Tìm theo
Cyproheptadine
Các tên gọi khác (13 ) :
  • 1-methyl-4-(5-dibenzo(a,e)cycloheptatrienylidene)piperidine
  • 1-Methyl-4-(5H-dibenzo(a,d)cycloheptenylidene)piperidine
  • 4-(5-Dibenzo(a,D)cyclohepten-5-ylidine)-1-methylpiperidine
  • 4-(5H-Dibenzo(a,D)cyclohepten-5-ylidene)-1-methylpiperidine
  • 4-Dibenzo[a,D]cyclohepten-5-ylidene-1-methyl-piperidine
  • 5-(1-methylpiperidylidene-4)-5H-dibenzo(a,d)cyclopheptene
  • Axoprol
  • Ciproheptadina
  • Cyproheptadin
  • Cyproheptadine
  • Cyproheptadinum
  • Dihexazin
  • Glutodina
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 129-03-3
ATC: R06AX02
ĐG : Actavis Group , http://www.actavis.com
CTHH: C21H21N
PTK: 287.3981
A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H21N
Phân tử khối
287.3981
Monoisotopic mass
287.167399677
InChI
InChI=1S/C21H21N/c1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21/h2-11H,12-15H2,1H3
InChI Key
InChIKey=JJCFRYNCJDLXIK-UHFFFAOYSA-N
IUPAC Name
1-methyl-4-{tricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-2-ylidene}piperidine
Traditional IUPAC Name
cyproheptadine
SMILES
CN1CCC(CC1)=C1C2=CC=CC=C2C=CC2=CC=CC=C12
Độ tan chảy
112.3-113-3
Độ hòa tan
Soluble
logP
4.69
logS
-4.3
pKa (Strongest Basic)
8.05
PSA
3.24 Å2
Refractivity
105.17 m3·mol-1
Polarizability
34.17 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Cyproheptadine is a piperidine antihistamine. Unlike other antihistamines, this drug also antagonizes serotonin receptors. This action makes Cyproheptadine useful in conditions such as vascular headache and anorexia. Cyproheptadine does not prevent the release of histamine but rather competes with free histamine for binding at HA-receptor sites. Cyproheptadine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. Most antihistamines possess significant anticholinergic properties, but Cyproheptadine exerts only weak anticholinergic actions. Blockade of central muscarinic receptors appears to account for Cyproheptadine's antiemetic effects, although the exact mechanism is unknown. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. Cyproheptadine also has been used to counter vascular headaches, which many believe are caused by changes in serotonin activity, however it is unclear how Cyproheptadine exerts a beneficial effect on this condition.
Cơ Chế Tác Dụng : A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. [PubChem] Cyproheptadine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite.
Dược Động Học :
▧ Absorption :
Well absorbed after oral administration.
▧ Protein binding :
96 to 99%
▧ Metabolism :
Hepatic (cytochrome P-450 system) and some renal.
▧ Route of Elimination :
After a single 4 mg oral dose of14C-labelled cyproheptadine HCl in normal subjects, given as tablets 2% to 20% of the radioactivity was excreted in the stools. At least 40% of the administered radioactivity was excreted in the urine.
Chỉ Định : For treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis due to inhalant allergens and foods, mild uncomplicated allergic skin manifestations of urticaria and angioedema, amelioration of allergic reactions to blood or plasma, cold urticaria, dermatographism, and as therapy for anaphylactic reactions adjunctive to epinephrine.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Fluoxetine Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Metyrapone This combination renders test invalid
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Cyproheptadine, 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.
  • Triprolidine Triprolidine and Cyproheptadine, 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 Cyproheptadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Syrup - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Radicura
    Sản phẩm biệt dược : Apeplus
  • Công ty : Universal
    Sản phẩm biệt dược : Apitup
  • Công ty : Biofarm
    Sản phẩm biệt dược : Biohept
  • Công ty : Cipla
    Sản phẩm biệt dược : Ciplactin
  • Công ty : Teriak
    Sản phẩm biệt dược : Cipractine
  • Công ty : Arena
    Sản phẩm biệt dược : Ciproheptadina
  • Công ty :
    Sản phẩm biệt dược : Ciprovit
  • Công ty : IBN
    Sản phẩm biệt dược : Ciptadine
  • Công ty : Greater Pharma
    Sản phẩm biệt dược : Cyheptine
  • Công ty : CCPC
    Sản phẩm biệt dược : Cyllermin
  • Công ty : Merck
    Sản phẩm biệt dược : Periactin
  • Công ty : Teofarma
    Sản phẩm biệt dược : Periactine
  • Công ty : Apex
    Sản phẩm biệt dược : Periatin
  • Công ty : Orion
    Sản phẩm biệt dược : Reactin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00434
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2913
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508613
ChemSpider
http://www.chemspider.com/Chemical-Structure.2810.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50017721
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/49884-043-01
PharmGKB
http://www.pharmgkb.org/drug/PA164749366
Wikipedia
http://en.wikipedia.org/wiki/Cyproheptadine
RxList
http://www.rxlist.com/cgi/generic2/cyprohept.htm
Drugs.com
http://www.drugs.com/cdi/cyproheptadine.html
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