トルバプタン

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

  H361：生殖能または胎児への悪影響のおそれの疑い

  H362：授乳中の子に害を及ぼすおそれ

• 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。

  P260：粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。

  P263：妊娠中/授乳期中は接触を避けること。

  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。

  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。

  P281：指定された個人用保護具を使用すること。

  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。

  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。

トルバプタン 価格

トルバプタン 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色, 結晶～結晶性粉末

• 用途

  バソプレシンV2 受容体阻害 剤です。バソプレシンによる水再吸収を阻害 し、電解質排泄の増加を伴わない利尿作用を 示します。

• 効能

  利尿薬, バソプレシンV2受容体拮抗薬

• 商品名

  サムスカ (大塚製薬)

• 使用上の注意

  不活性ガス封入

• 説明

  The potent antidiuretic hormone AVP orchestrates the regulation of free water absorption, body fluid osmolality, cell contraction, blood volume, and blood pressure through stimulation of three G-proteincoupled receptor subtypes:V₁-vascular types a and b, V₂-renal, and V₃-pituitary. Increased AVP secretion is the trademark of several pathophysiological disorders, including heart failure, impaired renal function, liver cirrhosis, and SIADH. As a consequence, these patients experience excess water retention or inadequate free-water excretion, which results in the dilution of sodium concentrations, frequently manifesting as clinical hyponatremia (serum sodium concentration <135 mmol/L). This electrolyte imbalance increases mortality rates by 60-fold. Selective antagonism of the AVP V₂receptor promotes water excretion without perturbing electrolyte balance making it an appealing target for preventing disease progression. Following the introduction of the dual AVP V_1a/V₂ receptor antagonist conivaptan, tolvaptan has recently been launched as a nonpeptide, selective V₂ receptor antagonist with potent aquaretic attributes for the treatment of hypervolemic and euvolemic hyponatremia (serum sodium concentration of <125 mmol/L or less distinct hyponatremia that is symptomatic and has resisted correction with fluid restriction). As a more potent and selective V₂ receptor antagonist, tolvaptan is a follow-up to mozavaptan, which possesses weak V₁ receptor antagonism and was approved for the treatment of SIADH in Japan. .

• 化学的特性

  White Solid

• 来歴

  Tolvaptan was discovered by Otsuka Pharmaceutical Co., Ltd. (Otsuka). In May 2009, tolvaptan (Samsca; Otsuka) was approved by the US FDA for the treatment of clinically significant hypervolaemic and euvolaemic hyponatraemia. The U.S. Food and Drug Administration (FDA) granted tolvaptan a fast track designation for clinical trials investigating its use for the treatment of polycystic kidney disease. The FDA granted Jynarque an orphan drug designation in April 2012, for the treatment of autosomal dominant polycystic kidney disease.

• 使用

  Labelled Tolvaptan s, and the syndrome of inappropriate antidiuretic hormone (SIADH).

• 臨床応用

  Tolvaptan, also known as OPC-41061, is a selective, competitive arginine vasopressin receptor 2 antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Otsuka Pharmaceutical licensed tolvaptan under the trade name Samsca after the FDA approved the drug in May 2009. Tolvaptan has also shown efficacy against polycystic kidney disease. In a 2004 trial, tolvaptan administered with traditional diuretics was noted to increase excretion of excess fluids and improve blood sodium levels in patients with heart failure without producing side effects such as hypotension (low blood pressure) or hypokalemia (decreased blood levels of potassium). The drug also exhibited no adverse effect on kidney function.

• 副作用

  The most common adverse events were thirst, dry mouth, asthenia, constipation, pollakiuria or polyuria, and hyperglycemia. The recommended starting dose is 15 mg daily with a daily 15-mg adjustment to a maximum of 60 mg daily to raise serum sodium concentration. Initiation should be in a hospital setting where serum sodium and volume status may be monitored since too rapid correction of hyponatremia (>12 mEq/L/24 h) can cause osmotic demyelination resulting in dysarthria, mutism, dysphagia, lethargy, spastic quadriparesis, seizures, coma, and death. In addition to avoiding concomitant use of strong CYP3A4 inhibitors, tolvaptan is contraindicated in settings of urgent need to raise serum sodium acutely, in patients with an inability to sense or appropriately respond to thirst, in hypovolemic hyponatremia conditions, and in anuric patients.

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トルバプタン スペクトルデータ(¹HNMR)

150683-30-0, トルバプタン キーワード