塩酸プロパラカイン 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
表面麻酔薬 (点眼薬)
説明
Proparacaine Hydrochloride is the hydrochloride salt form of proparacaine, a benzoic acid derivative with local anesthetic property. Proparacaine hydrochloride stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting sodium ion influx required for the initiation and conduction of impulses within the neuronal cell, and resulting in a loss of sensation.
使用
Topical anesthetic (ophthalmic); Neuronal conductance inhibitor.
brand name
Alcaine (Alcon); Ophthetic (Allergan); Paracaine (Optopics).
臨床応用
Proparacaine Hydrochloride Ophthalmic Solution is indicated for topical anesthesia in ophthalmic practice.
副作用
Occasional temporary stinging, burning and conjunctival redness may occur with the use of proparacaine. A rare, severe, immediate-type, apparently hyperallergic corneal reaction characterized by acute, intense and diffuse epithelial keratitis, a gray, ground glass appearance, sloughing of large areas of necrotic epithelium, corneal filaments and sometimes iritis with descemetitis has been reported. Allergic contact dermatitis from proparacaine with drying and fissuring of the fingertips has been reported.
Mode of action
The mechanism of action of proparacaine hydrochloride is to reduce the instantaneous permeability of neurons to sodium, stabilize the nerve cell membrane, and prevent the generation and conduction of nerve electrical impulses, thereby producing anesthesia.Likely inhibits epithelial voltage gated sodium channels like other local anesthetics.
参考文献
1. Identification, synthesis and structural confirmation of process-related impurities in proparacaine hydrochloride. DOI:
10.1016/j.jpba.2020.1134972.
https://pi.bausch.com/globalassets/pdf/PackageInserts/Pharma/Rx-Generics/Proparacaine-HCl-Ophthalmic-Solution.pdf 3. Imming P., Sinning C., Meyer A. Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct; 5(10):821-34. DOI:
10.1038/nrd21324. T., Levent T., Inci M.A. Toxic keratopathy associated with abuse of topical anesthetics and amniotic membrane transplantation for treatment. Int J Ophthalmol. 2015; 8(5): 938–944. DOI:
10.3980/j.issn.2222-3959.2015.05.155. Proparacaine Hydrochloride Topical Drop and Intracameral 0.5% Lignocaine for Phacotrabeculectomy in Patients with Primary Open Angle Glaucoma DOI:
10.4103/0974-9233.1346696.
https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=447a2a64-0507-4fe8-bb44-cc36c3916151&type=display
塩酸プロパラカイン 上流と下流の製品情報
原材料
準備製品