Fundamentals of Pharmacology

Question 1

What is pharmacology

Answer 1

Science of drugs

Mechanism of action

Question 2

What is therapeutics

Answer 2

Medicinal use of drugs

Question 3

What is pharmacy

Answer 3

preparation and dispensing of drugs

Question 4

What is toxicology

Answer 4

harmful effects of drugs

Question 5

what is a drug

Answer 5

chemical substance of know structure, not a nutrient, which when administered to a living organism produces a biological response

Question 6

How many names do drugs have and what are they grouped by

Answer 6

3 names - chemical, common, trade

therapeutic use (analgesia) and mechanism

Question 7

What 4 things can drugs bind to and what are these drugs called

Answer 7

Enzymes, ion channels, carrier molecules, receptors (for neurotr and horm)

ligands

Question 8

what is meant by a drug being an agonist or an antagonist

Answer 8

agonist - activates receptor and produces a response

antagonist - prevents receptor from being activated

Question 9

What is the mechanism of drug action

Answer 9

drugs are exogenous molecules which mimic or block the action of endogenous molecules

Question 10

what is meant by selectivity and specificity

Answer 10

for a drug to be useful therapeutically it needs to be very SELECTIVE in its action, however will produce side effects.

solution - design a drug with a high SPECIFICITY to a the target cell

Question 11

what is meant by pharmacodynamics

Answer 11

what a drug does to the body

Question 12

what is meant by pharmacokinetics

Answer 12

what the body does to a drug

ADME (absorption, distribution, metabolism, excretion)

Question 13

what is meant by absorption and what is it affected by

Answer 13

determines how much and how quickly a drug can enter the body.

molecular size, lipid solubility, route of adminis, properties of patient e.g size

Question 14

what is meant by distribution and what is it affected by

Answer 14

determines whether the drugs effects are local or systematic (travels throughout whole body)

• patients circulation
• does the drug bind to proteins in the blood
• does the drug have access to the organ it will act on

Question 15

what is meant by metabolism and excretion

Answer 15

determines how long the drugs effects last. drugs are metabolised into metabolites in the liver and excreted by the kidneys.

is the liver healthy, are the liver enzymes effective

Question 16

what is meant by the half life of a drug + clearance

Answer 16

Affected by met and exc, the time it takes for the drug conc in the blood to half.

volume of blood cleared of the drug per unit time

Question 17

what is the shape of a drug conc-response curve and log drug conc-response curve

Answer 17

drug conc-response - rectangular hyperbola

log drug conc-response - symmetrical sigmoid

Question 18

what are the 3 types of pharmacological experiment

Answer 18

in vitro
in vivo
ex vivo

Question 19

describe how in vitro works

Answer 19

drug effects are studied on a piece of tissue taken from an animal/human and kept alive outside the body

Question 20

describe how in vivo works

Answer 20

drug effects studied in the living animal/human. eg clinical trials

Question 21

describe how ex vivo works

Answer 21

tissue removed from an animal/human who was treated with the drug

Question 22

what is milli, micro and nano

Answer 22

10-3
10-6
10-9

Question 23

what are the units of in vitro drug conc

Answer 23

Molar (moles per litre)
1 Molar solution=1 mole of drug dissolved in 1 litre of solution
eg. 45mM=4.5x10-2

Question 24

what are the units of in vivo drug conc

Answer 24

we cant use molar conc as we dont know the volume of solvent eg blood, so we use mg per kg

Question 25

what is Emax

Answer 25

the maximum response a drug can produce

Question 26

what is EC50

Answer 26

the conc of the drug which produces 50% of the maximum response

Question 27

what is meant by potency

Answer 27

describes the conc at which the drug is effective (produces an effective response) a potent drug is one which is effective in small conc

Question 28

how do we quantify potency

Answer 28

using EC50

Question 29

What is the potency ratio (M) and what do we use it to compare

Answer 29

compares the EC50s of 2 drugs. | often we compare a new drug (test) and an already available drug (standard)

Question 30

How do we calculate the potency ratio (M)

Answer 30

M = EC50 (test) / EC50 (standard) OR logM = log EC50 (test ) - log EC50 (standard)

Question 31

if the value of M is less than 1 what does that mean

Answer 31

M is less than 1 means that the EC50 of the test drug is lower so is potent

Question 32

what is meant by the therapeutic index

Answer 32

Ratio between the toxic dose of a drug and the dose producing the desired therapeutic effect

Question 33

if there is a higher therapeutic index, what does this mean

Answer 33

lower chance of the drug producing toxic side effects

Question 34

what are the 2 therapeutic index formulas

Answer 34

LD50/ED50 (lethal dose in 50% of the population) | TD50/ED50 (toxic)

Question 35

why is LD50/ED50 not used anymore

Answer 35

death is an extreme side effect | unethical to obtain LD50 values from animals

Question 36

Problems with TD50/ED50 (used for humans)

Answer 36

Drug effects are different for every person | drug can have different ED50 values depending on the condition being treated

Question 37

what do receptors do

Answer 37

recognise extracellular molecules | transducers - having detected the extracellular molecules they can then bring about changes in the cell

Question 38

what is meant by specificity

Answer 38

only one or a few drugs can bind to a receptor

Question 39

what is meant by affinity

Answer 39

ability of a drug to bind to a receptor

Question 40

how can we quantify affinity

Answer 40

using Kd - [drug] required to occupy 50% of receptors at equilibrium. high affinity = low Kd

Question 41

what is meant by efficacy

Answer 41

ability of a drug to activate a receptor

Question 42

what are the two types of agonist and explain them

Answer 42

full agonist - has affinity and HIGH efficacy | partial agonist - has affinity and LOW efficacy so less effective

Question 43

explain the graph for full and partial agonists for p (receptors) against response

Answer 43

full - produces max response while only activating a small number of receptors partial - fails to produce max response despite occupying all the receptors

Question 44

what are antagonists

Answer 44

prevent receptor from being activated | act as inhibitors, inhibiting the effects of neuro, hormones etc.

Question 45

what are the 5 types of antagonists

Answer 45

``` competitive non competitive chemical pharmacodynamic physiological ```

Question 46

what is a comp antagonist

Answer 46

competes with the agonist for the same receptor but doesn't activate it (has zero efficacy) R or IR

Question 47

what is a non comp antagonist

Answer 47

acts at a diff site on the receptor, causing a conform change. R or IR

Question 48

what is a chemical antagonist

Answer 48

uses one drug to chemically inactivate another

Question 49

what is a pharmacokinetic antagonist

Answer 49

one drug alters the way the body deals with another

Question 50

what is a physiological antagonist

Answer 50

two drugs act to produce opposing effects, cancelling each other out

Question 51

describe the graph for rev and irrev comp antagonist | log

Answer 51

symmetrical sigmoid rev - moves to the right still parallel, effects can be overcome by increasing [agonist] irrev - curve gets lower and doesn't reach the same response, inhibition cant be overcome by an inc in [agonist], blockade is not surmountable