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低用量経口プロプラノロルの後のベータブロックと血中濃度:肝臓の"ファーストパス"の値が再検討されました
Lancet (London, England)
|February 25, 1978
まとめ
低用量プロプラノロルは,心拍数と血圧に対するイソプレナリンの効果を効果的に阻害し,ベータ阻害を示す. これは,ヒトにおける肝臓における提案された"ファーストパス効果"の値に異議を唱える.
科学分野:
- 薬理学 薬理学とは
- 心血管生理学 心血管の生理学
背景:
- 肝臓系は肝臓系である.
- ファーストパス効果です.
- 経口薬剤の生物利用可能性に影響を与える薬理学的な現象である.
- ヒトにおけるプロプラノロールのこの効果を飽和させるための値投与量を提案しています.
研究 の 目的:
- 低用量の経口プロプラノロールのβ阻害効果を調査する.
- 低用量プロプラノロルのイソプレナリン誘発の心血管およびプラズマレニン活性変化に対する影響を評価する.
- ヒトにおける肝臓の"ファーストパス効果"仮説を評価する.
主な方法:
- 6人の健康な被験者は,口服プロプラノロール (5回8時間毎に5mg) を受け,その後にイソプレナリン注射を受けた.
- 測定には,心拍数,血圧,および静止状態の血レニン活性,およびイソプレナリン投与後の測定が含まれていました.
- プロプラノロールの血濃度は,フッ素測定とガス液体染色学を用いて定量化されました.
主要な成果:
- プロプラノロールは,静止時の心拍数,静脈圧,およびプラズマレニン活性を著しく低下させた.
- イソプレナリンによって誘発された心拍数,気圧,および血レニン活性の増加は,プロプラノロールによって有意に減少しました.
- プロプラノロールはイソプレナリンの効果を65~78%遮断し,血濃度2.3~8.5ng/mlに達した.
結論:
- 低用量プロプラノロルは,有意なベータ阻害を示し,イソプレナリンの心血管およびレニン放出効果を効果的に抑制します.
- 低用量プロプラノロルで観察されたβ阻害は,ヒトにおける肝臓の"ファーストパス効果"のための高用量値の存在と矛盾しています.
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