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[Y2] Pharmacology & Toxicology > concepts and calculations > Flashcards

concepts and calculations Flashcards

1
Q

define pharmacology

A

the study of the effect of drugs on the function of living systems

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2
Q

define pharmacodynamics

A

the effects of the drug on the body
Example: Paracetamol- mechanism of action is dependent on the inhibition of prostaglandin synthesis.

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3
Q

define pharmacokinetics

A

the effects of the body on the drug
(relates to Absorption, Distribution, Metabolism, Excretion (ADME))

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4
Q

define drug

A

A biologically active compound (other than a nutrient or essential dietary ingredient) taken with the intent to produce a change in the body.

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5
Q

define medicine

A

A chemical preparation which usually contains one or more drugs administered with the purpose of producing a therapeutic effect. Medicines usually contain other substances to make them more convenient to use.

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6
Q

who pioneered the treatment of syphilis?

A

Paul Ehrlich

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7
Q

how long did it take Ehrlich to produce ‘salvarsan’

A

It took him three years’ and three hundred syntheses

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8
Q

who proposed the magic bullet theory?

A

Ehrlich

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9
Q

what is the magic bullet theory?

A
  • Whereby a drug would have selectively toxicity e.g. against a microbial agent or cancer cell.
  • Ideally with little action on the host cell even at high doses = therapy without toxicity.
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10
Q

who described drug action (at the neuromuscular junction)?

A

Langley

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11
Q

how did Langley describe drug action (at the neuromuscular junction)?

A

in terms of interaction with a “receptor” substance.

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12
Q

what does receptor represent in a drug?

A

the major target of a drug (the ‘bullets’)

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13
Q

why are there multiple drug classes?

A

Drugs cannot be classified according to a single rational system because of the need of chemists, pharmacologists, doctors differ.

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14
Q

Any drug may have names in _ different classes.

A

3

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15
Q

what are the 3 drug classes?

A
  • chemical class
  • IUPAC name
  • drug name
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16
Q

define target in terms of drugs

A

the molecular recognition site to which a drug will bind.

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17
Q

what are the majority of targets?

A

proteins

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18
Q

what percentage of drug targets are human?

A

73%

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19
Q

what percentage of drug targets are microbial, viral?

A

16%

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20
Q

what percentage of drug targets are miscellaneous?

A

11%

21
Q

how are drug targets identified?

A
  • exploring disease mechanisms (classical)
  • analysing genetic basis or susceptibility to disease (post-genomic)
22
Q

how many drugs were FDA approved in 2021?

A

50

23
Q

what are the 2 conventional routes of identifying drug targets?

A
  • Analysis pathophysiology
  • Analysis of mechanism of action of existing therapeutic drugs.
24
Q

what is the 1 novel route of identifying drug targets?

A

trawl the genome

25
Q

what is the logical starting point for drug discovery?

A

to understand the mechanisms of disease.

26
Q

who were the pioneers of understanding the mechanisms of disease?

A

Hitchings and Elion (1944) and their unravelling of the synthesis of DNA.

27
Q

what are disease genes?

A

Genes, mutations of which cause or predispose to the development of human disease

28
Q

what are disease modifying genes?

A

Genes whose altered expression may be involved in the development of the disease state OR genes that encode functional proteins, whose activity is altered in disease state

29
Q

what is an example of sucess from trawling the genome?

A

Imatinib, highly specific tyrosine kinase inhibitor. Treats chronic myeloid leukaemia

30
Q

what is an example of a frustration from trawling the genome?

A

Alzheimer’s disease

31
Q

what are transgenic models?

A

Genetically engineered animalmodelsencompasstransgenicor knockout model groups where the mice are genetically engineeredto overexpressorlackthegene of interest.

32
Q

define molarity

A

How much of the substance is available in a given volume.

33
Q

what are the units for molarity?

A

mol/l or M

34
Q

what is the equation for molarity?

A

Mass (g) = Concentration (mol/L) x Volume (L) x Formula Weight (g/mol)

35
Q

what is a mole?

A

The mole is the unit that defines the amount of a given substance

36
Q

one mole contains __________ molecules of a substance

A

6x10 ^23

37
Q

what is the mass of one mole in grams?

A

the molecular weight of that substance.

38
Q

By definition a 1M solution of NaCl contains 1 mole (6 x1023 molecules) in 1 litre of solution. So how would you prepare 250 ml of a 0.5mM solution?

A

7.3mg of NaCl into 250ml

39
Q

what is a biological assay?

A
  • A method of measuring the effects of a biologically active substance using an intermediate in vivo or in vitro tissue or cell model under controlled conditions.
  • For pharmacology; test the activity of a compound against a given ‘target’.
40
Q

what is used to create a concentration response curve?

A

logarithmic scales

41
Q

define logarithm

A

defined as the power to which a base (10) must be raised to produce a given number (e.g. Log 100 = 2)

42
Q

what are theraputic concentrations?

A

The therapeutic range of a drug is the dosage range or blood plasma or serum concentration usually expected to achieve the desired therapeutic effect.

43
Q

what is homeopathy?

A

an alternative medicine based on the theory of treating ‘like with like’.
- doesn’t work

44
Q

what are the 4 main steps to develop a new medicine?

A
  • discovery
  • exploratory development
  • full development
  • registration
45
Q

how much on average does it cost to develop a new medicine?

A

$1.3 billion

46
Q

how long does it take to develop a new medicine?

A

12-15 years

47
Q

what are the 7 steps for drug discovery?

A
  1. target discovery
  2. target validation
  3. screen development
  4. hit discovery
  5. lead development
  6. candidate identification
  7. candidate drug development
48
Q

what are the 4 pharmacology principles?

A
  • active ingredient (drug molecule)
  • Selectively bind to certain molecular targets (e.g proteins) and
    • Exerts cellular effect
    • Exerts effect on system
  • Produce a therapeutic effect in a concentration-related or concentration-dependent fashion
  • efficacy (usefullness) of drug is supported by clinical trials using agreed ‘outcome measures’ and statistical validation

[Y2] Pharmacology & Toxicology (2 decks)

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