Tìm theo
Methylphenobarbital
Các tên gọi khác (15 ) :
  • 1-Methylphenobarbital
  • 5-Ethyl-1-methyl-5-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrione
  • 5-Ethyl-1-methyl-5-phenyl-pyrimidine-2,4,6-trione
  • 5-Ethyl-1-methyl-5-phenylbarbituric acid
  • Enphenemal
  • Mebaral
  • Mephobarbital
  • Mephobarbitone
  • Méthylphénobarbital
  • Methylphenobarbital
  • Methylphenobarbitalum
  • Methylphenobarbitone
  • Metilfenobarbital
  • Metilfenobarbitale
  • N-Methylphenobarbital
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 115-38-8
ATC: N03AA01
ĐG : Bayer Healthcare , http://www.bayerhealthcare.com
CTHH: C13H14N2O3
PTK: 246.2619
A barbiturate that is metabolized to phenobarbital. It has been used for similar purposes, especially in epilepsy, but there is no evidence mephobarbital offers any advantage over phenobarbital. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H14N2O3
Phân tử khối
246.2619
Monoisotopic mass
246.100442324
InChI
InChI=1S/C13H14N2O3/c1-3-13(9-7-5-4-6-8-9)10(16)14-12(18)15(2)11(13)17/h4-8H,3H2,1-2H3,(H,14,16,18)
InChI Key
InChIKey=ALARQZQTBTVLJV-UHFFFAOYSA-N
IUPAC Name
5-ethyl-1-methyl-5-phenyl-1,3-diazinane-2,4,6-trione
Traditional IUPAC Name
mephobarbital
SMILES
CCC1(C(=O)NC(=O)N(C)C1=O)C1=CC=CC=C1
Độ tan chảy
176 °C
Độ hòa tan
Slightly soluble
logP
1.84
logS
-2.5
pKa (strongest acidic)
8.4
PSA
66.48 Å2
Refractivity
64.64 m3·mol-1
Polarizability
24.62 Å3
Rotatable Bond Count
2
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
7.8
Dược Lực Học : Methylphenobarbital, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia.
Cơ Chế Tác Dụng : A barbiturate that is metabolized to phenobarbital. It has been used for similar purposes, especially in epilepsy, but there is no evidence mephobarbital offers any advantage over phenobarbital. [PubChem] Methylphenobarbital 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.
Dược Động Học :
▧ Absorption :
Approximately 50% of an oral dose of mephobarbital is absorbed from the gastrointestinal tract.
▧ Protein binding :
70-76%
▧ Metabolism :
Hepatic, primarily by the hepatic microsomal enzyme system. About 75% of a single oral dose of mephobarbital is metabolized to phenobarbital in 24 hours.
▧ Half Life :
34 (range 11-67) hours
Chỉ Định : For the relief of anxiety, tension, and apprehension, also used as an anticonvulsant for the treatment of epilepsy.
Tương Tác Thuốc :
  • Aminophylline The barbiturate, methylphenobarbital, decreases the effect of aminophylline.
  • Betamethasone The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Clomifene The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, clomifene.
  • Conjugated Estrogens The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, conjugated estrogens.
  • Cyclosporine The barbiturate, methylphenobarbital, increases the effect of cyclosporine.
  • Delavirdine The anticonvulsant, methylphenobarbital, decreases the effect of delavirdine.
  • Dexamethasone The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Diethylstilbestrol The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, diethylstilbestrol.
  • Doxycycline The anticonvulsant, methylphenobarbital, decreases the effect of doxycycline.
  • Estradiol The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, estradiol.
  • Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
  • Felodipine The barbiturate, methylphenobarbital, decreases the effect of felodipine.
  • Fludrocortisone The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Folic Acid Folic acid decreases the effect of anticonvulsant, methylphenobarbital.
  • Gefitinib The CYP3A4 inducer, methylphenobarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
  • Griseofulvin The barbiturate, methylphenobarbital, decreases the effect of griseofulvin.
  • Hydrocortisone The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
  • Medroxyprogesterone Acetate The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
  • Megestrol acetate The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, megestrol.
  • Methadone The barbiturate, methylphenobarbital, decreases the effect of methadone.
  • Metronidazole The barbiturate, methylphenobarbital, decreases the effect of metronidazole.
  • Nifedipine The barbiturate, methylphenobarbital, decreases the effect of the calcium channel blocker, nifedipine.
  • Norethindrone This product may cause a slight decrease of contraceptive effect
  • Oxtriphylline The barbiturate, methylphenobarbital, decreases the effect of oxtriphylline.
  • Prednisolone The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, prednisolone.
  • Prednisone The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, prednisone.
  • Quinidine The anticonvulsant, methylphenobarbital, decreases the effect of quinidine.
  • Theophylline The barbiturate, methylphenobarbital, decreases the effect of theophylline.
  • Triamcinolone The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, triamcinolone.
  • Verapamil Methylphenobarbital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Methylphenobarbital is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Mebaral 50 mg tablet
    Giá bán buôn : USD >1.28
    Đơn vị tính : tablet
  • Biệt dược thương mại : Mebaral 100 mg tablet
    Giá bán buôn : USD >1.73
    Đơn vị tính : tablet
  • Biệt dược thương mại : Mentax 1% cream
    Giá bán buôn : USD >4.0
    Đơn vị tính : g
  • Biệt dược thương mại : Mebaral 32 mg tablet
    Giá bán buôn : USD >0.87
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty : Lundbeck A/S
    Sản phẩm biệt dược : Mebaral
  • Công ty :
    Sản phẩm biệt dược : Mephyltaletten
  • Công ty :
    Sản phẩm biệt dược : Phemiton
  • Công ty :
    Sản phẩm biệt dược : Phemitone
  • Công ty :
    Sản phẩm biệt dược : Phenmiton
  • Công ty :
    Sản phẩm biệt dược : Prominal
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00849
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=8271
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505197
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07829
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00700
ChemSpider
http://www.chemspider.com/Chemical-Structure.7972.html
PharmGKB
http://www.pharmgkb.org/drug/PA450374
Wikipedia
http://en.wikipedia.org/wiki/Mephobarbital
RxList
http://www.rxlist.com/cgi/generic2/mephobarbital.htm
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