Tìm theo
Amobarbital
Các tên gọi khác (9 ) :
  • 5-Ethyl-5-(3-methylbutyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
  • 5-Ethyl-5-(3-methylbutyl)barbituric acid
  • 5-Ethyl-5-isoamylbarbituric acid
  • 5-Ethyl-5-isopentylbarbituric acid
  • Amobarbital
  • Amylobarbitone
  • Amytal
  • Barbamil
  • Barbamyl
Thuốc Gốc
Small Molecule
CAS: 57-43-2
ATC: N05CA02
ĐG : AAIPharma Inc. , http://www.aaipharma.com
CTHH: C11H18N2O3
PTK: 226.2722
A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H18N2O3
Phân tử khối
226.2722
Monoisotopic mass
226.131742452
InChI
InChI=1S/C11H18N2O3/c1-4-11(6-5-7(2)3)8(14)12-10(16)13-9(11)15/h7H,4-6H2,1-3H3,(H2,12,13,14,15,16)
InChI Key
InChIKey=VIROVYVQCGLCII-UHFFFAOYSA-N
IUPAC Name
5-ethyl-5-(3-methylbutyl)-1,3-diazinane-2,4,6-trione
Traditional IUPAC Name
amobarbital
SMILES
CCC1(CCC(C)C)C(=O)NC(=O)NC1=O
Độ tan chảy
157 °C
Độ hòa tan
603 mg/L (at 25 °C)
logP
2.07
logS
-2.57
pKa (strongest acidic)
8.48
PSA
75.27 Å2
Refractivity
58 m3·mol-1
Polarizability
23.45 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
7.84
Cơ Chế Tác Dụng : A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565) Amobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Amobarbital also appears to bind neuronal nicotinic acetylcholine receptors.
Tương Tác Thuốc :
  • Aminophylline The barbiturate, amobarbital, decreases the effect of aminophylline.
  • Betamethasone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Clomifene The enzyme inducer, amobarbital, decreases the effect of the hormone agent, clomifene.
  • Conjugated Estrogens The enzyme inducer, amobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Cyclosporine The barbiturate, amobarbital, increases the effect of cyclosporine.
  • Dexamethasone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Diethylstilbestrol The enzyme inducer, amobarbital, decreases the effect of the hormone agent, diethylstilbestrol.
  • Doxycycline The anticonvulsant, amobarbital, decreases the effect of doxycycline.
  • Eltrombopag Affects hepatic CYP1A2 metabolism, will decrease effect/level of eltrombopag. Affects hepatic CYP2C9/10 metabolism, will decrease effect/level of eltrombopag.
  • Estradiol The enzyme inducer, amobarbital, decreases the effect of the hormone agent, estradiol.
  • Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
  • Felodipine The barbiturate, amobarbital, decreases the effect of felodipine.
  • Fludrocortisone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Folic Acid Folic acid decreases the effect of anticonvulsant, amobarbital.
  • Gefitinib The CYP3A4 inducer, amobarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
  • Griseofulvin The barbiturate, amobarbital, decreases the effect of griseofulvin.
  • Hydrocortisone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
  • Medroxyprogesterone Acetate The enzyme inducer, amobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Megestrol acetate The enzyme inducer, amobarbital, decreases the effect of the hormone agent, megestrol.
  • Methadone The barbiturate, amobarbital, decreases the effect of methadone.
  • Metronidazole The barbiturate, amobarbital, decreases the effect of metronidazole.
  • Nifedipine The barbiturate, amobarbital, decreases the effect of the calcium channel blocker, nifedipine.
  • Norethindrone This product may cause a slight decrease of contraceptive effect
  • Oxtriphylline The barbiturate, amobarbital, decreases the effect of oxtriphylline.
  • Prednisolone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Prednisone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisone.
  • Quinidine The anticonvulsant, amobarbital, decreases the effect of quinidine.
  • Theophylline The barbiturate, amobarbital, decreases the effect of theophylline.
  • Triamcinolone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, triamcinolone.
  • Trimipramine The barbiturate, Amobarbital, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Amobarbital is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required.
  • Triprolidine The CNS depressants, Triprolidine and Amobarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Verapamil Amobarbital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Amobarbital is initiated, discontinued or dose changed.
  • Voriconazole Amobarbital may reduce serum concentrations and efficacy of voriconazole. Concomitant voriconazole and long-acting barbiturates therapy is contraindicated.
  • Warfarin Amobarbital may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if amobarbital is initiated, discontinued or dose changed.
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Isomytal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01351
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2164
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508165
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07536
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00555
ChemSpider
http://www.chemspider.com/Chemical-Structure.2079.html
PharmGKB
http://www.pharmgkb.org/drug/PA448401
Wikipedia
http://en.wikipedia.org/wiki/Amobarbital
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