Tìm theo
Promethazine
Các tên gọi khác (10 ) :
  • (2-dimethylamino-2-methyl)ethyl-N-dibenzoparathiazine
  • 10-(2-Dimethylaminopropyl)phenothiazine
  • 10-[2-(dimethylamino)Propyl]phenothiazine
  • N-(2'-dimethylamino-2'-Methyl)ethylphenothiazine
  • N,N,alpha-Trimethyl-10H-phenothiazine-10-ethanamine
  • N,N,α-trimethyl-10H-phenothiazine-10-ethanamine
  • Proazamine
  • Prometazina
  • Promethazine
  • Promethazinum
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 60-87-7
ATC: D04AA10, R06AD02, R06AD05
ĐG : Actavis Group , http://www.actavis.com
CTHH: C17H20N2S
PTK: 284.419
A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals. [PubChem]
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/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19/h4-11,13H,12H2,1-3H3
InChI Key
InChIKey=PWWVAXIEGOYWEE-UHFFFAOYSA-N
IUPAC Name
dimethyl[1-(10H-phenothiazin-10-yl)propan-2-yl]amine
Traditional IUPAC Name
promethazine
SMILES
CC(CN1C2=CC=CC=C2SC2=CC=CC=C12)N(C)C
Độ tan chảy
60 °C
Độ sôi
190-192 °C at 3.00E+00 mm Hg
Độ hòa tan
15.6 mg/L (at 24 °C)
logP
4.81
logS
-4.26
pKa (Strongest Basic)
9.05
PSA
6.48 Å2
Refractivity
88.5 m3·mol-1
Polarizability
32.38 Å3
Rotatable Bond Count
3
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
9.1
Dược Lực Học : Promethazine, a phenothiazine, is an H1-antagonist with anticholinergic, sedative, and antiemetic effects and some local anesthetic properties. Promethazine is used as an antiemetic or to prevent motion sickness.
Cơ Chế Tác Dụng : A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals. [PubChem] Like other H1-antagonists, promethazine competes with free histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. The relief of nausea appears to be related to central anticholinergic actions and may implicate activity on the medullary chemoreceptor trigger zone.
Dược Động Học :
▧ Absorption :
On average, 88% of a promethazine dose is absorbed after oral administration; however, the absolute bioavailability is only 25% because of first-pass clearance.
▧ Protein binding :
93%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Promethazine hydrochloride is metabolized in the liver, with the sulfoxides of promethazine and N-desmethylpromethazine being the predominant metabolites appearing in the urine.
▧ Half Life :
16-19 hours
Độc Tính : Symptoms of overdose include mild depression of the central nervous system and cardiovascular system to profound hypotension, respiratory depression, unconsciousness, and sudden death. Other reported reactions include hyperreflexia, hypertonia, ataxia, athetosis, and extensor-plantar reflexes (Babinski reflex). LD50=55mg/kg (I.V. in mice)
Chỉ Định : For the treatment of allergic disorders, and nausea/vomiting.
Tương Tác Thuốc :
  • Amphetamine Decreased anorexic effect, may increase pyschotic symptoms
  • Benzphetamine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Bromocriptine The phenothiazine decreases the effect of bromocriptine
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Dexfenfluramine Decreased anorexic effect, may increase pyschotic symptoms.
  • Dextroamphetamine Decreased anorexic effect, may increase pyschotic 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 Promethazine may decrease the effect of guanethidine.
  • Levofloxacin Increased risk of cardiotoxicity and arrhythmias
  • Mazindol Decreased anorexic effect, may increase psychotic symptoms.
  • Methamphetamine Decreased anorexic effect, may increase pyschotic symptoms
  • Metrizamide Increased risk of convulsions
  • Phendimetrazine Decreased anorexic effect, may increase pyschotic symptoms
  • Phenmetrazine Decreased anorexic effect, may increase pyschotic symptoms
  • Phentermine Decreased anorexic effect, may increase psychotic symptoms.
  • Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms.
  • Rivastigmine Possible antagonism of action
  • Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Promethazine, 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.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Promethazine. Consider alternate therapy or monitor for therapeutic/adverse effects of Promethazine if Terbinafine is initiated, discontinued or dose changed.
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Thiotepa Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Promethazine, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Promethazine if Thiotepa is initiated, discontinued or dose changed.
  • Tramadol Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Tranylcypromine Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome.
  • Trazodone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trimethobenzamide Trimethobenzamide and Promethazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trimipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Triprolidine Triprolidine and Promethazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Promethazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Venlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Zolmitriptan Use of two serotonin modulators, such as zolmitriptan and promethazine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
Liều Lượng & Cách Dùng : Cream - Topical
Liquid - Intramuscular
Solution - Intravenous
Syrup - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Avomine
  • Công ty :
    Sản phẩm biệt dược : Fargan
  • Công ty :
    Sản phẩm biệt dược : Farganesse
  • Công ty :
    Sản phẩm biệt dược : Lergigan
  • Công ty :
    Sản phẩm biệt dược : PHENADOZ
  • Công ty :
    Sản phẩm biệt dược : Phenergan
  • Công ty :
    Sản phẩm biệt dược : Promethegan
  • Công ty :
    Sản phẩm biệt dược : Prothiazine
  • Công ty :
    Sản phẩm biệt dược : Receptozine
  • Công ty :
    Sản phẩm biệt dược : Romergan
  • Công ty :
    Sản phẩm biệt dược : Sominex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01069
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4927
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507798
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07404
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00494
ChemSpider
http://www.chemspider.com/Chemical-Structure.4758.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0143-9869-22
PharmGKB
http://www.pharmgkb.org/drug/PA451128
Wikipedia
http://en.wikipedia.org/wiki/Promethazine
RxList
http://www.rxlist.com/cgi/generic3/phenergan.htm
Drugs.com
http://www.drugs.com/promethazine.html
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