Podcast
Questions and Answers
Lipophilic substituents on ICS can decrease receptor affinity
Lipophilic substituents on ICS can decrease receptor affinity
False
Prednisolone and hydrocortisone are more effective as inhaled steroids due to their higher water solubility and lower lipophilicity
Prednisolone and hydrocortisone are more effective as inhaled steroids due to their higher water solubility and lower lipophilicity
False
There is a sharp increase in water solubility when the lipophilicity is logP ≥ 4
There is a sharp increase in water solubility when the lipophilicity is logP ≥ 4
False
High lipophilicity correlates well with high oral bioavailability and low protein binding
High lipophilicity correlates well with high oral bioavailability and low protein binding
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Lipophilicity can accelerate the rate of dissolution and reduce tissue retention
Lipophilicity can accelerate the rate of dissolution and reduce tissue retention
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Study Notes
Lipophilic Substituents on Inhaled Corticosteroids (ICS)
- Lipophilic substituents on ICS can improve receptor affinity and affect pharmacokinetics (PK).
- Lipophilicity can delay the rate of dissolution and prolong tissue retention.
Comparison of Systemic Steroids and Inhaled Steroids
- Systemic steroids (e.g., prednisolone and hydrocortisone) are less effective as inhaled steroids due to their:
- Higher water solubility
- Lower lipophilicity
Impact of Lipophilicity on Solubility and Bioavailability
- A sharp drop in water solubility occurs when lipophilicity is logP ≥ 4 (P = 10,000).
- High lipophilicity correlates with:
- Low oral bioavailability
- High protein binding
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Description
This quiz explores the role of lipophilicity in improving receptor affinity and affecting pharmacokinetics of steroids, particularly inhaled steroids.
