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解説
ジメチソキンとともにキノリン誘導体の合成局所麻酔薬である。ジブカインは，表面，浸潤，伝達，脊髄の各麻酔に使用される。水溶液は煮沸可能で，コカインのようには分解せず，コカインの約 12倍，プロカインの約 48倍の効力を示す。持続時間はコカインの約2倍，プロカインの約9倍である。毒性はコカインの5～9倍，プロカインの約 40倍である。血管分布の多い組織に注射したときや，誤って血管内に注射したときには，けいれん，振戦，血圧下降，心機能抑制，房室ブロック，心停止，過敏反応などを呈することもある。ブリタニカ国際大百科事典 小項目事典 ブリタニカ
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効能
局所麻酔薬
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使用
Cinchocaine is a local anesthesic,used for Na+ channel blocker.
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定義
ChEBI: A monocarboxylic acid amide that is the 2-(diethylamino)ethyl amide of 2-butoxyquinoline-4-carboxylic acid. One of the most potent and toxic of the long-acting local anesthetics, its parenteral use was restricted to spinal anesthesia. It is now generally o
ly used (usually as the hydrochloride) in creams and ointments and in suppositories for temporary relief of pain and itching associated with skin and anorectal conditions.
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一般的な説明
Articaine has a secondary nitrogen with a pKa of 7.8. It containsan aromatic thiophene ring bioisostere of the phenylring found in most other amide anesthetics. The log P of abenzene ring is 2.13 and the thiophene ring log P is 1.81,thus the thiophene ring is more hydrophilic than a phenylring. Although the thiophene ring has less lipid solubilitythan a phenyl ring, articaine is a lipid-soluble compound dueto the propylamine, the branched methyl and the substitutionson the thiophene ring. The onset of action of articaineis similar to lidocaine’s onset of action.
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接触アレルゲン
Dibucaine hydrochloride is an amide group local anesthetic
that can induce allergic contact dermatitis.
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臨床応用
Articaine is availablein a 4% solution with epinephrine for use in infiltrationand nerve block anesthesia.Articaine is metabolized rapidly via plasma and tissuecarboxyesterase to its primary metabolite, the inactive,water-soluble carboxylic acid. Approximately 40% to 70%of articaine administered epidurally is metabolized to thecarboxylic acid, articainic acid. Approximately 4% to 15%of the articainic acid undergoes glucuronide conjugationand only 3% of the dose is recovered unchanged in theurine. The rapid plasma metabolism and reported inactivityof the carboxylic acid metabolite make articaine a potentiallysafer anesthetic agent when multiple or large dosesare necessary.
