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药品详细

Chloroprocaine(氯普鲁卡因)

化学结构式图
中文名
氯普鲁卡因
英文名
Chloroprocaine
分子式
C13H19ClN2O2
化学名
2-(diethylamino)ethyl 4-amino-2-chlorobenzoate
分子量
Average: 270.755
Monoisotopic: 270.113505569
CAS号
133-16-4
ATC分类
N01B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Chloroprocaine hydrochloride is a local anesthetic given by injection during surgical procedures and labor and delivery. Chloroprocaine, like other local anesthetics, blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse and by reducing the rate of rise of the action potential.

生产厂家
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Hospira 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
  • Aminobenzoates
Substructures
  • Aminobenzoates
  • Carboxylic Acids and Derivatives
  • Benzyl Alcohols and Derivatives
  • Acetates
  • Benzoates
  • Aliphatic and Aryl Amines
  • Ethers
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Aromatic compounds
  • Benzoyl Derivatives
  • Anilines
适应症
药理
Indication For the production of local anesthesia by infiltration and peripheral nerve block. They are not to be used for lumbar or caudal epidural anesthesia.
Pharmacodynamics Chloroprocaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Chloroprocaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Chloroprocaine is an ester anesthetic.
Mechanism of action Chloroprocaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. It is hypothesized that Chloroprocaine binds or antagonizes the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
Absorption The rate of systemic absorption of local anesthetic drugs is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic injection.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase.
Route of elimination Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase. Urinary excretion is affected by urinary perfusion and factors affecting urinary pH.
Half life 21 +/- 2 seconds
Clearance Not Available
Toxicity In mice, the intravenous LD50 of chloroprocaine HCl is 97 mg/kg and the subcutaneous LD50 of chloroprocaine HCl is 950 mg/kg.
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00394 Chloroprocaine Pathway SMP00394
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility 0.665 mg/mL Not Available
logP 2.86 HANSCH,C ET AL. (1995)
Predicted Properties
Property Value Source
water solubility 1.30e+00 g/l ALOGPS
logP 2.72 ALOGPS
logP 2.48 ChemAxon
logS -2.3 ALOGPS
pKa (strongest basic) 8.96 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 55.56 ChemAxon
rotatable bond count 7 ChemAxon
refractivity 75.1 ChemAxon
polarizability 28.74 ChemAxon
药物相互作用
食物相互作用
Not Available

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