Tìm theo
Hexobarbital
Các tên gọi khác (8 ) :
  • 5-(1-Cyclohexen-1-yl)-1,5-dimethyl-2,4,6(1H,3H,5H)-pyrimidinetrione
  • 5-(1-cyclohexen-1-yl)-1,5-dimethylbarbituric acid
  • 5-Cyclohex-1-enyl-1,5-dimethyl-pyrimidine-2,4,6-trione
  • Evipan
  • Hexobarbital
  • Hexobarbitone
  • Methexenyl
  • Methylhexabital
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 56-29-1
ATC: N05CA16, N01AF02
CTHH: C12H16N2O3
PTK: 236.267
A barbiturate that is effective as a hypnotic and sedative. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H16N2O3
Phân tử khối
236.267
Monoisotopic mass
236.116092388
InChI
InChI=1S/C12H16N2O3/c1-12(8-6-4-3-5-7-8)9(15)13-11(17)14(2)10(12)16/h6H,3-5,7H2,1-2H3,(H,13,15,17)
InChI Key
InChIKey=UYXAWHWODHRRMR-UHFFFAOYSA-N
IUPAC Name
5-(cyclohex-1-en-1-yl)-1,5-dimethyl-1,3-diazinane-2,4,6-trione
Traditional IUPAC Name
hexobarbital
SMILES
CN1C(=O)NC(=O)C(C)(C1=O)C1=CCCCC1
Độ tan chảy
146.5 °C
Độ hòa tan
435 mg/L (at 25 °C)
logP
1.98
logS
-2.74
pKa (strongest acidic)
8.41
PSA
66.48 Å2
Refractivity
61.95 m3·mol-1
Polarizability
24.14 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.2
Dược Lực Học : Hexobarbital is a barbiturate derivative having hypnotic and sedative effects. It was used in the 1940s-1950s as an agent for inducing anesthesia for surgery and has a relatively fast onset of effects and short duration of action. However it can be difficult to control the depth of anesthesia with hexobarbital which makes it quite dangerous, and it has now been replaced by safer drugs in human medicine, usually thiopental would be the barbiturate of choice for this application these days.
Cơ Chế Tác Dụng : A barbiturate that is effective as a hypnotic and sedative. [PubChem] Hexobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABA-A receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Dược Động Học :

▧ Protein binding :
25%
▧ Metabolism :
Hepatic.
Độc Tính : Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.
Chỉ Định : For the induction of anesthesia prior to the use of other general anesthetic agents and for induction of anesthesia for short surgical, diagnostic, or therapeutic procedures associated with minimal painful stimuli.
Tương Tác Thuốc :
  • Aminophylline The barbiturate, hexobarbital, decreases the effect of aminophylline.
  • Betamethasone The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Clomifene The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, clomifene.
  • Conjugated Estrogens The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Cyclosporine The barbiturate, hexobarbital, increases the effect of cyclosporine.
  • Dexamethasone The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Diethylstilbestrol The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, diethylstilbestrol.
  • Doxycycline The anticonvulsant, hexobarbital, decreases the effect of doxycycline.
  • Estradiol The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, estradiol.
  • Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
  • Felodipine The barbiturate, hexobarbital, decreases the effect of felodipine.
  • Fludrocortisone The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Folic Acid Folic acid decreases the effect of anticonvulsant, hexobarbital.
  • Gefitinib The CYP3A4 inducer, hexobarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
  • Griseofulvin The barbiturate, hexobarbital, decreases the effect of griseofulvin.
  • Hydrocortisone The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
  • Medroxyprogesterone Acetate The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Megestrol acetate The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, megestrol.
  • Methadone The barbiturate, hexobarbital, decreases the effect of methadone.
  • Metronidazole The barbiturate, hexobarbital, decreases the effect of metronidazole.
  • Nifedipine The barbiturate, hexobarbital, decreases the effect of the calcium channel blocker, nifedipine.
  • Norethindrone This product may cause a slight decrease of contraceptive effect
  • Oxtriphylline The barbiturate, hexobarbital, decreases the effect of oxtriphylline.
  • Prednisolone The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Prednisone The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, prednisone.
  • Quinidine The anticonvulsant, hexobarbital, decreases the effect of quinidine.
  • Theophylline The barbiturate, hexobarbital, decreases the effect of theophylline.
  • Triamcinolone The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Liều Lượng & Cách Dùng : Tablet - Oral - 250 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Evipal
  • Công ty :
    Sản phẩm biệt dược : Evipan
  • Công ty :
    Sản phẩm biệt dược : Tobinal
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01355
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C11723
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01071
PharmGKB
http://www.pharmgkb.org/drug/PA449875
Wikipedia
http://en.wikipedia.org/wiki/Hexobarbital
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