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药品详细

Pyridostigmine(吡啶斯的明)

化学结构式图
中文名
吡啶斯的明
英文名
Pyridostigmine
分子式
C9H13N2O2
化学名
3-[(dimethylcarbamoyl)oxy]-1-methylpyridin-1-ium
分子量
Average: 181.2117
Monoisotopic: 181.09770267
CAS号
155-97-5
ATC分类
N07A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A cholinesterase inhibitor with a slightly longer duration of action than neostigmine. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants. [PubChem]

生产厂家
  • Barr laboratories inc
  • Corepharma llc
  • Impax laboratories inc
  • Sandoz canada inc
  • Solvay pharmaceuticals
  • United states army office surgeon general
  • Valeant pharmaceuticals international
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Singer W, Opfer-Gehrking TL, McPhee BR, Hilz MJ, Bharucha AE, Low PA: Acetylcholinesterase inhibition: a novel approach in the treatment of neurogenic orthostatic hypotension. J Neurol Neurosurg Psychiatry. 2003 Sep;74(9):1294-8. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Carbamates and Derivatives
  • Pyridines and Derivatives
Substructures
  • Carbamates and Derivatives
  • Pyridines and Derivatives
  • Ethers
  • Heterocyclic compounds
  • Aromatic compounds
  • Cations
适应症
药理
Indication For the treatment of myasthenia gravis.
Pharmacodynamics Pyridostigmine is a parasympathomimetic and a reversible cholinesterase inhibitor. Since it is a quaternary amine, it is poorly absorbed in the gut and doesn't cross the blood-brain barrier. Pyridostigmine has a slightly longer duration of action than NEOSTIGMINE. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants.
Mechanism of action Pyridostigmine inhibits acetylcholinesterase in the synaptic cleft by competing with acetylcholine for attachment to acetylcholinesterase, thus slowing down the hydrolysis of acetylcholine, and thereby increases efficiency of cholinergic transmission in the neuromuscular junction and prolonges the effects of acetylcholine.
Absorption Poorly absorbed from the GI tract with an oral bioavailability of 7.6 +/- 2.4%.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hydrolysis by cholinesterases and by liver.
Route of elimination Not Available
Half life 3 hours following oral administration.
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 153 °C Not Available
logP 1.554 Not Available
Predicted Properties
Property Value Source
water solubility 1.04e+00 g/l ALOGPS
logP -3.1 ALOGPS
logP -3.5 ChemAxon
logS -2.3 ALOGPS
pKa (strongest acidic) 19.53 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 1 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 33.42 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 49.66 ChemAxon
polarizability 19.38 ChemAxon
药物相互作用
Drug Interaction
Betamethasone The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, pyridostigmine.
Corticotropin The corticosteroid, corticotropin, may decrease the effect of the anticholinesterase, pyridostigmine.
Cortisone acetate The corticosteroid, cortisone acetate, may decrease the effect of the anticholinesterase, pyridostigmine.
Dexamethasone The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, pyridostigmine.
Fludrocortisone The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, pyridostigmine.
Hydrocortisone The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, pyridostigmine.
Methylprednisolone The corticosteroid, methylprednisolone, may decrease the effect of the anticholinesterase, pyridostigmine.
Paramethasone The corticosteroid, paramethasone, may decrease the effect of the anticholinesterase, pyridostigmine.
Prednisolone The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, pyridostigmine.
Prednisone The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, pyridostigmine.
Triamcinolone The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, pyridostigmine.
食物相互作用
  • Take with food to decrease adverse effects.

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