4-アミノ歇息香酸 エチル 化学特征,用处語,生産方式
外観
红色〜わずかにうすい黄色, 結晶〜結晶性粉末
定義
本品は、パラアミノ歇息香酸(PABA(*))のエチルエステルであり、次の化学式で表される。
参照表现称号：ＰＡＢＡ
消融性
エタノール及びアセトンに溶け、水にほとんど溶けない。
解説
C9H11NO2(165.19)．p-アミノ放置香酸エチルは，ベンゾカイン，アネステシンともいう．p-ニトロトルエンを二クロム酸カリウムと硫酸钠で过酸してp-ニトロ放置香酸とし，これを亜鉛と塩酸で還元して生じたp-アミノ放置香酸を，エタノールと塩化水素でエステル化すると得られる．紫色の結晶．融点89～91 ℃．無臭でやや苦味をもち，舌を麻ひさせる．エタノール，クロロホルム，エーテルに微溶，オリブ油に可溶，水に難溶．局所麻酔剤として外抹する．森北出书「化学工业辞典（第2版）
用处
牛、羊、豚および馬の局所麻酔薬、及び魚介類の鎮静?麻酔剤
用处
有機分解质料(医薬品、染料)。
用处
外表麻酔として感化します。
化粧品の成份用处
口腔ケア剤、口腔衛生剤、退色避免剤、外用鎮痛剤
効能
鎮痛薬, 外表麻酔薬, 鎮痒薬
商品名
アミノ歇息香酸エチル (マイラン製薬)
説明
Benzocaine (ethyl p-aminobenzoate) is used topically by itself or in combination with menthol or
phenol in nonprescription dosage forms such as gels, creams, ointments, lotions, aerosols, and
lozenges to relieve pain or irritation caused by such conditions as sunburn, insect bites,
toothache, teething, cold sores or canker sores in or around the mouth, and fever blisters.
Benzocaine is a lipophilic local anesthetic agent with a short duration of action.
Like most amino ester-type local anesthetics, it is easily hydrolyzed by plasma cholinesterase.
Because of its low pKa, however, it is un-ionized under most physiological conditions and, therefore, can only bind
to the lipid side of the local anesthetic receptor. It also can easily cross membranes
into systemic circulation to cause systemic toxicities. Furthermore, being a PABA derivative, it
has similar allergenic properties to procaine and is contraindicated with sulfonamide antibacterial
agents.
化学的特征
Benzocaine is a white odourless needle-like crystal, slightly soluble in water and easily soluble in organic solvents. For example: ethanol, chloroform, ether, soluble in almond oil, olive oil.
利用
Benzocaine is used as an anesthetic (Local and topical) that in products such as burn and sunburn remedies, hemorrhoidal creams, suppositories, creams for treatment of poison ivy, oral and gingival products, sore-throat sprays/lozenges, astringents, appetite suppressants, callus and wart remedies, athlete's-foot remedies, toothache- and denture-irritation products.
定義
ChEBI: Benzocaine is a benzoate ester having 4-aminobenzoic acid as the acid component and ethanol as the alcohol component. A surface anaesthetic, it is used to suppress the gag reflex, and as a lubricant and topical anaesthetic on the larynx, mouth, nasal cavity, respiratory tract, oesophagus, rectum, urinary tract, and vagina. It has a role as a topical anaesthetic, an antipruritic drug, an allergen and a sensitiser. It is a benzoate ester and a substituted aniline.
生物学の機能
Benzocaine is a PABA derivative used primarily for
topical application to skin and mucous membranes. Its
low aqueous solubility allows it to stay at the site of application
for long periods. Its minimal rate of absorption
after topical administration is associated with a low incidence
of systemic toxicity. Benzocaine is contraindicated
in patients with known sensitivity to ester-linked
anesthetics or PABA-containing compounds.
普通的な説明
Benzocaine is a unique local anesthetic because it does notcontain a tertiary amine. The pKa of the aromatic amine is 3.5ensuring that benzocaine is uncharged at physiological pH.Because it is uncharged, it is not water soluble but is ideal fortopical applications. The onset of action is within 30 secondsand the duration of drug action is 10 to 15 minutes.
臨床応用
Benzocaine is used for endoscopy, bronchoscopy, and topicalanesthesia. Benzocaine is available as a 20% solution topicalspray, in a 1% gel for mucous membrane application, and a14% glycerin suspension for topical use in the outer ear.Toxicity to benzocaine can occur when the topical doseexceeds 200 to 300 mg resulting in methemoglobinemia.Infants and children are more susceptible to this and methemoglobinemiahas been reported after benzocaine lubricationof endotracheal tubes and after topical administration to treata painful diaper rash.
宁静性プロファイル
Poison by ingestion and
intraperitoneal routes. Human systemic
effects by rectal route:
methemoglobinemia/carboxyhemoglobinem
ia in infants. A skin irritant and a mild
sensitizer. Local contact may cause contact
dermatitis. Used as a topical anesthetic and
as a sun-screening agent. When heated to
decomposition it emits highly toxic fumes of
NOx. See also ETHYL ALCOHOL and
ESTERS
純化方式
Crystallise Benzocaine from EtOH/H2O or EtOH (m 93-94o), and dry it in air. [Beilstein 14 H 422, 14 IV 1129.]
4-アミノ歇息香酸 エチル 下贱と下贱の製品情報
原资料
準備製品