Week 1:
What is true about competitive inhibitors?
They promote the binding of an agonist at an active
site. They bind to a different place on the same
molecule.
Competitive and allosteric inhibitors act at the same place of the molecule.
*They act at the same site as the drug.
They are less effective than agonists.
Which term describes the ability of a drug to activate a biological effect?
Affinity
**Agonism
Efficacy
Potency
Incidence
What best describes the selectivity of a drug?
The effect of multiple drugs
The ability to activate the mechanisms to cause a biological
effect The strength of the bond between a drug and a receptor
**The proportion of preference a receptor has for a drug
Which statement most accurately describes a drug with high efficacy and high potency?
**It requires only a small dose to exert a significant
effect. It requires a large dose to exert a significant
effect.
Even a large dose will not cause a significant effect.
The maximum dose does not cause a significant
effect.
No dose change will lead to a change in the clinical effect.
,If a patient starts taking Drug A with a Kd of 100 nM (nanomolar) and then switches to Drug B
with a Kd of 100 µM (micromolar), and both drugs target the same receptor, which of the
following statements is true?
**The binding affinity of Drug A is much higher than the binding affinity of
Drug B. The binding affinities of the two drugs are not different.
More people in a population will respond to Drug A than to Drug
B. Drug B has higher efficacy.
The toxicity of Drug A is much higher than the toxicity of Drug B.
,what best describes EC50?
The effective concentration of a drug that produces 50% of the minimum effect.
**The effective concentration of a drug produces 50% of the maximal
effect. The dose required to get 50% of the population reporting toxic
side effects. The dose required to achieve 50% mortality from toxicity.
The dose that is required to achieve 50% of the desired response in 50% of the population.
A patient is being treated for depression with a specific medication. The pharmacokinetic profile
of this medication reveals a dissociation constant (Kd) of 344 pg/mL and an effective dose for
50% of the population (ED50) of 200 pg/mL. What can be inferred from these pharmacokinetic
parameters?
The medication is likely to cause severe side effects due to high potency.
The drug's high Kd value indicates it has a very high binding affinity.
**The presence of spare receptors can be inferred from these
values. An ED50 lower than Kd suggests the drug is ineffective.
The drug requires full receptor saturation to be effective, as indicated by the Kd and
ED50 values.
Which of the following drug characteristics makes a drug more likely to enter a cell through a
protein channel?
**Water solubility
Basophilic
property
Acidophilic
property
Neutrality
Fat solubility
How does the lipophilicity of a drug affect its efficacy?
A lower lipophilicity leads to a higher rate of absorption into the circulatory
system. A higher lipophilicity leads to a lower membrane permeability of the
drug.
A lower lipophilicity leads to a higher rate of desorption into the
food. A higher lipophilicity leads to a lower metabolic clearance of
the drug.
**A higher lipophilicity leads to a higher membrane permeability and metabolic
clearance of the drug.
What is the main reason behind limited bioavailability of benzylpenicillin?
, The beta-lactam ring of benzylpenicillin is highly prone to alkali catalyzed intramolecular
hydrolysis.
The beta-lactam ring of benzylpenicillin is highly prone to alkali catalyzed intermolecular
hydrolysis.
**The beta-lactam ring of benzylpenicillin is highly prone to acid catalyzed intramolecular
hydrolysis.