Pharmacology

Question 1

pharmacokinetics is

Answer 1

what the body does to a drug

Question 2

pharmacodynamics is

Answer 2

what a drug does to the body

Question 3

what is selectivity

Answer 3

ability of a drug to distinguish targets within the body

Question 4

what is selective toxicity

Answer 4

drug targets are selective to pathogenic species only

Question 5

what is an agonist

Answer 5

drug binding to receptor to produce a response

Question 6

what is an antagonist

Answer 6

drug binding to a receptor to block or reduce actions of agonist

Question 7

what is affinity

Answer 7

strength of association between ligand and receptor

Question 8

what is efficacy

Answer 8

ability of an agonist to evoke cellular response

Question 9

what is EC50

Answer 9

concentration of agonist eliciting half maximal effect

Question 10

dose plotted against effectiveness produces a ___ curve on a log graph

Answer 10

sigmoidal

Question 11

what is potency

Answer 11

ability of a drug to elicit EC50 at lesser dosages

Question 12

what is reversible competitive antagonism

Answer 12

reversible agonist/antagonist at orthosteric site

Question 13

what happens to the dose/response curve in reversible competitive antagonism

Answer 13

right shift - more drug required for effect

Question 14

what is reversible non-competitive antagonism

Answer 14

antagonist binds to allosteric site

Question 15

what happens to dose/response curve in reversible non-competitive antagonism

Answer 15

max response decreases but no right shift - efficacy lost but no increase in drug dose can help it

Question 16

what is an autocrine signal

Answer 16

signal generated within cell to evoke its own response

Question 17

what is a paracrine signal

Answer 17

short distance signalling to target local cells

Question 18

what is an endocrine signal

Answer 18

slow acting and long range

Question 19

types of ligand gated ion channels

Answer 19

chemical
voltage
mechanical/thermal

Question 20

what does the alpha subunit of a g protein do

Answer 20

modulates enzyme effector

Question 21

what does beta/gamma subunit of g protein do

Answer 21

modulates ion channels

Question 22

nuclear receptors are bound to by hydrophilic/hydrophobic ligands

Answer 22

hydrophobic

Question 23

ADME

Answer 23

Absorption
Distribution
metabolism
Excretion

Question 24

4 ways a drug can pass across the cell membrane

Answer 24

endocytosis
passive diffusion
facilitated diffusion
active transport

Question 25

principle sites for mediated drug transport

Answer 25

``` blood brain barrier GI tract placenta renal tubule biliary tract ```

Question 26

when pKa=pH a drug is

Answer 26

half ionised

Question 27

weak bases accumulate in?

Answer 27

low pH

Question 28

weak acids accumulate in?

Answer 28

high pH

Question 29

small water soluble molecules accumulate in

Answer 29

total body water

Question 30

large water soluble molecules accumulate in

Answer 30

ECF

Question 31

highly plasma protein bound molecules, very large with charge accumulate in

Answer 31

blood plasma

Question 32

what is the apparent volume of distribution

Answer 32

extent that a drug partitions between plasma and tissue

Question 33

volume of distribution equation

Answer 33

Vd=dose/[drug]plasma

Question 34

low Vd drugs remain in

Answer 34

vascular system

Question 35

high Vd drugs remain in

Answer 35

adipose, muscle and non muscle

Question 36

high Vd is anything around or greater than?

Answer 36

41L, average body volume

Question 37

most important drug metabolising organ

Answer 37

liver

Question 38

polar/non polar molecules are more readily metabolised

Answer 38

non polar

Question 39

example of a drug that bypasses phase I metabolism

Answer 39

codeine

Question 40

phase I metabolism

Answer 40

breakdown by oxidation, reduction or hydrolysis to produce a reactive metabolite

Question 41

oxidation can produce harmful metabolites in phase I metabolism. name one

Answer 41

paracetemol broken down can cause liver failure

Question 42

high P450 activity means

Answer 42

lower drug plasma levels as metabolised faster

Question 43

low P450 activity levels means

Answer 43

higher drug plasma levels so potential adverse reaction

Question 44

Phase II metabolism

Answer 44

combination of drug with polar molecules to form water soluble metabolite

Question 45

true/false - phase II metabolism terminates all biological activity

Answer 45

true

Question 46

principle organ for drug elimination

Answer 46

kidneys

Question 47

how do toxic drug effects come about

Answer 47

metabolites bind to cell membrane in phase I and are not eliminated increased drug dose so drug binds to off target receptor

Question 48

true/false - drug absorption IV is gradual

Answer 48

false - it is gradual in oral/IM and instantaneous IV

Question 49

what is clearance

Answer 49

volume of blood removed of drug per unit time

Question 50

clearance drug graph follows first/second order kinetics

Answer 50

first

Question 51

why is clearance important

Answer 51

estimates dose needed to maintain desired drug concentration in plasma

Question 52

clearance equation

Answer 52

CL= rate of drug elimination/[drug]plasma

Question 53

what does elimination half life determine

Answer 53

how much time required for a drug to be eliminated from body

Question 54

generally how many half lives before drug is eliminated from body

Answer 54

5

Question 55

calculation of t1/2

Answer 55

t1/2=0.693 x Vd/CL

Question 56

what is depolarisation

Answer 56

membrane becoming less negative

Question 57

what is hyperpolarisation

Answer 57

membrane becoming more negative

Question 58

what is repolarisation

Answer 58

membrane returning to resting value

Question 59

influx of sodium will cause cell to become more

Answer 59

positive

Question 60

efflux of potassium will cause cell to become more

Answer 60

negative

Question 61

what is the absolute refractory period

Answer 61

no stimulus can elicit 2nd AP

Question 62

what is the relative refractory period

Answer 62

some strong stimuli can elicit 2nd AP

Question 63

true/false - AP will always have same amplitude across an axon

Answer 63

true

Question 64

ways to increase AP transmission

Answer 64

increased axon diameter | increased myelin

Question 65

branches of ANS

Answer 65

sympathetic parasympathetic enteric

Question 66

what splits the preganglionic and postganglionic neurons

Answer 66

autonomic ganglion

Question 67

true/false - the sympathetic and parasympathetic systems oppose each other

Answer 67

false - they work complementary to each other

Question 68

the sympathetic nervous system orchestrates what response

Answer 68

stress and energy consumption

Question 69

the parasympathetic nervous system orchestrates what response

Answer 69

restorative, energy conservative

Question 70

neurotransmitter of preganglionic neuron

Answer 70

ACh

Question 71

neurotransmitters of postganglionic neuron

Answer 71

ACh | NA

Question 72

ACh from preganglionic neuron binds to what receptor?

Answer 72

nicotinic ACh receptors

Question 73

NA from postganglionic neuron binds to what receptor?

Answer 73

g protein coupled adrenoceptors

Question 74

ACh from postganglionic neuron binds to what receptor?

Answer 74

muscarinic ACh receptor

Question 75

alternative sympathetic neurotransmitters

Answer 75

ATP | Neuropeptide Y

Question 76

alternative parasympathetic neurotransmitters

Answer 76

VIP | NO

Question 77

___ and ___ provide rapid relaxation

Answer 77

ACh and NO

Question 78

___ provides slow relaxation

Answer 78

VIP

Question 79

___ provides very fast contraction

Answer 79

ATP

Question 80

____ provides moderately fat contraction

Answer 80

NA

Question 81

____ provides slow contraction

Answer 81

neuropeptide Y

Question 82

muscarinic ACh are ligand gated/g protein and have ___ subtypes

Answer 82

g protein | 5

Question 83

features of cholinergic transmission

Answer 83

``` uptake synthesis of ACh storage AP release degradation and reuptake ```

Question 84

how many types of nicotinic ACh receptors are there

Answer 84

4

Question 85

the all or nothing AP response is caused by what ion

Answer 85

sodium

Question 86

M1 muscarinic ACh receptors

Answer 86

Gq phospholipase C increased acid secretion in stomach

Question 87

M2 muscarinic ACh receptors

Answer 87

Gi inhibits adenylyl cyclase decreased HR

Question 88

M3 muscarinic ACh receptors

Answer 88

Gq Phospholipase C contraction of smooth muscle in bronchioles

Question 89

features of noradrenergic trnasmission

Answer 89

``` uptake synthesis storage AP release reuptake by U1 and U2 metabolism in cell my MAO and COMT ```

Question 90

B1 adrenoceptors

Answer 90

Gs - adenylyl cyclase to increase cardiac rate and force

Question 91

B2 adrenoceptors

Answer 91

Gs - adenylyl cyclase | relax bronchial and vascular smooth muscle

Question 92

A1 adrenoceptors

Answer 92

phospholipase C | Vascular smooth muscle contraction

Question 93

A2 adrenoceptors

Answer 93

inhibits adenylyl cyclase | inhibits NA release

Question 94

what do presynaptic autoreceptors do

Answer 94

mediate negative feedback inhibition of transmitter release

Question 95

what antiplatelet blocks production of thromboxane 2 to prevent binding to receptor

Answer 95

aspirin

Question 96

how do prasugrel and clopidogrel act as antiplatelet

Answer 96

block ADP binding

Question 97

why are anticoagulants indicated in AF patients

Answer 97

risk of stroke

Question 98

how does warfarin act as an anticoagulant

Answer 98

inhibits vitamin K - used to synthesise VII, X, IX, II

Question 99

how does heparin act as an anticoagulant

Answer 99

binds to antithrombin III to increase affinity for it for IIa and Xa

Question 100

TPA acts as fibrinolysis as it

Answer 100

increases conversion of plasminogen to plasmin