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効能
局所麻酔薬, 抗不整脈薬, ナトリウムチャネル遮断薬
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商品名
オリベス (高田製薬); キシロカイン (アスペンジャパン); キシロカイン (アスペンジャパン); キシロカイン (アスペンジャパン); キシロカイン (アスペンジャパン); キシロカイン (アスペンジャパン); キシロカイン (アスペンジャパン); キシロカイン (アスペンジャパン); リドカイン (ナガセ医薬品); リドカイン (ナガセ医薬品); リドカイン (高田製薬)
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化学的特性
White to Off-White Solid
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使用
Anesthetic (local); antiarrhythmic (class IB). Long-acting, membrane stabilizing agent against ventricular arrhythmia. Originally developed as a local anesthetic.
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定義
ChEBI: Lidocaine hydrochloride is the anhydrous form of the hydrochloride salt of lidocaine. It functions as both a local anesthetic and cardiac depressant, and is commonly used as an antiarrhythmic agent. Its potency is higher and its effects last longer than those of procaine, but its duration of action is shorter than that of bupivacaine or prilocaine.
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生物学の機能
Lidocaine hydrochloride (Xylocaine) is the most commonly
used local anesthetic. It is well tolerated, and in
addition to its use in infiltration and regional nerve
blocks, it is commonly used for spinal and topical anesthesia
and as an antiarrhythmic agent.
Lidocaine has a more rapidly occurring, more intense,
and more prolonged duration of action than does procaine.
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一般的な説明
Lidocaine hydrochloride,2-(diethylamino)-2 ,6 -acetoxylidide monohydrochloride(Xylocaine), was conceived as a derivative of gramine(3-dimethylaminomethylindole) and introduced as a localanesthetic. It is now being used intravenously as a standardparenteral agent for suppression of arrhythmias associatedwith acute myocardial infarction and cardiac surgery.It isthe drug of choice for the parenteral treatment of prematureventricular contractions.
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臨床応用
Lidocaine hydrochloride is a class IB antiarrhythmicagent with a different effect on the electrophysiologicalproperties of myocardial cells from that of procainamideand quinidine. It binds with equal affinity to the active (A)and inactive (I) Na+ ion channels. It depresses diastolic depolarizationand automaticity in the Purkinje fiber networkand increases the functional refractory period relative toaction potential duration, as do procainamide and quinidine.It differs from the latter two drugs, however, in that it doesnot decrease, and may even enhance, conduction velocity and increase membrane responsiveness to stimulation.There are fewer data available on the subcellular mechanismsresponsible for the antiarrhythmic actions of lidocainethan on the more established drug quinidine. It has been proposedthat lidocaine has little effect on membrane cation exchangeof the atria. Sodium ion entrance into ventricularcells during excitation is not influenced by lidocaine becauseit does not alter conduction velocity in this area.Lidocaine hydrochloride does depress Na+ influx duringdiastole, as do all other antiarrhythmic drugs, to diminishautomaticity in myocardial tissue. It also alters membraneresponsiveness in Purkinje fibers, allowing increased conductionvelocity and ample membrane potential at the timeof excitation.
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安全性プロファイル
Poison by ingestion,
intraperitoneal, intravenous, subcutaneous,
intramuscular, and intratracheal routes.
Human systemic effects: somnolence,
respiratory depression, low blood pressure,
cardiomyopathy includmg infarction, pulse
rate increase. An experimental teratogen.
Other experimental reproductive effects. A
skin and eye irritant. An anesthetic. When
heated to decomposition it emits very toxic
fumes of NOx and HCl.
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貯蔵
Store in a tightly closed container at room temperature away from light
and moisture. Do not store in the bathroom. Do not freeze. Keep all medications away from children and pets.
