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Questions and Answers
What is the main purpose of a carrier prodrug?
What is the main purpose of a carrier prodrug?
- Decrease bioavailability of the drug
- Increase toxicity of the drug
- Enhance chemical and biological characteristics of the drug (correct)
- Extend the duration of action of the drug
In prodrug design, why are simple aliphatic or aromatic esters not preferred?
In prodrug design, why are simple aliphatic or aromatic esters not preferred?
- Due to higher toxicity in vivo
- Because they lead to extremely rapid drug metabolism
- As they are not labile enough in vivo, resulting in poor conversion of the pro-drug (correct)
- Because they enhance the drug's solubility
What issues can a prodrug help resolve?
What issues can a prodrug help resolve?
- Increasing drug toxicity
- Enhancing drug resistance
- Reducing bioavailability
- Improving patient compliance (correct)
What is the classification based on in broad classification of prodrugs?
What is the classification based on in broad classification of prodrugs?
Why are carrier prodrugs formed by combining an active drug with a carrier?
Why are carrier prodrugs formed by combining an active drug with a carrier?
What is the key advantage of a bioprecursor prodrug?
What is the key advantage of a bioprecursor prodrug?
What is the purpose of using drug carbidopa in conjunction with levodopa for Parkinson's treatment?
What is the purpose of using drug carbidopa in conjunction with levodopa for Parkinson's treatment?
Why is it challenging to use peptides and proteins directly as drugs?
Why is it challenging to use peptides and proteins directly as drugs?
Why are antibodies important in drug therapy?
Why are antibodies important in drug therapy?
Which strategy is NOT used to optimize access to a drug target?
Which strategy is NOT used to optimize access to a drug target?
What is a key concern regarding the use of natural hormones as drugs?
What is a key concern regarding the use of natural hormones as drugs?
How are oligonucleotides stabilized for drug development?
How are oligonucleotides stabilized for drug development?
What is the main advantage of designing prodrugs for drug delivery to the brain?
What is the main advantage of designing prodrugs for drug delivery to the brain?
Why are prodrugs linked to a polymer for colon delivery?
Why are prodrugs linked to a polymer for colon delivery?
Which characteristic is NOT an ideal property of an effective prodrug?
Which characteristic is NOT an ideal property of an effective prodrug?
Why are carrier prodrugs designed for site specificity?
Why are carrier prodrugs designed for site specificity?
What is a key reason for designing prodrugs for improved solubility?
What is a key reason for designing prodrugs for improved solubility?
How does a prodrug linked to a lipophilic carrier aid in brain drug delivery?
How does a prodrug linked to a lipophilic carrier aid in brain drug delivery?
What is the purpose of designing prodrugs for colon delivery?
What is the purpose of designing prodrugs for colon delivery?
Why does a prodrug have higher affinity for a specific site?
Why does a prodrug have higher affinity for a specific site?
What does a prodrug linked to a polymer achieve in colon delivery?
What does a prodrug linked to a polymer achieve in colon delivery?
Which is a common reason for designing prodrugs with a lipophilic carrier for brain delivery?
Which is a common reason for designing prodrugs with a lipophilic carrier for brain delivery?
Which approach is commonly used for esters/amides to block the approach of nucleophile or enzyme?
Which approach is commonly used for esters/amides to block the approach of nucleophile or enzyme?
What modification can be used to make drugs less resistant to metabolism?
What modification can be used to make drugs less resistant to metabolism?
Which modification can reduce the metabolic susceptibility of drugs?
Which modification can reduce the metabolic susceptibility of drugs?
For what purpose are prodrugs typically used?
For what purpose are prodrugs typically used?
Which type of drug is given alongside analgesics for migraine to increase absorption?
Which type of drug is given alongside analgesics for migraine to increase absorption?
What is the major goal of modifying drugs to target exact locations?
What is the major goal of modifying drugs to target exact locations?
Which approach involves attaching drugs to important building blocks needed by rapidly dividing tumor cells?
Which approach involves attaching drugs to important building blocks needed by rapidly dividing tumor cells?
'Chlorpropamide (X = Cl, n = 2)' was modified from which anti-diabetic drug?
'Chlorpropamide (X = Cl, n = 2)' was modified from which anti-diabetic drug?
'Levodopa' is a prodrug for which neurotransmitter?
'Levodopa' is a prodrug for which neurotransmitter?
'A group that can't be important for binding can be masked temporarily in which type of modification?'
'A group that can't be important for binding can be masked temporarily in which type of modification?'
What is the key factor that influences a drug's solubility and ADME?
What is the key factor that influences a drug's solubility and ADME?
Which type of drugs are preferentially distributed to hydrophobic compartments like the lipid bilayers of cells?
Which type of drugs are preferentially distributed to hydrophobic compartments like the lipid bilayers of cells?
Why are too polar/hydrophilic drugs unable to cross cell membranes effectively?
Why are too polar/hydrophilic drugs unable to cross cell membranes effectively?
What is the measure of a chemical substance's hydrophobic or hydrophilic nature?
What is the measure of a chemical substance's hydrophobic or hydrophilic nature?
Which strategy can help in improving a drug's absorption by increasing molecular flexibility?
Which strategy can help in improving a drug's absorption by increasing molecular flexibility?
What type of modifications for polar groups can be used as bioisosteres?
What type of modifications for polar groups can be used as bioisosteres?
Which type of substituents can be varied to alter a drug's pKa value?
Which type of substituents can be varied to alter a drug's pKa value?
Why is it important to be cautious when changing substituents in drugs?
Why is it important to be cautious when changing substituents in drugs?
Which type of modifications can help improve a drug's efficacy by making it more resistant to hydrolysis?
Which type of modifications can help improve a drug's efficacy by making it more resistant to hydrolysis?
What is the purpose of prodrugs like Lisdexamphetamine and Methyldopa?
What is the purpose of prodrugs like Lisdexamphetamine and Methyldopa?
Why are dipeptide analogues of Methyldopa preferred over Methyldopa?
Why are dipeptide analogues of Methyldopa preferred over Methyldopa?
What makes Lisdexamphetamine inactive prior to its absorption?
What makes Lisdexamphetamine inactive prior to its absorption?
How does Methyldopa act as an antihypertensive?
How does Methyldopa act as an antihypertensive?
How does Lisdexamphetamine become active after GI absorption?
How does Lisdexamphetamine become active after GI absorption?
What is a common feature of prodrugs like Prodrug Parecoxib, Nalbumetone, and Lisdexamphetamine?
What is a common feature of prodrugs like Prodrug Parecoxib, Nalbumetone, and Lisdexamphetamine?
Which strategy is NOT mentioned for optimizing access to drug targets?
Which strategy is NOT mentioned for optimizing access to drug targets?
What role does the PepT1 transporter play in enhancing drug properties?
What role does the PepT1 transporter play in enhancing drug properties?
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Study Notes
Prodrugs and Optimizing Access to the Target
- A prodrug is a pharmacologically inactive compound that is metabolized to the active drug by chemical or enzymatic process.
- Prodrugs can be used to resolve issues of acid sensitivity, poor membrane permeability, toxicity, bad taste, short duration of action, etc.
- Bioprecursor prodrugs have the active drug already inside the structure, whereas carrier prodrugs are formed by combining an active drug with a carrier to form a compound with desired chemical and biological characteristics.
Design Strategies for Prodrugs
- Improve oral bioavailability
- Improve patient compliance
- Improve solubility
- Improve site specificity
- Improve resistance to chemical and enzymatic degradation
- Decrease resistance to drug metabolism
- Targeting drugs
- Drug alliances
- Endogenous compounds as drugs
Prodrug Design for Better Patient Acceptance
- Masking bitter taste or odor of the drug
- Improve solubility for parenteral dosage forms
- Use of palmitate ester in liquid formulations to mask bitter taste of chloramphenicol
Prodrug Design for Improved Solubility
- Use of disodium phosphate or hemi-succinate prodrugs to improve solubility
- Example: dexamethasone disodium phosphate
Prodrug Design for Site Specificity
- Design prodrugs that have a higher affinity for the specific site of action
- Use an enzyme that is mainly found at the target site to release the drug
- Example: brain delivery using dihydropyridine system
Prodrug Design for Brain Delivery
- Use a lipophilic carrier that distributes quickly in the body but eliminates quickly from other organs except the brain
- Use an enzyme that is mainly found in the brain to release the drug
Prodrug Design for Colon Delivery
- Link the active drug to a polymer to produce a prodrug that cannot be absorbed
- The drug is released in the colon by bacterial reductive enzyme
Resistance to Chemical and Enzymatic Degradation
- Use bioisosteres to stabilize labile functional groups
- Block susceptible positions
- Remove or replace susceptible metabolic groups
- Use fluoro substituent or H/D exchange
- Group shifts to move vulnerable groups
- Ring variation and ring substituents
- Introduce metabolically susceptible groups to reduce toxicity
Targeting Drugs
- Use targeting strategies to deliver the drug to the specific site of action
- Examples: tumor cells, gastrointestinal infections, peripheral regions, and nervous system
Drug Alliances
- Use a second drug to guard or assist the principal drug
- Examples: metaclopromide with analgesics for migraine, adrenaline with procaine for localized anesthesia
Endogenous Compounds as Drugs
- Natural hormones as drugs
- Peptides and proteins as drugs
- Oligonucleotides as drugs
- Antibodies as drugs
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