Tìm theo
Methdilazine
Các tên gọi khác (3) :
  • Methdilazinum
  • Metodilazina
  • Tacaryl
histamine antagonists
Thuốc Gốc
Small Molecule
CAS: 1982-37-2
ATC: R06AD04
CTHH: C18H20N2S
PTK: 296.43
Methdilazine is a phenothiazine compound with antihistaminic activity. It is used in the treatment of various dermatoses to relieve pruritus.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H20N2S
Phân tử khối
296.43
Monoisotopic mass
296.13471934
InChI
InChI=1S/C18H20N2S/c1-19-11-10-14(12-19)13-20-15-6-2-4-8-17(15)21-18-9-5-3-7-16(18)20/h2-9,14H,10-13H2,1H3
InChI Key
InChIKey=HTMIBDQKFHUPSX-UHFFFAOYSA-N
IUPAC Name
10-[(1-methylpyrrolidin-3-yl)methyl]-10H-phenothiazine
Traditional IUPAC Name
methdilazine
SMILES
CN1CCC(CN2C3=CC=CC=C3SC3=CC=CC=C23)C1
Độ tan chảy
87-88 °C
Độ hòa tan
0.348 mg/L
logP
5.23
logS
-4.3
pKa (Strongest Basic)
8.81
PSA
6.48 Å2
Refractivity
91.64 m3·mol-1
Polarizability
33.37 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Methdilazine is a histamine H1 antagonist. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
Cơ Chế Tác Dụng : Methdilazine is a phenothiazine compound with antihistaminic activity. It is used in the treatment of various dermatoses to relieve pruritus. Methdilazine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Dược Động Học :
▧ Absorption :
Well absorbed in the digestive tract.
Độc Tính : Symptoms of overdose include clumsiness or unsteadiness, convulsions, drowsiness, dryness of mouth, nose, or throat, feeling faint, flushing or redness of face, hallucinations, muscle spasms (especially of neck and back), restlessness, shortness of breath or troubled breathing, shuffling walk, tic-like movements of head and face, trembling and shaking of hands, and trouble in sleeping.
Chỉ Định : Used for the symptomatic relief of hypersensitivity reactions and particularly for the control of pruritic skin disorders
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 Methdilazine 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
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Dilosyn
  • Công ty :
    Sản phẩm biệt dược : Tacaryl
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00902
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=14677
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505472
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07175
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04979
ChemSpider
http://www.chemspider.com/Chemical-Structure.14009.html
PharmGKB
http://www.pharmgkb.org/drug/PA164743018
Wikipedia
http://en.wikipedia.org/wiki/Methdilazine
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