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药品详细

Benzatropine(苯甲托品)

化学结构式图
中文名
苯甲托品
英文名
Benzatropine
分子式
C21H25NO
化学名
(1R,3R,5S)-3-(diphenylmethoxy)-8-methyl-8-azabicyclo[3.2.1]octane
分子量
Average: 307.4293
Monoisotopic: 307.193614427
CAS号
86-13-5
ATC分类
N04A 未知
药物类型
small molecule
阶段
approved
商品名
Akitan;Apo-Benztropine (Apotex);Cobrentin;Cogentin (Merck Frosst);Cogentinol (Astra (Germany, discontinued));PMS Benztropine (Pharmascience);
同义名
Benzatropina [INN-Spanish];Benzatropine;Benzatropine mesilate;Benzatropinum [INN-Latin];Benztropine Mesylate;Benztropinum;Tropine Benzohydryl Ether;
基本介绍

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.

生产厂家
  • Actavis totowa llc
  • Corepharma llc
  • Hikma farmaceutica (portugal) sa
  • Invagen pharmaceuticals inc
  • Lannett holdings inc
  • Lundbeck inc
  • Merck and co inc
  • Mutual pharmaceutical co inc
  • Nexus pharmaceuticals inc
  • Pharmaforce inc
  • Pliva inc
  • Quantum pharmics ltd
  • Usl pharma inc
  • Vintage pharmaceuticals llc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Wszola BA, Newell KM, Sprague RL: Risk factors for tardive dyskinesia in a large population of youths and adults. Exp Clin Psychopharmacol. 2001 Aug;9(3):285-96. Pubmed
  2. van Harten PN, Hoek HW, Matroos GE, Koeter M, Kahn RS: Intermittent neuroleptic treatment and risk for tardive dyskinesia: Curacao Extrapyramidal Syndromes Study III. Am J Psychiatry. 1998 Apr;155(4):565-7. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes Not Available
Substructures Not Available
适应症
PARKINSON 帕金森氏症;
药理
Indication 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.
Pharmacodynamics 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.
Mechanism of action 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.
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.
Volume of distribution Not Available
Protein binding ~95% to serum proteins
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity 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.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility Very soluble Not Available
logP 4.3 Not Available
Predicted Properties
Property Value Source
water solubility 1.21e-03 g/l ALOGPS
logP 4.47 ALOGPS
logP 4.19 ChemAxon
logS -5.4 ALOGPS
pKa (strongest basic) 9.54 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 12.47 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 94.24 ChemAxon
polarizability 35.42 ChemAxon
药物相互作用
Drug Interaction
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.
食物相互作用
  • Avoid alcohol.
  • Take with food to reduce irritation.

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