Drug Distribution and pKa

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?

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 effect does the pKa of a drug have on its distribution in the body?

In what form do HA acids, in terms of ionization, cross nonpolar membranes easily?

Where do drug molecules first encounter different pH values after oral administration?

Which pH range in the stomach allows HA acids with pKa's of 4 to 5 to be nonionic and partially absorbed?

What does the LD50 represent in pharmacology?

What does the MIC indicate about a drug's effectiveness against infections?

What is the role of a drug's partition coefficient in its movement within the body?

Why is obtaining a linear correlation between partition coefficient and concentrations important in pharmacology?

What is the main role of quantitative structure–activity relationships (QSAR) in drug design and discovery?

How does the Number of Hydrogen Bond Donor/Acceptor parameter influence drug design?

What does Polar Surface Area refer to in drug design?

What is the significance of ED50 in pharmacology and drug design?

What is the purpose of generating pharmacophores in computational chemistry methods in drug design?

What is the primary goal of Virtual High Throughput Screening (vHTS) in computational drug discovery?

What is the role of a lead compound in the process of drug development?

Which feature is NOT typically considered in generating pharmacophores for drug design?

Drugs in an ionized form tend to distribute more slowly throughout the body than un-ionized molecules.

For HA acids, the parent acid readily crosses nonpolar membranes.

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.

The unionized conjugate base (B, free amine) is the form of BH+ acids that easily crosses nonpolar membranes.

Phosphoglycerides are not major components of lipid bilayers.

The hydrophobic portion of the lipid membranes is mainly composed of saturated fatty acids.

Cholesterol esters, protein, and charged mucopolysaccharides are not found in lipid membranes.

Cellular membranes do not have dynamic channels that form and disappear based on the cell's needs.

A drug's partition coefficient is the ratio of the molar concentration of chemical in the nonaqueous phase versus that in the aqueous phase.

The lower the LD50 value for a drug, the less toxic it is.

The MIC indicates the lowest concentration of a drug that promotes bacterial growth.

To achieve a linear correlation between partition coefficient and concentrations, it is more common to use an exponential expression.

Virtual High Throughput Screening uses traditional experimental methods to assess large databases of chemical compounds.

Lead Compound Optimization involves developing a potential therapeutic agent from a chemical entity identified in the late stages of drug discovery.

A pharmacophore represents the essential structural and chemical features needed for a molecule to interact with any biological target.

Computational chemistry methods in drug design mainly focus on analyzing physical properties of drugs rather than chemical interactions with biological targets.

HA acids with pKa's of 4 to 5 will tend to be nonionic and be absorbed fully through the gastric mucosa.

The unionized conjugate base (B, free amine) is the species most readily crossing the polar membranes.

Cholesterol esters, proteins, and charged mucopolysaccharides are major components of lipid bilayers.

Cellular membranes have dynamic channels that form and disappear based on the cell's needs.

Phosphoglycerides are not major components of lipid bilayers.

The hydrophobic portion of the lipid membranes is mainly composed of saturated fatty acids.

Cholesterol esters, protein, and charged mucopolysaccharides are not found in lipid membranes.

Cellular membranes do not have dynamic channels that form and disappear based on the cell's needs.

Pharmacophores represent the non-essential structural and chemical features necessary for a molecule to interact with a specific biological target.

Virtual High Throughput Screening (vHTS) is primarily based on experimental methods rather than computer simulations.

Lead Compound Optimization is the process of identifying potential therapeutic agents at the late stages of drug discovery.

Computational chemistry methods in drug design mainly focus on analyzing chemical interactions rather than physical properties of drugs.

Charged proteins and mucopolysaccharides are predominantly found in the interior of the membrane.

Hexane/water and chloroform/water systems are excellent models for lipid bilayer/water systems in the body.

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.

Water-saturated octanol contains approximately 2.3 M water due to the clustering of large water molecules around octanol’s hydroxy moiety.