Pharmaceutical Chemistry Assignment

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Health Science Department (TENP)

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Choose the most suitable alternative from the choices given or as instructed otherwise
(TOTAL - 50 MARKS)
1. Medicinal Chemistry is best defined as:
A. Studying sources and uses of crude drugs
B. Studying the composition of medicines
C. Studying how xenobiotic substances are developed and designed
D. Studying the art and science of preparation of dosage forms and provision of
medicines
2. Which of the following statements correctly describes the generic name of a drug?
A. The general name of a drug
B. The name given in official reference books
C. The name given by the non-innovators of the drug
D. The name given after patent expiry of 20 years
3. Which of the following groups of drugs may be classified as pharmacodynamic agents?
A. Drugs used in malaria prophylaxis
B. Drugs that control hypertension
C. Synthetic antimicrobial agents
D. Drugs for prevention of tuberculosis
4. The name assigned to a drug during the research process is called________?
A. Code name
B. Research name
C. Non proprietary name
D. Generic name
E. Company name
5. The most comprehensive definition of a drug is__________ A. A chemical compound
obtained from plants and animals
B. A chemical substance that changes biological function
C. A substance that is used to treat diseases
D. A substance that is abused
6. The treatment of systemic infection with drugs that have selective toxicity for the infective
organism is__________?
A. Pharmacotherapeutics C. Chemotherapy
B. Pharmacology D. Toxicology
7. Use the below drug classification to respond to the following question.
i) Pain killers
ii) Ethylene diamines
iii) Calcium channel antagonists
iv) Antihypertensives
v) Antidiabetic
agents
Carboxylic acids
vii) Adrenergic receptor blockers
Which of the above classifications consists of pharmacological classification only
A. i,iv,v C.i, iii, iv,v

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B. iii, vii D. ii, vi

8. Which of the following statements correctly describes generic drugs?
A. The drugs manufactured after patent expiry
B. Drugs which are fake or counterfeit
C. Drugs which are not original
D. The drugs present in official compendia
E. Drugs whose formulation is copied from others
9. Why is paracetamol not a first-line drug in pain accompanied by inflammation?
A. Higher doses are required thus increasing risk of toxicity
B. It only acts in the central nervous system
C. It is not a selective COX enzyme inhibitor
D. It has unreliable anti-inflammatory activity
E. It is has poor penetration into the capillaries
10. Select the correct drug regarding the acid base chemistry of drugs.
A. A weakly acidic drug with high Pka is a stronger acid than one with a low Pka
B. A strong base is more ionized than a weaker base
C. Drug absorption is not affected by the degree of dissociation D. Elimination of acidic
drugs can be enhanced by acidification of urine.
11. The difference between NSAIDS and narcotic analgesics is that:
A. Narcotics have low analgesic activity
B. Narcotics lack anti-inflammatory activity
C. NSAIDS are steroidal in structure
D. NSAIDS have sedative effects
12. Which statement best explains the mode of action of the organophosphate poisoning
antidote, atropine?
A. It neutralizes the poison by complexation
B. It is a weaker nucleophile than water
C. It blocks muscarinic receptors
D. Acts as a nucleophile that hydrolyses the phosphorylated enzyme
13. NSAIDS may be considered to be:
A. Drugs with high inflammatory effects
B. Drugs which enhance synthesis of inflammatory mediators
C. Drugs whose use is limited to inflammation
D. Drugs which block the synthesis of prostaglandins
Consider the structure of acetylcholine below and respond to the following question.

14. When the methyl group on the acetoxy moiety is substituted by an amine group, the resulting
compound may be said to be__________?
A. A carbamic acid ester
B. A cholinergic antagonist
C. A Neuromuscular junction blocker
D. An acetylcholinesterase inhibitor

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15. The compound so derived by the structural modification in question 13 above is:
A. Pilocarpine
B. Carbachol
C. Physostigmine
D. Atropine
16. What is the correct pharmacological uses direct acetylcholine agonists.
A. Management of organophosphate poisoning
B. Glaucoma
C. Gastric hypermotility disorders
D. Muscle relaxants in surgery
17. Select the correct statement regarding organophosphates.
A. They lead to mydriasis
B. They cause constipation
C. Their inhibition of acetylcholine metabolism is reversible
D. If no treatment is initiated, their effects will go on until new enzymes are synthesized
18. Below is the chemical structure atropine. Use it to respond to the following questions?

Which of the following description is correct regarding the above drug?

A. It cannot exhibit optical isomerism
B. It is a blocker of M3 receptors
C. Its use may lead to organophosphate poisoning
D. Atropine and related compounds lead to airway blockade
E. It can lead to diarrhoea
19. Which of the following is the likely effect of enzyme inhibition during drug metabolism?
A. Increased drug activity of the substrate drug
B. Failure of the substrate drug to produce expected effects
C. Reduced toxic effects of the substrate drug
D. Increased metabolism of the substrate drug
20. Select the correct statement regarding drug metabolism.
A. Drug metabolism results in non-polar derivatives
B. Detoxification is the same as metabolism
C. Some drugs have biological effects only after being metabolised
D. Liver disease has little effect on drug metabolism
21. Select the true statement as far as the NSAIDS is concerned
A. They promote inflammation because of their effect on prostaglandin synthesis
B. They are all inhibitors of cycloxygenase(COX) enzyme
C. Paracetamol may be classified as a phenyl derivative
D. Use of COX 2 selective inhibitors may predispose one to peptic ulcers

The structure below represents the β phenyl ethyl amines adrenergic agents. Use it to respond to
the following questions.

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22. If the R substituent is a hydrogen , the resulting compounds are____________

A. α blockers
B. β blockers
C. β agonists
D. α agonists
23. The ephedrine series of β phenyl ethyl amines_____________
A. Have an alkyl substituent at position 2 above
B. Have No OH group on the side chain
C. Include adrenaline and isoprenaline
D. Have no CNS effects
24. Select the correct description of the following sympathetic drugs
A. Salbutamol – Blocks noradrenaline effect in the bronchioles
B. Adrenaline - Causes anaphylactic reactions
C. Ephedrine – may be used in cold and flu congestion
D. Noradrenaline- lowers blood pressure
25. Prostaglandin analogs are synthetic analogs of prostaglandins which are indicated in the
following conditions except one. Which one?
A. To close the ductus arteriosus in neonates born with congenital heart defects
beforesurgery is undertaken
B. Protect against peptic ulcer disease in patients taking NSAIDS
C. Cervical ripening
D. Incomplete abortion
26. It is correct to say that; The higher the lipophilicity of a drug, _______________________:
A. The lower its partition coefficient in octanol and phosphate buffer shall be.
B. The better the absorption of the drug in the GIT
C. The more the presence of polar groups in the chemical structure of the drug
D. The lower the log P value
27. Select the correct statement regarding aqueous solubility and ionization. A. A strong acid
attains greater ionization in an environment with low pH
B. Urinary alkalinization promotes excretion of basic drugs
C. Dipole dipole bonds promote water solubility
D. The more the ionization of molecules, the greater the reabsorption in the renal tubules.
28. Which of the following acidic drugs will be least ionized in aqueous solution?
A. Aspirin: Pka=3.5
B. Indomethacin: pKa=4.5
C. Phenobarbitone: pKa=7.4
D. Ibuprofen: pKa=5.2
29. Which of the following explain the relationship between drug activity and stereochemistry?
A. Stereoisomers are always equipotent
B. Receptors are stereospecific

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C. Stereochemistry is how drugs exist in different crystal polymorphs

D. Stereoisomers have similar physicochemical properties
30. Use the structure below to respond to the following questions.

Which of the following statements is correct regarding the above molecule?

A. It is an aryl acetic acid derivative
B. It can be metabolized by hydrolysis
C. It has no antipyretic activity
D. It exhibits optical activity
31. Select the correct explanation of the drug below.

A. It is a derivative of salicylic acid

B. It is a selective COX I inhibitor
C. It is used topically, orally and parenterally as an NSAID
D. Its use has no risk of peptic ulceration.
32. Regarding aspirin:
A. It is a centrally acting NSAID
B. It exhibits toxicity only in high doses
C. It is a highly preferred uricosuric agent
D. It inhibits COX I enzyme inhibition more appreciably than COX II33. Select the
correct statement regarding the drug below.

A. It has poor antinflammatory activity

B. If the N hetero atom is replaced by C, it results in active derivatives

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C. The above drug exhibits no isomerism D. The above molecule may be said to be an
oxicam 34. As regards oxicams, it is true to say that:
A. They exhibit keto-enol tautomerism
B. They are COX II selective inhibitors
C. They include ketorolac and etodolac
D. They are short acting NSAIDS
35. Preferential COX II inhibitors include all the following except which one?
A. Aceclofenac
B. Etodolac
C. Indomethacin
D. Meloxicam
36. The following are propionic acid derivatives except which one?
A. Ketoprofen
B. Naproxen
C. Ketotifen
D. Ibuprofen
37. Which of the following statements regarding selective COX inhibitors is correct?
A. They are not associated with adverse effects
B. They can be safely used in patient with heart disease
C. They may cause peptic ulcers on prolonged use or in higher doses
D. They are selective inhibitors of COX I enzyme
E. They have all been withdrawn
38. Match the descriptions in column A with the correct drug in column B. Note that the
agents in column B may be used once or not at all. (6 marks)
Column A Column B s/no. Description ANSWER Drug
a) Cholinergic agonist at muscarinic receptors D A. Atropine
for urinary retention
b) Causes prolonged depolarization at NMJ F B. Benzhexol
c) Has nasal decongestant effect H C. Pancuronium
d) Its injection will elevate blood pressure I D. Bethanechol
e) Amino alcohol acetylcholine antagonist B E. Pralidoxime
with CNS activity
f) Prevents acetylcholinestesterase enzyme E F. Succinylcholine
ageing due to poisoning by irreversible
anticholinesterases I Adrenaline
G. Di
azinon
H. Ph
enylephrine 39. In development, the lead molecule may be obtained from natural
products, side effects of existing drugs or by chance among many other
approaches. Write one example of a drug that has been obtained or improved from
any of the above three sources of the lead molecule.
Write your answers in the provided space (3 marks)
A. Natural sources - atropine, aspirin, morphine, codeine, pilorcapine etc
B. Side effects - aspirin,chlorpromazine, many antihistamines, sildenafil etc

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C. By chance - penicillins, aspirin etc

40. Chemical bonding affects drug activity in the following ways. Write True or False
Write your answer in the provided spaces (½mark each)
a) Destruction of foreign cells in the body T
b) Interaction of neurotransmitters with receptor sites T
c) Affect solubility of chemical substances T
d) Interactions of drugs with plasm proteins T
e) Chemical interaction of drugs with each other T
f) Determine the extent of ionization of molecules F

41. Using chemical structures, illustrate one metabolic pathway for each of the following drugs
(Show the products). Give the name of the reaction. (6 marks)

Use the space in front of the structure for your response.

a)

O-dealkylation →

b) hydrolysis of the amide, N -dealkylation

c) - oxidative deamination, aromatic hydroxylation

ANSWER SHEET
Use this answer sheet for question 1-37 only.

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