introduction to pharmacology

Question 1

what is a drug

Answer 1

any compound used to treat disease

Question 2

common drugs

Answer 2

paracetamol, ibuprofen, cannabis, nicotine, alcohol

Question 3

what are the three different sources of drugs

Answer 3

-plants and natural products-digoxin for heart conditions from foxglove plant
-micro-organisms- penicillin from mould
animals- insulin from pancreas of various animals

Question 4

factors important to consider when producing a drug

Answer 4

mechanism
dose
selectivity
side effects
risk/benefit ratio

Question 5

what is a receptor

Answer 5

protein that has a structure that enables it to bind to a drug

Question 6

agonist function

Answer 6

to activate receptors

Question 7

what are antagonists

Answer 7

-block receptor so that the agonist cannot bind

Question 8

what are the two types of agonists

Answer 8

-full agonists
-partial agonists

Question 9

what is a full agonist

Answer 9

-fully binds to and activates the receptor
-produces a maximum response
examples morphine- bind to opioid receptors

Question 10

what is a partial agonist

Answer 10

binds to receptors but activates them to a lesser extent
produces a weaker response despite occupying the same receptor
example is buprenorphine which binds to opioid receptors

Question 11

what are the three types of antagonists

Answer 11

reversible competitive antagonists
irreversible competitive antagonists
non competitive antagonists

Question 12

what are reversible competitive antagonists

Answer 12

bind at the site of agonist so competes with it
increasing concentration of agonist can overcome effect

Question 13

what are irreversible competitive antagonists

Answer 13

bind to receptor via strong covalent bonds
increasing concentration of agonist has no effect, so to overcome the effect, new receptors must be synthesised

Question 14

what are non competitive antagonists

Answer 14

bind to a distinct site
alter function of the receptor

Question 15

what does potency mean

Answer 15

concentration of drug needed to produce a desired effect- effectiveness
low concentration of drug needed- higher potency

Question 16

what does the ec50 mean

Answer 16

the concentration of a drug needed to produce half of its maximum effect
increase in potency- lower ec50

Question 17

what happens to the ec50 as the potency increases

Answer 17

ec50 lowers

Question 18

what does efficacy mean

Answer 18

magnitude of effect a drug can produce
the ability of a drug to activate a receptor once it binds to it

Question 19

what is the efficacy of full agonists

Answer 19

1

Question 20

what is the efficacy of partial agonists

Answer 20

between 1 and 0

Question 21

what is the efficacy of an antagonist

Answer 21

0

Question 22

what is the TI therapeutic index

Answer 22

measure of drug safety
margin between therapeutic and toxic effect
TI= TD50/ED50

Question 23

what is the TD50

Answer 23

dose toxic to 50% population

Question 24

what is the ED50

Answer 24

dose effective in 50% of the population

Question 25

what does a lower therapeutic index mean

Answer 25

more likely for toxicity to be a problem

Question 26

what are allosteric modulators

Answer 26

act at distinct sites to which the agonist (neurotransmitter) binds to
negative- non competitive antagonists
positive- increase potency of agonist
dose response curve shifts to left

Question 27

what is an example of a positive allosteric modulator

Answer 27

diazepam

Question 28

what is an example of a negative allosteric modulator

Answer 28

GABA