Tìm theo
Trimethobenzamide
Các tên gọi khác (3) :
  • N-[[4-(2-Dimethylaminoethoxy)phenyl]methyl]-3,4,5-trimethoxybenzamide
  • Trimethobenzamidum
  • Trimetobenzamida
antiemetics
Thuốc Gốc
Small Molecule
CAS: 138-56-7
ĐG : Actavis Group , http://www.actavis.com
CTHH: C21H28N2O5
PTK: 388.4574
Trimethobenzamide is a novel antiemetic which prevents nausea and vomiting in humans. Its actions are unclear but most likely involves the chemoreceptor trigger zone (CTZ). In dogs pretreated with trimethobenzamide HCl, the emetic response to apomorphine is inhibited, while little or no protection is afforded against emesis induced by intragastric copper sulfate.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H28N2O5
Phân tử khối
388.4574
Monoisotopic mass
388.199822016
InChI
InChI=1S/C21H28N2O5/c1-23(2)10-11-28-17-8-6-15(7-9-17)14-22-21(24)16-12-18(25-3)20(27-5)19(13-16)26-4/h6-9,12-13H,10-11,14H2,1-5H3,(H,22,24)
InChI Key
InChIKey=FEZBIKUBAYAZIU-UHFFFAOYSA-N
IUPAC Name
N-({4-[2-(dimethylamino)ethoxy]phenyl}methyl)-3,4,5-trimethoxybenzamide
Traditional IUPAC Name
trimethobenzamide
SMILES
COC1=CC(=CC(OC)=C1OC)C(=O)NCC1=CC=C(OCCN(C)C)C=C1
Độ tan chảy
188.7 °C
Độ hòa tan
40 mg/L
logP
2.29
logS
-4
pKa (strongest acidic)
14.36
pKa (Strongest Basic)
8.77
PSA
69.26 Å2
Refractivity
108.52 m3·mol-1
Polarizability
43.19 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.78
Dược Lực Học : Trimethobenzamide is a novel antiemetic which prevents nausea and vomiting in humans. Its actions are unclear but most likely involves the chemoreceptor trigger zone (CTZ). In dogs pretreated with trimethobenzamide HCl, the emetic response to apomorphine is inhibited, while little or no protection is afforded against emesis induced by intragastric copper sulfate.
Cơ Chế Tác Dụng : Trimethobenzamide is a novel antiemetic which prevents nausea and vomiting in humans. Its actions are unclear but most likely involves the chemoreceptor trigger zone (CTZ). In dogs pretreated with trimethobenzamide HCl, the emetic response to apomorphine is inhibited, while little or no protection is afforded against emesis induced by intragastric copper sulfate. The mechanism of action of trimethobenzamide as determined in animals is obscure, but may involve the chemoreceptor trigger zone (CTZ), an area in the medulla oblongata through which emetic impulses are conveyed to the vomiting center; direct impulses to the vomiting center apparently are not similarly inhibited.
Dược Động Học :
▧ Absorption :
The relative bioavailability of the capsule formulation compared to the solution is 100%.
▧ Metabolism :
Hepatic.
▧ Route of Elimination :
Between 30 – 50% of a single dose in humans is excreted unchanged in the urine within 48–72 hours.
▧ Half Life :
The mean elimination half-life of trimethobenzamide is 7 to 9 hours.
Độc Tính : Oral LD50 in mice is 1600 mg/kg.
Chỉ Định : For the treatment of postoperative nausea and vomiting and for nausea associated with gastroenteritis.
Tương Tác Thuốc :
  • Acetophenazine Trimethobenzamide and Acetophenazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Alimemazine Trimethobenzamide and Trimeprazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Amitriptyline Trimethobenzamide and Amitriptyline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Amoxapine Trimethobenzamide and Amoxapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Atropine Trimethobenzamide and Atropine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Azelastine Trimethobenzamide and Azelastine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Benzatropine Trimethobenzamide and Benztropine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Biperiden Trimethobenzamide and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Bromodiphenhydramine Trimethobenzamide and Bromodiphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Brompheniramine Trimethobenzamide and Brompheniramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Carbinoxamine Trimethobenzamide and Carbinoxamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Chlorphenamine Trimethobenzamide and Chlorpheniramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Chlorpromazine Trimethobenzamide and Chlorpromazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Clemastine Trimethobenzamide and Clemastine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Clidinium Trimethobenzamide and Clidinium, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Clomipramine Trimethobenzamide and Clomipramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Clozapine Trimethobenzamide and Clozapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Cyclizine Trimethobenzamide and Cyclizine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Dexbrompheniramine Trimethobenzamide and Dexbrompheniramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Dicyclomine Trimethobenzamide and Dicyclomine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Dimenhydrinate Trimethobenzamide and Dimenhydrinate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Diphenhydramine Trimethobenzamide and Diphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Donepezil The therapeutic effects of the anticholinergic, Trimethobenzamide, and/or the acetylcholinesterase inhibitor (central), Donepezil, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
  • Doxepin Trimethobenzamide and Doxepin, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Doxylamine Trimethobenzamide and Doxylamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Dronabinol Anticholinergics, such as Trimethobenzamide, may increase the tachycardic effect of cannabinoids such as Marinol. Close monitoring of cardiovascular effects is recommended.
  • Droperidol Trimethobenzamide and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Fexofenadine Trimethobenzamide and Fexofenadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Flavoxate Trimethobenzamide and Flavoxate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Flupentixol Trimethobenzamide and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Fluphenazine Trimethobenzamide and Fluphenazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Galantamine The therapeutic effects of the anticholinergic, Trimethobenzamide, and/or the acetylcholinesterase inhibitor (central), Galantamine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
  • Glycopyrrolate Trimethobenzamide and Glycopyrrolate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Haloperidol Trimethobenzamide and Haloperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Homatropine Methylbromide Trimethobenzamide and Homatropine Methylbromide, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Hydroxyzine Trimethobenzamide and Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Hyoscyamine Trimethobenzamide and Hyoscyamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Imipramine Trimethobenzamide and Imipramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Ipratropium bromide Trimethobenzamide and Ipratropium, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Isocarboxazid Trimethobenzamide and Isocarboxazid, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Ketotifen Trimethobenzamide and Ketotifen, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Loratadine Trimethobenzamide and Loratadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Loxapine Trimethobenzamide and Loxapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Maprotiline Trimethobenzamide and Maprotiline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Meclizine Trimethobenzamide and Meclizine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Mepenzolate Trimethobenzamide and Mepenzolate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Mesoridazine Trimethobenzamide and Mesoridazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Methantheline Trimethobenzamide and Methantheline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Methylscopolamine bromide Trimethobenzamide and Methylscopolamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Moclobemide Trimethobenzamide and Moclobemide, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Molindone Trimethobenzamide and Molindone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Nabilone Anticholinergics, such as Trimethobenzamide, may increase the tachycardic effect of cannabinoids such as Nabilone. Close monitoring of cardiovascular effects is recommended.
  • Nortriptyline Trimethobenzamide and Nortriptyline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Olanzapine Trimethobenzamide and Olanzapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Orphenadrine Trimethobenzamide and Orphenadrine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Oxybutynin Trimethobenzamide and Oxybutynin, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Perphenazine Trimethobenzamide and Perphenazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Phenelzine Trimethobenzamide and Phenelzine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Phenindamine Trimethobenzamide and Phenindamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Pimozide Trimethobenzamide and Pimozide, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Pizotifen Trimethobenzamide and Pizotifen, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Potassium Chloride The ulcerative effects of solid oral dosage forms of KCl may be enhanced by Trimethobenzamide, an anticholinergic. Anticholinergics slow gastric emptying, increasing the contact time between the gastrointestinal mucosa and KCl. Prolonged exposure to KCl increases the risk of gastric and intestinal irritation and ulceration. Solid oral dosage forms of KCl should be avoided; alternatives include liquid or effervescent potassium preparations.
  • Pramlintide The anticholinergic effects of Trimethobenzamide 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.
  • Prochlorperazine Trimethobenzamide and Prochlorperazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Procyclidine Trimethobenzamide and Procyclidine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Promethazine Trimethobenzamide and Promethazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Propantheline Trimethobenzamide and Propantheline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Protriptyline Trimethobenzamide and Protriptyline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Quetiapine Trimethobenzamide and Quetiapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Risperidone Trimethobenzamide and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Rivastigmine The therapeutic effects of the anticholinergic, Trimethobenzamide, and/or the acetylcholinesterase inhibitor (central), Rivastigmine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
  • Scopolamine Trimethobenzamide and Scopolamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Secretin The stimulatory effect of Secretin may be reduced by anticholinergics such as Trimethobenzamide. Concomitant use of Secretin and drugs with substantial anticholinergic effects should be avoided. If combination therapy must be used, Secretin efficacy should be closely monitored.
  • Solifenacin Trimethobenzamide and Solifenacin, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Trimethobenzamide, 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.
  • Thioridazine Trimethobenzamide and Thioridazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Thiothixene Trimethobenzamide and Thiothixene, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Tiotropium Trimethobenzamide and Tiotropium, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Tolterodine Trimethobenzamide and Tolterodine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Tranylcypromine Trimethobenzamide and Tranylcypromine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trifluoperazine Trimethobenzamide and Trifluoperazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trihexyphenidyl Trimethobenzamide and Trihexyphenidyl, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trimipramine Trimethobenzamide and Trimipramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Concomitant therapy with Triprolidine and Trimethobenzamide, two anticholinergics, may result in additive anticholinergic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Trimethobenzamide, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Zuclopenthixol Trimethobenzamide and Zuclopenthixol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Capsule - Oral
Injection, solution - Intramuscular
Suppository - Rectal
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Benzacot
  • Công ty :
    Sản phẩm biệt dược : Stemetic
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Tebamide
  • Sản phẩm biệt dược : Tigan
  • Công ty :
    Sản phẩm biệt dược : Tribenzagan
  • Công ty :
    Sản phẩm biệt dược : Trimazide
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00662
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5577
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507787
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07178
ChemSpider
http://www.chemspider.com/Chemical-Structure.5375.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/21695-448-10
PharmGKB
http://www.pharmgkb.org/drug/PA164764516
Wikipedia
http://en.wikipedia.org/wiki/Trimethobenzamide
RxList
http://www.rxlist.com/cgi/generic3/trimethbenz.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/tig1443.shtml
Drugs.com
http://www.drugs.com/cdi/trimethobenzamide.html
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