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Chapter 11

Instructions
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Question 1

Which of the following statements best describes pharmacodynamics?

a) The study of how drugs reach their target in the body and how the levels of a drug
in the blood are affected by absorption, distribution, metabolism, and excretion.
b) The study of how drugs can be designed using molecular modelling based on a
drug's pharmacophore.
c) The study of how a drug interacts with its target binding site at the molecular level.
d) The study of which functional groups are important in binding a drug to its target
binding site and the identification of a pharmacophore.

Question 2

Which of the following statements best describes pharmacokinetics?

a) The study of how drugs reach their target in the body and how the levels of a drug
in the blood are affected by various factors.
b) The study of how drugs can be designed using molecular modelling based on a
drug's pharmacophore.
c) The study of how a drug interacts with its target binding site at the molecular level.
d) The study of which functional groups are important in binding a drug to its target
binding site and the identification of a pharmacophore.

Question 3

Which of the following characteristics is detrimental to oral activity?

a) Stability to digestive enzymes.


b) Susceptibility to metabolic enzymes.
c) Stability to stomach acids.
d) Solubility in both aqueous and fatty environments.
Question 4

Which of the following is one of the rules in Lipinski's rule of five?

a) A molecular weight equal to 500


b) No more than five hydrogen bond acceptor groups
c) No more than 10 hydrogen bond donor groups
d) A calculated logP value less than +5

Question 5

Some orally active drugs do not obey the rule of five. For example, some drugs with
molecular weights greater than 500 are found to be orally active. Which of the following
mechanisms is the most likely reason for this?

a) Transport by transport proteins.


b) Passage through pores between the cells of the gut wall.
c) Pinocytosis.
d) Ion channels.

Question 6

Some orally active drugs do not obey the rule of five. For example, some highly polar
drugs with a molecular weight less than 200 are found to be orally active. Which of the
following mechanisms is the most likely reason for this?

a) Transport by transport proteins.


b) Passage through pores between the cells of the gut wall.
c) Pinocytosis.
d) Ion channels.

Question 7

Which type of infection could be orally treated with a highly polar antibacterial agent?

a) brain infection
b) kidney infection
c) gut infection
d) lung infection

Question 8

Which of the following statements is false regarding the blood-brain barrier?

a) The walls of the capillaries supplying the brain have tight fitting cells making it
difficult for polar drugs to leave the capillaries.
b) The capillaries in the brain have a fatty coating making it more difficult for drugs
to enter the brain.
c) The walls of the capillaries supplying the brain are made up of several layers of
cells, which act as a barrier to the release of drugs.
d) Hydrophobic drugs pass through the blood brain barrier more easily than
hydrophilic drugs.

Question 9

Which of the following statements is the closest description of Phase I metabolism?

a) Reactions which add a polar molecule to a functional group already present on a


drug or one of its metabolites.
b) Reactions which occur in the blood supply.
c) Reactions which add a polar functional group to a drug.
d) Reactions which occur in the gut wall.

Question 10

Which of the following statements is the closest description of Phase II metabolism?

a) Reactions which add a polar molecule to a functional group already present on a


drug or one of its metabolites.
b) Reactions which occur in the blood supply.
c) Reactions which add a polar functional group to a drug.
d) Reactions which occur in the gut wall.

Question 11

Which of the following statements is not true about cytochrome P450 enzymes?
a) They contain haem and magnesium.
b) They belong to a general class of enzymes called monooxygenases.
c) There are over 30 different cytochrome P450 enzymes.
d) Variation in cytochrome P450 enzyme profile between individuals can explain
individual variation in drug susceptibility.

Question 12

Which of the following groups is least susceptible to cytochrome P450 enzymes?

a) terminal methyl groups


b) allylic carbons
c) benzylic carbon atoms
d) quaternary carbon atoms

Question 13

Alkenes and aromatic groups can be metabolised to diols. Which enzymes are involved?

a) cytochrome P450 enzymes


b) epoxide hydrolase
c) Both of the above.
d) Neither of the above.

Question 14

Which of the following enzymes is not involved in catalysing a Phase I metabolic


reaction?

a) flavin-containing monooxygenases
b) monoamine oxidases
c) glucuronyltransferase
d) esterases

Question 15

Which of the following reactions is not a Phase I metabolic transformation?


a) reduction of ketones
b) conjugation to alcohols
c) oxidation of alkyl groups
d) ester hydrolysis

Question 1

Which of the following statements best describes pharmacodynamics?

You did not answer the question.

Correct Answer:

c)

Feedback:

Pharmacokinetics is the study of how drugs reach their target in the body and how the
levels of a drug in the blood are affected by absorption, distribution, metabolism and
excretion.
The study of how drugs can be designed using molecular modelling based on a drug's
pharmacophore is part of a process known as structure-based drug design.
Pharmacodynamics is the study of how a drug interacts with its target binding site at the
molecular level.
Structure activity relationships are studies which are carried out to find which functional
groups are important in binding a drug to its target binding site, and hence lead to the
identification of a pharmacophore.
Page reference: 152

Question 2

Which of the following statements best describes pharmacokinetics?

You did not answer the question.

Correct Answer:

a) The study of how drugs reach their target in the body and how the levels of a drug in
the blood are affected by various factors.

Feedback:

Pharmacokinetics is the study of how drugs reach their target in the body and how the
levels of a drug in the blood are affected by absorption, distribution, metabolism and
excretion.
The study of how drugs can be designed using molecular modelling based on a drug's
pharmacophore is part of a process known as structure-based drug design.
Pharmacodynamics is the study of how a drug interacts with its target binding site at the
molecular level.
Structure activity relationships are studies which are carried out to find which functional
groups are important in binding a drug to its target binding site, and hence lead to the
identification of a pharmacophore.
Page reference: 152

Question 3

Which of the following characteristics is detrimental to oral activity?

You did not answer the question.

Correct Answer:

b) Susceptibility to metabolic enzymes.

Feedback:
If an orally administered drug is rapidly metabolised, its lifetime will be short and this
will be detrimental to activity. The exceptions to the rule are prodrugs. These are inactive
compounds which are converted to active compounds by metabolic reactions.
Page reference: 152

Question 4

Which of the following is one of the rules in Lipinski's rule of five?

You did not answer the question.

Correct Answer:

d) A calculated logP value less than +5

Feedback:

The molecular weight should be less than 500. There should be no more than 5 hydrogen
bond donor groups and no more than 10 hydrogen bond acceptor groups. Statement d) is
correct.
Page reference: 153

Question 5

Some orally active drugs do not obey the rule of five. For example, some drugs with
molecular weights greater than 500 are found to be orally active. Which of the following
mechanisms is the most likely reason for this?

You did not answer the question.

Correct Answer:

c) Pinocytosis.

Feedback:

Some polar drugs can be transported across cell membranes by transport proteins if the
drug resembles the molecule which is normally carried by that transport protein. Small
polar drugs with a molecular weight less than 200 can squeeze through the pores between
the cells lining the gut wall. Large polar molecules can be transported across cells by a
process known as pinocytosis. Ion channels are not relevant to the absorption process.
Page reference: 154

Question 6
Some orally active drugs do not obey the rule of five. For example, some highly polar
drugs with a molecular weight less than 200 are found to be orally active. Which of the
following mechanisms is the most likely reason for this?

You did not answer the question.

Correct Answer:

b) Passage through pores between the cells of the gut wall.

Feedback:

Some polar drugs can be transported across cell membranes by transport proteins if the
drug resembles the molecule which is normally carried by that carrier protein. Small
polar drugs with a molecular weight less than 200 can squeeze through the pores between
the cells lining the gut wall. Large polar molecules can be transported across cells by a
process known as pinocytosis. Ion channels are not relevant to the absorption process.
Page reference: 154

Question 7

Which type of infection could be orally treated with a highly polar antibacterial agent?

You did not answer the question.

Correct Answer:

c) gut infection

Feedback:

A highly polar antibacterial drug will not be able to cross the gut wall, since it will not be
able to pass through hydrophobic cell membranes. It will, therefore, remain in the gut and
can be used to treat gut infections.
Page reference: 154

Question 8

Which of the following statements is false regarding the blood-brain barrier?

You did not answer the question.

Correct Answer:

c) The walls of the capillaries supplying the brain are made up of several layers of cells,
which act as a barrier to the release of drugs.
Feedback:

The cells making up the walls of capillaries supplying the brain are only one cell thick,
but the cells are more tightly packed than those supplying other parts of the body. As a
result, drugs have to cross cell membranes to depart the blood vessels and enter the brain.
There is also a fatty coating which surrounds the blood vessels and acts as a further
barrier. This fatty coating is not part of the capillary wall.
Page reference: 155

Question 9

Which of the following statements is the closest description of Phase I metabolism?

You did not answer the question.

Correct Answer:

c) Reactions which add a polar functional group to a drug.

Feedback:

Option c) is the closest description. Options b) and d) are incorrect. Some phase I
metabolic reactions can occur in the blood supply or the gut wall, but they do not take
place exclusively at either of these sites. Most Phase I reactions take place in the liver.
Option a) describes Phase II metabolism where a polar molecule is attached to a polar
functional group already present on the drug, or placed there by Phase I metabolism.
Page reference: 156-157

Question 10

Which of the following statements is the closest description of Phase II metabolism?

You did not answer the question.

Correct Answer:

a) Reactions which add a polar molecule to a functional group already present on a drug
or one of its metabolites.

Feedback:

Option a) describes Phase II metabolism where a polar molecule is attached to a polar


functional group already present on the drug, or placed there by Phase I metabolism.
Option c) describes the process of Phase I metabolism.
Options b) and d) are incorrect. Some Phase I metabolic reactions can occur in the blood
supply or the gut wall, but they do not take place exclusively at either of these sites. Most
Phase I reactions take place in the liver.
Page reference: 157

Question 11

Which of the following statements is not true about cytochrome P450 enzymes?

You did not answer the question.

Correct Answer:

a) They contain haem and magnesium.

Feedback:

The cytochrome P450 enzymes contain haem and iron. Statements b, c and d are
accurate.
Page reference: 157-160

Question 12

Which of the following groups is least susceptible to cytochrome P450 enzymes?

You did not answer the question.

Correct Answer:

d) quaternary carbon atoms

Feedback:

Exposed groups such as terminal methyl groups are susceptible to oxidation by


cytochrome P450 enzymes, as are activated carbons such as allylic and benzylic carbons.
Quaternary carbon atoms are 'buried' and unlikely to be susceptible to cytochrome P450
enzymes.
Page reference: 157-160

Question 13

Alkenes and aromatic groups can be metabolised to diols. Which enzymes are involved?

You did not answer the question.

Correct Answer:

c) Both of the above.


Feedback:

Cytochrome P450 enzymes catalyse the formation of an epoxide from an aromatic ring or
alkene. Epoxide hydrolase then catalyses the hydrolysis of the epoxide to form a diol.
Page reference: 157-160

Question 14

Which of the following enzymes is not involved in catalysing a Phase I metabolic


reaction?

You did not answer the question.

Correct Answer:

c) glucuronyltransferase

Feedback:

Flavin-containing monooxygenases catalyse a variety of Phase I oxidation reactions.


Monoamine oxidase catalyses the formation of aldehydes from primary amines. Esterases
catalyse the hydrolysis of esters. All of these are Phase I metabolic reactions.
Glucuronyltransferase catalyses the transfer or attachment of a sugar moiety onto a polar
functional group. This is a conjugation reaction which represents a Phase II metabolic
reaction.
Page reference: 160-161

Question 15

Which of the following reactions is not a Phase I metabolic transformation?

You did not answer the question.

Correct Answer:

b) conjugation to alcohols

Feedback:

Reactions which introduce, modify or reveal functional groups are Phase I metabolic
reactions. Conjugation reactions involve the attachment of a polar molecule to a polar
functional group and are Phase II metabolic reactions.
The reduction of a ketone is a functional group modification (ketone to alcohol). The
oxidation of an alkyl group introduces a functional group (alcohol, ketone or carboxylic
acid). Ester hydrolysis reveals functional groups (the carboxylic acid and the alcohol).
Conjugation to an alcohol is a Phase II metabolic reaction.
Page reference: 160-161