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药品详细

Pancuronium(泮库溴铵)

化学结构式图
中文名
泮库溴铵
英文名
Pancuronium
分子式
C35H60N2O4
化学名
1-[(1S,2S,4S,5S,7S,10R,11S,13S,14R,15S)-5,14-bis(acetyloxy)-2,15-dimethyl-4-(1-methylpiperidin-1-ium-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-13-yl]-1-methylpiperidin-1-ium
分子量
Average: 572.8619
Monoisotopic: 572.455308418
CAS号
15500-66-0
ATC分类
M03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than curare but has less effect on the circulatory system and on histamine release.

生产厂家
  • Astrazeneca lp
  • Elkins sinn div ah robins co inc
  • Hospira inc
  • Organon usa inc
  • Teva parenteral medicines inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Steroids and Steroid Derivatives
Substructures
  • Steroids and Steroid Derivatives
  • Carboxylic Acids and Derivatives
  • Anions
  • Acetates
  • Sterols
  • Ethers
  • Quaternary Ammonium Salts
  • Bicyclohexanes
  • Heterocyclic compounds
  • Piperidines
  • Cations
适应症
药理
Indication Used as a muscle relaxant during anesthesia and surgical procedures.
Pharmacodynamics Pancuronium is a typical non-depolarising curare-mimetic muscle relaxant. It acts as a competitive acetylcholine antagonist on neuromuscular junctions, displacing acetylcholine (hence competitive) from its post-synaptic nicotinic acetylcholine receptors. It is, unlike suxamethonium, a non-depolarising agent, which means, that it causes no spontaneous depolarisations upon association with the nicotinic receptor in neuromuscular junction, thus producing no muscle fasciculations upon administration. Pancuronium has no hormonal activity. It exerts slight vagolytic activity (i.e. diminishing activity of the vagus nerve) and no ganglioplegic (i.e., blocking ganglions) activity.
Mechanism of action Nondepolarizing neuromuscular blocking agents inhibit neuromuscular transmission by competing with acetylcholine for the cholinergic receptors of the motor end plate, thereby reducing the response of the end plate to acetylcholine. This type of neuromuscular block is usually antagonized by anticholinesterase agents.
Absorption Not Available
Volume of distribution
  • 241 to 280 mL/kg
Protein binding 77 to 91%
Metabolism
Hepatic.
Route of elimination Not Available
Half life 1.5 to 2.7 hours.
Clearance
  • Plasma cl=1.1–1.9 mL/minute/kg
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 215 °C PhysProp
water solubility 5E+005 mg/L MERCK INDEX (1996)
Predicted Properties
Property Value Source
water solubility 3.08e-06 g/l ALOGPS
logP 1.04 ALOGPS
logP -3.3 ChemAxon
logS -8.3 ALOGPS
pKa (strongest basic) -6.7 ChemAxon
physiological charge 2 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 52.6 ChemAxon
rotatable bond count 6 ChemAxon
refractivity 185.22 ChemAxon
polarizability 69.44 ChemAxon
药物相互作用
Drug Interaction
Amikacin The agent increases the effect of muscle relaxant
Aminophylline Theophylline decreases the effect of muscle relaxant
Azathioprine The agent decreases the effect of the muscle relaxant
Carbamazepine Decreases the effect of muscle relaxant
Clindamycin The agent increases the effect of muscle relaxant
Colistimethate Colistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).
Fosphenytoin Phenytoin decreases the effect of muscle relaxant
Gentamicin The agent increases the effect of muscle relaxant
Lincomycin The agent increases the effect of muscle relaxant
Mercaptopurine The agent dereases the effect of the muscle relaxant
Netilmicin The agent increases the effect of muscle relaxant
Oxtriphylline Theophylline decreases the effect of muscle relaxant
Phenytoin Phenytoin decreases the effect of the muscle relaxant
Piperacillin The agent increases the effect of the muscle relaxant
Quinidine The quinine derivative increases the effect of the muscle relaxant
Quinine The quinine derivative increases the effect of the muscle relaxant
Theophylline Theophylline decreases the effect of the muscle relaxant
Tobramycin The agent increases the effect of the muscle relaxant
食物相互作用
Not Available

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