concepts and calculations

Question 1

define pharmacology

Answer 1

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

Question 2

define pharmacodynamics

Answer 2

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

Question 3

define pharmacokinetics

Answer 3

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

Question 4

define drug

Answer 4

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

Question 5

define medicine

Answer 5

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.

Question 6

who pioneered the treatment of syphilis?

Answer 6

Paul Ehrlich

Question 7

how long did it take Ehrlich to produce ‘salvarsan’

Answer 7

It took him three years’ and three hundred syntheses

Question 8

who proposed the magic bullet theory?

Answer 8

Ehrlich

Question 9

what is the magic bullet theory?

Answer 9

• 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.

Question 10

who described drug action (at the neuromuscular junction)?

Answer 10

Langley

Question 11

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

Answer 11

in terms of interaction with a “receptor” substance.

Question 12

what does receptor represent in a drug?

Answer 12

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

Question 13

why are there multiple drug classes?

Answer 13

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

Question 14

Any drug may have names in _ different classes.

Answer 14

3

Question 15

what are the 3 drug classes?

Answer 15

• chemical class
• IUPAC name
• drug name

Question 16

define target in terms of drugs

Answer 16

the molecular recognition site to which a drug will bind.

Question 17

what are the majority of targets?

Answer 17

proteins

Question 18

what percentage of drug targets are human?

Answer 18

73%

Question 19

what percentage of drug targets are microbial, viral?

Answer 19

16%

Question 20

what percentage of drug targets are miscellaneous?

Answer 20

11%

Question 21

how are drug targets identified?

Answer 21

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

Question 22

how many drugs were FDA approved in 2021?

Answer 22

50

Question 23

what are the 2 conventional routes of identifying drug targets?

Answer 23

• Analysis pathophysiology
• Analysis of mechanism of action of existing therapeutic drugs.

Question 24

what is the 1 novel route of identifying drug targets?

Answer 24

trawl the genome

Question 25

what is the logical starting point for drug discovery?

Answer 25

to understand the mechanisms of disease.

Question 26

who were the pioneers of understanding the mechanisms of disease?

Answer 26

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

Question 27

what are disease genes?

Answer 27

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

Question 28

what are disease modifying genes?

Answer 28

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

Question 29

what is an example of sucess from trawling the genome?

Answer 29

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

Question 30

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

Answer 30

Alzheimer's disease

Question 31

what are transgenic models?

Answer 31

Genetically engineered animal models encompass transgenic or knockout model groups where the mice are genetically engineered to overexpress or lack the gene of interest.

Question 32

define molarity

Answer 32

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

Question 33

what are the units for molarity?

Answer 33

mol/l or M

Question 34

what is the equation for molarity?

Answer 34

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

Question 35

what is a mole?

Answer 35

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

Question 36

one mole contains __________ molecules of a substance

Answer 36

6x10 ^23

Question 37

what is the mass of one mole in grams?

Answer 37

the molecular weight of that substance.

Question 38

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?

Answer 38

7.3mg of NaCl into 250ml

Question 39

what is a biological assay?

Answer 39

- 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’.

Question 40

what is used to create a concentration response curve?

Answer 40

logarithmic scales

Question 41

define logarithm

Answer 41

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

Question 42

what are theraputic concentrations?

Answer 42

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

Question 43

what is homeopathy?

Answer 43

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

Question 44

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

Answer 44

- discovery - exploratory development - full development - registration

Question 45

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

Answer 45

$1.3 billion

Question 46

how long does it take to develop a new medicine?

Answer 46

12-15 years

Question 47

what are the 7 steps for drug discovery?

Answer 47

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

Question 48

what are the 4 pharmacology principles?

Answer 48

- 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