Tìm theo
Gabapentin
Các tên gọi khác (8 ) :
  • 1-(Aminomethyl)cyclohexaneacetic acid
  • Gabapentin GR
  • Gabapentina
  • Gabapentine
  • Gabapentino
  • Gabapentinum
  • Gabapetin
  • Neurontin
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 60142-96-3
ATC: N03AX12
ĐG : 4uOrtho LLC , http://www.4udr.com
CTHH: C9H17NO2
PTK: 171.2368
Gabapentin (brand name Neurontin) is a medication originally developed for the treatment of epilepsy. Presently, gabapentin is widely used to relieve pain, especially neuropathic pain. Gabapentin is well tolerated in most patients, has a relatively mild side-effect profile, and passes through the body unmetabolized.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H17NO2
Phân tử khối
171.2368
Monoisotopic mass
171.125928793
InChI
InChI=1S/C9H17NO2/c10-7-9(6-8(11)12)4-2-1-3-5-9/h1-7,10H2,(H,11,12)
InChI Key
InChIKey=UGJMXCAKCUNAIE-UHFFFAOYSA-N
IUPAC Name
2-[1-(aminomethyl)cyclohexyl]acetic acid
Traditional IUPAC Name
gabapentin
SMILES
NCC1(CC(O)=O)CCCCC1
Độ tan chảy
162-166 °C
Độ hòa tan
4490 mg/L
logP
-1.10
logS
-1.6
pKa (strongest acidic)
4.63
pKa (Strongest Basic)
9.91
PSA
63.32 Å2
Refractivity
46.33 m3·mol-1
Polarizability
18.92 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Gabapentin, an analog of GABA, is used as an anticonvulsant to treat partial seizures, amyotrophic lateral sclerosis (ALS), and painful neuropathies. Potential uses include monotherapy of refractory partial seizure disorders, and treatment of spasticity in multiple sclerosis, tremor. mood disorders, and attenuation of disruptive behaviors in dementia. Gabapentin has high lipid solubility, is not metabolized by the liver, has no protein binding, and doesn't possess the usual drug interactions.
Cơ Chế Tác Dụng : Gabapentin (brand name Neurontin) is a medication originally developed for the treatment of epilepsy. Presently, gabapentin is widely used to relieve pain, especially neuropathic pain. Gabapentin is well tolerated in most patients, has a relatively mild side-effect profile, and passes through the body unmetabolized. Gabapentin interacts with cortical neurons at auxillary subunits of voltage-sensitive calcium channels. Gabapentin increases the synaptic concentration of GABA, enhances GABA responses at non-synaptic sites in neuronal tissues, and reduces the release of mono-amine neurotransmitters. One of the mechanisms implicated in this effect of gabapentin is the reduction of the axon excitability measured as an amplitude change of the presynaptic fibre volley (FV) in the CA1 area of the hippocampus. This is mediated through its binding to presynaptic NMDA receptors. Other studies have shown that the antihyperalgesic and antiallodynic effects of gabapentin are mediated by the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors. Gabapentin has also been shown to bind and activate the adenosine A1 receptor.
Dược Động Học :
▧ Absorption :
Rapid. Absorbed in part by the L-amino acid transport system, which is a carrier-mediated, saturable transport system; as the dose increases, bioavailability decreases. Bioavailability ranges from approximately 60% for a 900 mg dose per day to approximately 27% for a 4800 milligram dose per day. Food has a slight effect on the rate and extent of absorption of gabapentin (14% increase in AUC).
▧ Volume of Distribution :
* 58±6 L
▧ Protein binding :
Less than 3% of gabapentin circulates bound to plasma protein.
▧ Metabolism :
All pharmacological actions following gabapentin administration are due to the activity of the parent compound; gabapentin is not appreciably metabolized in humans.
▧ Route of Elimination :
Gabapentin is eliminated from the systemic circulation by renal excretion as unchanged drug. Gabapentin is not appreciably metabolized in humans.
▧ Half Life :
5-7 hours
▧ Clearance :
* 190 mL/min
Độc Tính : Symptoms of overdose include ataxia, labored breathing, ptosis, sedation, hypoactivity, and excitation.
Chỉ Định : For the management of postherpetic neuralgia in adults and as adjunctive therapy in the treatment of partial seizures with and without secondary generalization in patients over 12 years of age with epilepsy.
Tương Tác Thuốc :
  • Ethotoin Increases the effect of hydantoin
  • Fosphenytoin Gabapentin may increase the effect of fosphenytoin.
  • Mephenytoin Increases the effect of hydantoin
  • Phenytoin Gabapentin may increase the therapeutic and adverse effects of phenytoin.
  • Triprolidine The CNS depressants, Triprolidine and Gabapentin, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aclonium
  • Công ty :
    Sản phẩm biệt dược : Gralise
  • Công ty :
    Sản phẩm biệt dược : Neurontin
  • Công ty :
    Sản phẩm biệt dược : Novo-Gabapentin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00996
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3446
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506529
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00332
ChemSpider
http://www.chemspider.com/Chemical-Structure.3328.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0228-2665-11
PharmGKB
http://www.pharmgkb.org/drug/PA449720
Wikipedia
http://en.wikipedia.org/wiki/Gabapentin
RxList
http://www.rxlist.com/cgi/generic/gabapent.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/neu1289.shtml
Drugs.com
http://www.drugs.com/gabapentin.html
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