Tìm theo
Benzatropine
Các tên gọi khác (13 ) :
  • 3-alpha-(diphenylmethoxy)tropane
  • 3alpha-(Diphenylmethoxy)-1alphah,5alphah-tropane
  • 3alpha-(Diphenylmethoxy)tropane
  • 3alpha-Benzhydryloxy-8-methyl-8-azabicyclo[3.2.1]octane
  • 3endo-benzhydryloxytropane
  • 3α-(diphenylmethoxy)-1αH,5αH-tropane
  • 3α-(diphenylmethoxy)tropane
  • 3α-benzhydryloxy-8-methyl-8-azabicyclo[3.2.1]octane
  • Benzatropina
  • Benzatropinum
  • Benzhydryl 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ether
  • Benztropine
  • Tropine Benzohydryl Ether
dopamine uptake inhibitors, antiparkinson agents, muscarinic antagonists, parasympatholytics, antidyskin
Thuốc Gốc
Small Molecule
CAS: 86-13-5
ATC: N04AC01
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C21H25NO
PTK: 307.4293
Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson’s disease. It may also be used to treat extrapyramidal reactions, such as dystonia and Parkinsonism, caused by antipsychotics (e.g. phenothiazines). Symptoms of Parkinson’s disease and extrapyramidal reactions arise from decreases in dopaminergic activity which creates an imbalance between dopaminergic and cholinergic activity. Anticholinergic therapy is thought to aid in restoring this balance leading to relief of symptoms. In addition to its anticholinergic effects, benztropine also inhibits the reuptake of dopamine at nerve terminals via the dopamine transporter. Benzotropine also produces antagonistic effects at the histamine H1 receptor.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H25NO
Phân tử khối
307.4293
Monoisotopic mass
307.193614427
InChI
InChI=1S/C21H25NO/c1-22-18-12-13-19(22)15-20(14-18)23-21(16-8-4-2-5-9-16)17-10-6-3-7-11-17/h2-11,18-21H,12-15H2,1H3/t18-,19+,20+
InChI Key
InChIKey=GIJXKZJWITVLHI-PMOLBWCYSA-N
IUPAC Name
(1R,3R,5S)-3-(diphenylmethoxy)-8-methyl-8-azabicyclo[3.2.1]octane
Traditional IUPAC Name
benztropine
SMILES
[H][C@]12CC[C@]([H])(C[C@@]([H])(C1)OC(C1=CC=CC=C1)C1=CC=CC=C1)N2C
Độ tan chảy
138-140
Độ hòa tan
Very soluble
logP
4.3
logS
-5.4
pKa (Strongest Basic)
9.54
PSA
12.47 Å2
Refractivity
94.24 m3·mol-1
Polarizability
35.42 Å3
Rotatable Bond Count
4
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 : Benztropine is an anticholinergic used in the symptomatic treatment of all etiologic groups of parkinsonism and drug-induced extrapyramidal reactions (except tardive dyskinesia). Benztropine possesses both anticholinergic and antihistaminic effects, although only the former has been established as therapeutically significant in the management of parkinsonism. Benztropine's anticholinergic activity is about equal to that of atropine. Benztropine also inhibits dopamine reuptake via the dopamine transporter at nerve terminals.
Cơ Chế Tác Dụng : Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson’s disease. It may also be used to treat extrapyramidal reactions, such as dystonia and Parkinsonism, caused by antipsychotics (e.g. phenothiazines). Symptoms of Parkinson’s disease and extrapyramidal reactions arise from decreases in dopaminergic activity which creates an imbalance between dopaminergic and cholinergic activity. Anticholinergic therapy is thought to aid in restoring this balance leading to relief of symptoms. In addition to its anticholinergic effects, benztropine also inhibits the reuptake of dopamine at nerve terminals via the dopamine transporter. Benzotropine also produces antagonistic effects at the histamine H1 receptor. Benztropine is a selective M1 muscarinic acetylcholine receptor antagonist. It is able to discriminate between the M1 (cortical or neuronal) and the peripheral muscarinic subtypes (cardiac and glandular). Benztropine partially blocks cholinergic activity in the CNS, which is responsible for the symptoms of Parkinson's disease. It is also thought to increase the availability of dopamine, a brain chemical that is critical in the initiation and smooth control of voluntary muscle movement.
Dược Động Học :
▧ Absorption :
Onset of action is 1-2 hours following oral administration. The onset of action is within minutes when administered by IM or IV injection.
▧ Protein binding :
~95% to serum proteins
Độc Tính : Signs of overdose include confusion, nervousness, listlessness, hallucinations, dizziness; muscle weakness, ataxia, dry mouth, mydriasis, blurred vision, palpitations, tachycardia, elevated blood pressure, nausea, vomiting, dysuria, numbness of fingers, headache, delirium, coma, shock, convulsions, respiratory arrest, anhidrosis, hyperthermia, glaucoma, and constipation.
Chỉ Định : For use as an adjunct in the therapy of all forms of parkinsonism and also for use in the control of extrapyramidal disorders due to neuroleptic drugs.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Benztropine, 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.
  • Trimethobenzamide Trimethobenzamide and Benztropine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Benztropine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Benztropine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Injection - Intramuscular - 1 mg/ml
Injection - Intravenous - 1 mg/ml
Tablet - Oral - 0.5 mg
Tablet - Oral - 1 mg
Tablet - Oral - 2 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00245
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06846
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0182-1299-89
PharmGKB
http://www.pharmgkb.org/drug/PA448591
Wikipedia
http://en.wikipedia.org/wiki/Benztropine
RxList
http://www.rxlist.com/cgi/generic2/benztrop.htm
Drugs.com
http://www.drugs.com/cdi/benztropine.html
... loading
... loading