Tìm theo
Cyclobenzaprine
Các tên gọi khác (6 ) :
  • (3-Dibenzo[a,d]cyclohepten-5-ylidene-propyl)-dimethyl-amine
  • Ciclobenzaprina
  • Cyclobenzaprine
  • Cyclobenzaprinum
  • N,N-Dimethyl-5H-dibenzo(a,D)cycloheptene-delta(5,gamma)-propylamine
  • N,N-dimethyl-5H-dibenzo(a,d)cycloheptene-Δ5,γ-propylamine
tranquilizing agents, neuromuscular agents, muscle relaxant skeletal
Thuốc Gốc
Small Molecule
CAS: 303-53-7
ATC: M03BX08
ĐG : 4uOrtho LLC , http://www.4udr.com
CTHH: C20H21N
PTK: 275.3874
Cyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine acts on the locus coeruleus where it results in increased norepinephrine release, potentially through the gamma fibers which innervate and inhibit the alpha motor neurons in the ventral horn of the spinal cord. It is structurally similar to Amitriptyline, differing by only one double bond.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H21N
Phân tử khối
275.3874
Monoisotopic mass
275.167399677
InChI
InChI=1S/C20H21N/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20/h3-6,8-14H,7,15H2,1-2H3
InChI Key
InChIKey=JURKNVYFZMSNLP-UHFFFAOYSA-N
IUPAC Name
dimethyl({3-[(2E)-tricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-2-ylidene]propyl})amine
Traditional IUPAC Name
cyclobenzaprine
SMILES
CN(C)CCC=C1C2=CC=CC=C2C=CC2=CC=CC=C12
Độ sôi
173-177
Độ hòa tan
Freely Soluble
logP
5.2
logS
-4.6
pKa (Strongest Basic)
9.76
PSA
3.24 Å2
Refractivity
102.62 m3·mol-1
Polarizability
32.95 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.47
Dược Lực Học : Cyclobenzaprine, closely related to the antidepressant amitriptyline, is used as a skeletal muscle relaxant to reduce pain and tenderness and improve mobility. Unlike dantrolene, cyclobenzaprine cannot be used to treat muscle spasm secondary to cerebral or spinal cord disease.
Cơ Chế Tác Dụng : Cyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine acts on the locus coeruleus where it results in increased norepinephrine release, potentially through the gamma fibers which innervate and inhibit the alpha motor neurons in the ventral horn of the spinal cord. It is structurally similar to Amitriptyline, differing by only one double bond. Like other tricyclic antidepressants, cyclobenzaprine exhibits anticholinergic activity, potentiation of norepinephrine, and antagonism of reserpine. Cyclobenzaprine does not directly act on the neuromuscular junction or the muscle but relieves muscle spasms through a central action, possibly at the brain stem level. Cyclobenzaprine binds to the serotonin receptor and is considered a 5-HT2 receptor antagonist that reduces muscle tone by decreasing the activity of descending serotonergic neurons.
Dược Động Học :
▧ Absorption :
Slowly but well absorbed after oral administration
▧ Protein binding :
Very high (93%)
▧ Metabolism :
Extensively metabolized (gastrointestinal and hepatic).
▧ Route of Elimination :
Cyclobenzaprine is extensively metabolized, and is excreted primarily as glucuronides via the kidney.
▧ Half Life :
18 hours (range 8-37 hours)
▧ Clearance :
* 0.7 L/min
Độc Tính : Oral mouse and rat LD50 are 338 mg/kg and 425 mg/kg respectively. Signs of overdose include agitation, coma, confusion, congestive heart failure, convulsions, dilated pupils, disturbed concentration, drowsiness, hallucinations, high or low temperature, increased heartbeats, irregular heart rhythms, muscle stiffness, overactive reflexes, severe low blood pressure, stupor, and vomiting.
Chỉ Định : For use as an adjunct to rest and physical therapy for relief of muscle spasm associated with acute, painful musculoskeletal conditions.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Indacaterol Concomitant therapy with monoamine oxidase inhibitors, tricyclic antidepressants, or other drugs that prolong the QTc interval should be monitored closely. These drugs may potentiate the effect of adrenergic agonist on the cardiovascular system.
  • Rasagiline Increased risk of toxicity with this association
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Cyclobenzaprine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Thiabendazole The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Cyclobenzaprine by decreasing Cyclobenzaprine metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Cyclobenzaprine if Thiabendazole is initiated, discontinued or dose changed.
  • Tramadol Increases risk of seizure.
  • Tranylcypromine Increased risk of serotonin syndrome. Concomitant use should be avoided. These agents should not be administered within 14 days of each other.
  • Triprolidine Triprolidine and Cyclobenzaprine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Cyclobenzaprine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Anesta
    Sản phẩm biệt dược : Amrix
  • Công ty :
    Sản phẩm biệt dược : FEXMID
  • Công ty : Janssen
    Sản phẩm biệt dược : Flexeril
  • Công ty : SIT
    Sản phẩm biệt dược : Flexiban
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00924
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2895
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508313
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06931
ChemSpider
http://www.chemspider.com/Chemical-Structure.2792.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0179-0057-30
PharmGKB
http://www.pharmgkb.org/drug/PA449160
Wikipedia
http://en.wikipedia.org/wiki/Cyclobenzaprine
RxList
http://www.rxlist.com/cgi/generic/cyclobnz.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/fle1179.shtml
Drugs.com
http://www.drugs.com/cyclobenzaprine.html
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