Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
212.116092388
InChI
InChI=1S/C10H16N2O3/c1-3-5-6-10(4-2)7(13)11-9(15)12-8(10)14/h3-6H2,1-2H3,(H2,11,12,13,14,15)
InChI Key
InChIKey=STDBAQMTJLUMFW-UHFFFAOYSA-N
IUPAC Name
5-butyl-5-ethyl-1,3-diazinane-2,4,6-trione
Traditional IUPAC Name
butethal
SMILES
CCCCC1(CC)C(=O)NC(=O)NC1=O
Độ hòa tan
4880 mg/L (at 25 °C)
pKa (strongest acidic)
8.48
Refractivity
53.45 m3·mol-1
Dược Lực Học :
Butethal (also known as butobarbitone and butobarbital) belongs to a group of medicines called the barbiturates. It is thought to act on receptors in the brain (GABA receptors) causing the release of the chemical GABA. This chemical inhibits certain areas of the brain resulting in sleepiness.
Cơ Chế Tác Dụng :
Butethal is a sedative and a hypnotic drug.
Butethal binds at a distinct binding site associated with a Cl- ionopore at the GABAA 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. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration.
▧ Metabolism :
Hepatic.
▧ Half Life :
37 hours
Độc Tính :
Signs of overdose include confusion (severe), decrease in or loss of reflexes, drowsiness (severe), fever, irritability (continuing), low body temperature, poor judgment, shortness of breath or slow or troubled breathing, slow heartbeat, slurred speech, staggering, trouble in sleeping, unusual movements of the eyes, weakness (severe).
Chỉ Định :
For the treatment of insomnia.
Tương Tác Thuốc :
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Aminophylline
The barbiturate, butethal, decreases the effect of aminophylline.
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Betamethasone
The barbiturate, butethal, may decrease the effect of the corticosteroid, betamethasone.
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Clomifene
The enzyme inducer, butethal, decreases the effect of the hormone agent, clomifene.
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Conjugated Estrogens
The enzyme inducer, butethal, decreases the effect of the hormone agent, conjugated estrogens.
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Cyclosporine
The barbiturate, butethal, increases the effect of cyclosporine.
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Dexamethasone
The barbiturate, butethal, may decrease the effect of the corticosteroid, dexamethasone.
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Diethylstilbestrol
The enzyme inducer, butethal, decreases the effect of the hormone agent, diethylstilbestrol.
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Doxycycline
The anticonvulsant, butethal, decreases the effect of doxycycline.
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Estradiol
The enzyme inducer, butethal, decreases the effect of the hormone agent, estradiol.
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Ethinyl Estradiol
This product may cause a slight decrease of contraceptive effect
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Felodipine
The barbiturate, butethal, decreases the effect of felodipine.
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Fludrocortisone
The barbiturate, butethal, may decrease the effect of the corticosteroid, fludrocortisone.
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Folic Acid
Folic acid decreases the effect of anticonvulsant, butethal.
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Gefitinib
The CYP3A4 inducer, butethal, may decrease the serum concentration and therapeutic effects of gefitinib.
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Griseofulvin
The barbiturate, butethal, decreases the effect of griseofulvin.
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Hydrocortisone
The barbiturate, butethal, may decrease the effect of the corticosteroid, hydrocortisone.
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Levonorgestrel
Phenobarbital decreases the effect of levonorgestrel
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Medroxyprogesterone Acetate
The enzyme inducer, butethal, decreases the effect of the hormone agent, medroxyprogesterone.
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Megestrol acetate
The enzyme inducer, butethal, decreases the effect of the hormone agent, megestrol.
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Methadone
The barbiturate, butethal, decreases the effect of methadone.
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Metronidazole
The barbiturate, butethal, decreases the effect of metronidazole.
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Nifedipine
The barbiturate, butethal, decreases the effect of the calcium channel blocker, nifedipine.
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Norethindrone
This product may cause a slight decrease of contraceptive effect
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Oxtriphylline
The barbiturate, butethal, decreases the effect of oxtriphylline.
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Prednisolone
The barbiturate, butethal, may decrease the effect of the corticosteroid, prednisolone.
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Prednisone
The barbiturate, butethal, may decrease the effect of the corticosteroid, prednisone.
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Quinidine
The anticonvulsant, butethal, decreases the effect of quinidine.
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Theophylline
The barbiturate, butethal, decreases the effect of theophylline.
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Triamcinolone
The barbiturate, butethal, may decrease the effect of the corticosteroid, triamcinolone.