Tìm theo
Clonazepam
Các tên gọi khác (6 ) :
  • 1,3-dihydro-7-Nitro-5-(2-chlorophenyl)-2H-1,4.benzodiazepin-2-one
  • 5-(2-Chloro-phenyl)-7-nitro-1,3-dihydro-benzo[e][1,4]diazepin-2-one
  • 5-(2-Chlorophenyl)-7-nitro-1H-benzo[e][1,4]diazepin-2(3H)-one
  • 5-(O-Chlorophenyl)-7-nitro-1,3-dihydro-2H-1,4-benzodiazepin-2-one
  • CLONAZEPAM
  • Clonazepamum
Thuốc chống co giật, chống động kinh
Thuốc Gốc
Small Molecule
CAS: 1622-61-3
ATC: N03AE01
ĐG : Actavis Group , http://www.actavis.com
CTHH: C15H10ClN3O3
PTK: 315.711
An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of gamma-aminobutyric acid receptor responses. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H10ClN3O3
Phân tử khối
315.711
Monoisotopic mass
315.041068908
InChI
InChI=1S/C15H10ClN3O3/c16-12-4-2-1-3-10(12)15-11-7-9(19(21)22)5-6-13(11)18-14(20)8-17-15/h1-7H,8H2,(H,18,20)
InChI Key
InChIKey=DGBIGWXXNGSACT-UHFFFAOYSA-N
IUPAC Name
5-(2-chlorophenyl)-7-nitro-2,3-dihydro-1H-1,4-benzodiazepin-2-one
Traditional IUPAC Name
clonazepam
SMILES
[O-][N+](=O)C1=CC2=C(NC(=O)CN=C2C2=CC=CC=C2Cl)C=C1
Độ tan chảy
238-240
Độ hòa tan
100 mg/L (at 25 °C)
logP
2.41
logS
-4.5
pKa (strongest acidic)
11.89
pKa (Strongest Basic)
1.86
PSA
87.28 Å2
Refractivity
84.02 m3·mol-1
Polarizability
29.59 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Clonazepam, a benzodiazepine, is used primarily as an anticonvulsant in the treatment of absence seizures, petit mal variant seizures (Lennox-Gastaut syndrome), akinetic and myoclonic seizures, and nocturnal myoclonus. It enhances the activity of gamma aminobutyric acid (GABA), which is a major inhibitory neurotransmitter in the central nervous system. In animals, convulsions are antagonized occurs following administration of clonazepam. In humans, clonazepam suppresses the spike and wave discharge in absence seizures (petit mal) and decreases the frequency, amplitude, duration, and spread of discharge in minor motor seizures.
Cơ Chế Tác Dụng : An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of gamma-aminobutyric acid receptor responses. [PubChem] Allosteric interactions between central benzodiazepine receptors and gamma-aminobutyric acid (GABA) receptors potentiate the effects of GABA. As GABA is an inhibitory neurotransmitter, this results in increased inhibition of the ascending reticular activating system. Benzodiazepines, in this way, block the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
Dược Động Học :
▧ Absorption :
Clonazepam is rapidly and completely absorbed after oral administration. The absolute bioavailability of clonazepam is about 90%. Cmax, oral administration = 1 -4 hours.
▧ Protein binding :
85% bound to plasma proteins.
▧ Metabolism :
Hepatic (cytochrome P450, including CYP3A). Biotransformation occurs mainly by reduction of the 7-nitro group to the 4-amino derivative. This derivative can be acetylated, hydroxylated, and glucuronidated.
▧ Route of Elimination :
Clonazepam is highly metabolized, with less than 2% unchanged clonazepam being excreted in the urine. Metabolites of Klonopin are excreted by the kidneys. Clonazepam also undergoes acetylation via NAT2.
▧ Half Life :
30-40 hours
Độc Tính : Somnolence, confusion, coma, and diminished reflexes. The most commonly reported adverse event when clonazepam is used for seizure disorders is CNS depression. LD50, oral, rats = >15000 mg/kg.
Chỉ Định : Clonazepam is used as an anticonvulsant in the treatment of the Lennox-Gastaut syndrome (petit mal variant), akinetic and myoclonic seizures. It can also be used for the treatment of panic disorders.
Tương Tác Thuốc :
  • Cimetidine Cimetidine may increase the effect of the benzodiazepine, clonazepam.
  • Clozapine Increased risk of toxicity
  • Fluconazole Fluconazole may increase the effect of the benzodiazepine, clonazepam.
  • Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, clonazepam.
  • Itraconazole Itraconazole may increase the effect of the benzodiazepine, clonazepam.
  • Kava Kava may increase the effect of the benzodiazepine, clonazepam.
  • Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, clonazepam.
  • Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, clonazepam.
  • Omeprazole Omeprazole may increase the effect of the benzodiazepine, clonazepam.
  • Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, clonazepam.
  • Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, clonazepam.
  • St. John's Wort St. John's Wort may decrease the effect of the benzodiazepine, clonazepam.
  • Telithromycin Telithromycin may reduce clearance of Clonazepam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Clonazepam if Telithromycin is initiated, discontinued or dose changed.
  • Tipranavir Tipranavir may decrease the metabolism and clearance of Clonazepam. Consider alternate therapy or monitor for Clonazepam toxic effects if Tipranavir is initiated or dose increased.
  • Triprolidine The CNS depressants, Triprolidine and Clonazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Vigabatrin Vigabatrin increases Cmax of clonazepam by 30% and decreases Tmax by 45%
  • Voriconazole Voriconazole may increase the serum concentration of clonazepam by decreasing its metabolism. Monitor for clonazepam toxicity if voriconazole is initiated or dose increased.
Liều Lượng & Cách Dùng : Tablet - Oral - 0.5 mg, 1 mg, 2 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : AWD
    Sản phẩm biệt dược : Antelepsin
  • Công ty : Roche
    Sản phẩm biệt dược : Iktorivil
  • Công ty : Roche
    Sản phẩm biệt dược : Klonopin
  • Công ty : Roche
    Sản phẩm biệt dược : Rivotril
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01068
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2802
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507677
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00280
ChemSpider
http://www.chemspider.com/Chemical-Structure.2700.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50019213
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0004-0068-01
PharmGKB
http://www.pharmgkb.org/drug/PA449050
Wikipedia
http://en.wikipedia.org/wiki/Clonazepam
RxList
http://www.rxlist.com/cgi/generic/clonaz.htm
Drugs.com
http://www.drugs.com/clonazepam.html
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