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危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

  H361：生殖能または胎児への悪影響のおそれの疑い

  H411：長期的影響により水生生物に毒性

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P281：指定された個人用保護具を使用すること。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P332+P313：皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。

  P362：汚染された衣類を脱ぎ、再使用す場合には洗濯をすること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

ラベタロール 価格

ラベタロール 化学特性,用途語,生産方法

• 効能

  血圧降下薬, α1β遮断薬

• 説明

  Labetalol is an α-adrenergic and α-1 blocking agent which caused contact dermatitis and a contact anaphylactoid reaction during patch testing in a nurse.

• 使用

  Labetalol is used to treat essential hypertension.

• 定義

  ChEBI: A secondary amino compound formally derived from ammonia by replacing two of the hydrogens by 2-(3-carbamoyl-4-hydroxyphenyl)-2-hydroxyethyl and 4-phenylbutan-2-yl groups. It is an adrenergic antagonist used to treat high blood pressure.

• 生物学の機能

  Labetalol (Normodyne, Trandate) possesses both - blocking and β-blocking activity and is approximately one-third as potent as propranolol as a -blocker and one-tenth as potent as phentolamine as an -blocker. The ratio of β- to α-activity is about 3:1 when labetalol is administered orally and about 7: 1 when it is administered intravenously. Thus the drug can be most conveniently thought of as a β -blocker with some -blocking properties.

• 一般的な説明

  Labetalol is a phenylethanolamine derivative, is representative of a classof drugs that act as competitive blockers at α1-, β1-, andβ2-receptors. It is a more potent β-blocker than α-blocker.Because it has two asymmetric carbon atoms (1 and 1' ), it existsas a mixture of four isomers. It is this mixture that is usedclinically in treating hypertension. The different isomers,however, possess different α- and β-blocking activities. The -blocking activity resides solely in the (1R,1 'R) isomer,whereas the 1-blocking activity is seen in the (1S,1 R) and(1S,1'S) isomers, with the (1S,1'R) isomer possessing thegreater therapeutic activity.

• 接触アレルゲン

  This beta-adrenergic and alpha-1 blocking agent caused contact dermatitis and a contact anaphylactoid reaction during patch testing in a nurse.

• 作用機序

  Labetalol produces equilibrium-competitive antagonism at β-receptors but does not exhibit selectivity for β1- or β2-receptors. Like certain other β-blockers (e.g., pindolol and timolol), labetalol possesses some degree of intrinsic activity. This intrinsic activity, or partial agonism, especially at β2-receptors in the vasculature, has been suggested to contribute to the vasodilator effect of the drug. The membrane-stabilizing effect, or local anesthetic action, of propranolol and several other β-blockers, is also possessed by labetalol, and in fact the drug is a reasonably potent local anesthetic.
  Labetalol appears to produce relaxation of vascular smooth muscle not only by α-blockade but also by a partial agonist effect at β2-receptors. In addition, labetalol may produce vascular relaxation by a direct non–receptor-mediated effect. Labetalol can block the neuronal uptake of norepinephrine and other catecholamines. This action, plus its slight intrinsic activity at α-receptors, may account for the seemingly paradoxical, although infrequent, increase in blood pressure seen on its initial administration.

• 薬物動態学

  Labetalol is almost completely absorbed from the gastrointestinal tract. However, it is subject to considerable first-pass metabolism, which occurs in both the gastrointestinal tract and the liver, so that only about 25% of an administered dose reaches the systemic circulation. While traces of unchanged labetalol are recovered in the urine, most of the drug is metabolized to inactive glucuronide conjugates.The plasma half-life of labetalol is 6 to 8 hours, and the elimination kinetics are essentially unchanged in patients with impaired renal failure.

• 臨床応用

  Labetalol is a clinically usefulantihypertensive agent. The rationale for its use in themanagement of hypertension is that its α-receptor–blockingeffects produce vasodilation and its β-receptor–blockingeffects prevent the reflex tachycardia usually associated withvasodilation. Although labetalol is very well absorbed, it undergoesextensive first-pass metabolism.

• 副作用

  There have been reports of excessive hypotension and paradoxical pressor effects following intravenous administration of labetalol. These latter effects may be due to a labetalol-induced blockade of neuronal amine uptake, which increases the concentrations of norepinephrine in the vicinity of its receptors.
  Approximately 5% of the patients who receive labetalol complain of side effects typical of noradrenergic nervous system suppression. These include postural hypotension, gastrointestinal distress, tiredness, sexual dysfunction, and tingling of the scalp. Most of these effects are related to α-blockade, although the tingling of the scalp may be due to the drug’s intrinsic activity at α-receptors. Side effects associated with β-blockade, such as induction of bronchospasm and congestive heart failure, may also occur, but generally at a lower frequency than -receptor–associated effects.
  Skin rashes have been reported, as has an increase in the titer of antinuclear antibodies. Despite the latter observation, the appearance of a systemic lupus syndrome is rare. Labetalol also has been reported to interfere with chemical measurements of catecholamines and metabolites.

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