プロカイン塩酸塩

外観

白色、結晶～結晶性粉末

溶解性

水に易溶、エタノールに可溶、クロロホルムに難溶、エーテルに不溶。

解説

塩酸プロカイン，プロカイン塩酸塩ともいう．p-ニトロ安息香酸をp-ニトロベンゾイルクロリドとし，これをベンゼン中で2-(ジエチルアミノ)エタノールと反応させてから還元して合成する．白色の板状結晶または結晶性の粉末．無臭で，味は苦く舌を麻ひする．融点51 ℃．水に易溶，エタノールに難溶．毒性はコカインの1/6～1/10．局所麻酔薬に使用される．

用途

局所麻酔剤、生理作用研究用。

用途

ナトリウム透過性抑制作用を 示します。

用途

ナトリウム透過性抑制作用を 示します。

効能

局所麻酔薬

商品名

プロカイン塩酸塩 (日医工); プロカイン塩酸塩 (東和薬品); プロカニン (光製薬); ロカイン (扶桑薬品工業); ロカイン (扶桑薬品工業); 塩プロ (共和クリティケア); 塩プロ (共和クリティケア); 塩酸プロカイン (マイラン製薬); 塩酸プロカイン (日新製薬－山形)

説明

Procaine hydrochloride, also called Novocain, or Novocaine, a topical anesthetic, which can block the nerve fiber conduction temporarilyand has a narcotic effect,strong effect, low toxicity, and non-addictive, but on the skin, mucosal penetration is weak, unsuitable for surface anesthesia, patients are used for infiltration, conduction and spinal anesthesia.
The structure of procaine hydrochloride with aromatic primary amino, easy oxidation discoloration pH, temperature, UV, oxygen and metal ions can accelerate the oxidation discoloration. The aqueous solution was stable in pH3.0~5. So preparation of procaine hydrochloride injection, it generally takes add acid to regulate pH 3.3 to 5.5, and strictly control the sterilization temperature and time. to 100 ℃ steam sterilization 30min circulation is appropriate, and should pay attention to shading, sealed save.
The above information is edited by the chemicalbook of Kui Xiongfeng.

化学的特性

Procaine hydrochloride is a white crystalline, odorless powder that is freely soluble in water, but less soluble in alcohol and almost insoluble in ether; solutions acid to litmus. Because the ester bond in the structure can be hydrolyzed to produce p-aminobenzoic acid and diethylaminoethanol, under certain conditions, p-aminobenzoic acid can be further decarboxylated to produce toxic aniline. Procaine hydrochloride has aromatic primary amino groups in its structure, which can be easily oxidized and discolored. pH, temperature, ultraviolet light, oxygen and metal ions can accelerate the oxidation and discoloration.

主な応用

Procaine hydrochloride has been used as a component of Krebs Henseleit buffer for incubating the left ventricular cardiac tissue in its resting length. It has also been used as an inducer in M9 media for induction assay. It is a sodium channel blocker and DNA methylation inhibitor.

副作用

おもな適用は手術のための麻酔で、脊椎(せきつい)麻酔、硬膜外麻酔、伝達麻酔、浸潤麻酔に用いられる。極量は硬膜外麻酔や伝達麻酔で1回0.6グラム、浸潤麻酔で1回1グラムである。副作用としてショックやアレルギー反応がみられるほか、悪心(おしん)、嘔吐(おうと)、めまい、不安、興奮などの中枢神経刺激症状、血圧下降、徐脈などの心血管症状がある。なお、プロカインには心筋の被刺激性を抑制する抗不整脈効果が認められているが、持続性が短いことや中枢神経への刺激が強いことなどのために使われず、この欠点をなくしたものとして塩酸プロカインアミドが抗不整脈剤に繁用されている。

一般的な説明

Procaine hydrochloride is a synthetic compound that belongs to the class of local anesthetic drugs. It has a structure similar to the natural compounds that participate in nerve impulse transmission. It shows interaction with the cellular membranes causing membrane lipids to expand, membrane-bound calcium to displace and change the structure of the proteins that are responsible for regulating the cell permeability and shape.

危険性

Toxic by ingestion.

接触アレルゲン

Procaine is a local anesthetic with para-amino function. Sensitization mainly concerns the medical, dental, and veterinary professions.

安全性プロファイル

Poison by ingestion, subcutaneous, intravenous, and intraperitoneal routes. Human systemic effects: acute renal fdure. May have human reproductive effects. See also ESTERS. When heated to decomposition it emits very toxic fumes of HCl and NO,. Used as a local anesthetic.

純化方法

Novocain is recrystallised from aqueous EtOH. It is soluble at 25o in H2O (86.3%), EtOH (2.6%) and Me2CO (1%), it is slightly soluble in CHCl3, but is almost insoluble in Et2O. The anhydrous free base is recrystallised from ligroin or Et2O and has m 61o. [Einhorn Justus Liebigs Ann Chem 371 125 1909, IR: Szymanski & Panzica J Amer Pharm Assoc 47 443 1958, Beilstein 14 IV 1138.]

予防処置

Procaine hydrochloride is used for infiltration, nerve block, peridural and spinal anest sthesia. It is considered a fairly safe drug if suitable precautions are observed. However, as with any anesthetic， idiosyncrasy may be encountered. Slow administration and avoidance of accidental intravenous injection are advisable. In local administration, if increased sensitivity to procaine is suspected, as in patients with cardiac disease or endocrine disorders (such as hyperthyroidism), an initial small dose to test tolerance is recommended. (Physicians' Desk Reference, 35th ed, p. 695)