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药品详细

Carbachol(卡巴)

化学结构式图
中文名
卡巴
英文名
Carbachol
分子式
C6H15ClN2O2
化学名
2-(trimethylazaniumyl)ethyl carbamate chloride
分子量
Average: 182.649
Monoisotopic: 182.082205441
CAS号
51-83-2
ATC分类
N07A 未知;S01E 抗青光眼制剂及缩瞳药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A slowly hydrolyzed cholinergic agonist that acts at both muscarinic and nicotinic receptors. [PubChem]

生产厂家
  • Alcon laboratories inc
  • Novartis pharmaceuticals corp
  • Pharmafair 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 Not Available
Substructures Not Available
适应症
药理
Indication Primarily used in the treatment of glaucoma, but is also used during ophthalmic surgery.
Pharmacodynamics Carbachol is a potent cholinergic (parasympathomimetic) agent which produces constriction of the iris and ciliary body resulting in reduction in intraocular pressure. The exact mechanism by which carbachol lowers intraocular pressure is not precisely known. In the cat and rat, carbachol is well-known for its ability to induce rapid eye movement (REM) sleep when microinjected into the pontine reticular formation. Carbachol elicits this REM sleep-like state via activation of postsynaptic muscarinic cholinergic receptors (mAChRs).
Mechanism of action Carbachol is a parasympathomimetic that stimulates both muscarinic and nicotinic receptors. In topical ocular and intraocular administration its principal effects are miosis and increased aqueous humour outflow.
Absorption Not well absorbed in the gastro-intestinal tract, and does not cross the blood-brain barrier.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Oral, mouse: LD50 = 15 mg/kg; Oral, rat: LD50 = 40 mg/kg.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 210 dec °C PhysProp
water solubility 1 g/ml Not Available
logP -3.78 Not Available
Predicted Properties
Property Value Source
water solubility 9.48e-01 g/l ALOGPS
logP -3.5 ALOGPS
logP -4.6 ChemAxon
logS -2.3 ALOGPS
pKa (strongest acidic) 15.23 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 1 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 52.32 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 50.02 ChemAxon
polarizability 16.14 ChemAxon
药物相互作用
Drug Interaction
Tacrine The acetylcholinesterase inhibitor, Tacrine, may increase the cholinergic effects of Carbachol, a cholinergic agonist. Monitor for increased cholinergic effects.
食物相互作用
Not Available

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