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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

Oxford University Press, Online Resource Centre, Chapter 11.

Chapter 11

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