Podcast
Questions and Answers
Which factors predominantly influence the absorption of drugs according to their physicochemical properties?
Which factors predominantly influence the absorption of drugs according to their physicochemical properties?
Which drug is noted for having low polarity and high absorption?
Which drug is noted for having low polarity and high absorption?
What technique is used to enhance metabolic stability by protecting esters or amides from hydrolysis?
What technique is used to enhance metabolic stability by protecting esters or amides from hydrolysis?
Which statement about Valacyclovir is accurate?
Which statement about Valacyclovir is accurate?
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What issue does Acetyl Choline face that affects its pharmacokinetics?
What issue does Acetyl Choline face that affects its pharmacokinetics?
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What is the role of the steric shield in the context of drug stability?
What is the role of the steric shield in the context of drug stability?
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Which modification to acetylcholine results in the creation of Bethanechol?
Which modification to acetylcholine results in the creation of Bethanechol?
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What type of chemical structure is Lido Procaine?
What type of chemical structure is Lido Procaine?
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How does Megesterol acetate improve metabolic stability?
How does Megesterol acetate improve metabolic stability?
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Which feature of methacholine contributes to its stability against hydrolysis?
Which feature of methacholine contributes to its stability against hydrolysis?
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Study Notes
Optimizing Pharmacokinetic Properties
- Improving Absorption: Log P and pKa are key physicochemical properties controlling absorption. High or low values of log P correlate with reduced absorption.
- Examples: Acyclovir has poor absorption due to high polarity, requiring administration 6-8 times daily. Valacyclovir (a prodrug) is better absorbed (85-90%), allowing for a twice-daily dose. Drug optimization involves adjusting alkyl substituents (drug latentiation).
Improving Metabolic Stability
- Techniques: Steric shielding protects amide or ester groups from esterase/amidase enzymes, improving stability. Bulkier tert-butyl groups are examples of steric shields.
Electronic Effects
- Acetylcholine: Electron-donating groups, like methyl groups, increase metabolic stability. Replacing a methyl group with another group, like amino, can improve stabilization. This method is called electronic effect.
Stereoelectronic Modification
- Acetylcholine: Adding methyl groups creates a steric shield, enhancing stability, particularly against hydrolysis. This is steric electronic modification.
Metabolic Blockers
- Progesterone: Modifying the C17 position, for instance, by adding OCOCH3 groups, can improve metabolic stability by blocking metabolic pathways. Example : Megesterol acetate.
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Description
Test your understanding of pharmacokinetic properties and strategies for optimizing them, including absorption, metabolic stability, and electronic effects. This quiz covers key concepts such as Log P, pKa, and steric shielding, necessary for improving drug formulation.
