drug targets within the body

1. With regard to drug targets within the body, which is the best answer?
a. Carriers: regulate protein concentrations & bioactive products
b. Enzymes: move nutrients & waste in and out of cells
c. Ion channels: move small ions, eg sodium and potassium, in and out of cells
d. Receptors: recognise only drugs to change cellular response

2. An agonist is different from an antagonist with regard to the following, which is the best
answer?
a. It has affinity
b. It has efficacy
c. It can’t mimic the response of an endogenous ligand
d. It does not bind to a drug target

3. With regard to an antagonist, which of the following is false?
a. It can be competitive or non-competitive, irreversible or reversible
b. It has affinity
c. It can shift the dose-response curve of an agonist to the right
d. It has efficacy

4. The four receptor superfamilies fall into categories on the basis of structure. Which
superfamily has a DNA binding domain as a structural feature?
a. Ligand gated ion channel
b. G-protein coupled
c. Kinase linked
d. Nuclear

5. A pharmaceutical company has designed a new drug. Which of the following methods is
correctly matched to pharmacodynamics information it provides about the drug?
a. Organ bath / site of drug action
b. Ligand binding / affinity of drug for receptor
c. Autoradiography / structure-activity relationship
d. In vivo animal model / receptor density

4. Enzymes involved in Phase I reactions include:

(i)__________________________________________________________________________
(ii)_________________________________________________________________________
(iii)_________________________________________________________________________
(iv)_______________________________________________________________________

6. Common enzymes involved in Phase II reactions include:
(i) _________________________________________________
(ii) _________________________________________________
(iii) ________________________________________________

You can use either the notes or the simulation at http://www.icp.org.nz/icp_t3.html for the
following question

7. If a drug has one the following Volume of Distribution, which body compartment(s) would you expect it to be distributed into?
Vd=5L______________________________________________________________________
Vd=15L_____________________________________________________________________
Vd=150L____________________________________________________________________

You can use either the notes or the simulation at http://www.icp.org.nz/icp_t2.html for the
following question

8. A patient is administered a drug which is predominantly cleared through the liver, if the patient has their liver function reduced by 50%, what kind of adjustment (if any) to the drug dosage

must be made to ensure the drug reaches a therapeutic concentration in their body?

________________________________________________

1. What are the physiological consequences of activating the main two components of the
autonomic nervous system on a) gastrointestinal motility & secretion b) heart function and
c) airway function d) lung e) adrenal medulla? In each case include the target organ transmitters involved and the types of receptors involved.
i) Parasympathetic system:

ii) Sympathetic system:

2. Using a representative diagram, illustrate the anatomical differences between
parasympathetic and sympathetic nerve fibres in terms of their origin, relays and
termination to a) blood vessels, b) heart and c) adrenal medulla.

3. What are the main neurotransmitters & receptor types involved in neurotransmission at
the following sites? Use your textbook to help you answer this question.

Type of Nerve Terminal Neurotransmitter Receptors Involved
preganglionic sympathetic fibres

preganglionic parasympathetic
fibres

postganglionic sympathetic fibres
at vascular smooth muscle

postganglionic parasympathetic
fibres at cardiac muscle

4. Outline the main differences between the metabolism of acetylcholine and noradrenaline
at the nerve terminal. Name one drug that can influence the metabolism of each and how
it works.
1. Using a diagram, outline the principle differences between cyclo-oxygenase (COX) inhibition by
non selective and COX-2 selective drugs. [3 marks]
1. Describe how gastric acid is produced and discuss the mechanisms of action and major side
effects of THREE major classes of drugs used to treat gastric/duodenal ulcers. [10 marks]

1. What is the main challenge to modern antibiotic therapy? Give some examples of the origin of
this challenge and how it might be overcome.

2. What is the difference between a bacteriostatic drug and a bactericidal drug? Give an example of
each.

3. With a brief sketch illustrate the different parts of the HIV virus life cycle which can he
interrupted by drug therapy.

5. What mode of therapy is common to anti-viral therapy and anti-cancer therapy?

6. Why are microtubules important in cancer? Illustrate this with the mode of action of one
anticancer drug?

7. What is the new therapy for Chronic Myeloid Leukemia? Explain how this represents a new
approach to cancer therapy.

8. There are multiple steps in the bacterial translation process that can be attacked by antibiotics,
gives 4 examples and an antibiotic that works at each step.

1. Which of the following statements about gamma-aminobutyric acid (GABA) is CORRECT?
a. it is a major excitatory neurotransmitter in the central nervous system
b. it is formed from aspartate by the enzyme glutamic acid decarboxylase
c. it activates GABAB receptors which are found mainly at postsynaptic site
d. it activates GABAA receptors which leads to Cl- influx

2. Which of the following statements about dopamine is CORRECT?
a. it is present at high concentrations within the regions of the limbic system
b. its reduction within the nigrostriatal pathway is associated with schizophernia
c. it can only have excitatory effect within the central nervous system
d. its hyperactivity in the nigrostriatal pathway is associated with Parkinson’s disease

3. Which of the following statements about drugs that act as selective inhibitors of monoamine
oxidase type A (MAO-A) is CORRECT?

a) they increase 5-HT receptor activity in the central nervous system
b) their pharmacological action is mainly restricted within the periphery
c) they are used to treat patients suffering from Schizophrenia
d) they decrease the presynaptic cellular levels of dopamine

Part B: Short Answer Questions
1. Describe briefly the mechanisms of action and major side effects of TWO Drug classes that affect
central 5-hydroxytryptamine systems. (3 marks)

2. Describe the pharmacodynamic targets for amphetamines and their adverse effects. (3 marks)

1. Describe the use of drugs in the treatment of schizophrenia, focusing on the mechanisms of action and main side effects of TWO major classes of antipsychotic drugs. (10 marks)

2. What are the THREE main criteria that define whether a person is dependent on a drug/substance?
a.
b.
c.
3) How do opioids work to provide analgesia?

Q2. What sort of steps are involved in developing new drugs?

Q3. Compare and contrast combinatorial chemistry and rational drug design

Q4. What approaches were used in the design of the drug Zanamavir? Did it
work?

Q5. With a quick sketch, illustrate the success rate of potential drugs at each
step of the drug discovery process
Q6. With a quick sketch illustrate the proportion of modern pharmaceuticals
that come from natural or synthetic routes.

Q8 We often use a natural product as a basis from a pharmaceutical therapy,
why is this? Give one illustration of a natural compound that has been
modified to give a therapeutic (and why it was modified)

1. G-protein coupled receptors depend on 2nd messengers to elicit their effects
on cell function. Name 3 of these messengers and explain their role in this process. [3 marks]
3. What are the key factors that influence drug absorption across biological membranes? [3 marks]
4. List two important organ structures that are innervated via ß2 adrenoceptors.
In addition, briefly describe the functional (physiological) role that ß2 adrenoceptor activation plays in those organs related to homeostasis (e.g. fight or flight response). [3 marks]

7. Describe briefly why drugs that block histamine (H2) or muscarinic (M1) receptors are used to treat duodenal or gastric ulcers. [3 marks]
10. Describe briefly why we use drugs that affect brain 5-HT levels or 5-HT
receptors to treat major brain disorders. [3 marks]

11. What is the active ingredient of Khat and what is its relevance to western
drug use? [3 marks]

12. Using brief notes compare and contrast the mechanisms of resistance to
anticancer drugs and antiviral drugs. [3 marks]

13. Compare and contrast the use of complementary therapies by asthmatics
and people with depression. [3 marks]

3. Some anti-viral drugs and some anti-cancer drugs share a common
mechanism. Explain what this mechanism is, why it is important to both viral
and cancer chemotherapy and give one example of such a therapy. If possible,
also name a drug that has been used as both anti-viral and anti-cancer therapy. [10marks]

4. Aspirin is one of the most commonly used non-steroidal anti-inflammatory drugs
(NSAID) for many different pain conditions as well as fever. Aspirin can also
cause duodenal or gastric ulcer, platelet disorders and renal function
impairment. Explain why these side effects occur and suggest an alternative
NSAID with reduced side effects. [10marks]

5. With a simple illustration, draw the autonomic innervation which projects to the
adrenal medulla and heart. Include relevant transmitters and receptors in your answer.
[6 marks]
10. Compare and contrast the use of complementary therapies by pregnant women
and healthy people. [3 marks]
12. Non-steroidal anti-inflammatory drugs (NSAID) are used for many different pain
conditions as well as fever. Some of these drugs cause platelet disorders and
gastric ulcer. Explain why these side effects occur. [3 marks]
3. Describe the pharmacodynamic effects of amphetamines, their mechanisms of
action, and explain how this relates to their chemical structure. [10marks]

4. Describe why drug effects within the central nervous system are far more complex
than on the autonomic nervous system by focussing on antidepressant and
antipsychotic drugs. Explain mechanisms of action and main side effects of these
drugs. [10marks]

5. Compare and contrast rational drug design and combinatorial chemistry as
methods of drug discovery. [10marks]

6. Production of gastric acid is finely regulated both by neurons and by hormones.
Describe effects of drugs that act as an agonist at histamine (H2) and muscarinic
(M1) receptors on gastric acid production. Can these drugs be used to treat
duodenal or gastric ulcers? Explain your answer. [10marks]

2010
5. Describe the dynamics of acetylcholine production, storage, release and
inactivation at the synapse. Use a diagram to assist your answer if you wish.
Also, name one type of drug that can prevent acetylcholine mediating its
effect there. [3 marks]
2. What major therapeutic challenge is common to both anti-bacterial and anti-viral
therapy? [10marks]

3. A pharmaceutical company has developed a new drug “Whimsolidine”. Following in
vitro and in vivo experiments they have the following information about the drug’s
action:
(i) organ bath: drug at low concentrations causes a significant contraction response.
(ii) autoradiography: drug binds to receptors in the brain, stomach, liver, and kidney.
(iii) dosing in rats: drug response following oral administration was observed on day 1
but diminished on day 2-5 of dosing and most of the drug was excreted in the urine as
metabolites.
(iv) dosing in rats with liver disease: drug accumulated in the plasma causing severe
toxicity after heightened response.

Referring to the above information, discuss the pharmacological properties of the drug
including: type of drug (agonist/antagonist), site of action, pharmacokinetics
(absorption and clearance organ), changes in dosing required with continued
administration, and patient groups who should not take the drug due to toxicity. [10marks]

4. Compare and contrast natural versus synthetic drugs. Include in your answer a
discussion of the differences in concepts between natural products used as pure drugs
and herbal medicines. What problems may arise with the use of herbal preparations as
medicines?

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