Question 1
Question
What is pharmacodynamics?
Question 2
Question
What is pharmacokinetics?
Question 3
Question
Pharmacodynamics allows us to...
Answer
-
determine the appropriate dose range for patients and compare how safe or effective different drugs are.
-
design and optimise treatment plans for individuals.
-
determine the best route and frequency of administration of a new drug.
Question 4
Question
What does ADME stand for?
Answer
-
Administration
-
Affect
-
Absorption
-
Distribution
-
Dissolving
-
Metabolism
-
Modification
-
Excretion
-
Editing
Question 5
Question
Absorption is...
Answer
-
how a drug gets from the site of administration into the blood.
-
how a drug moves from the blood to target cells.
-
how the drug elicits its effect on the body.
-
how a drug is eliminated from the body.
Question 6
Question
Distribution is...
Answer
-
how the drug moves in the body, for example leaving the blood stream and distributing non uniformly into intracellular fluids.
-
how long the drug moves around in the blood for.
-
how the drug is inactivated by the body.
-
how the drug is eliminated from the body, for example in bile.
Question 7
Question
Metabolism is...
Answer
-
how the body inactivates the drug.
-
enzymatic modification.
-
how the drug travels through the body.
-
how the drug passes cell walls.
Question 8
Answer
-
how the drug is eliminated from the body, for example in urine, bile or faeces.
-
how long the drug can stay in the body unchanged.
-
how the drug gets from the site of administration to the GI tract.
-
how the drug elicits a cellular response.
Question 9
Question
From what sources can we create drugs?
Answer
-
Completely synthetic materials.
-
Plants.
-
Synthetic materials but using the template of a naturally occurring compound.
-
Biologics (derived from growth factors and recombinant proteins).
-
Electricity.
-
Nitrogen gas.
-
Laptops.
Question 10
Question
How many types of proteins act as drug targets?
Question 11
Question
What are the four types of proteins that can act as drug targets?
Answer
-
Receptors, Ion Channels, Enzymes and Carriers.
-
Hormonal Receptors, Gated Ion Channels, Metabolic Enzymes, Carriers.
-
Receptors, Ion Channels, Enzymes, Channels.
-
Ion Channels, Reception, Enzyme Inhibitors, Carriers.
-
Ion Channels, Receptors, Enzymes, Channels.
Question 12
Question
Drug interaction with the target is determined by two factors. What are they?
Answer
-
Shape
-
Charge Distribution
-
Colour
-
Name
-
Time
Question 13
Question
This determines the ability of a drug to bind to it's target. It it the right __________ to bind to the target or not? Lock and Key mechanism.
Question 14
Question
This determines the strength of associations between the drug and it's target, because it determines the bonds that the drug can make.
Answer
-
Charge Distribution
-
Shape
-
Colour
-
Mass
Question 15
Question
Order these forces, weakest to strongest.
Ionic Bonds
Hydrogen Bonds
Van der Waals Forces
Covalent Bonds
Answer
-
Van der Waals Forces, Hydrogen Bonds, Ionic Bonds, Covalent Bonds
-
Covalent Bonds, Ionic Bonds, Hydrogen Bonds, Van der Waals Forces
-
Van der Waals Forces, Ionic Bonds, Hydrogen Bonds, Covalent Bonds
-
Covalent Bonds, Hydrogen Bonds, Ionic Bonds, Van der Waals Forces
Question 16
Question
Why are antidotes, antacids and laxatives unusual drugs?
Answer
-
They do not target proteins, they simply act by virtue of their physiochemical properties.
-
They target more than one type of protein.
-
They are never metabolised by the body, they stay unchanged in the liver forever.
-
They are always available as over the counter medicines.
-
They do not have to be licensed.
Question 17
Question
What is the target of an antidote?
Answer
-
Hormone
-
Ion Channel
-
Enzyme
-
Poison
Question 18
Question
Drugs that act on receptors...
Question 19
Question
Drugs that act on ion channels...
Answer
-
can block the channel.
-
can modulate the opening and closing of the channel.
-
can denature the channel.
-
can stimulate the production of many more channels than normal.
-
can break down the ion that normally uses the channel.
Question 20
Question
Drugs that act on enzymes...
Answer
-
either inhibit the enzyme or act as a false substrate.
-
block the enzymes active site.
-
denature the enzyme.
-
cause the release of neurotransmitter.
-
activate the enzyme.
Question 21
Question
Agonists are ligands. Which of these can be examples of ligands?
Answer
-
Drugs
-
Hormones
-
Neurotransmitters
-
Enzymes
-
Ion Channels
Question 22
Question
An antagonist is...
Answer
-
a drug which blocks the response to an agonist.
-
a drug that combines with a receptor to elicit a cellular response.
-
a drug that binds with an ion channel.
Question 23
Question
Receptors within a given family generally occur in several molecular varieties (subtypes). They often have similar structures but very different pharmacological responses.
Question 24
Question
All drug targets can be considered generally as...
Answer
-
receptors.
-
ion channels.
-
enzymes.
-
carriers.
Question 25
Question
Receptor subtypes are identified on the basis of selectivity of agonists and/or antagonists. What technique is used to determine this?
Answer
-
ligand binding assay
-
plaque assay
-
ELISA
-
dose/response curve
Question 26
Question
Channel linked (ionotrophic) receptors can be...
Answer
-
ligand gated
-
voltage gated
-
temperature gated
-
concentration gated
-
time centred
Question 27
Question
Ligand gated ion channels require...
Answer
-
an agonist to open the channel.
-
energy (in the form of ATP) to open the channel.
-
an antagonist to open the channel.
Question 28
Question
Voltage gated ion channels are not linked to receptors.
Question 29
Question
Which of these are true of voltage gated ion channels?
Answer
-
They are not linked to receptors.
-
They require a change in electrical charge across a membrane in order to open and close.
-
They can be blocked by antagonist drugs.
-
There are binding sites for agonist drugs.
-
They are linked to G-protein coupled receptors.
-
They require an agonist to open the channel.
Question 30
Question
How many transmembrane helices do G-Protein coupled receptors have?
Question 31
Question
What is another name for G-Protein coupled receptors?
Answer
-
Ionotrophic
-
Metabotrophic
-
Kinase
Question 32
Question
How many subunits do G-Protein coupled receptors have?
Question 33
Question
What are the subunits of a G-Protein coupled receptor?
Answer
-
alpha
-
beta
-
gamma
-
theta
-
delta
-
eta
-
zeta
-
omega
Question 34
Question
Which subunit of a G-Protein receptor alters between different receptors, giving variation?
Answer
-
Alpha
-
Beta
-
Gamma
-
Eta
-
Zeta
Question 35
Question
What do Gs receptors do?
Question 36
Question
What do Gi G-Protein receptors do?
Question 37
Question
What do Gq receptors do?
Question 38
Question
Another name for enzyme linked receptors is kinase linked receptors.
Question 39
Question
How many transmembrane domains do kinase linked receptors have?
Question 40
Question
Guanylyl cyclase-linked and cytokine are types of...
Question 41
Question
There are four main types of kinase linked receptor, these are:
receptor tyrosine kinase
serine/threonine kinase
cytokine
guanylyl cyclase - linked
Question 42
Question
The mode of action of kinase linked receptors is:
Answer
-
ligand binding ➨ dimerisation ➨ autophosphorylation
-
dimerisation ➨ ligand binding ➨ autophosphorylation
-
ligand binding ➨ autophosphorylation ➨ dimerisation
-
change in membrane potential ➨ autophosphorylation ➨ dimerisation
-
change in membrane potential ➨ dimerisation ➨ autophosphorylation
Question 43
Question
Nuclear receptors are insoluble receptors.
Question 44
Question
There are two classes of nuclear receptors. Class 1 receptors...
Answer
-
are located in the cytoplasm
-
are located in the nucleus
-
form homodimers (dimers with other receptors of the same type)
-
form heterodimers
-
have endocrine ligands (steroids/hormones)
-
have lipid (fatty acid) ligands
-
have a positive feedback effect
Question 45
Question
Nuclear receptors are harder to target with drugs because...
Question 46
Question
The binding of hormone response elements to nuclear receptors directly initiates changes in what process?
Answer
-
Gene Transcription
-
Gene Translation
-
Protein Degredation
-
Apoptosis
-
Acidosis
Question 47
Question
Drug binding to nuclear receptors has rapid and dramatic effects.
Question 48
Question
Most receptors have multiple binding sites, what are the two kinds of sites that drugs can target?
Answer
-
Orthosteric
-
Allosteric
-
Metabotrophic
-
Ionotrophic
-
Left side
-
Primary
Question 49
Question
Orthosteric binding sites...
Answer
-
house full and partial agonists, and reversible competitive antagonists.
-
bind positive and negative, non competitive antagonists.
Question 50
Question
Allosteric binding sites...
Answer
-
house full and partial agonists, and reversible competitive antagonists.
-
bind positive and negative, non competitive antagonists.
Question 51
Question
An agonist is...
Question 52
Question
Dose/response curves are similar to concentration/effect curves.
Question 53
Question
Dose/response curves are semi logarithmic. The correct set up of the graph is...
Answer
-
X axis : [log] drug dose
Y axis : % response
-
X axis : [log] agonist concentration
Y axis : measure of response
-
X axis : % response
Y axis : [log] drug dose
-
X axis : measure of response
Y axis : [log] agonist concentration
Question 54
Question
Graded relationships use Concentration/Effect curves and are used to show...
Question 55
Question
Quantal relationships use Dose/Response curves and are used to show...
Question 56
Question
Why plot a concentration effect curve?
Answer
-
you can estimate Emax
-
you can estimate EC50 and ED50
-
you can compare the efficacy and potency of different drugs
-
you can calculate Emax
-
you can calculate half life
-
you can estimate clearance
Question 57
Question
KD is a physiochemical constant and is the same for a drug/receptor combination in any species, anywhere in the universe.
Question 58
Question
KD can be used to determine an unknown receptor.
Question 59
Question
KD can be used to quantitatively compare the ___________ of different drugs on the same receptor.
Question 60
Question
The ________ the KD the greater the potency.
Question 61
Question
The lower the EC50 the ________ the potency.
Question 62
Question
Efficacy describes...
Answer
-
the ability of an agonist to activate a receptor (refers to the maximum effect an agonist can produce regardless of dose).
-
the likelihood the an agonist will bind to a receptor (refers to the maximum binding of an agonist regardless of dose).
Question 63
Question
Full agonists have...
Question 64
Question
Partial agonists have...
Question 65
Question
Antagonists are...
Question 66
Question
Pure agonists cause a cellular effect by binding to a receptor.
Question 67
Question
There three classes of antagonist. What are they?
Answer
-
chemical
-
physiological
-
pharmacological
-
enterohepatic
-
primary
-
active site
Question 68
Question
Pharmacological antagonists are also known as "receptor antagonists".
Question 69
Question
Which class of antagonists are also known as "chelating agents"?
Answer
-
chemical
-
physiological
-
pharmacological
Question 70
Question
Competitive antagonists bind to the ____________ site of a receptor.
Question 71
Question
Non competitive antagonists bind to the ___________ site of receptors.
Question 72
Question
Reversible competitive antagonists...
Answer
-
directly compete with agonists for binding at the active site.
-
block the active site permanently because they form covalent bonds with it. The receptor must be replaced before more agonist can bind.
-
reversibly bind to an allosteric site on the receptor, altering binding at the active site.
-
irreversibly bind at an allosteric site, permanently altering the active site.
Question 73
Question
Irreversible competitive antagonists...
Answer
-
reversibly bind to an allosteric site on the receptor, altering binding at the active site.
-
irreversibly bind at an allosteric site, permanently altering the active site.
-
block the active site permanently because they form covalent bonds with it. The receptor must be replaced before more agonist can bind.
-
directly compete with agonists for binding at the active site.
Question 74
Question
Non competitive reversible antagonists...
Answer
-
reversibly bind to an allosteric site on the receptor, altering binding at the active site.
-
irreversibly bind at an allosteric site, permanently altering the active site.
-
block the active site permanently because they form covalent bonds with it. The receptor must be replaced before more agonist can bind.
-
directly compete with agonists for binding at the active site.
Question 75
Question
Irreversible non competitive antagonists...
Answer
-
reversibly bind to an allosteric site on the receptor, altering binding at the active site.
-
block the active site permanently because they form covalent bonds with it. The receptor must be replaced before more agonist can bind.
-
irreversibly bind at an allosteric site, permanently altering the active site.
-
directly compete with agonists for binding at the active site.
Question 76
Question
Antagonists have no efficacy.
Question 77
Question
The effect of reversible competitive antagonists...
Answer
-
can be overcome with increased agonist concentration.
-
causes a shift to the right on the agonist response curve.
-
causes reduced maximum response on the agonist response curve.
-
reduces slope of the agonist response curve.
-
is due to covalent binding with the active site.
Question 78
Question
The effect of irreversible competitive antagonists...
Answer
-
can be overcome with increased agonist concentration.
-
causes a shift to the right on the agonist response curve.
-
causes reduced maximum response on the agonist response curve.
-
is due to covalent bonding at the active site.
-
reduces slope on the agonist response curve.
Question 79
Question
Non-competitive antagonist effects...
Answer
-
cause reduced slope of the agonist response curve.
-
cause a shift to the right of the agonist response curve.
-
cause reduced maximum response on the agonist response curve.
Question 80
Question
Water soluble molecules cross membranes easier so are more rapidly absorbed than their lipid soluble counterparts.
Question 81
Question
Uncharged molecules are absorbed easier than charged molecules.
Question 82
Question
The route of administration of a drug is determined by...
Question 83
Question
The parenteral route of administration (injected) is used for...
Answer
-
drugs that are poorly absorbed by or are unstable in the GI tract.
-
drugs that require rapid onset of action.
-
drugs that require slow onset of action.
-
for drugs that require a high level of control over dose.
Question 84
Question
Select the correct definitions:
Answer
-
bolus: all at once
-
infusion: over time
-
depot: solid/oil
-
bolus: over time
-
bolus: solid/oil
-
infusion: solid/oil
-
infusion: all at once
Question 85
Question
Sub routes of the parenteral route include...
Answer
-
intravenous
-
intramuscular
-
subcutaneous
-
submuscular
-
thyroidal
-
femural
Question 86
Question
What is the most important site of absorption in the body?
Answer
-
Stomach
-
Small Intestine
-
Large Intestine
Question 87
Question
Which of the following are properties of the small intestine that help it to absorb drugs?
Answer
-
large, highly permeable surface area
-
varies in pH along it's length
-
constant pH
-
enterocytes contain drug metabolising enzymes
-
enterocytes contain transporters in their membranes
-
tought, flat surface area
-
contains stomach acid
-
it is very short in length
Question 88
Question
The rectal route of administration is used when...
Question 89
Question
Which of these is true of the vaginal route of drug administration?
Answer
-
It bypasses first pass metabolism.
-
It bypasses 2/3 of first pass metabolism.
-
It has a rich blood supply.
-
pH can vary.
-
pH is always around 8.
Question 90
Question
Which of these is true of the transdermal route of drug administration?
Question 91
Question
Drugs given as an inhaled substance are generally intended to be distributed via the systemic circulation.
Question 92
Question
How well a drug is absorbed when it is inhaled, depends strongly on particle size.
Question 93
Question
First pass metabolism occurs in both the _________ and ___________ . It occurs when a drug is metabolised before entering the ________________ .
Answer
-
liver
-
intestine
-
systemic circulation
-
pulmonary circulation
-
heart
-
kidneys
Question 94
Question
Factors affecting absorption include:
Answer
-
Formulation of the drug
-
Charge on the drug
-
Blood flow to the site of absorption
-
Surface area of the site of absorption
-
Contact time at absorptive surface
-
Gastric emptying
-
Cost of drug
-
Kidney function
Question 95
Question
Which of the correct description of this pharmacokinetic parameter?
Cmax
Answer
-
maximum concentration of a compound after administration
-
time at which Cmax is reached
-
area under the concentration/time curve
-
measure of the extent of absorption
-
absorption rate constant
Question 96
Question
Which of the correct description of this pharmacokinetic parameter?
Tmax
Answer
-
maximum concentration of a compound after administration
-
time at which Cmax is reached
-
area under the concentration time curve (considered a measure of systemic exposure)
-
measure of the extent of absorption compared to IV
-
absorption rate constant (a measure of the speed of absorption)
Question 97
Question
Which of the correct description of this pharmacokinetic parameter?
AUC
Answer
-
maximum concentration of a compound after administration
-
time at which Cmax is reached
-
area under the concentration/time curve (considered a measure of systemic exposure)
-
measure of the extent of absorption compared to IV
-
absorption rate constant (a measure of the speed of absorption)
Question 98
Question
Which of the correct description of this pharmacokinetic parameter?
F (Bioavailability)
Answer
-
maximum concentration of a compound after administration
-
time at which Cmax is reached
-
area under the concentration/time curve (considered a measure of systemic exposure)
-
measure of extent of absorption compared to IV
-
absorption rate constant (a measure of the speed of absorption)
Question 99
Question
Which of the correct description of this pharmacokinetic parameter?
Ka
Answer
-
maximum concentration of compound after administration
-
time at which Cmax is reached
-
area under the concentration/time curve (considered a measure of systemic exposure)
-
measure of extent of absorption compared to IV
-
absorption rate constant (a measure of the speed of absorption)
Question 100
Question
What is the correct equation for calculating Bioavailability?
Question 101
Question
A drugs ability to distribute around the body depends on...
Answer
-
it's ability to cross cell membranes (based on physiochemical properties)
-
the amount of blood flow to individual tissues (perfusion)
-
the extent of its plasma protein binding
-
the site of administration
-
CYP polymorphisms
Question 102
Question
Drugs with a high molecular weight and/or high degree of binding to plasma proteins will...
Question 103
Answer
-
is produced by the liver
-
binds mostly acidic and some neutral drugs
-
concentration is decreased in malnutrition and cirrhosis
-
is normally present at around 3.5-5g/L
-
binds basic and some neutral drugs
-
is normally present at around 0.4-1.1mg/L
Question 104
Question
Alpha 1 acid glycoprotein...
Answer
-
is a plasma protein
-
is produced by the kidneys
-
is produced by the liver
-
binds basic and some neutral drugs
-
binds acidic drugs
-
is present at around 0.4-1.1mg/L
-
is present at around 3.5-5g/L
-
is an acute phase protein which elevated in some diseases such as cancer
Question 105
Question
Albumin is also known as HSA.
Question 106
Question
Only unbound (free) fraction of drug in the plasma is free to partition into cells.
Question 107
Question
What distribution parameter is being described below?
A measure of the extent of distribution.
A 'dilution factor', representing the relationship between the amount of compound in the body and the plasma concentration.
Expressed in units of volume or volume per weight e.g. L/Kg.
Many ways to calculate but basically it is equal to: total amount of drug in the body/drug blood plasma concentration.
Question 108
Question
Volatile gases are eliminated...
Question 109
Question
Water soluble compounds are...
Answer
-
often eliminated unchanged in the urine.
-
eliminated in the urine or bile after metabolism to make them more water soluble.
-
always stored in the body.
-
eliminated by exhalation.
Question 110
Question
Lipid soluble compounds...
Answer
-
typically undergo metabolism to form water soluble metabolites before elimination.
-
are eliminated unchanged.
-
are stored as starch.
-
are eliminated by a process called first pass metabolism.
Question 111
Question
The best measure of the ability of eliminating organs to remove a drug from the body is...
Question 112
Question
Clearance can be defined as...
Answer
-
the volume of plasma (or blood) cleared of the compound in a given time. (e.g. L/hr)
-
how long it takes for half of the drug to be eliminated.
-
the process by which the body metabolises a drug.
Question 113
Question
The elimination rate constant...
Question 114
Question 115
Question
Cytochrome P450 enzymes...
Answer
-
are a large superfamily of heme-cofactor containing enzymes.
-
metabolise thousands of endogenous and exogenous compounds.
-
are abbreviated to CYPs.
-
are mostly highly concentrated in the heart and lungs.
-
are found in the cytoplasm of cells.
Question 116
Question
CYPs are only found in the endoplasmic reticulum of cells.
Question 117
Question
The largest concentration of CYPs in the human body is in the liver, in hepatocytes.
Question 118
Question
In phase 1 drug metabolism...
Question 119
Question
Inhibition of CYPs causes:
Answer
-
reduced metabolism of substrate drug
-
increased metabolism of substrate drug
-
increased drug exposure
-
reduced drug exposure
-
risk of toxicity
-
risk of lacking therapeutic effect
Question 120
Question
Induction of CYPs causes:
Answer
-
increase in biosynthesis of the enzymes (due to increased gene transcription)
-
increased metabolism of substrate
-
decreased metabolism of substrate
-
increased drug exposure
-
decreased drug exposure
-
toxicity risk
-
risk of lack of therapeutic effects
Question 121
Question
If phase 1 metabolites are too lipophilic they cannot be retained in kidney tubular fluid. They must be reacted with an endogenous substrate to make them more water soluble. What is the name of this reaction?
Answer
-
Conjugation
-
Acid/Base
-
Esterification
-
Elimination
Question 122
Question
If phase 1 metabolites are too lipophilic they cannot be retained in kidney tubular fluid. They must be reacted with an endogenous substrate to make them more water soluble. Which of these are examples of those endogenous substrates?
Answer
-
sulphuric acid
-
amino acids
-
glucuronic acid