Podcast
Questions and Answers
What is the focus of PHAM1126?
What is the focus of PHAM1126?
- Drug discovery
- Drug-receptor interactions (correct)
- Pharmacodynamics
- Pharmacokinetics
Which area does Chapter 14 of 'An introduction to medicinal chemistry' focus on?
Which area does Chapter 14 of 'An introduction to medicinal chemistry' focus on?
- Pharmacokinetics
- Optimizing access to the target (correct)
- Pharmacodynamics
- Drug discovery
What does MSOP1016 primarily cover?
What does MSOP1016 primarily cover?
- Drug-receptor interactions
- Pharmacokinetics (correct)
- Covalent binding for drug-receptor interactions
- QSAR and Isosteres
What is the main topic of Lecture 3: Prodrugs and optimising access to the target?
What is the main topic of Lecture 3: Prodrugs and optimising access to the target?
Which of the following approaches is NOT used to improve drug efficacy?
Which of the following approaches is NOT used to improve drug efficacy?
What is the purpose of self-destruct drugs?
What is the purpose of self-destruct drugs?
Which drug is used to increase the absorption of another drug, particularly analgesics for migraine?
Which drug is used to increase the absorption of another drug, particularly analgesics for migraine?
What is the function of alliance drugs?
What is the function of alliance drugs?
Which approach is used to make drugs more resistant to hydrolysis and metabolism?
Which approach is used to make drugs more resistant to hydrolysis and metabolism?
What can be changed to optimize the hydrophilic/hydrophobic properties of drugs?
What can be changed to optimize the hydrophilic/hydrophobic properties of drugs?
What is an example of a prodrug used to increase the absorption of dopamine?
What is an example of a prodrug used to increase the absorption of dopamine?
Which drug constricts the blood vessels near the injection site to keep another drug in the vicinity for longer?
Which drug constricts the blood vessels near the injection site to keep another drug in the vicinity for longer?
What type of drugs can be made highly polar or ionized to prevent absorption for gastrointestinal infections?
What type of drugs can be made highly polar or ionized to prevent absorption for gastrointestinal infections?
What is the purpose of using steric shields, electronic effects, and group shifts in drug design?
What is the purpose of using steric shields, electronic effects, and group shifts in drug design?
What approach can be used to make specific use of molecular transport systems in tumour cells?
What approach can be used to make specific use of molecular transport systems in tumour cells?
What is an example of a drug that is chemically stable under one set of conditions but unstable and degradable under another?
What is an example of a drug that is chemically stable under one set of conditions but unstable and degradable under another?
Which type of prodrug involves combining an active drug with a carrier to produce a compound with desired chemical and biological properties?
Which type of prodrug involves combining an active drug with a carrier to produce a compound with desired chemical and biological properties?
What is the main example of a bioprecursor prodrug mentioned in the text?
What is the main example of a bioprecursor prodrug mentioned in the text?
Which property is considered ideal for prodrugs to help improve patient acceptance?
Which property is considered ideal for prodrugs to help improve patient acceptance?
What is the primary purpose of prodrug design?
What is the primary purpose of prodrug design?
What can carrier prodrugs help address?
What can carrier prodrugs help address?
What is a characteristic of polymer prodrugs?
What is a characteristic of polymer prodrugs?
How can prodrugs be helpful in addressing side-effects associated with NSAIDs?
How can prodrugs be helpful in addressing side-effects associated with NSAIDs?
What do ideal prodrug properties include?
What do ideal prodrug properties include?
What characteristic can help ensure a prodrug reaches the target site?
What characteristic can help ensure a prodrug reaches the target site?
What is an example of a side-effect that prodrugs can help address related to opiates?
What is an example of a side-effect that prodrugs can help address related to opiates?
How can bioprecursor prodrugs be classified?
How can bioprecursor prodrugs be classified?
What do carrier prodrugs involve?
What do carrier prodrugs involve?
Which enzyme metabolises most of the Levodopa before it reaches the Central Nervous System?
Which enzyme metabolises most of the Levodopa before it reaches the Central Nervous System?
Which compound has been used to inhibit dopa decarboxylase and reduce the necessary dose of Levodopa?
Which compound has been used to inhibit dopa decarboxylase and reduce the necessary dose of Levodopa?
What is the primary reason for using carbidopa alongside Levodopa in Parkinson's treatment?
What is the primary reason for using carbidopa alongside Levodopa in Parkinson's treatment?
Why is carbidopa unable to cross the Blood-Brain Barrier (BBB)?
Why is carbidopa unable to cross the Blood-Brain Barrier (BBB)?
Which strategy involves modifying the drug itself to optimize hydrophilic/hydrophobic properties and resistance to chemical and enzymatic degradation?
Which strategy involves modifying the drug itself to optimize hydrophilic/hydrophobic properties and resistance to chemical and enzymatic degradation?
What is the main issue with oligonucleotides as drugs?
What is the main issue with oligonucleotides as drugs?
What approach involves linking a drug to polymers or antibodies to improve its delivery to specific targets?
What approach involves linking a drug to polymers or antibodies to improve its delivery to specific targets?
Why are peptides and proteins used as peptidomimetics in drug design?
Why are peptides and proteins used as peptidomimetics in drug design?
Which compound is used as a mimic of a peptide lead in drug development?
Which compound is used as a mimic of a peptide lead in drug development?
What is the primary use of antibodies as drugs?
What is the primary use of antibodies as drugs?
Which type of prodrug is Valdecoxib?
Which type of prodrug is Valdecoxib?
What is the function of Lisdexamphetamine as a prodrug?
What is the function of Lisdexamphetamine as a prodrug?
What strategy is NOT a part of prodrug design?
What strategy is NOT a part of prodrug design?
What is the main focus of drug optimisation with regards to target access?
What is the main focus of drug optimisation with regards to target access?
What happens if a drug is too polar or hydrophilic?
What happens if a drug is too polar or hydrophilic?
How is hydrophobic character measured in drugs?
How is hydrophobic character measured in drugs?
What is the primary purpose of using prodrugs?
What is the primary purpose of using prodrugs?
What role do COX-2 inhibitors play in prodrug design?
What role do COX-2 inhibitors play in prodrug design?
What distinguishes Lisdexamphetamine from other prodrugs mentioned in the text?
What distinguishes Lisdexamphetamine from other prodrugs mentioned in the text?
What characteristic should hydrophobic drugs possess for distribution?
What characteristic should hydrophobic drugs possess for distribution?
What strategy aims to prolong drug activity?
What strategy aims to prolong drug activity?
Which commercially available prodrug enhances water solubility for parenteral use?
Which commercially available prodrug enhances water solubility for parenteral use?
Study Notes
- NSAIDs and prodrugs: Many have been made, only a few reached clinical use
- Non-selective COX-2 inhibitors: Avoid GI irritation by using prodrugs
- COX-2 inhibitors: Enhance water solubility for parenteral use or improve bioavailability
- Commercially available NSAID prodrugs:
- Parecoxib: Water-soluble injectable
- Valdecoxib: COX-2 selective prodrug
- Nalbumetone: Bioprecursor prodrug metabolized in the liver
- Flurbiprofen: Carrier prodrug
- Flurbiprofen axetil
- Lisdexamphetamine: Prodrug of dextroamphetamine used in ADHD treatment
- Methyldopa: Prodrug of methyldopamine, decarboxylated in the brain to methyldopamine
- Prodrug design:
- Improve membrane permeability
- Esters, N-methylation, Trojan horse approach
- Prolong drug activity
- Mask drug side effects and toxicity
- Lower water solubility, improve taste
- Increase chemical stability, activated by external agents
- Drug optimisation:
- Aim for drugs that are absorbed, reach target effectively, stable, eliminated in a reasonable time
- Strategies to optimize access to targets: modification of drug, hydrophilic/hydrophobic properties, resistance to degradation, targeting
- Hydrophilic/hydrophobic properties:
- Balance crucial for solubility and ADME
- Too polar/hydrophilic: can't cross cell membranes
- Too non-polar/hydrophobic: go into fats/fatty tissue
- Hydrophobic drugs (high P) distributed to hydrophobic compartments
- Hydrophilic drugs (low P) found in aqueous compartments
- Absorption and distribution:
- For a drug to cross a membrane barrier, it must be soluble in both lipid and aqueous phases.
- Hydrophobic character measured by the partition coefficient (P).
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Description
Test your knowledge about NSAIDs and prodrugs, including their clinical use, COX-2 inhibitors, water solubility, bioavailability, and commercially available options. Explore the concepts of prodrugs and their application in pharmaceuticals.
