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Stage 2, Cycle 2 - PSFC2 > Med Chem 1 > Flashcards

Med Chem 1 Flashcards

1
Q

Define Pharmacognosy

A

The study of the physical, chemical, biochemical and biological properties of drugs, drug substances or potential drug substances of natural origin. As well as the search for new drugs from natural sources

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2
Q

Name different ‘pools’ natural drugs can be extracted from and give examples of drugs

A
  • Plant kingdom (Morphine, Salicin, Quinine, Taxol, Reserpine)
  • Microbial world (Penicillin and Statins)
  • Marine world (curacin A; obtained from a marine cyanobacterium)
  • Animals (Epibatidine; from the skin of Ecuadorian poison frog)
  • Toxins/Venoms (Teprotide; a peptide isolated from venom of Brazilian pit viper)
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3
Q

The plant kingdom is a ‘plentiful, rich supply of complex and varied chemical compounds’. TRUE or FALSE

A

TRUE

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4
Q

Many plant species in the rainforest are ‘untapped sources still wanting to be discovered’. TRUE or FALSE

A

TRUE

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5
Q

Plants evolved for the purpose of producing medicines. TRUE or FALSE

A

FALSE. Plants did not evolve for the purpose of producing medicines.

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6
Q

All plant chemicals are good chemicals. TRUE or FALSE

A

FALSE. Many are irritant/toxic and provide defense against predators (herbivores and omnivores)

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7
Q

Herbal remedies involve experimentation with berries, leaves and roots. TRUE or FALSE

A

TRUE

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8
Q

Herbal remedies are often useless and dangerous. TRUE or FALSE

A

TRUE

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9
Q

Herbal remedies are an example of placebo effects -state of mind and no real differences. TRUE or FALSE

A

TRUE

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10
Q

State 5 facts about herbal remedies

A

1) 80% OF THE WORLD’S POPULATION use herbal drugs as part of their normal health care routine
2) In the USA, herbal remedies are the FASTEST GROWING SEGMENT of pharmacy trade
3) Tend to be LESS EXPENSIVE than prescription drugs
4) They’re NOT PURE substances (contain many constituents)
5) They’re NOT STANDARDISED OR ANALYSED for content of active principle

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11
Q

Define the term ‘Herb’

A

A crude material, containing multiple pharmacologically active compounds

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12
Q

What method can be used to verify the composition and quality of herbal remedies?

A

HPLC (High performance liquid chromatography)

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13
Q

Herbal remedies may contain some compounds that reinforce others. TRUE or FALSE

A

TRUE

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14
Q

Herbal remedies may work through SYNERGY. TRUE or FALSE

A

TRUE. The mixture acts together to generate beneficial effect

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15
Q

Why should pharmacists be aware of patients taking herbal preparations?

A

Any prescribed medication may be inhibited or show response consistent with an overdose

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16
Q

State an example of a drug and a herbal remedy that may cause an overdose ?

A

Drug = Coumadin (Warfarin)
Herbal remedy = Gingko biloba extracts (from chinese kew tree)

Gingko inhibits platelet-activating factor, PAF causing an overdose effect of coumadin. This leads to increased bleeding as a result of excessive blood thinning.

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17
Q

Gingko biloba extracts include ginkgolide A and B. TRUE or FALSE

A

TRUE

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18
Q

How does gingko affect the arterial and venous circulation ?

A

It produces VASODILATORY EFFECTS on the arterial and venous circulation (increasing peripheral and cerebral blood flow)

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19
Q

Why are natural products usually hard to synthesise in the lab ?

A

They usually have complex structures, for example ARTEMISININ (contains a Trioxane ring)

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20
Q

What is ARTEMISININ ?l

A

An antimalarial agent (Chinese herbal medicine)

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21
Q

Draw Morphine structure

A

C17H19NO3

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22
Q

Where is the natural drug Reserpine extracted from ?

A

Indian Snakeroot plant

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23
Q

Reserpine breaks down in the presence of light (especially in clear glass containers). TRUE or FALSE

A

TRUE

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24
Q

Describe the structure of Reserpine

A
  • Light yellow crystalline alkaloid

- Indole nucleus

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25
Q

What is the role of Reserpine

A

Reduces blood pressure (anti-hypertensive)

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26
Q

‘Salicin’ is a glycoside. TRUE or FALSE

A

TRUE

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27
Q

When in the body, Salicin is converted to?

A

Salicyclic acid

28
Q

What was Quinine initially used as ?

A

A muscle relaxant (stopping the shivering brought on by cold weather)

29
Q

What is Quinine extracted from?

A

The bark of the Cinchona tree

30
Q

What is Quinine now used to treat?

A

Malaria (arrests patient fevers)

31
Q

Morphine is extracted from ?

A

Ancient Egyptian opium poppy (found in the opium juice)

32
Q

Salicin is extracted from ?

A

Medieval England Willow tree

33
Q

Quinine is extracted from ?

A

S.American (Quechua Indians of Peru) Cinchona bark

34
Q

Name 2 examples of more recent Natural drugs

A

1) Combretastatin

2) Taxol (Paclitaxel)

35
Q

What is Combretastatin extracted from ?

A

The South African ‘combretum caffrum’ tree

36
Q

What is the role of Combretastatin ?

A

A potent cytotoxic against a variety of human cancer cells (still in clinical trials but may be the next anticancer choice of drug)

37
Q

What is the main drawback of Combretastatin ?

A

Has poor water solubility

38
Q

In vitro studies shows Taxol had ….. activity ? Fill in the gap

A

Cytotoxic

39
Q

Name 4 types of Cancer Taxol can be used to treat ?

A

1) Ovarian cancer
2) Lung cancer
3) Prostate cancer
4) Metastatic breast cancer

40
Q

Define Alkaloids

A

Amines found in plants (in the seeds, roots, bark and leaves)

41
Q

Is Morphine an Alkaloid ?

A

Yes, It has a tertiary amine

42
Q

Name 5 Semi-synthetic drugs

A

1) Aspirin
2) Taxol
3) Taxotere (docetaxel) - modified from Taxol
4) Galanthamine
5) Heroin

43
Q

What is a semi-synthetic drug ?

A

A drug from natural sources that has been modified in the lab

44
Q

What is the role of Aspirin ?

A

An analgesic

45
Q

When was Aspirin marketed ?

A

After curing toothache (highlighting its Analgesic properties)

46
Q

Taxol can be extracted from Pacific yew trees ? TRUE or FALSE ?

A

TRUE

47
Q

Why do we need to use the Semi-synthetic approach when making Taxol ?

A

Because we’d need 4 Pacific Yew trees per patient! therefore we need to harvest a bio-synthetic intermediate

48
Q

Name a bio-synthetic intermediate for making Taxol (Paclitaxel)

A

10-deacetylbaccatin III (easier to extract from the tree as it is found in the needles of the tree)

49
Q

How many more steps are required to convert 10-Deacetylbaccatin III to Taxol

A

4

50
Q

What is Taxotere (docetaxel) approved to treat ?

A

Advanced breast cancer

51
Q

What is Galanthamine extracted from ?

A

European daffodils and snowdrops

52
Q

Galanthamine is a tertiary alkaloid ?TRUE or FALSE

A

TRUE

53
Q

What is Galanthamine used to treat and why?

A

Mild Alzheimer’s Disease (as significant improvements in performance and attention have been found)

54
Q

(-)-galanthamine is prepared by ?

A

The stereospecific reduction of (-)-narwedine

55
Q

Synthetic drugs include drugs originating from the screening of …. ?Fill in gap

A

Dyes

56
Q

Name a scientist who made an important contribution to synthetic drugs/ the dye industry?

A

Paul Ehrlich

57
Q

Describe Paul Ehrlich’s initial work…

A

Initial work involved the use of natural dyes/analogues in histological staining. (staining microbes and viewing them under microscope)

58
Q

Paul Ehrlich ‘s thesis was critical of ?

A

Histologists that failed to base their work on the understanding of how dyes bind to tissue components

59
Q

Paul Ehrlich suggested that …. and ….. …… are important for the UPTAKE and DISTRIBUTION of dye in cellular and animal models

A

Size and Chemical structure

60
Q

Name 3 Synthetic drugs (originating from the screening of dyes)

A

1) Methylene blue (Ehrlich & Guttman)
2) Antibacterial azodyes (Chrysoidine and Pheazopyridine)
3) Heterocyclic sulfonamides (Sulfapyridine)

61
Q

What is Methylene blue used to treat ? state strength and dose

A

Malaria, 5 x100mg capsules per day

62
Q

Name the first synthetic drug (originated from dye screening) successfully used to treat against a specific disease

A

Methylene blue

63
Q

What properties do Chrysoidine possess ?

A

Powerful antiseptic properties

64
Q

What is Phenazopyridine used as ?

A

A Urinary antiseptic (relief for urinary tract pain)

65
Q

Give an example of a potent antibacterial sulfonamide

A

Sulfapyridine

  • Winston Churchill saved by this in 1943
  • Reduced mortarlity in pneumonia patients from 1 in 4 to 1 in 25
66
Q

Natural products vs Synthetic products. State 3 things that Natural products have more …

A

1) More protonated amine and free hydroxy functionalities
2) More single bonds
3) More fused rings containing more chiral centres

Stage 2, Cycle 2 - PSFC2 (11 decks)

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