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Flashcards in Section A Deck (82):
1

What are the symptoms of ergot poisoning?

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

2

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

Ergotamine (migraines)
Ergonovine (arrest bleeding AFTER childbirth)

3

What accurate observations did the Ebers papyrus contain?

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

4

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

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

5

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

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

6

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

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

7

What compound can be isolated from foxglove?

Digoxin (Lanoxin) can be isolated from foxglove

8

Who discovered amyl nitrate? What was it used for?

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

9

Who discovered nitroglycerin?

William Murrell

10

Describe nitroglycerin's mechanism of action.

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

11

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

Quinine may be isolated for the treatment of malaria

12

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

Quinidine may be used for the treatment of arrhythmias

13

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

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

14

Which modern drug is a suitable replacement for reserpine?

Chlorpromazine

15

Who discovered LSD?

Albert Hofmann

16

Which compounds are structurally similar to LSD?

Ergotamine and ergonovine

17

Paul Ehrlich?

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

18

Gerhard Domagk?

Introduced sulfa drugs

19

Alexander Fleming?

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

20

Selman Waksman?

Discovered streptomycin (tuberculosis and Gram-negative bacteria)

21

Humphrey Davy?

Showed the pain-releiving effects of nitrous oxide

22

Colton?

Gave public demonstrations of nitrous oxide

23

Wells?

Dentist; used nitrous oxide during tooth extraction

24

Faraday?

Pointed out ether has similar properties as nitrous oxide

25

Morton?

Performed the first surgery under ether anaesthesia

26

List drug advertising techniques (6).

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

27

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

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)

28

What is phase 1 of a clinical trial?

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

29

What is phase 2 of a clinical trial?

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

30

What is phase 3 of a clinical trial?

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

31

What is phase 4 of a clinical trial?

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

32

What are placebo effects?

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

33

Beecher?

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

34

What are conditions that may be responsive to placebos?

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

35

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

An older drug of proven value; placebo if nonexistent

36

What is cross-over design?

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

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

37

What is parallel design?

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

38

What is the best, unbiased experimental design?

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

39

Define potency.

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

40

Define efficacy.

The maximum effect that is obtainable with a given drug

41

Define selective toxicity.

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

42

Pasteur and Koch

Demonstrated that diseases of many types are caused by microbes

43

How are sulfanilamides selectively toxic?

Disrupt the manufacture of folic acid through resemblance to PABA

44

What compound do bacteria utilize to manufacture folic acid?

PABA (para-aminobenzoic acid)

45

Define antimetabolite.

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

46

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

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)

47

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

Accidental poisoning (mostly children under 5) and suicide

48

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

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

49

What is the major drug group implicated in suicide?

Barbiturates

50

List 4 types of adverse effects to drugs.

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

51

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

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

52

Define the 3 P's of drug introduction

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"

53

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

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)

54

Define TD50

Dose toxic to 50% of the population of animals

55

ED50

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

56

What ratio does the therapeutic index equal?

TD50/ED50

57

What does a high therapeutic index mean?

Greater safety of the drug, wider safety margin

58

What does a low therapeutic index mean?

Low drug safety, narrow safety margin

59

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

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

60

What are the enteral routes of drug administration?

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

61

What are the parenteral routes of drug administration?

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

62

List disadvantages of intravenous administration.

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

63

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

Parathion and malathion (insecticides) and nicotine

64

Describe how a drug allergy arises.

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

65

What is the most common route of drug administration?

Oral

66

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

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

67

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

Intestine

68

What tests does the government require for tablets?

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

69

Define bioavailability.

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.

70

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

Absorption
Distribution
Biotransformation (metabolism)
Excretion

71

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

Muscle or fat

72

Where are most drugs excreted from?

The kidneys

73

How is a water soluble drug excreted?

In urine from the kidneys

74

How is a fat soluble drug excreted?

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)

75

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

Cytochromes P450

76

Describe drug interactions caused by absorption.

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

77

Describe drug interactions caused by displacement.

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

78

Describe drug interactions caused by changes in liver handling.

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.

79

Describe drug interactions caused by changes in excretion.

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

80

Describe interactions of drugs with potentially toxic substances in food.

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)

81

What is tyramine?

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).

82

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

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