Section A

Question 1

What are the symptoms of ergot poisoning?

Answer 1

Burning in limbs (St. Anthony’s Fire)
Constriction of blood vessels
Mental frenzy
Abortion

Question 2

What two active principles have been isolated from ergot? What are their modern uses?

Answer 2

Ergotamine (migraines)

Ergonovine (arrest bleeding AFTER childbirth)

Question 3

What accurate observations did the Ebers papyrus contain?

Answer 3

Information about purgatives (to cause bowel movements); recommended drugs included castor oil, figs and senna

Question 4

What compounds can be isolated from opium (in what amounts)?

Answer 4

10% morphine (morphine may be chemically converted to heroin)
0.5% codeine

Question 5

What compound is isolated from the plant Colchicum? What is its modern use?

Answer 5

Colchicine is extracted from the plant; used in the treatment of gout

Question 6

Who isolated a compound from digitalis purpurea? What are its uses?

Answer 6

William Withering isolated digitalis drugs from foxglove for the treatment of weak heart muscles or disordered rhythms

Question 7

What compound can be isolated from foxglove?

Answer 7

Digoxin (Lanoxin) can be isolated from foxglove

Question 8

Who discovered amyl nitrate? What was it used for?

Answer 8

Lauder Brunton discovered the use of amyl nitrate in the treatment of angina pectoris; one disadvantage is that it is short lived

Question 9

Who discovered nitroglycerin?

Answer 9

William Murrell

Question 10

Describe nitroglycerin’s mechanism of action.

Answer 10

Nitroglycerin is used in the treatment of angina pectoris. It dilates blood vessels in the heart and elsewhere in the body.

Question 11

What compound can be isolated from the Cinchona tree? What are its uses?

Answer 11

Quinine may be isolated for the treatment of malaria

Question 12

What drug is related to quinine? What are its uses?

Answer 12

Quinidine may be used for the treatment of arrhythmias

Question 13

What can be isolated from the rauwolfia plant? What are its uses?

Answer 13

Reserpine can be isolated from the plant. It was used for the treatment of uncontrollable patients (now there are better drugs) and still used in the treatment of hypertension

Question 14

Which modern drug is a suitable replacement for reserpine?

Answer 14

Chlorpromazine

Question 15

Who discovered LSD?

Answer 15

Albert Hofmann

Question 16

Which compounds are structurally similar to LSD?

Answer 16

Ergotamine and ergonovine

Question 17

Paul Ehrlich?

Answer 17

The father of chemotherapy; discovered organoarsenicals, which cured syphilis (Salvarsan)

Question 18

Gerhard Domagk?

Answer 18

Introduced sulfa drugs

Question 19

Alexander Fleming?

Answer 19

Discovered the first antibiotic, penicillin (treatment of Gram-positive bacteria)

Question 20

Selman Waksman?

Answer 20

Discovered streptomycin (tuberculosis and Gram-negative bacteria)

Question 21

Humphrey Davy?

Answer 21

Showed the pain-releiving effects of nitrous oxide

Question 22

Colton?

Answer 22

Gave public demonstrations of nitrous oxide

Question 23

Wells?

Answer 23

Dentist; used nitrous oxide during tooth extraction

Question 24

Faraday?

Answer 24

Pointed out ether has similar properties as nitrous oxide

Question 25

Morton?

Answer 25

Performed the first surgery under ether anaesthesia

Question 26

List drug advertising techniques (6).

Answer 26

``` Catch audience attention Use of celebrities or authority Fear Offering an easy solution to problems Before-after technique Discredit competing drugs; praise own drug ```

Question 27

What are the steps to introducing a new drug into therapeutics?

Answer 27

1. Proof of safety and efficacy of drug in several animal species to government regulatory agency 2. Methods for proposed human clinical trial 3. Clinical trials by pharmacologists (P1-P4)

Question 28

What is phase 1 of a clinical trial?

Answer 28

In a limited number of healthy volunteers the absorption, distribution, elimination and adverse effects are tested.

Question 29

What is phase 2 of a clinical trial?

Answer 29

Proof of concept - drug is tested to see if it is effective in treating the condition for which it is recommended; safety is studied

Question 30

What is phase 3 of a clinical trial?

Answer 30

Drug is testing in a larger number of people (1000+); safety and efficacy examined

Question 31

What is phase 4 of a clinical trial?

Answer 31

Drug released for general use; post-marketing surveillance for delayed risks

Question 32

What are placebo effects?

Answer 32

Effects which occur as a result of drug administration; unrelated to pharmacological effects

Question 33

Beecher?

Answer 33

Studied placebo effects; found satisfactory relief in 35% of patients

Question 34

What are conditions that may be responsive to placebos?

Answer 34

Angina pectoris, common cold, anxiety, cough, mood changes, headache, seasickness, post operative wound pain, asthma, hypertension, mental depression

Question 35

What should a new drug always be compared to (if available)?

Answer 35

An older drug of proven value; placebo if nonexistent

Question 36

What is cross-over design?

Answer 36

First occasion Group A - new drug Group B - old drug (or placebo) Second occasion Group A - old drug (or placebo) Group B - new drug

Question 37

What is parallel design?

Answer 37

Group A - new drug | Group B - old drug (or placebo)

Question 38

What is the best, unbiased experimental design?

Answer 38

Parallel design (with old drug), randomized group assignment, double-blind design, controlled elements

Question 39

Define potency.

Answer 39

Potency refers only to the amount of drug that must be given to obtain a particular response

Question 40

Define efficacy.

Answer 40

The maximum effect that is obtainable with a given drug

Question 41

Define selective toxicity.

Answer 41

Injury to one kind of living matter without harming some other kind

Question 42

Pasteur and Koch

Answer 42

Demonstrated that diseases of many types are caused by microbes

Question 43

How are sulfanilamides selectively toxic?

Answer 43

Disrupt the manufacture of folic acid through resemblance to PABA

Question 44

What compound do bacteria utilize to manufacture folic acid?

Answer 44

PABA (para-aminobenzoic acid)

Question 45

Define antimetabolite.

Answer 45

Something that acts against substances required for the metabolism of an organism

Question 46

Describe chemical differences between a normal cell and a cancer cell.

Answer 46

Certain cancer cells cannot manufacture asparagine (an aa required for protein synthesis) and require it from the blood. Cancer cells also divide continuously (while most normal cells are in a non-dividing state)

Question 47

What are twin hazards associated with the widespread distribution of drugs?

Answer 47

Accidental poisoning (mostly children under 5) and suicide

Question 48

List some of the most common items accidentally swallowed by children.

Answer 48

aspirin, acetaminophen, bleach, diaper-pail deodorizer, chocolate flavoured laxatives, children's fever drops, cough syrups, tranquilizers, birth control pills and cigarette butts

Question 49

What is the major drug group implicated in suicide?

Answer 49

Barbiturates

Question 50

List 4 types of adverse effects to drugs.

Answer 50

1. Extension of therapeutic effect 2. Unrelated to main drug action 3. Idiosyncrasy 4. Drug allergy

Question 51

Define idiosyncrasy in terms of an adverse effect to drug consumption.

Answer 51

The genetic makeup of some individuals renders them sensitive to the adverse effects of some drugs. For example, some patients lack a blood enzyme required to inactivate certain drugs

Question 52

Define the 3 P's of drug introduction

Answer 52

Panacea - Assumption that drug is a major new advance Poison - Adverse effects revealed; sales drop Pedestrian - Benefit/risk ratio easier to assess; realization that drug is "average"

Question 53

List the reasons as to why a new drug later turns out to be toxic (4).

Answer 53

1. The toxic reaction may be a rare event 2. The toxic reaction may only appear after the drug has been in prolonged use 3. Toxic effect not detectable in animals 4. Toxic effect unique to a certain period (ex. pregnancy)

Question 54

Define TD50

Answer 54

Dose toxic to 50% of the population of animals

Question 55

ED50

Answer 55

Median effective dose; dose which is effective in 50% of the population

Question 56

What ratio does the therapeutic index equal?

Answer 56

TD50/ED50

Question 57

What does a high therapeutic index mean?

Answer 57

Greater safety of the drug, wider safety margin

Question 58

What does a low therapeutic index mean?

Answer 58

Low drug safety, narrow safety margin

Question 59

If given the same dose, why would blood concentration of a drug differ between individuals?

Answer 59

1. genetic factors 2. environmental factors 3. disease 4. presence of other drugs

Question 60

What are the enteral routes of drug administration?

Answer 60

1. Drug taken by mouth (oral) 2. Rectal administration 3. Under the tongue (sublingual)

Question 61

What are the parenteral routes of drug administration?

Answer 61

1. intramuscular 2. subcutaneous 3. intravenous 4. inhalation 5. spinal canal 6. skin

Question 62

List disadvantages of intravenous administration.

Answer 62

1. A drug injected into a vein cannot be retrieved 2. If given too rapidly, can lead to disaster 3. Danger of infection is sterile technique is not used

Question 63

What are poisonous materials that can be absorbed through the skin?

Answer 63

Parathion and malathion (insecticides) and nicotine

Question 64

Describe how a drug allergy arises.

Answer 64

First time administered - drug forms an antigen; antibody is generated Second time administered - previous antibodies combine with antigens, provoking an adverse reaction

Question 65

What is the most common route of drug administration?

Answer 65

Oral

Question 66

Describe the steps a oral drug must undergo before it exerts an effect.

Answer 66

1. Disintegrates into small particles; dissolves in fluid of stomach/intestine 2. Absorption through stomach or intestine wall 3. Carried via bloodstream to site of action

Question 67

What is the major site of drug absorption (orally)?

Answer 67

Intestine

Question 68

What tests does the government require for tablets?

Answer 68

1. Must contain adequate amounts of the active chemical | 2. Must disintegrate in a test tube

Question 69

Define bioavailability.

Answer 69

The percentage of drug contained in a drug product that enters the systemic circulation in an unchanged form after administration. Also considers the rate of entry.

Question 70

List the processes that occur after a drug has been orally administered.

Answer 70

Absorption Distribution Biotransformation (metabolism) Excretion

Question 71

Where could a drug affecting the brain redistribute to (during termination)?

Answer 71

Muscle or fat

Question 72

Where are most drugs excreted from?

Answer 72

The kidneys

Question 73

How is a water soluble drug excreted?

Answer 73

In urine from the kidneys

Question 74

How is a fat soluble drug excreted?

Answer 74

It is filtered through the kidneys, but then reabsorbed via the renal tubules. It is then transported to the liver, which converts to a more water soluble product (via enzymes such as cytochromes P450)

Question 75

What is the main enzyme group responsible for converting fat-soluble drugs to water-soluble products?

Answer 75

Cytochromes P450

Question 76

Describe drug interactions caused by absorption.

Answer 76

1. One drug may combine with another in the stomach/intestine and form a complex which cannot be absorbed into blood 2. A drug increasing intestinal movements may speed the passage of a second drug 3. A drug may hinder intestinal movement, increasing drug absorption

Question 77

Describe drug interactions caused by displacement.

Answer 77

A second drug may displace the first drug from its binding site on a blood protein (free drug exerts more effect)

Question 78

Describe drug interactions caused by changes in liver handling.

Answer 78

Drug B may block the mechanisms in the liver responsible for the inactivation of Drug A. Drug B may also speed up the inactivation of Drug A.

Question 79

Describe drug interactions caused by changes in excretion.

Answer 79

Drug B may hinder the excretion of Drug A by the kidneys. Drug B may facilitate the excretion of Drug A by the kidney.

Question 80

Describe interactions of drugs with potentially toxic substances in food.

Answer 80

Tyramine (in old cheeses) is broken down in the liver by an enzyme known as monoamine oxidase (MAO). Some depression drugs are MAO inhibitors, which leads to excess tyramine (causing high BP)

Question 81

What is tyramine?

Answer 81

Tyramine is contained in foods such as old cheeses. It is related to adrenaline and raises BP. It is broken down in the liver by monoamine oxidase (MAO).

Question 82

What would happen is a tetracycline antibiotic is administered with an antacid?

Answer 82

They might combine in the intestine to form a complex that can not be absorbed by the blood