About: Peripherally selective drug

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Peripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood–brain barrier. By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opioids cause sedation when given at a sufficiently high dose, but peripherally selective opioids can act on the rest of the body without entering the brain and are less likely to cause sedation. These peripherally selective opioids can be used as antidiarrheals, for instance loperamide (Imodium).

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  • Peripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood–brain barrier. By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opioids cause sedation when given at a sufficiently high dose, but peripherally selective opioids can act on the rest of the body without entering the brain and are less likely to cause sedation. These peripherally selective opioids can be used as antidiarrheals, for instance loperamide (Imodium). Mechanisms of peripheral selectivity include physicochemical hydrophilicity and large molecular size, which prevent drug permeation through the lipid bilayer cell membranes of the blood–brain barrier, and efflux out of the brain by blood–brain barrier transporters such as P-glycoprotein among many others. Transport out of the brain by P-glycoprotein is thought to be responsible for the peripheral selectivity of many drugs, including loperamide, domperidone, fexofenadine, bilastine, cetirizine, ivermectin, and dexamethasone, among others. (en)
  • 末梢選択性薬剤(Peripherally selective drug)は、血液脳関門によって中枢神経系 (CNS) から排除されるため、その主な作用機序が中枢神経系を除いて生じる。中枢神経系から排除されることで、これらの薬剤は脳や脊髄への影響によって生じる副作用を生じることなく、身体の他の部分に作用しえる。例えば、多くのオピエート（鎮痛性麻薬）は高用量では鎮静を起こすが、末梢選択性薬剤では脳へと侵入せずに体の残りの部分に作用することができ、鎮静の原因となる可能性は低い。 (ja)
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  • 末梢選択性薬剤(Peripherally selective drug)は、血液脳関門によって中枢神経系 (CNS) から排除されるため、その主な作用機序が中枢神経系を除いて生じる。中枢神経系から排除されることで、これらの薬剤は脳や脊髄への影響によって生じる副作用を生じることなく、身体の他の部分に作用しえる。例えば、多くのオピエート（鎮痛性麻薬）は高用量では鎮静を起こすが、末梢選択性薬剤では脳へと侵入せずに体の残りの部分に作用することができ、鎮静の原因となる可能性は低い。 (ja)
  • Peripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood–brain barrier. By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opioids cause sedation when given at a sufficiently high dose, but peripherally selective opioids can act on the rest of the body without entering the brain and are less likely to cause sedation. These peripherally selective opioids can be used as antidiarrheals, for instance loperamide (Imodium). (en)
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  • 末梢選択性薬剤 (ja)
  • Peripherally selective drug (en)
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