Question:

If the lipophilicity of benzodiazepines increases, what is the effect:

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Lipophilic = "Fat-loving" = Crosses the fatty Blood-Brain Barrier easily.
Updated On: May 25, 2026
  • Increase in CNS penetration
  • Increase in water solubility
  • Increase in metabolic clearance
  • Increase in renal excretion
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The Correct Option is A

Solution and Explanation

Step 1: Concept
Lipophilicity (lipid solubility) is a key factor in determining how easily a drug crosses biological membranes.

Step 2: Meaning

The Blood-Brain Barrier (BBB) is a highly selective semipermeable border that favors the passage of lipid-soluble substances.

Step 3: Analysis

Benzodiazepines act on GABA receptors in the brain. Increasing their lipophilicity allows them to dissolve more readily in the lipid bilayer of the BBB, leading to faster and more extensive entry into the Central Nervous System (CNS).

Step 4: Conclusion

Higher lipophilicity directly correlates with enhanced CNS penetration for this class of drugs. Final Answer: (A)
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