Tìm theo
Pentobarbital
Các tên gọi khác (7 ) :
  • 5-Ethyl-5-(1-methyl-butyl)-pyrimidine-2,4,6-trione
  • 5-Ethyl-5-(1-methylbutyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
  • 5-ethyl-5-(1-methylbutyl)barbituric acid
  • 5-ethyl-5-(sec-pentyl)barbituric acid
  • Nembutal
  • Pentobarbital
  • Pentobarbitone
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 76-74-4
ATC: N05CA01
ĐG : Breckenridge Pharmaceuticals , http://www.bpirx.com
CTHH: C11H18N2O3
PTK: 226.2722
A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)
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/c1-4-6-7(3)11(5-2)8(14)12-10(16)13-9(11)15/h7H,4-6H2,1-3H3,(H2,12,13,14,15,16)
InChI Key
InChIKey=WEXRUCMBJFQVBZ-UHFFFAOYSA-N
IUPAC Name
5-ethyl-5-(pentan-2-yl)-1,3-diazinane-2,4,6-trione
Traditional IUPAC Name
pentobarbital
SMILES
CCCC(C)C1(CC)C(=O)NC(=O)NC1=O
Độ tan chảy
129.5 °C
Độ hòa tan
679 mg/L (at 25 °C)
logP
2.10
logS
-2.52
pKa (strongest acidic)
8.48
PSA
75.27 Å2
Refractivity
58 m3·mol-1
Polarizability
23.41 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
8.11 (at 25 °C)
Dược Lực Học : Pentobarbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
Cơ Chế Tác Dụng : A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236) Pentobarbital 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 :
Barbiturates are absorbed in varying degrees following oral, rectal, or parenteral administration.
▧ Metabolism :
by hepatic microsomal enzyme system
▧ Route of Elimination :
Barbiturates are metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine, and less commonly, in the feces. Approximately 25 to 50 percent of a dose of aprobarbital or phenobarbital is eliminated unchanged in the urine, whereas the amount of other barbiturates excreted unchanged in the urine is negligible.
▧ Half Life :
5 to 50 hours (dose dependent)
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 short-term treatment of insomnia.
Tương Tác Thuốc :
  • Aminophylline The barbiturate, pentobarbital, decreases the effect of aminophylline.
  • Bendamustine Increases levels of bendamustine by decreasing metabolism. Ethinyl Estradiol is a CYP1A2 inhibitor and concurrent administration may result in elevated plasma concentrations of bendamustine.
  • Betamethasone The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Clomifene The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, clomifene.
  • Conjugated Estrogens The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Cyclosporine The barbiturate, pentobarbital, increases the effect of cyclosporine.
  • Dexamethasone The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Diethylstilbestrol The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, diethylstilbestrol.
  • Doxycycline The anticonvulsant, pentobarbital, decreases the effect of doxycycline.
  • Estradiol The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, estradiol.
  • Estradiol valerate/Dienogest Affects CYP3A4 metabolism, decreases or effects levels of Estradiol valerate/Dienogest.
  • Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
  • Felodipine The barbiturate, pentobarbital, decreases the effect of felodipine.
  • Fludrocortisone The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Folic Acid Folic acid decreases the effect of anticonvulsant, pentobarbital.
  • Gefitinib The CYP3A4 inducer, pentobarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
  • Griseofulvin The barbiturate, pentobarbital, decreases the effect of griseofulvin.
  • Hydrocortisone The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
  • Medroxyprogesterone Acetate The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Megestrol acetate The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, megestrol.
  • Methadone The barbiturate, pentobarbital, decreases the effect of methadone.
  • Metronidazole The barbiturate, pentobarbital, decreases the effect of metronidazole.
  • Nifedipine The barbiturate, pentobarbital, decreases the effect of the calcium channel blocker, nifedipine.
  • Norethindrone This product may cause a slight decrease of contraceptive effect
  • Oxtriphylline The barbiturate, pentobarbital, decreases the effect of oxtriphylline.
  • Prednisolone The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Prednisone The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisone.
  • Quinidine The anticonvulsant, pentobarbital, decreases the effect of quinidine.
  • Roflumilast Affects CYP3A4 metabolism, decreases level or effect of roflumilast.
  • Telithromycin Pentobarbital may decrease the plasma concentration of Telithromycin. Consider alternate therapy.
  • Temsirolimus Pentobarbital may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
  • Theophylline The barbiturate, pentobarbital, decreases the effect of theophylline.
  • Tramadol Pentobarbital may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
  • Trazodone The CYP3A4 inducer, Pentobarbital, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Pentobarbital is initiated, discontinued or dose changed.
  • Triamcinolone The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, triamcinolone.
  • Trimipramine The barbiturate, Pentobarbital, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Pentobarbital is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required.
  • Triprolidine The CNS depressants, Triprolidine and Pentobarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Vandetanib Decreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
  • Verapamil Pentobarbital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Pentobarbital is initiated, discontinued or dose changed.
  • Warfarin Pentobarbital may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if pentobarbital is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Lundbeck
    Sản phẩm biệt dược : Nembutal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00312
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4737
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508399
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07422
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00499
ChemSpider
http://www.chemspider.com/Chemical-Structure.4575.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/67386-501-55
PharmGKB
http://www.pharmgkb.org/drug/PA450859
Wikipedia
http://en.wikipedia.org/wiki/Pentobarbital
RxList
http://www.rxlist.com/cgi/generic2/pentob.htm
Drugs.com
http://www.drugs.com/mtm/pentobarbital.html
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