,28)
InChI Key
InChIKey=RMEDXOLNCUSCGS-UHFFFAOYSA-N
IUPAC Name
1-{1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydropyridin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one
Traditional IUPAC Name
droperidol
SMILES
FC1=CC=C(C=C1)C(=O)CCCN1CCC(=CC1)N1C(=O)NC2=CC=CC=C12
Độ tan chảy
145-146.5
Độ hòa tan
4.21 mg/L
logP
3.50
logS
-3.6
pKa (strongest acidic)
12.72
pKa (Strongest Basic)
6.75
PSA
52.65 Å2
Refractivity
109.52 m3·mol-1
Polarizability
40.31 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
pKa
7.46
Dược Lực Học : Droperidol produces marked tranquilization and sedation. It allays apprehension and provides a state of mental detachment and indifference while maintaining a state of reflex alertness. Droperidol produces an antiemetic effect as evidenced by the antagonism of apomorphine in dogs. It lowers the incidence of nausea and vomiting during surgical procedures and provides antiemetic protection in the postoperative period. Droperidol potentiates other CNS depressants. It produces mild alpha-adrenergic blockade, peripheral vascular dilatation and reduction of the pressor effect of epinephrine. It can produce hypotension and decreased peripheral vascular resistance and may decrease pulmonary arterial pressure (particularly if it is abnormally high). It may reduce the incidence of epinephrine-induced arrhythmias, but it does not prevent other cardiac arrhythmias.
Cơ Chế Tác Dụng : A butyrophenone with general properties similar to those of haloperidol. It is used 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 surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593) The exact mechanism of action is unknown, however, droperidol causes a CNS depression at subcortical levels of the brain, midbrain, and brainstem reticular formation. It may antagonize the actions of glutamic acid within the extrapyramidal system. It may also inhibit cathecolamine receptors and the reuptake of neurotransmiters and has strong central antidopaminergic action and weak central anticholinergic action. It can also produce ganglionic blockade and reduced affective response. The main actions seem to stem from its potent Dopamine(2) receptor antagonism with minor antagonistic effects on alpha-1 adrenergic receptors as well.
Dược Động Học :
▧ Absorption :
Completely absorbed following intramuscular administration.
▧ Metabolism :
Extensively metabolized.
▧ Half Life :
Biphasic distribution. The rapid distribution phase is 1.4 ± 0.5 minutes and the slower distribution phase is 14.3 ± 6.5 minutes. Elimination half-life in adults is 134 ± 13 minutes and may be increased in geriatric patients. In children, it is 101.5 ± 26.4 minutes.
Độc Tính : The intravenous LD50 of droperidol is 20-43 mg/kg in mice; 30 mg/kg in rats; 25 mg/kg in dogs and 11-13 mg/kg in rabbits. The intramuscular LD50 of droperidol is 195 mg/kg in mice, 104-110 mg/kg in rats; 97 mg/kg in rabbits and 200 mg/kg in guinea pigs. The manifestations of droperidol overdosage are an extension of its pharmacologic actions.
Chỉ Định : Droperidol is ssed to produce tranquilization and to reduce the incidence of nausea and vomiting in surgical and diagnostic procedures.
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Brimonidine Droperidol may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
  • Buprenorphine Droperidol may enhance the CNS depressant effect of CNS Depressants like buprenorphine. Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use.
  • Butabarbital Droperidol may enhance the CNS depressant effect of CNS Depressants like butabarbital. Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use.
  • Butalbital Droperidol may enhance the CNS depressant effect of CNS depressants such as butalbital. Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use.
  • Butorphanol Droperidol may enhance the CNS depressant effect of butorphanol. Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use.
  • Carisoprodol Droperidol may enhance the CNS depressant effect of carisoprodol. Consider dose reductions of droperidol or of other CNS agents with concomitant use.
  • Dihydrocodeine Enhanced CNS depressant effects are possible. Consider dose reduction of a CNS agent, if concurrent use is not avoidable.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Quinupristin This combination presents an increased risk of toxicity
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Droperidol, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. May cause dopamine deficiency. Similar pharmacologic properties thus combination therapy will worsen the severity of sedative, parkinsonian, and extrapyramidal adverse effects.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimethobenzamide Trimethobenzamide and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Triprolidine Triprolidine and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Solution - Intramuscular
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Janssen
    Sản phẩm biệt dược : Dehydrobenzperidol
  • Công ty : Prostrakan
    Sản phẩm biệt dược : Dridol
  • Công ty : Daiichi Sankyo
    Sản phẩm biệt dược : Droleptan
  • Công ty : Excelsior
    Sản phẩm biệt dược : Dropedol
  • Công ty : Siu Guan
    Sản phẩm biệt dược : Dropel
  • Công ty : Cristália
    Sản phẩm biệt dược : Droperdal
  • Công ty : Grindeks
    Sản phẩm biệt dược : Droperidols
  • Công ty : Akorn
    Sản phẩm biệt dược : Inapsine
  • Sản phẩm biệt dược : Xomolix
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00450
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3168
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505291
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00308
ChemSpider
http://www.chemspider.com/Chemical-Structure.3056.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50017705
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/11098-010-01
PharmGKB
http://www.pharmgkb.org/drug/PA449422
Wikipedia
http://en.wikipedia.org/wiki/Droperidol
RxList
http://www.rxlist.com/cgi/generic3/droperidol.htm
Drugs.com
http://www.drugs.com/cdi/droperidol.html
... loading
... loading