Tìm theo
Carisoprodol
Các tên gọi khác (15 ) :
  • (+-)-2-Methyl-2-propyl-1,3-propanediol carbamate isopropylcarbamate
  • (1-Methylethyl)carbamic acid 2-(((aminocarbonyl)oxy)methyl)-2-methylpentyl ester
  • (RS)-2-{[(aminocarbonyl)oxy]methyl}-2-methylpentyl isopropylcarbamate
  • 2-Methyl-2-propyl-1,3-propanediol carbamate isopropylcarbamate
  • 2-Methyl-2-propyltrimethylene carbamate isopropylcarbamate
  • Carbamic acid 2-isopropylcarbamoyloxymethyl-2-methyl-pentyl ester
  • Carisoprodate
  • Carisoprodol
  • Carisoprodolum
  • Isobamate
  • Isomeprobamate
  • Isopropyl meprobamate
  • Isopropylmeprobamate
  • N-Isopropy-2-methyl-2-propyl-1,3-propanediol dicarbamate
  • Someprobamate
muscle relaxants central, neuromuscular agents, muscle relaxant skeletal
Thuốc Gốc
Small Molecule
CAS: 78-44-4
ATC: M03BA02
ĐG : Aidarex Pharmacuticals LLC , http://www.aidarex.com
CTHH: C12H24N2O4
PTK: 260.33
A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H24N2O4
Phân tử khối
260.33
Monoisotopic mass
260.173607266
InChI
InChI=1S/C12H24N2O4/c1-5-6-12(4,7-17-10(13)15)8-18-11(16)14-9(2)3/h9H,5-8H2,1-4H3,(H2,13,15)(H,14,16)
InChI Key
InChIKey=OFZCIYFFPZCNJE-UHFFFAOYSA-N
IUPAC Name
2-methyl-2-({[(propan-2-yl)carbamoyl]oxy}methyl)pentyl carbamate
Traditional IUPAC Name
carisoprodol
SMILES
CCCC(C)(COC(N)=O)COC(=O)NC(C)C
Độ tan chảy
89-91
Độ hòa tan
300 mg/L (at 25 °C)
logP
2.1
logS
-2.5
pKa (strongest acidic)
15.06
PSA
90.65 Å2
Refractivity
67.1 m3·mol-1
Polarizability
28.77 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
0
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Carisoprodol is used as a skeletal muscle relaxant. One of its metabolites, meprobamate, is available as an anxiolytic agent.
Cơ Chế Tác Dụng : A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202) Carisoprodol is a central nervous system depressant that acts as a sedative and skeletal muscle relaxant. Rather than acting directly on skeletal muscle, carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. Its exact mechanism of action is not yet known.
Dược Động Học :

▧ Protein binding :
60%
▧ Metabolism :
Hepatic. Metabolized in the liver via the cytochrome P450 oxidase isozyme CYP2C19.
▧ Route of Elimination :
Carisoprodol is eliminated by both renal and non-renal routes.
▧ Half Life :
8 hours
▧ Clearance :
* oral cl=0.772 L/hour/kg [Women] * oral cl=0.38 L/hour/kg [Men]
Độc Tính : Symptoms of overdose include drowsiness, giddiness, nausea, indigestion, or rash. Other adverse effects attributed to therapeutic use of carisoprodol include dizziness, irritability, insomnia, diplopia, temporary loss of vision, ataxia, weakness, headache, and dysarthria. Non-CNS adverse effects include gastrointestinal complaints, tachycardia, and postural hypotension. Patients sensitive to sulfites or tartrazine may experience wheezing, allergic rashes including erythema multiforme, or anaphylaxis after using some preparations of carisoprodol which contain such additives
Chỉ Định : For the relief of discomfort associated with acute, painful, musculoskeletal conditions.
Tương Tác Thuốc :
  • Delavirdine Strong CYP2C19 inhibitors such as delavirdine may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Droperidol Droperidol may enhance the CNS depressant effect of carisoprodol. Consider dose reductions of droperidol or of other CNS agents with concomitant use.
  • Fluconazole Strong CYP2C19 inhibitors such as fluconazole may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Fluvoxamine Strong CYP2C19 inhibitors such as fluvoxamine may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Gemfibrozil Strong CYP2C19 inhibitors such as gemfibrozil may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Isoniazid Strong CYP2C19 inhibitors such as isoniazid may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Methotrimeprazine Carisoprodol, a CNS depressant, may enhance the CNS depressant effect of methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants like carisoprodol. Reduce the dosage of CNS depressants by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose has been established. Monitor for increased CNS depression with concomitant therapy.
  • Modafinil Strong CYP2C19 inhibitors such as modafinil may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Sitaxentan Strong CYP2C19 inhibitors such as sitaxentan may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Ticlopidine Ticlopidine may decrease the metabolism and clearance of Carisoprodol. Consider alternate therapy or monitor for adverse/toxic effects of Carisoprodol if Ticlopidine is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Carisoprodol, 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
  • Biệt dược thương mại : Carisoprodol powder
    Giá bán buôn : USD >1.17
    Đơn vị tính : g
  • Biệt dược thương mại : Soma 250 mg tablet
    Giá bán buôn : USD >3.24
    Đơn vị tính : tablet
  • Biệt dược thương mại : Soma Compound 200-325 mg tablet
    Giá bán buôn : USD >4.58
    Đơn vị tính : tablet
  • Biệt dược thương mại : Soma 350 mg tablet
    Giá bán buôn : USD >5.75
    Đơn vị tính : tablet
  • Biệt dược thương mại : Flexall 7% gel
    Giá bán buôn : USD >0.05
    Đơn vị tính : g
  • Biệt dược thương mại : Flexall 16% gel
    Giá bán buôn : USD >0.06
    Đơn vị tính : g
  • Biệt dược thương mại : Flexall plus gel
    Giá bán buôn : USD >0.08
    Đơn vị tính : g
  • Biệt dược thương mại : Carisoprodol 350 mg tablet
    Giá bán buôn : USD >0.57
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Carisoma
  • Công ty : Genovate
    Sản phẩm biệt dược : Gencari
  • Công ty : Genovate
    Sản phẩm biệt dược : Genesafe
  • Công ty : Hwang's
    Sản phẩm biệt dược : Hiranin
  • Công ty : Finadiet
    Sản phẩm biệt dược : Listaflex
  • Công ty :
    Sản phẩm biệt dược : Sanoma
  • Công ty : Meda
    Sản phẩm biệt dược : Soma
  • Công ty : Newport
    Sản phẩm biệt dược : Tensaprin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00395
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2576
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506377
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07927
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00768
ChemSpider
http://www.chemspider.com/Chemical-Structure.2478.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/12634-437-91
PharmGKB
http://www.pharmgkb.org/drug/PA448809
Wikipedia
http://en.wikipedia.org/wiki/Carisoprodol
RxList
http://www.rxlist.com/cgi/generic/carisop.htm
Drugs.com
http://www.drugs.com/carisoprodol.html
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