テトラカイン 塩酸塩 化学特性,用途語,生産方法
外観
白色の結晶～結晶性粉末
溶解性
水,氷酢酸に易溶、エタノールに可溶、エーテルに不溶。水,氷酢酸に易溶、ぎ酸に極めて易溶、エタノールに可溶、無水酢酸に難溶、エーテル,ベンゼンにほとんど不溶。
解説
2-(dimethylamino)ethyl 4-(butylamino)benzoate monohydrochloride．C15H24N2O2·HCl(300.82)．p-アミノ安息香酸エステルを，まずN-ブチル化し，ついでジメチルアミノエタノールと反応させると得られる．
"融点147～150 ℃．水，氷酢酸，エタノールに可溶，エーテル，ベンゼンに不溶．局所麻酔薬として，脊椎麻酔に使用される．鎮痛の目的で軟膏としても用いられる．LD50 6.4 mg/kg(マウス，静注)．[CAS 136-47-0]
森北出版「化学辞典（第2版）
用途
薬理研究用。
用途
テトラカイン (tetracaine) とは局所麻酔剤の1つである。作用の強い麻酔薬であり、副作用も強いため用途は限られており、主に脊椎麻酔に使用されている。またリドカインと混合して局所麻酔として使用される場合もある。
用途
作用の強い麻酔薬であり、副作用も強いため用途は限られており、主に脊椎麻酔に使用されている。またリドカインと混合して局所麻酔として使用される場合もある。
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
コーパロン (昭和薬品化工); テトカイン (杏林製薬)
化学的特性
Tetracaine hydrochloride is a white, crystalline powder, odourless; hygroscopic; it has a slightly bitter taste and causes local numbness after being placed on the tongue. Soluble in water, soluble in ethanol (~750 g/l), practically insoluble in ether. even in the absence of light, it is gradually degraded on exposure to a humid atmosphere, the decomposition being faster at higher temperatures.
使用
Tetracaine hydrochloride is a local anesthetic used topically in opthalmology.It is a highly effective local anesthetic that reversibly blocks nerve function. It is clinically used for infiltration anesthesia, nerve block anesthesia, epidural anesthesia, etc. Compared with procaine, its local anesthesia effect is remarkable. Tetracaine hydrochloride has been widely used in clinical practice.
主な応用
Tetracaine hydrochloride is also known as ropivacaine hydrochloride, pantocaine, pantocaine and four ropivacaine hydrochloride. It is easily soluble in water and ethanol, but insoluble in ether, benzene. Tetracaine hydrochloride is a local anesthetic with long-acting ester. In addition, procaine is widely used in clinical, but because of its poor permeability and poor narcotic performance, a small tetracaine was found in 1930 found.
Tetracaine hydrochloride can be used for topical anesthesia, and 0.05%-0.1% tetracaine hydrochloride can provide long-term and good effect of surface anesthesia. Meanwhile, tetracaine hydrochloride is still widely used in ophthalmic surface anesthesia, which has a long time for surface anesthesia and sensory resistance.
製造方法
Synthesis of tetracaine hydrochloride using 4-Methyl-2-pentanone as starting material: To the reaction kettle, first add 320.0kg of methyl isobutyl ketone, then add 40.0kg (207mol) of 4-Butylaminobenzoic acid and 56.8kg of anhydrous potassium carbonate in turn, heat the oil bath to 116°C for reflux reaction for 4h, stop heating, and react for a while. Cool for 0.5h, then add 38.3kg (266mol) of 2-Dimethylaminoethyl Chloride Hydrochloride, continue to heat to 116°C for reflux reaction for 4h, and cool to below 30°C after the reaction is complete, then add deionized water 127.0 kg stirred for 30min, left standing for 1h, separated the organic layer, dried and concentrated to obtain an oily substance, then added 169.0kg of acetone and stirred, adjusted the pH value with concentrated hydrochloric acid to 3-4, and precipitated a large number of crystals, which continued to crystallize for 12h after freezing. , centrifugal filtration and drying to obtain 53.0kg of white solid which is tetracaine hydrochloride, the yield is 85.07%, and the HPLC purity is 99.34%.
定義
ChEBI: Tetracaine hydrochloride is a benzoate ester. It is a potent local anesthetic of the ester type used for surface and spinal anesthesia.
一般的な説明
Tetracaine hydrochloride is a local anesthetic drug and an ester derivative of
p-amino benzoic acid. It acts by interfering with the entry of sodium ions into nerve cells and is one of the commonly used topical anesthetics.
接触アレルゲン
Amethocaine is a local anesthetic used in dental surgery.
It was reported as an agent of contact dermatitis
in dentists or dental nurses and in ophthalmologists
副作用
Tetracaine hydrochloride is in the ester-type local anesthetic family of medications. It works by blocking the sending of nerve impulses. common side effects include Transient stinging, burning, and conjunctival redness, eye irritation, eye pain, ocular discomfort. Allergic reactions may uncommonly occur. Long term use is generally not recommended as it may slow healing of the eye. It is unclear if use during pregnancy is safe for the baby.
健康への影響
Tetracaine hydrochloride (TTC) is a long-lasting local anesthetic commonly used for topical anesthesia, which is water-soluble, has strong penetrability and a good anesthetic effect. However, TTC has a higher cytotoxicity compared with other local anesthetics due to its high permeability. Previous studies have reported that TTC exerts a cytotoxic effect on certain cell types, such as human corneal stromal cells and human corneal epithelial cells, inducing apoptosis and necrosis. Research jave found that large doses of intrathecal TTC increase the concentration of glutamate in cerebrospinal fluid, thereby causing neuronal injury in rabbits. In addition, AMPA receptor activation was revealed to be involved in TTC-induced neurotoxicity in the spinal cord. TTC-induced apoptosis may be triggered through Fas death receptors and mediated by Bcl-2 family proteins, in a mitochondria-dependent pathway. TTC-induced human corneal epithelial (HCEP) cell apoptosis via a death receptor-mediated mitochondrion-dependent pathway. Low concentrations of TTC induced the apoptosis of human T-lymphoma cells, whereas a higher concentration of TTC induced necrosis[1].
テトラカイン 塩酸塩 上流と下流の製品情報
原材料
準備製品