Tìm theo
Alimemazine
Các tên gọi khác (4 ) :
  • Alimemazine
  • Methylpromazine
  • Repeltin
  • Trimeprazine
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 84-96-8
ATC: R06AD01
ĐG : Emcure Pharmaceuticals Ltd. , http://www.emcure.co.in
CTHH: C18H22N2S
PTK: 298.446
A phenothiazine derivative that is used as an antipruritic. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H22N2S
Phân tử khối
298.446
Monoisotopic mass
298.150369404
InChI
InChI=1S/C18H22N2S/c1-14(12-19(2)3)13-20-15-8-4-6-10-17(15)21-18-11-7-5-9-16(18)20/h4-11,14H,12-13H2,1-3H3
InChI Key
InChIKey=ZZHLYYDVIOPZBE-UHFFFAOYSA-N
IUPAC Name
dimethyl[2-methyl-3-(10H-phenothiazin-10-yl)propyl]amine
Traditional IUPAC Name
trimeprazine
SMILES
CC(CN(C)C)CN1C2=CC=CC=C2SC2=CC=CC=C12
Độ tan chảy
68 °C
Độ sôi
150-175 °C at 3.00E-01 mm Hg
Độ hòa tan
0.942 mg/L
logP
4.71
logS
-4.5
pKa (Strongest Basic)
9.42
PSA
6.48 Å2
Refractivity
93.37 m3·mol-1
Polarizability
34.83 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
9.05
Dược Lực Học : Trimeprazine (also known as Alimemazine) is a tricyclic antihistamine, similar in structure to the phenothiazine antipsychotics, but differing in the ring-substitution and chain characteristics. Trimeprazine is in the same class of drugs as chlorpromazine (Thorazine) and trifluoperazine (Stelazine); however, unlike the other drugs in this class, trimeprazine is not used clinically as an anti-psychotic. It acts as an anti-histamine, a sedative, and an anti-emetic (anti-nausea). Trimeprazine is used principally as an anti-emetic, to prevent motion sickness or as an anti-histamine in combination with other medications in cough and cold preparations. Tricyclic antihistamines are also structurally-related to the tricyclic antidepressants, explaining the antihistaminergic adverse effects of these two drug classes and also the poor tolerability profile of tricyclic H1-antihistamines.
Cơ Chế Tác Dụng : A phenothiazine derivative that is used as an antipruritic. [PubChem] Trimeprazine 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.
Dược Động Học :
▧ Absorption :
Well absorbed in the digestive tract.
▧ Metabolism :
Hepatic
Độc Tính : Symptoms of overdose clumsiness or unsteadiness, seizures, severe drowsiness, flushing or redness of face, hallucinations, muscle spasms (especially of neck and back), restlessness, shortness of breath, shuffling walk, tic-like (jerky) movements of head and face, trembling and shaking of hands, and insomnia.
Chỉ Định : Used to prevent and relieve allergic conditions which cause pruritus (itching) and urticaria (some allergic skin reactions).
Tương Tác Thuốc :
  • Bromocriptine The phenothiazine decreases the effect of bromocriptine
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Diethylpropion Decreased anorexic effect, may increase psychotic symptoms
  • Donepezil Possible antagonism of action
  • Fenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Galantamine Possible antagonism of action
  • Guanethidine Trimeprazine may decrease the effect of guanethidine.
  • Mazindol Decreased anorexic effect, may increase psychotic symptoms
  • Phentermine Decreased anorexic effect, may increase psychotic symptoms
  • Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms
  • Pramlintide The anticholinergic effects of Trimeprazine may be enhanced by Pramlintide. Additive effects of reduced GI motility may occur. Pramlintide slows gastic emptying and should not be used with drugs that alter GI motility (e.g. anticholinergics). Consider alternative treatments or use caution during concomitant therapy.
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Trimeprazine, 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.
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Trimethobenzamide Trimethobenzamide and Trimeprazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Trimeprazine, 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 Trimeprazine, 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
  • Biệt dược thương mại : Panectyl 2.5 mg Tablet
    Giá bán buôn : USD >0.3
    Đơn vị tính : tablet
  • Biệt dược thương mại : Panectyl 5 mg Tablet
    Giá bán buôn : USD >0.37
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Alimezine
  • Công ty :
    Sản phẩm biệt dược : Nedeltran
  • Công ty :
    Sản phẩm biệt dược : Panectyl
  • Công ty :
    Sản phẩm biệt dược : Theralen
  • Công ty :
    Sản phẩm biệt dược : Theralene
  • Công ty :
    Sản phẩm biệt dược : Vallergan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01246
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5574
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508449
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07172
ChemSpider
http://www.chemspider.com/Chemical-Structure.5373.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50062261
PharmGKB
http://www.pharmgkb.org/drug/PA164744009
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