Tìm theo
Meprobamate
Các tên gọi khác (6 ) :
  • Equanil
  • Meprobamat
  • Meprobamato
  • Meprobamatum
  • Meprobamic acid
  • Miltown
Thuốc chống lo âu, hoảng sợ
Thuốc Gốc
Small Molecule
CAS: 57-53-4
ATC: N05BC01
ĐG : C.O. Truxton Inc.
CTHH: C9H18N2O4
PTK: 218.2502
A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of anxiety disorders, and also for the short-term management of insomnia but has largely been superseded by the benzodiazepines. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) Meprobamate is a controlled substance in the U.S.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H18N2O4
Phân tử khối
218.2502
Monoisotopic mass
218.126657074
InChI
InChI=1S/C9H18N2O4/c1-3-4-9(2,5-14-7(10)12)6-15-8(11)13/h3-6H2,1-2H3,(H2,10,12)(H2,11,13)
InChI Key
InChIKey=NPPQSCRMBWNHMW-UHFFFAOYSA-N
IUPAC Name
2-[(carbamoyloxy)methyl]-2-methylpentyl carbamate
Traditional IUPAC Name
meprobamate
SMILES
CCCC(C)(COC(N)=O)COC(N)=O
Độ tan chảy
105 °C
Độ hòa tan
4700 mg/L (at 25 °C)
logP
0.70
logS
-1.67
pKa (strongest acidic)
15.17
PSA
104.64 Å2
Refractivity
53.04 m3·mol-1
Polarizability
22.65 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
0
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Meprobamate is an anxiolytic drug. It was the best selling minor tranquilizer for a time but has largely been replaced by benzodiazepines. Meprobamate has most of the pharmacological effects and dangers of the barbiturates (though it was marketed as being safer). However, it is less sedating at effective doses. It is reported to have some anticonvulsant properties against absence seizures, but can exacerbate generalized tonic-clonic seizures. It has also been used as a hypnotic (sleeping pill). However, its is currently only licensed as an anxiolytic and it is a third or fourth-order choice.
Cơ Chế Tác Dụng : A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of anxiety disorders, and also for the short-term management of insomnia but has largely been superseded by the benzodiazepines. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) Meprobamate is a controlled substance in the U.S. Meprobamate's mechanism of action is not known. It has been shown in animal studies to have effects at multiple sites in the central nervous system, including the thalamus and limbic system. Meprobamate binds to GABAA receptors which interrupt neuronal communication in the reticular formation and spinal cord, causing sedation and altered perception of pain.
Dược Động Học :
▧ Absorption :
Well absorbed from the gastrointestinal tract.
▧ Metabolism :
Hepatic.
▧ Half Life :
Plasma half-life is about 10 hours.
Độc Tính : Symptoms of overdose include coma, drowsiness, loss of muscle control, severely impaired breathing, shock, sluggishness, and unresponsiveness. Death has been reported with ingestion of as little as 12 g meprobamate and survival with as much as 40 g.
Chỉ Định : For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Wyeth
    Sản phẩm biệt dược : Equanil
  • Công ty :
    Sản phẩm biệt dược : Meprospan
  • Sản phẩm biệt dược : Miltown
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00371
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4064
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508142
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00376
ChemSpider
http://www.chemspider.com/Chemical-Structure.3924.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/23155-128-03
PharmGKB
http://www.pharmgkb.org/drug/PA450377
Wikipedia
http://en.wikipedia.org/wiki/Meprobamate
RxList
http://www.rxlist.com/cgi/generic2/meprobamate.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/mil1268.shtml
Drugs.com
http://www.drugs.com/cdi/meprobamate.html
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