グアンファシン塩酸塩

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H301：飲み込むと有毒

• 注意書き

  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。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P405：施錠して保管すること。

グアンファシン塩酸塩 価格

グアンファシン塩酸塩 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色粉末～結晶

• 効能

  血圧降下薬, α2アドレナリン受容体作動薬

• 商品名

  インチュニブ (塩野義製薬)

• 使用

  Centrally acting a-adrenoceptor agonist. Antihypertensive

• 一般的な説明

  Guanfacine hydrochloride,N-(aminoiminomethyl)-2,6-dichlorobenzeneacetamide(Tenex), is structurally related to clonidine hydrochloride andguanabenz acetate and shares many of their pharmacologicalproperties. The drug has a longer duration of action than eitherclonidine hydrochloride or guanabenz acetate. It lasts upto 24 hours. It also requires much longer (8–12 hours) for apeak effect to occur after the drug is administered.

• 生物活性

  Selective α 2A -adrenoceptor agonist (K d = 31 nM). Displays 60-fold selectivity over α 2B -adrenoceptors. Also available as part of the α 2 -Adrenoceptor Tocriset™ .

• 薬物動態学

  The pharmacokinetic properties for guanfacine differ from those of clonidine, guanabenz, and α-methyldopa. At pH 7.4, guanfacine is predominately (67%) in the nonionized, lipid-soluble base form, which accounts for its high oral bioavailability (>80%). Following an oral dose, peak plasma concentrations occur in 1 to 4 hours, with a relatively long elimination half-life of 14 to 23 hours. The maximum blood pressure response occurs in 8 to 12 hours after oral administration and is maintained up to 36 hours following its discontinuation. Following IV dosing, guanfacine achieves the highest concentrations in liver and kidney, with low concentrations in the brain. Guanfacine is 64% bound to plasma proteins. In patients with hepatic or renal impairment, its elimination half-life may be prolonged.
  Guanfacine is metabolized principally by hepatic hydroxylation to its inactive metabolite, 3-hydroxyguanfacine (20%), which is eliminated in the urine as its glucuronide (30%), sulfate (8%), or mercapturic acid conjugate (10%), and 24 to 37% is excreted as unchanged guanfacine. Its nearly complete bioavailability suggests no evidence of any first-pass effect. Guanfacine and its inactive metabolites are excreted principally in urine, with approximately 80% of its oral dose excreted in urine within 48 hours.

• 臨床応用

  Overall, the therapeutic applications for guanfacine are similar to those of the other centrally acting α2-adrenergic agonists and methyldopa. It has been effective as monotherapy in the treatment of patients with mild to moderate hypertension. One advantage for guanfacine is its once-a-day dosing schedule. The use of diuretics to prevent accumulation of fluid may allow a reduction in the dosage for guanfacine.

• 副作用

  Overall, although the frequency of troublesome adverse effects produced by guanfacine is similar to that produced by clonidine and the other centrally acting sympatholytics, their incidence and severity are lower with guanfacine. Unlike clonidine, abrupt discontinuation of guanfacine rarely results in rebound hypertension. When a withdrawal syndrome has occurred, its onset was slower and its symptoms less severe than the syndrome observed with clonidine.

グアンファシン塩酸塩 上流と下流の製品情報

グアンファシン塩酸塩 生産企業

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グアンファシン塩酸塩 スペクトルデータ(¹HNMR)

29110-48-3, グアンファシン塩酸塩 キーワード