プロピトカイン
アストラ1515 · プリロカイン · N-(2-メチルフェニル)-2-(プロピルアミノ)プロパンアミド · プロピトカイン · アストラ1512 · プロピトカイン (JAN) · PRILOCAINE BASE · Aβ25-35
識別子と物理属性
| CAS No. | 721-50-6 |
|---|---|
| 分子式 | C13H20N2O |
| 平均分子量 | 220.31 g/mol |
| 単同位体質量 | 220.15756326 g/mol |
| SMILES | CCCNC(C)C(=O)Nc1ccccc1C |
| InChIKey | MVFGUOIZUNYYSO-UHFFFAOYSA-N |
| PubChem CID | 4906 |
| ChEMBL | CHEMBL1194 |
| ChEBI | CHEBI:8404 |
| EC No. | 211-957-0 |
| DTXSID | DTXSID7031955 |
| 現地名 | プロピトカイン |
化学・物理的性質
| XLogP | 2.1 |
|---|---|
| 極性表面積 | 41.1 |
| 水素結合供与体数 | 2 |
| 水素結合受容体数 | 2 |
| 回転可能結合数 | 5 |
| 重原子数 | 16 |
| 形式電荷 | 0 |
| 複雑度 | 218 |
| 医薬品 | Pharmaceuticals |
| LogP（分配係数） | log Kow= 2.11 |
| 臭い | ODORLESS |
| 味 | INITIALLY ACID & THEN BITTER TASTE |
| Color/Form | NeedlesWHITE |
| 溶解度 | Crystals from ethanol + isopropyl etherreadily sol in watermp 167-168 °C /Hydrochloride/FREELY SOL IN ALCSLIGHTLY SOL IN CHLOROFORMVERY SLIGHTLY SOL IN ACETONEPRACTICALLY INSOL IN ETHER3.26e-01 g/L水にやや溶けやすく、アセトンとエタノールによく溶ける（96%）。6.169g/L(25℃) |
| Human Drugs | Breast FeedingLactationAnesthetics, LocalFDA approved drugs -> Active ingredientPharmaceuticals |
| 沸点 | 159-162 °C at 1.00E-01 mm Hg159-162 °C @ 1 mm Hgbp0.1 159-162° |
| 融点 | 37-38 °C37 - 38 °C37-38° |
| 屈折率 | Index of refraction: 1.5298 @ 20 °C/DnD20 1.5298 |
| Physical Description | Solid |
| Stability/Shelf Life | STABLE IN LIGHT & AIR |
| 密度 | 1.0117 (rough estimate) |
| 貯蔵条件 | 2-8°C |
| pKa（酸解離定数） | pKa 7.32 or 7.89 (Uncertain) |
| 外観・状態 | Solid |
| 色 | White to off-white |
| 主な用途 | 医薬品（低分子化合物） |
| InChI | InChI=1S/C13H20N2O/c1-4-9-14-11(3)13(16)15-12-8-6-5-7-10(12)2/h5-8,11,14H,4,9H2,1-3H3,(H,15,16) |
| InChIKey | MVFGUOIZUNYYSO-UHFFFAOYSA-N |
| SMILES | C(NC1=CC=CC=C1C)(=O)C(NCCC)C |
| CAS データベース | 721-50-6(CAS DataBase Reference) |
| NISTの化学物質情報 | Propanamide, n-(2-methylphenyl)-2-(propylamino)-(721-50-6) |
化学的特性
White or almost white, crystalline powder.
安全性と法規制
| GHS 分類 | WarningH302 (98.6%): Harmful if swallowed [Warning Acute toxicity, oral]P264, P264+P265, P270, P273, P280, P301+P317, P302+P352, P305+P351+P338, P321, P330, P332+P317, P337+P317, P362+P364, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 69 reports by companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. |
|---|---|
| 規制情報 | Propanamide, N-(2-methylphenyl)-2-(propylamino)-: Does not have an individual approval but may be used under an appropriate group standard |
| その他の安全情報 | IMAP assessments - Propanamide, N-(2-methylphenyl)-2-(propylamino)-: Environment tier I assessment |
| FDA 要件 | Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended21 U.S.C. 321-392). |
| Hazard Classes and Categories | Acute Tox. 4 (98.6%) |
| 処分方法 | SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices. |
| 相互作用 | ...MOUSE TRIALS INDICATE INCR TOXICITY WHEN COMBINED WITH TETRACAINE....PRILOCAINE...REPORTED TO INTERACT WITH SUCCINYLCHOLINE /RESULTING IN INCR IN INTENSITY & DURATION OF SUCCINYLCHOLINE-INDUCED NEUROMUSCULAR BLOCKADE & RESP DEPRESSIONOTHER DEPOLARIZING MUSCLE RELAXANTS (EG DECAMETHONIUM) & NONDEPOLARIZING MUSCLE RELAXANTS (EG GALLAMINE TRIETHIODIDE & PANCURONIUM) MAY BEHAVE SIMILARLY/..../PRILOCAINE/ PRODUCED A SLIGHT INCR IN INTENSITY OF NEUROMUSCULAR BLOCKADE /OF ALCURONIUM CHLORIDE/. ...MARKED DECR IN TIDAL VOL, INDICATING RESP DEPRESSION, WAS OBSERVED...EPINEPHRINE PROLONGS THE EFFECT /OF PRILOCAINE/. /PRILOCAINE HCL/For more Interactions (Complete) data for PRILOCAINE (15 total), please visit the HSDB record page. |
| Non-Human Toxicity Excerpts | ...CAPABLE OF INDUCING METHEMOGLOBINEMIA IN LAB ANIMALS... /PRILOCAINE HCL/ |
| Antidote and Emergency Treatment | ALTHOUGH METHEMOGLOBINEMIA IS READILY REVERSED BY THE IV ADMIN OF METHYLENE BLUE ... THE THERAPEUTIC EFFECT MAY BE SHORT-LIVED BECAUSE METHYLENE BLUE MAY BE CLEARED BEFORE CONVERSION OF ALL THE METHEMOGLOBIN TO HEMOGLOBIN. /PRILOCAINE HCL/ |
| Effects During Pregnancy and Lactation | ◉ Summary of Use during Lactation◈ What is prilocaine? |
| 水環境危害等級（WGK） | WGK 3 |
| 税関コード | 2924296000 |
| 危険等級 | Acute Tox. 4 OralEye Irrit. 2 |
| 貯蔵分類 | 11 - Combustible Solids |
| 有害物質データ | 721-50-6(Hazardous Substances Data) |
用途
用途
プリロカイン（英: Prilocaine）は、アミド型の局所麻酔薬の一つ。
使用
Prilocaine is a local anesthetic of the amino amide type. Prilocaine is often used in dentistry. Prilocaine is also often combined with lidocaine as a preparation for dermal anesthesia (lidocaine/prilocaine or EMLA), for treatment of conditions like paresthesia.
一般的な説明
Prilocaine hydrochloride is a water-soluble salt available asa solution for nerve block or infiltration in dental procedures.Prilocaine is used for intravenous regional anesthesiaas the risk of CNS toxicity is low because of the quick metabolism.Prilocaine prepared in the crystal form is used inEMLA for topical administration to decrease painful needlesticks in children. Prilocaine 4% solution should be protectedfrom light and the manufacturer recommends discardingif the solution turns pinkish or slightly darker than lightyellow. Solutions are available in various concentrations upto 4%, with or without epinephrine and with or withoutpreservatives.