CNS Drug Delivery: Prodrug Approaches
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Questions and Answers

What is one of the major difficulties in the development of drugs for the CNS?

  • Crossing the blood-brain barrier (BBB) (correct)
  • Active efflux from the brain into the blood
  • Passive diffusion
  • Reaching peripheral immune cells

    • Which prodrug strategy involves increasing carrier-mediated or receptor mediated transport through the BBB?

  • Decreasing the active efflux of the drug from the brain into the blood
  • Increasing passive diffusion by masking polar groups on the parent drug
  • Increasing carrier-mediated or receptor mediated transport through the BBB (correct)
  • Decreasing the process of prodrug biotransformation in peripheral tissues

    • Why is it essential for prodrug biotransformation to be slow in peripheral tissues but fast in the brain?

  • To prevent transport of nutrients into the brain
  • To achieve therapeutically effective doses in the CNS (correct)
  • To prevent central neurotransmitters from reaching the circulatory system
  • To inhibit the passage of neurotoxic substances across the BBB

    • Which amino acid analog and precursor crosses the BBB via LAT1 and is then decarboxylated by AADC to dopamine?

    <p>L-DOPA</p> Signup and view all the answers

    How is transport of molecules across the BBB achieved?

    <p>Diffusion as a passive process</p> Signup and view all the answers

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