Tìm theo
Levetiracetam
Các tên gọi khác (5 ) :
  • e Keppra
  • Keppra
  • Levetiracetam
  • Levetiracetamum
  • Levitiracetam
nootropic agents, anticonvulsants
Thuốc Gốc
Small Molecule
CAS: 102767-28-2
ATC: N03AX14
ĐG : Actavis Group , http://www.actavis.com
CTHH: C8H14N2O2
PTK: 170.209
Levetiracetam is an anticonvulsant medication used to treat epilepsy. Levetiracetam may selectively prevent hypersynchronization of epileptiform burst firing and propagation of seizure activity. Levetiracetam binds to the synaptic vesicle protein SV2A, which is thought to be involved in the regulation of vesicle exocytosis. Although the molecular significance of levetiracetam binding to synaptic vesicle protein SV2A is not understood, levetiracetam and related analogs showed a rank order of affinity for SV2A which correlated with the potency of their antiseizure activity in audiogenic seizure-prone mice.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H14N2O2
Phân tử khối
170.209
Monoisotopic mass
170.105527702
InChI
InChI=1S/C8H14N2O2/c1-2-6(8(9)12)10-5-3-4-7(10)11/h6H,2-5H2,1H3,(H2,9,12)/t6-/m1/s1
InChI Key
InChIKey=HPHUVLMMVZITSG-ZCFIWIBFSA-N
IUPAC Name
(2R)-2-(2-oxopyrrolidin-1-yl)butanamide
Traditional IUPAC Name
levetiracetam
SMILES
CC[C@@H](N1CCCC1=O)C(N)=O
Độ hòa tan
2.98e+02 g/l
logP
-0.6
logS
0.24
pKa (strongest acidic)
16.09
pKa (Strongest Basic)
-1
PSA
63.4 Å2
Refractivity
44.08 m3·mol-1
Polarizability
17.78 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Cơ Chế Tác Dụng : Levetiracetam is an anticonvulsant medication used to treat epilepsy. Levetiracetam may selectively prevent hypersynchronization of epileptiform burst firing and propagation of seizure activity. Levetiracetam binds to the synaptic vesicle protein SV2A, which is thought to be involved in the regulation of vesicle exocytosis. Although the molecular significance of levetiracetam binding to synaptic vesicle protein SV2A is not understood, levetiracetam and related analogs showed a rank order of affinity for SV2A which correlated with the potency of their antiseizure activity in audiogenic seizure-prone mice. The precise mechanism(s) by which levetiracetam exerts its antiepileptic effect is unknown. The antiepileptic activity of levetiracetam was assessed in a number of animal models of epileptic seizures. Levetiracetam did not inhibit single seizures induced by maximal stimulation with electrical current or different chemoconvulsants and showed only minimal activity in submaximal stimulation and in threshold tests. Protection was observed, however, against secondarily generalized activity from focal seizures induced by pilocarpine and kainic acid, two chemoconvulsants that induce seizures that mimic some features of human complex partial seizures with secondary generalization. Levetiracetam also displayed inhibitory properties in the kindling model in rats, another model of human complex partial seizures, both during kindling development and in the fully kindled state. The predictive value of these animal models for specific types of human epilepsy is uncertain. Levetiracetam is thought to stimulate synaptic vesicle protein 2A (SV2A), inhibiting neurotransmitter release.
Dược Động Học :
▧ Absorption :
Rapidly and almost completely absorbed after oral administration (99%). Peak plasma concentrations occurring in about an hour following oral administration in fasted subjects.
▧ Protein binding :
Very low (<10%)
▧ Metabolism :
The major metabolic pathway of levetiracetam (24% of dose) is an enzymatic hydrolysis of the acetamide group. No CYP450 metabolism detected.
▧ Route of Elimination :
Sixty-six percent (66%) of the dose is renally excreted unchanged. The metabolites have no known pharmacological activity and are renally excreted. The mechanism of excretion is glomerular filtration with subsequent partial tubular reabsorption.
▧ Half Life :
6-8 hours
▧ Clearance :
* 0.96 mL/min/kg
Độc Tính : Side effects include aggression, agitation, coma, drowsiness, reduced consciousness, slowed breathing
Chỉ Định : Used as adjunctive therapy in the treatment of partial onset seizures in adults and children 4 years of age and older with epilepsy.
Tương Tác Thuốc :
  • Carbamazepine Concomitant therapy may results in additive adverse CNS effects.
  • Triprolidine The CNS depressants, Triprolidine and Levetiracetam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Keppra
  • Công ty :
    Sản phẩm biệt dược : Levetiractam
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01202
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=441341
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508406
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07841
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00709
ChemSpider
http://www.chemspider.com/Chemical-Structure.390096.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0121-4802-05
PharmGKB
http://www.pharmgkb.org/drug/PA450206
Wikipedia
http://en.wikipedia.org/wiki/Levetiracetam
RxList
http://www.rxlist.com/cgi/generic3/keppra.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/kep1561.shtml
Drugs.com
http://www.drugs.com/cdi/levetiracetam.html
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