Tìm theo
Tiagabine
Các tên gọi khác (3) :
  • Gabitril
  • Tiagabina
  • Tiagabinum
Thuốc chống co giật, chống động kinh
Thuốc Gốc
Small Molecule
CAS: 115103-54-3
ATC: N03AG06
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C20H25NO2S2
PTK: 375.548
Tiagabine is an anti-convulsive medication. It is also used in the treatment for panic disorder as are a few other anticonvulsants. Though the exact mechanism by which tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
375.548
Monoisotopic mass
375.132670429
InChI
InChI=1S/C20H25NO2S2/c1-14-7-11-24-18(14)17(19-15(2)8-12-25-19)6-4-10-21-9-3-5-16(13-21)20(22)23/h6-8,11-12,16H,3-5,9-10,13H2,1-2H3,(H,22,23)/t16-/m1/s1
InChI Key
InChIKey=PBJUNZJWGZTSKL-MRXNPFEDSA-N
IUPAC Name
(3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl]piperidine-3-carboxylic acid
Traditional IUPAC Name
tiagabine
SMILES
CC1=C(SC=C1)C(=CCCN1CCC[[email protected]](C1)C(O)=O)C1=C(C)C=CS1
Độ hòa tan
2.11e-02 g/l
logP
2.6
logS
-4.2
pKa (strongest acidic)
4.14
pKa (Strongest Basic)
9.26
PSA
40.54 Å2
Refractivity
115.32 m3·mol-1
Polarizability
41.7 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Tiagabine is used primarily as an anticonvulsant for the adjunctive treatment of epilepsy. The precise mechanism by which Tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, Tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells.
Cơ Chế Tác Dụng : Tiagabine is an anti-convulsive medication. It is also used in the treatment for panic disorder as are a few other anticonvulsants. Though the exact mechanism by which tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor. Though the exact mechanism by which Tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor.
Dược Động Học :
▧ Absorption :
Tiagabine is nearly completely absorbed (>95%).
▧ Protein binding :
96%
▧ Metabolism :
Tiagabine is likely metabolized primarily by the 3A isoform subfamily of hepatic cytochrome P450.
▧ Route of Elimination :
Approximately 2% of an oral dose of tiagabine is excreted unchanged, with 25% and 63% of the remaining dose excreted into the urine and feces, respectively, primarily as metabolites.
▧ Half Life :
7-9 hours
▧ Clearance :
* 109 mL/min [Healthy subjects]
Độc Tính : mptoms most often accompanying tiagabine overdose, alone or in combination with other drugs, have included: seizures including status epilepticus in patients with and without underlying seizure disorders, nonconvulsive status epilepticus, coma, ataxia, confusion, somnolence, drowsiness, impaired speech, agitation, lethargy, myoclonus, spike wave stupor, tremors, disorientation, vomiting, hostility, and temporary paralysis. Respiratory depression was seen in a number of patients, including children, in the context of seizures.
Chỉ Định : For the treatment of partial seizures
Tương Tác Thuốc :
  • Amprenavir The strong CYP3A4 inhibitor, Amprenavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Amprenavir is initiated, discontinued or dose changed.
  • Atazanavir The strong CYP3A4 inhibitor, Atazanavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Atazanavir is initiated, discontinued or dose changed.
  • Clarithromycin The strong CYP3A4 inhibitor, Clarithromycin, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Clarithromycin is initiated, discontinued or dose changed.
  • Conivaptan The strong CYP3A4 inhibitor, Conivaptan, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Conivaptan is initiated, discontinued or dose changed.
  • Darunavir The strong CYP3A4 inhibitor, Darunavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Darunavir is initiated, discontinued or dose changed.
  • Delavirdine The strong CYP3A4 inhibitor, Delavirdine, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Delavirdine is initiated, discontinued or dose changed.
  • Fosamprenavir The strong CYP3A4 inhibitor, Fosamprenavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Fosamprenavir is initiated, discontinued or dose changed.
  • Imatinib The strong CYP3A4 inhibitor, Imatinib, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Imatinib is initiated, discontinued or dose changed.
  • Indinavir The strong CYP3A4 inhibitor, Indinavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Indinavir is initiated, discontinued or dose changed.
  • Isoniazid The strong CYP3A4 inhibitor, Isoniazid, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Isoniazid is initiated, discontinued or dose changed.
  • Itraconazole The strong CYP3A4 inhibitor, Itraconazole, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Itraconazole is initiated, discontinued or dose changed.
  • Ketoconazole The strong CYP3A4 inhibitor, Ketoconazole, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Ketoconazole is initiated, discontinued or dose changed.
  • Lopinavir The strong CYP3A4 inhibitor, Lopinavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Lopinavir is initiated, discontinued or dose changed.
  • Mefloquine Mefloquine increases the risk of seizure and is contraindicated in persons with a history of convulsions. Possible reduction in the therapeutic effect of Tiagabine when used for other indications may also occur.
  • Miconazole The strong CYP3A4 inhibitor, Miconazole, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Miconazole is initiated, discontinued or dose changed.
  • Nefazodone The strong CYP3A4 inhibitor, Nefazodone, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Nefazodone is initiated, discontinued or dose changed.
  • Nelfinavir The strong CYP3A4 inhibitor, Nelfinavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Nelfinavir is initiated, discontinued or dose changed.
  • Nicardipine The strong CYP3A4 inhibitor, Nicardipine, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Nicardipine is initiated, discontinued or dose changed.
  • Posaconazole The strong CYP3A4 inhibitor, Posaconazole, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Posaconazole is initiated, discontinued or dose changed.
  • Quinidine The strong CYP3A4 inhibitor, Quinidine, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Quinidine is initiated, discontinued or dose changed.
  • Ritonavir The strong CYP3A4 inhibitor, Ritonavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Ritonavir is initiated, discontinued or dose changed.
  • Saquinavir The strong CYP3A4 inhibitor, Saquinavir, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Saquinavir is initiated, discontinued or dose changed.
  • Telithromycin The strong CYP3A4 inhibitor, Telithromycin, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Telithromycin is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Tiagabine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of tiagabine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of tiagabine if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Gabitril 4 mg tablet
    Giá bán buôn : USD >3.9
    Đơn vị tính : tablet
  • Biệt dược thương mại : Gabitril 2 mg tablet
    Giá bán buôn : USD >4.89
    Đơn vị tính : tablet
  • Biệt dược thương mại : Gabitril 12 mg tablet
    Giá bán buôn : USD >6.4
    Đơn vị tính : tablet
  • Biệt dược thương mại : Gabitril 16 mg tablet
    Giá bán buôn : USD >12.53
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Gabitril
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