Tìm theo
Baclofen
Các tên gọi khác (12 ) :
  • (+-)-Baclofen
  • 4-Amino-3-(4-chlorophenyl)butyric acid
  • Baclofene
  • Baclofeno
  • Baclofenum
  • beta-(4-Chlorophenyl)gaba
  • beta-(Aminomethyl)-4-chlorobenzenepropanoic acid
  • beta-(Aminomethyl)-P-chlorohydrocinnamic acid
  • beta-(P-Chlorophenyl)-gamma-aminobutyric acid
  • DL-4-Amino-3-P-chlorophenylbutanoic acid
  • DL-Baclofen
  • gamma-Amino-beta-(P-chlorophenyl)butyric acid
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 1134-47-0
ATC: M03BX01
ĐG : Actavis Group , http://www.actavis.com
CTHH: C10H12ClNO2
PTK: 213.661
Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant. Baclofen stimulates GABA-B receptors leading to decreased frequency and amplitude of muscle spasms. It is especially useful in treating muscle spasticity associated with spinal cord injury. It appears to act primarily at the spinal cord level by inhibiting spinal polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H12ClNO2
Phân tử khối
213.661
Monoisotopic mass
213.05565634
InChI
InChI=1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14)
InChI Key
InChIKey=KPYSYYIEGFHWSV-UHFFFAOYSA-N
IUPAC Name
4-amino-3-(4-chlorophenyl)butanoic acid
Traditional IUPAC Name
(+-)-baclofen
SMILES
NCC(CC(O)=O)C1=CC=C(Cl)C=C1
Độ tan chảy
206-208 °C
Độ hòa tan
2090 mg/L
logP
1.3
logS
-2.5
pKa (strongest acidic)
3.89
pKa (Strongest Basic)
9.79
PSA
63.32 Å2
Refractivity
54.83 m3·mol-1
Polarizability
21.13 Å3
Rotatable Bond Count
4
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 : Baclofen is a muscle relaxant and antispastic. Baclofen is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. Although Baclofen is an analog of the putative inhibitory neurotransmitter gamma-aminobutyric acid (GABA), there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects. In studies with animals, Baclofen has been shown to have general CNS depressant properties as indicated by the production of sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression. Baclofen is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Baclofen is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.
Cơ Chế Tác Dụng : Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant. Baclofen stimulates GABA-B receptors leading to decreased frequency and amplitude of muscle spasms. It is especially useful in treating muscle spasticity associated with spinal cord injury. It appears to act primarily at the spinal cord level by inhibiting spinal polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways. Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Baclofen is not fully known. It is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect.
Dược Động Học :
▧ Absorption :
Rapidly and almost completely absorbed from the GI tract.
▧ Volume of Distribution :
* 59 L
▧ Protein binding :
30%
▧ Metabolism :
~ 15% of the dose is metabolized in the liver, primarily by deamination. 70-80% of the dose is excreted unchanged or as metabolites in urine and the remainder is excreted in feces.
▧ Route of Elimination :
In a study using radiolabeled baclofen, approximately 85% of the dose was excreted unchanged in the urine and feces. Baclofen is excreted primarily by the kidney as unchanged drug; 70 - 80% of a dose appears in the urine as unchanged drug. The remainder is excreted as unchanged drug in the feces or as metabolites in the urine and feces.
▧ Half Life :
2.5-4 hours
▧ Clearance :
* 180 mL/min
Độc Tính : LD50=45 mg/kg (male mice, IV); LD50=78 mg/kg (male rat, IV)
Chỉ Định : For the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity.
Tương Tác Thuốc :
  • Triprolidine The CNS depressants, Triprolidine and Baclofen, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Injection, solution - Intrathecal - 0.05 mg/ml
Injection, solution - Intrathecal - 0.5 mg/ml
Injection, solution - Intrathecal - 2 mg/ml
Tablet - Oral - 10 mg
Tablet - Oral - 20 mg
Dữ Kiện Thương Mại
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Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00181
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2284
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508181
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00241
ChemSpider
http://www.chemspider.com/Chemical-Structure.2197.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=24182
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0091-3351-01
PharmGKB
http://www.pharmgkb.org/drug/PA448533
Wikipedia
http://en.wikipedia.org/wiki/Baclofen
RxList
http://www.rxlist.com/cgi/generic/baclofen.htm
Drugs.com
http://www.drugs.com/baclofen.html
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