Podcast
Questions and Answers
Which type of prodrug is formed by the reaction of amines to form mannich bases?
Which type of prodrug is formed by the reaction of amines to form mannich bases?
- Ester linkage
- Azo linkage
- Mannich bases (correct)
- Amide linkage
Why are esterases important enzymes for the activation of prodrugs containing carboxylic acids or alcohols?
Why are esterases important enzymes for the activation of prodrugs containing carboxylic acids or alcohols?
- They control ester stability through electronic and steric manipulations
- They decrease aqueous solubility of the prodrug
- They increase lipophilicity of the prodrug
- They can prepare esters with any degree of hydrophilicity or lipophilicity (correct)
What is the effect of carriers with aromatic or aliphatic functional groups on the aqueous solubility of ester carrier-linked prodrugs?
What is the effect of carriers with aromatic or aliphatic functional groups on the aqueous solubility of ester carrier-linked prodrugs?
- Decrease aqueous solubility (correct)
- Increase lipophilicity
- Increase aqueous solubility
- No effect on aqueous solubility
Which functional groups can be used to prepare carriers that increase the aqueous solubility of ester carrier-linked prodrugs?
Which functional groups can be used to prepare carriers that increase the aqueous solubility of ester carrier-linked prodrugs?
What is the rare approach for forming prodrugs involving amines?
What is the rare approach for forming prodrugs involving amines?
Which of the following is NOT a method for increasing the water solubility of an agent as mentioned in the text?
Which of the following is NOT a method for increasing the water solubility of an agent as mentioned in the text?
What is the main reason for using succinate esters containing ionizable carboxylate in prodrugs?
What is the main reason for using succinate esters containing ionizable carboxylate in prodrugs?
What is the role of phosphatase enzymes in the hydrolysis of phosphate esters?
What is the role of phosphatase enzymes in the hydrolysis of phosphate esters?
Which functional group of a drug can be reacted with a carboxylic acid of the carrier to give an amide, according to the text?
Which functional group of a drug can be reacted with a carboxylic acid of the carrier to give an amide, according to the text?
What is the primary reason for using phosphate esters in producing clindamycin phosphate?
What is the primary reason for using phosphate esters in producing clindamycin phosphate?
When is chemical hydrolysis of the ester function likely to occur?
When is chemical hydrolysis of the ester function likely to occur?
What allows control of the rate and extent of hydrolysis and when the active drug must be revealed at the correct point in its movement through the biological system?
What allows control of the rate and extent of hydrolysis and when the active drug must be revealed at the correct point in its movement through the biological system?
What is a potential drawback of succinate esters in solution?
What is a potential drawback of succinate esters in solution?
"Pain after parenteral administration is associated with local irritation caused by" what?
"Pain after parenteral administration is associated with local irritation caused by" what?
Study Notes
- Prodrugs are a group of compounds that can be transformed in the body into active drugs.
- Prodrugs are classified according to the functional groups of their parent drugs.
- The most common type of prodrug is formed by carboxylic acids and alcohols, which can be converted into esters.
- Esterases are enzymes responsible for the activation of ester prodrugs in the body.
- Ester carrier-linked prodrugs can be prepared with different carriers to control their hydrophilicity or lipophilicity.
- Hydrolysis of ester prodrugs can be accomplished by esterases in the body, microflora in the gut, or chemical reaction.
- Promoieties such as succinates, phosphates, and sulfonates are used to increase the hydrophilicity of prodrugs.
- Succinate esters are useful for rapid in vivo hydrolysis and are often somewhat unstable in solution.
- Phosphate esters offer another method for increasing the water solubility of agents and are stable in solution.
- Clindamycin phosphate is an example of a prodrug that increases water solubility and reduces pain at the injection site.
- Derivatization of amines to form amides is a less common approach for producing prodrugs.
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Description
Test your knowledge on prodrugs and drug delivery systems with this quiz based on lecture 6 by Assist. Lecturer Asmaa Adnan at Al-Nahrain University, College of Pharmacy. Explore the different types of prodrugs formed from functional groups and their chemical bonds.
