Tìm theo
Promazine
Các tên gọi khác (10 ) :
  • 10-(3-(Dimethylamino)propyl)phenothiazine
  • Frenil
  • N-(3-Dimethylaminopropyl)phenothiazine
  • N-Dimethylamino-1-methylethyl thiodiphenylamine
  • N,N-dimethyl-3-(10H-phenothiazin-10-yl)-propan-1-amine
  • Promazin
  • Promazina
  • Promazina
  • Promazine
  • Promazinum
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 58-40-2
ATC: N05AA03, N05AA02, N05AA01, N05AA04, N05AA05
ĐG : Baxter International Inc. , http://www.baxter.com
CTHH: C17H20N2S
PTK: 284.419
A phenothiazine with actions similar to chlorpromazine but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic. Promazine is not approved for use in the United States.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H20N2S
Phân tử khối
284.419
Monoisotopic mass
284.13471934
InChI
InChI=1S/C17H20N2S/c1-18(2)12-7-13-19-14-8-3-5-10-16(14)20-17-11-6-4-9-15(17)19/h3-6,8-11H,7,12-13H2,1-2H3
InChI Key
InChIKey=ZGUGWUXLJSTTMA-UHFFFAOYSA-N
IUPAC Name
dimethyl[3-(10H-phenothiazin-10-yl)propyl]amine
Traditional IUPAC Name
promazine
SMILES
CN(C)CCCN1C2=CC=CC=C2SC2=CC=CC=C12
Độ tan chảy
< 25 °C
Độ sôi
203-210 °C at 3.00E-01 mm Hg
Độ hòa tan
14.2 mg/L (at 24 °C)
logP
4.55
logS
-4.3
pKa (Strongest Basic)
9.2
PSA
6.48 Å2
Refractivity
88.95 m3·mol-1
Polarizability
32.74 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
9.36
Dược Lực Học : Promazine belongs to a group of medications known as the phenothiazine antipsychotics. It acts by blocking a variety of receptors in the brain, particularly dopamine receptors. Dopamine is involved in transmitting signals between brain cells. When there is an excess amount of dopamine in the brain it causes over-stimulation of dopamine receptors. These receptors normally act to modify behaviour and over-stimulation may result in psychotic illness. Promazine hydrochloride blocks these receptors and stops them becoming over-stimulated, thereby helping to control psychotic illness. Promazine has weak extrapyramidal and autonomic side effects which lead to its use in the elderly, for restless or psychotic patients. Its anti-psychotic effect is also weaker and it is not useful in general psychiatry.
Cơ Chế Tác Dụng : A phenothiazine with actions similar to chlorpromazine but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic. Promazine is not approved for use in the United States. Promazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine.
Dược Động Học :
▧ Absorption :
Absorption may be erratic and peak plasma concentrations show large interindividual differences.
▧ Protein binding :
94%
▧ Metabolism :
Hepatic, primarily to N-desmethylpromazine and promazine sulfoxide.
Độc Tính : Side effects include: extrapyramidal symptoms, drowsiness, weight gain, dry mouth, constipation, endocrine effects (such as gynaecomastia and menstrual disturbance), sensitivity to sunlight and haemolytic anaemia.
Chỉ Định : Used as an adjunct for short term treatment of moderate and severe psychomotor agitation. Also used to treat agitation or restlessness in the elderly.
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
  • Gatifloxacin Increased risk of cardiotoxicity and arrhythmias
  • Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
  • Guanethidine Promazine may decrease the effect of guanethidine.
  • Levofloxacin Increased risk of cardiotoxicity and arrhythmias
  • 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
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Combelen
  • Công ty : Pliva
    Sản phẩm biệt dược : Prazine
  • Công ty :
    Sản phẩm biệt dược : Sparine
  • Công ty : Abbott
    Sản phẩm biệt dược : Talofen
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00420
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4926
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504504
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07379
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08430
ChemSpider
http://www.chemspider.com/Chemical-Structure.4757.html
PharmGKB
http://www.pharmgkb.org/drug/PA451126
Wikipedia
http://en.wikipedia.org/wiki/Promazine
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