Tìm theo
Chlorzoxazone
Các tên gọi khác (16 ) :
  • 2-hydroxy-5-chlorobenzoxazole
  • 5-chloro-2-Benzoxazolinone
  • 5-chloro-2-Benzoxazolol
  • 5-chloro-2-Benzoxazolone
  • 5-chloro-2-Hydroxybenzoxazole
  • 5-chloro-2(3H)-benzoxazolone
  • 5-chloro-3H-benzooxazol-2-one
  • 5-Chlorobenzoxazolidone
  • 5-chlorobenzoxazolin-2-one
  • Chlorzoxane
  • Chlorzoxazon
  • Chlorzoxazona
  • Chlorzoxazone
  • Chlorzoxazonum
  • Clorzoxazona
  • Clorzoxazone
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 95-25-0
ATC: M03BB03
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C7H4ClNO2
PTK: 169.565
A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
169.565
Monoisotopic mass
168.993056084
InChI
InChI=1S/C7H4ClNO2/c8-4-1-2-6-5(3-4)9-7(10)11-6/h1-3H,(H,9,10)
InChI Key
InChIKey=TZFWDZFKRBELIQ-UHFFFAOYSA-N
IUPAC Name
5-chloro-2,3-dihydro-1,3-benzoxazol-2-one
Traditional IUPAC Name
chlorzoxazone
SMILES
ClC1=CC2=C(OC(=O)N2)C=C1
Độ tan chảy
191-191.5
Độ hòa tan
1000 mg/L
logP
1.6
logS
-1.8
pKa (strongest acidic)
9.39
pKa (Strongest Basic)
-2.2
PSA
38.33 Å2
Refractivity
41.07 m3·mol-1
Polarizability
14.94 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Dược Lực Học : Chlorzoxazone, a synthetic compound, inhibits antigen-induced bronchospasms and, hence, is used to treat asthma and allergic rhinitis. Chlorzoxazone is used as an ophthalmic solution to treat conjunctivitis and is taken orally to treat systemic mastocytosis and ulcerative colitis. Chlorzoxazone is also a centrally-acting agent for painful musculoskeletal conditions. Data available from animal experiments as well as human study indicate that chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain where it inhibits multisynaptic reflex a.c. involved in producing and maintaining skeletal muscle spasm of varied etiology. The clinical result is a reduction of the skeletal muscle spasm with relief of pain and increased mobility of the involved muscles.
Cơ Chế Tác Dụng : A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202) Chlorzoxazone inhibits degranulation of mast cells, subsequently preventing the release of histamine and slow-reacting substance of anaphylaxis (SRS-A), mediators of type I allergic reactions. Chlorzoxazone also may reduce the release of inflammatory leukotrienes. Chlorzoxazone may act by inhibiting calcium and potassium influx which would lead to neuronal inhibition and muscle relaxation. Data available from animal experiments as well as human study indicate that chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain where it inhibits multisynaptic reflex arcs involved in producing and maintaining skeletal muscle spasm
Dược Động Học :

▧ Protein binding :
13-18%
▧ Metabolism :
Chlorzoxazone is rapidly metabolized in the liver and is excreted in the urine, primarily in a conjugated form as the glucuronide.
▧ Route of Elimination :
Chlorzoxazone is rapidly metabolized and is excreted in the urine, primarily in a conjugated form as the glucuronide.
Độc Tính : Oral, mouse: LD50 = 440 mg/kg; Oral, rat: LD50 = 763 mg/kg; Symptoms of overdose include diarrhea, dizziness, drowsiness, headache, light-headedness, nausea, and vomiting.
Chỉ Định : For the relief of discomfort associated with acute painful musculoskeletal conditions.
Tương Tác Thuốc :
  • Disulfiram Disulfiram may increase the serum level of chlorzoxazone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of chlorzoxazone if diltiazem is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Chlorzoxazone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral
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