Podcast
Questions and Answers
How does the pKa of a drug affect its pharmacokinetics?
How does the pKa of a drug affect its pharmacokinetics?
Which form of acids, HA or BH+, is more likely to cross nonpolar membranes easily?
Which form of acids, HA or BH+, is more likely to cross nonpolar membranes easily?
In what pH environment will HA acids with pKa's of 4 to 5 tend to be nonionic?
In what pH environment will HA acids with pKa's of 4 to 5 tend to be nonionic?
What must a drug do to reach its site of action after leaving the plasma environment?
What must a drug do to reach its site of action after leaving the plasma environment?
Signup and view all the answers
What effect does the pKa of a drug have on its distribution in the body?
What effect does the pKa of a drug have on its distribution in the body?
Signup and view all the answers
In what form do HA acids, in terms of ionization, cross nonpolar membranes easily?
In what form do HA acids, in terms of ionization, cross nonpolar membranes easily?
Signup and view all the answers
Where do drug molecules first encounter different pH values after oral administration?
Where do drug molecules first encounter different pH values after oral administration?
Signup and view all the answers
Which pH range in the stomach allows HA acids with pKa's of 4 to 5 to be nonionic and partially absorbed?
Which pH range in the stomach allows HA acids with pKa's of 4 to 5 to be nonionic and partially absorbed?
Signup and view all the answers
What does the LD50 represent in pharmacology?
What does the LD50 represent in pharmacology?
Signup and view all the answers
What does the MIC indicate about a drug's effectiveness against infections?
What does the MIC indicate about a drug's effectiveness against infections?
Signup and view all the answers
What is the role of a drug's partition coefficient in its movement within the body?
What is the role of a drug's partition coefficient in its movement within the body?
Signup and view all the answers
Why is obtaining a linear correlation between partition coefficient and concentrations important in pharmacology?
Why is obtaining a linear correlation between partition coefficient and concentrations important in pharmacology?
Signup and view all the answers
What is the main role of quantitative structure–activity relationships (QSAR) in drug design and discovery?
What is the main role of quantitative structure–activity relationships (QSAR) in drug design and discovery?
Signup and view all the answers
How does the Number of Hydrogen Bond Donor/Acceptor parameter influence drug design?
How does the Number of Hydrogen Bond Donor/Acceptor parameter influence drug design?
Signup and view all the answers
What does Polar Surface Area refer to in drug design?
What does Polar Surface Area refer to in drug design?
Signup and view all the answers
What is the significance of ED50 in pharmacology and drug design?
What is the significance of ED50 in pharmacology and drug design?
Signup and view all the answers
What is the purpose of generating pharmacophores in computational chemistry methods in drug design?
What is the purpose of generating pharmacophores in computational chemistry methods in drug design?
Signup and view all the answers
What is the primary goal of Virtual High Throughput Screening (vHTS) in computational drug discovery?
What is the primary goal of Virtual High Throughput Screening (vHTS) in computational drug discovery?
Signup and view all the answers
What is the role of a lead compound in the process of drug development?
What is the role of a lead compound in the process of drug development?
Signup and view all the answers
Which feature is NOT typically considered in generating pharmacophores for drug design?
Which feature is NOT typically considered in generating pharmacophores for drug design?
Signup and view all the answers
Drugs in an ionized form tend to distribute more slowly throughout the body than un-ionized molecules.
Drugs in an ionized form tend to distribute more slowly throughout the body than un-ionized molecules.
Signup and view all the answers
For HA acids, the parent acid readily crosses nonpolar membranes.
For HA acids, the parent acid readily crosses nonpolar membranes.
Signup and view all the answers
Drugs with pKa's of 4 to 5 are more likely to be absorbed through the gastric mucosa if the stomach has a pH of 8 to 10.
Drugs with pKa's of 4 to 5 are more likely to be absorbed through the gastric mucosa if the stomach has a pH of 8 to 10.
Signup and view all the answers
The unionized conjugate base (B, free amine) is the form of BH+ acids that easily crosses nonpolar membranes.
The unionized conjugate base (B, free amine) is the form of BH+ acids that easily crosses nonpolar membranes.
Signup and view all the answers
Phosphoglycerides are not major components of lipid bilayers.
Phosphoglycerides are not major components of lipid bilayers.
Signup and view all the answers
The hydrophobic portion of the lipid membranes is mainly composed of saturated fatty acids.
The hydrophobic portion of the lipid membranes is mainly composed of saturated fatty acids.
Signup and view all the answers
Cholesterol esters, protein, and charged mucopolysaccharides are not found in lipid membranes.
Cholesterol esters, protein, and charged mucopolysaccharides are not found in lipid membranes.
Signup and view all the answers
Cellular membranes do not have dynamic channels that form and disappear based on the cell's needs.
Cellular membranes do not have dynamic channels that form and disappear based on the cell's needs.
Signup and view all the answers
A drug's partition coefficient is the ratio of the molar concentration of chemical in the nonaqueous phase versus that in the aqueous phase.
A drug's partition coefficient is the ratio of the molar concentration of chemical in the nonaqueous phase versus that in the aqueous phase.
Signup and view all the answers
The lower the LD50 value for a drug, the less toxic it is.
The lower the LD50 value for a drug, the less toxic it is.
Signup and view all the answers
The MIC indicates the lowest concentration of a drug that promotes bacterial growth.
The MIC indicates the lowest concentration of a drug that promotes bacterial growth.
Signup and view all the answers
To achieve a linear correlation between partition coefficient and concentrations, it is more common to use an exponential expression.
To achieve a linear correlation between partition coefficient and concentrations, it is more common to use an exponential expression.
Signup and view all the answers
Virtual High Throughput Screening uses traditional experimental methods to assess large databases of chemical compounds.
Virtual High Throughput Screening uses traditional experimental methods to assess large databases of chemical compounds.
Signup and view all the answers
Lead Compound Optimization involves developing a potential therapeutic agent from a chemical entity identified in the late stages of drug discovery.
Lead Compound Optimization involves developing a potential therapeutic agent from a chemical entity identified in the late stages of drug discovery.
Signup and view all the answers
A pharmacophore represents the essential structural and chemical features needed for a molecule to interact with any biological target.
A pharmacophore represents the essential structural and chemical features needed for a molecule to interact with any biological target.
Signup and view all the answers
Computational chemistry methods in drug design mainly focus on analyzing physical properties of drugs rather than chemical interactions with biological targets.
Computational chemistry methods in drug design mainly focus on analyzing physical properties of drugs rather than chemical interactions with biological targets.
Signup and view all the answers
HA acids with pKa's of 4 to 5 will tend to be nonionic and be absorbed fully through the gastric mucosa.
HA acids with pKa's of 4 to 5 will tend to be nonionic and be absorbed fully through the gastric mucosa.
Signup and view all the answers
The unionized conjugate base (B, free amine) is the species most readily crossing the polar membranes.
The unionized conjugate base (B, free amine) is the species most readily crossing the polar membranes.
Signup and view all the answers
Cholesterol esters, proteins, and charged mucopolysaccharides are major components of lipid bilayers.
Cholesterol esters, proteins, and charged mucopolysaccharides are major components of lipid bilayers.
Signup and view all the answers
Cellular membranes have dynamic channels that form and disappear based on the cell's needs.
Cellular membranes have dynamic channels that form and disappear based on the cell's needs.
Signup and view all the answers
Phosphoglycerides are not major components of lipid bilayers.
Phosphoglycerides are not major components of lipid bilayers.
Signup and view all the answers
The hydrophobic portion of the lipid membranes is mainly composed of saturated fatty acids.
The hydrophobic portion of the lipid membranes is mainly composed of saturated fatty acids.
Signup and view all the answers
Cholesterol esters, protein, and charged mucopolysaccharides are not found in lipid membranes.
Cholesterol esters, protein, and charged mucopolysaccharides are not found in lipid membranes.
Signup and view all the answers
Cellular membranes do not have dynamic channels that form and disappear based on the cell's needs.
Cellular membranes do not have dynamic channels that form and disappear based on the cell's needs.
Signup and view all the answers
Pharmacophores represent the non-essential structural and chemical features necessary for a molecule to interact with a specific biological target.
Pharmacophores represent the non-essential structural and chemical features necessary for a molecule to interact with a specific biological target.
Signup and view all the answers
Virtual High Throughput Screening (vHTS) is primarily based on experimental methods rather than computer simulations.
Virtual High Throughput Screening (vHTS) is primarily based on experimental methods rather than computer simulations.
Signup and view all the answers
Lead Compound Optimization is the process of identifying potential therapeutic agents at the late stages of drug discovery.
Lead Compound Optimization is the process of identifying potential therapeutic agents at the late stages of drug discovery.
Signup and view all the answers
Computational chemistry methods in drug design mainly focus on analyzing chemical interactions rather than physical properties of drugs.
Computational chemistry methods in drug design mainly focus on analyzing chemical interactions rather than physical properties of drugs.
Signup and view all the answers
Charged proteins and mucopolysaccharides are predominantly found in the interior of the membrane.
Charged proteins and mucopolysaccharides are predominantly found in the interior of the membrane.
Signup and view all the answers
Hexane/water and chloroform/water systems are excellent models for lipid bilayer/water systems in the body.
Hexane/water and chloroform/water systems are excellent models for lipid bilayer/water systems in the body.
Signup and view all the answers
The n-octanol/water partitioning system accurately reflects the lipid membranes/water systems found in the body due to the high water content in both phases.
The n-octanol/water partitioning system accurately reflects the lipid membranes/water systems found in the body due to the high water content in both phases.
Signup and view all the answers
Water-saturated octanol contains approximately 2.3 M water due to the clustering of large water molecules around octanol’s hydroxy moiety.
Water-saturated octanol contains approximately 2.3 M water due to the clustering of large water molecules around octanol’s hydroxy moiety.
Signup and view all the answers
