用户名： 密   码：
注册 | 忘记密码？
药品详细

Rivastigmine(卡巴拉汀)

化学结构式图
中文名
卡巴拉汀
英文名
Rivastigmine
分子式
C14H22N2O2
化学名
3-[(1S)-1-(dimethylamino)ethyl]phenyl N-ethyl-N-methylcarbamate
分子量
Average: 250.3367
Monoisotopic: 250.168127958
CAS号
123441-03-2
ATC分类
N06D 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Rivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer’s type. Rivastigmine is a cholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase.

生产厂家
  • Dr reddys laboratories inc
  • Novartis pharmaceuticals corp
  • Sun pharmaceutical industries ltd
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Camps P, Munoz-Torrero D: Cholinergic drugs in pharmacotherapy of Alzheimer’s disease. Mini Rev Med Chem. 2002 Feb;2(1):11-25. Pubmed
  2. Rosler M, Anand R, Cicin-Sain A, Gauthier S, Agid Y, Dal-Bianco P, Stahelin HB, Hartman R, Gharabawi M: Efficacy and safety of rivastigmine in patients with Alzheimer’s disease: international randomised controlled trial. BMJ. 1999 Mar 6;318(7184):633-8. Pubmed
  3. Finkel SI: Effects of rivastigmine on behavioral and psychological symptoms of dementia in Alzheimer’s disease. Clin Ther. 2004 Jul;26(7):980-90. Pubmed
  4. Rosler M, Retz W, Retz-Junginger P, Dennler HJ: Effects of two-year treatment with the cholinesterase inhibitor rivastigmine on behavioural symptoms in Alzheimer’s disease. Behav Neurol. 1998;11(4):211-216. Pubmed
  5. Emre M, Aarsland D, Albanese A, Byrne EJ, Deuschl G, De Deyn PP, Durif F, Kulisevsky J, van Laar T, Lees A, Poewe W, Robillard A, Rosa MM, Wolters E, Quarg P, Tekin S, Lane R: Rivastigmine for dementia associated with Parkinson’s disease. N Engl J Med. 2004 Dec 9;351(24):2509-18. Pubmed
  6. Birks J, Grimley Evans J, Iakovidou V, Tsolaki M, Holt FE: Rivastigmine for Alzheimer’s disease. Cochrane Database Syst Rev. 2009 Apr 15;(2):CD001191. Pubmed# Naik RS, Hartmann J, Kiewert C, Duysen EG, Lockridge O, Klein J: Effects of rivastigmine and donepezil on brain acetylcholine levels in acetylcholinesterase-deficient mice. J Pharm Pharm Sci. 2009;12(1):79-85. Pubmed
  7. Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Carbamates and Derivatives
  • Phenols and Derivatives
  • Anisoles
  • Phenyl Esters
Substructures
  • Carbamates and Derivatives
  • Phenols and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Aromatic compounds
  • Anisoles
  • Phenyl Esters
适应症
药理
Indication For the treatment of mild to moderate dementia associated with Parkinson's disease or of the Alzheimer's type.
Pharmacodynamics Rivastigmine is a parasympathomimetic and a reversible cholinesterase inhibitor. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus. Tacrine is postulated to exert its therapeutic effect by enhancing cholinergic function. While the precise mechanism of rivastigmine's action is unknown, it is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. If this proposed mechanism is correct, rivastigmine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact.
Mechanism of action Rivastigmine is a carbamate derivative that is structurally related to physostigmine, but not to donepezil and tacrine. The precise mechanism of rivastigmine has not been fully determined, but it is suggested that rivastigmine binds reversibly with and inactivates chlolinesterase (eg. acetylcholinesterase, butyrylcholinesterase), preventing the hydrolysis of acetycholine, and thus leading to an increased concentration of acetylcholine at cholinergic synapses. The anticholinesterase activity of rivastigmine is relatively specific for brain acetylcholinesterase and butyrylcholinesterase compared with those in peripheral tissues.
Absorption Not Available
Volume of distribution
  • 1.8 to 2.7 L/kg
Protein binding 40%
Metabolism
Rivastigmine is rapidly metabolized by cholinesterase-mediated hydrolysis.
Route of elimination Rivastigmine is extensively metabolized primarily via cholinesterase-mediated hydrolysis to the decarbamylated metabolite NAP226-90. Renal excretion of the metabolites is the major route of elimination. Less than 1% of the administered dose is excreted in the feces.
Half life 1.5 hours
Clearance
  • renal cl=2.1-2.8 L/hr
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 2.3 Not Available
Predicted Properties
Property Value Source
water solubility 2.04e+00 g/l ALOGPS
logP 2.45 ALOGPS
logP 2.41 ChemAxon
logS -2.1 ALOGPS
pKa (strongest basic) 8.89 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 32.78 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 73.37 ChemAxon
polarizability 28.53 ChemAxon
药物相互作用
Drug Interaction
Amantadine Possible antagonism of action
Amitriptyline Possible antagonism of action
Amoxapine Possible antagonism of action
Azatadine Possible antagonism of action
Benzatropine Possible antagonism of action
Biperiden Possible antagonism of action
Brompheniramine Possible antagonism of action
Chlorpheniramine Possible antagonism of action
Chlorpromazine Possible antagonism of action
Chlorprothixene Possible antagonism of action
Cimetidine Possible antagonism of action
Clemastine Possible antagonism of action
Clomipramine Possible antagonism of action
Clozapine Possible antagonism of action
Cyclizine Possible antagonism of action
Cyclobenzaprine Possible antagonism of action
Cyproheptadine Possible antagonism of action
Darifenacin Possible antagonism of action
Desipramine Possible antagonism of action
Dicyclomine Possible antagonism of action
Dimenhydrinate Possible antagonism of action
Diphenhydramine Possible antagonism of action
Disopyramide Possible antagonism of action
Doxepin Possible antagonism of action
Flavoxate Possible antagonism of action
Flupenthixol Possible antagonism of action
Glutethimide Possible antagonism of action
Glycopyrrolate Possible antagonism of action
Hydroxyzine Possible antagonism of action
Hyoscyamine Possible antagonism of action
Imipramine Possible antagonism of action
Isocarboxazid Possible antagonism of action
Loxapine Possible antagonism of action
Maprotiline Possible antagonism of action
Meclizine Possible antagonism of action
Meperidine Possible antagonism of action
Mesoridazine Possible antagonism of action
Methotrimeprazine Possible antagonism of action
Mirtazapine Possible antagonism of action
Moclobemide Possible antagonism of action
Nortriptyline Possible antagonism of action
Olanzapine Possible antagonism of action
Orphenadrine Possible antagonism of action
Oxybutynin Possible antagonism of action
Perphenazine Possible antagonism of action
Phenelzine Possible antagonism of action
Pimozide Possible antagonism of action
Procainamide Possible antagonism of action
Prochlorperazine Possible antagonism of action
Promethazine Possible antagonism of action
Propericiazine Possible antagonism of action
Quetiapine Possible antagonism of action
Quinidine Possible antagonism of action
Thioproperazine Possible antagonism of action
Thioridazine Possible antagonism of action
Tizanidine Possible antagonism of action
Trazodone Possible antagonism of action
Trifluoperazine Possible antagonism of action
Trihexyphenidyl Possible antagonism of action
Trimethobenzamide 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.
Trospium The therapeutic effects of the anticholinergic, Trospium, and/or the acetylcholinesterase inhibitor (central), Rivastigmine, may be reduced due to antagonism. Monitor therapeutic effects of both agents.
食物相互作用
Not Available

返回 | 收藏