Tìm theo
Metaxalone
Các tên gọi khác (5 ) :
  • Metassalone
  • Metaxalon
  • Metaxalona
  • Metaxalonum
  • Skelaxin
neuromuscular agents
Thuốc Gốc
Small Molecule
CAS: 1665-48-1
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C12H15NO3
PTK: 221.2524
Metaxalone (marketed by King Pharmaceuticals under the brand name Skelaxin®) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions. Its exact mechanism of action is not known, but it may be due to general central nervous system depression. It is considered to be a moderately strong muscle relaxant, with relatively low incidence of side effects. Skelaxin comes in an 800 mg scored tablet. It previously came in both 400 mg and 800 mg tablets. The 400 mg tablet has been discontinued. Possible side effects include nausea, vomiting, drowsiness and CNS side effects such as dizziness, headache, and irritability.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H15NO3
Phân tử khối
221.2524
Monoisotopic mass
221.105193351
InChI
InChI=1S/C12H15NO3/c1-8-3-9(2)5-10(4-8)15-7-11-6-13-12(14)16-11/h3-5,11H,6-7H2,1-2H3,(H,13,14)
InChI Key
InChIKey=IMWZZHHPURKASS-UHFFFAOYSA-N
IUPAC Name
5-(3,5-dimethylphenoxymethyl)-1,3-oxazolidin-2-one
Traditional IUPAC Name
metaxalone
SMILES
CC1=CC(OCC2CNC(=O)O2)=CC(C)=C1
Độ tan chảy
122 °C
Độ hòa tan
1.28e+00 g/l
logP
2.3
logS
-2.2
pKa (strongest acidic)
13.14
pKa (Strongest Basic)
-4.9
PSA
47.56 Å2
Refractivity
59.32 m3·mol-1
Polarizability
23.74 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Metaxalone is a skeletal muscle relaxant indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions. The mode of action of this drug has not been clearly identified, but may be related to its sedative properties. Metaxalone does not directly relax tense skeletal muscles in man.
Cơ Chế Tác Dụng : Metaxalone (marketed by King Pharmaceuticals under the brand name Skelaxin®) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions. Its exact mechanism of action is not known, but it may be due to general central nervous system depression. It is considered to be a moderately strong muscle relaxant, with relatively low incidence of side effects. Skelaxin comes in an 800 mg scored tablet. It previously came in both 400 mg and 800 mg tablets. The 400 mg tablet has been discontinued. Possible side effects include nausea, vomiting, drowsiness and CNS side effects such as dizziness, headache, and irritability. The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression.
Dược Động Học :
▧ Absorption :
The absolute bioavailability of metaxalone from Skelaxin tablets is not known.
▧ Volume of Distribution :
* 800 L
▧ Metabolism :
Probably hepatic.
▧ Route of Elimination :
Metaxalone is metabolized by the liver and excreted in the urine as unidentified metabolites.
▧ Half Life :
9.2 (+/- 4.8) hours
▧ Clearance :
* 68 +/- 50 L/h [Subjects received 1×400mg tablet under fasted conditions] * 66 +/- 51 L/h [Subjects received 2×400 mg tablets under fasted conditions]
Độc Tính : LD50=775mg/kg (Rat, oral); LD50=1690 mg/kg (Mouse, oral). When determining the LD50 in rats and mice, progressive sedation, hypnosis and finally respiratoryfailure were noted as the dosage increased. In dogs, no LD50 could be determined as the higher doses produced an emetic action in 15 to 30 minutes.
Chỉ Định : For the treatment of painful peripheral musculoskeletal conditions and spasticity from upper motor neuron syndromes.
Tương Tác Thuốc :
  • Triprolidine The CNS depressants, Triprolidine and Metaxalone, 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 : Sandoz
    Sản phẩm biệt dược : Metaxalone
  • Sản phẩm biệt dược : Skelaxin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00660
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=15459
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506253
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07934
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00773
ChemSpider
http://www.chemspider.com/Chemical-Structure.14709.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0185-0448-01
PharmGKB
http://www.pharmgkb.org/drug/PA164747189
Wikipedia
http://en.wikipedia.org/wiki/Metaxalone
RxList
http://www.rxlist.com/cgi/generic/metax.htm
Drugs.com
http://www.drugs.com/cdi/metaxalone.html
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