2634040
Descripción
Test por offersforalice, actualizado hace más de 1 año
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Creado por offersforalice
hace alrededor de 9 años
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Pregunta 1
Pregunta
What is pharmacodynamics?
Respuesta
-
The effects of a drug on the body.
-
What the body does to a drug.
Pregunta 2
Pregunta
What is pharmacokinetics?
Respuesta
-
The effects of a drug on the body.
-
What the body does to a drug.
Pregunta 3
Pregunta
Pharmacodynamics allows us to...
Respuesta
-
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.
Pregunta 4
Pregunta
What does ADME stand for?
Respuesta
-
Administration
-
Affect
-
Absorption
-
Distribution
-
Dissolving
-
Metabolism
-
Modification
-
Excretion
-
Editing
Pregunta 5
Pregunta
Absorption is...
Respuesta
-
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.
Pregunta 6
Pregunta
Distribution is...
Respuesta
-
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.
Pregunta 7
Pregunta
Metabolism is...
Respuesta
-
how the body inactivates the drug.
-
enzymatic modification.
-
how the drug travels through the body.
-
how the drug passes cell walls.
Pregunta 8
Pregunta
Excretion is...
Respuesta
-
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.
Pregunta 9
Pregunta
From what sources can we create drugs?
Respuesta
-
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.
Pregunta 10
Pregunta
How many types of proteins act as drug targets?
Respuesta
-
1
-
2
-
3
-
4
-
5
Pregunta 11
Pregunta
What are the four types of proteins that can act as drug targets?
Respuesta
-
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.
Pregunta 12
Pregunta
Drug interaction with the target is determined by two factors. What are they?
Respuesta
-
Shape
-
Charge Distribution
-
Colour
-
Name
-
Time
Pregunta 13
Pregunta
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.
Respuesta
-
Shape
-
Charge
-
Colour
-
Mass
Pregunta 14
Pregunta
This determines the strength of associations between the drug and it's target, because it determines the bonds that the drug can make.
Respuesta
-
Charge Distribution
-
Shape
-
Colour
-
Mass
Pregunta 15
Pregunta
Order these forces, weakest to strongest.
Ionic Bonds
Hydrogen Bonds
Van der Waals Forces
Covalent Bonds
Respuesta
-
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
Pregunta 16
Pregunta
Why are antidotes, antacids and laxatives unusual drugs?
Respuesta
-
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.
Pregunta 17
Pregunta
What is the target of an antidote?
Respuesta
-
Hormone
-
Ion Channel
-
Enzyme
-
Poison
Pregunta 18
Pregunta
Drugs that act on receptors...
Respuesta
-
always activate the receptor.
-
either activate the receptor or stop something else from activating it.
-
block the receptor.
-
denature the receptor.
Pregunta 19
Pregunta
Drugs that act on ion channels...
Respuesta
-
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.
Pregunta 20
Pregunta
Drugs that act on enzymes...
Respuesta
-
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.
Pregunta 21
Pregunta
Agonists are ligands. Which of these can be examples of ligands?
Respuesta
-
Drugs
-
Hormones
-
Neurotransmitters
-
Enzymes
-
Ion Channels
Pregunta 22
Pregunta
An antagonist is...
Respuesta
-
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.
Pregunta 23
Pregunta
Receptors within a given family generally occur in several molecular varieties (subtypes). They often have similar structures but very different pharmacological responses.
Respuesta
- True
- False
Pregunta 24
Pregunta
All drug targets can be considered generally as...
Respuesta
-
receptors.
-
ion channels.
-
enzymes.
-
carriers.
Pregunta 25
Pregunta
Receptor subtypes are identified on the basis of selectivity of agonists and/or antagonists. What technique is used to determine this?
Respuesta
-
ligand binding assay
-
plaque assay
-
ELISA
-
dose/response curve
Pregunta 26
Pregunta
Channel linked (ionotrophic) receptors can be...
Respuesta
-
ligand gated
-
voltage gated
-
temperature gated
-
concentration gated
-
time centred
Pregunta 27
Pregunta
Ligand gated ion channels require...
Respuesta
-
an agonist to open the channel.
-
energy (in the form of ATP) to open the channel.
-
an antagonist to open the channel.
Pregunta 28
Pregunta
Voltage gated ion channels are not linked to receptors.
Respuesta
- True
- False
Pregunta 29
Pregunta
Which of these are true of voltage gated ion channels?
Respuesta
-
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.
Pregunta 30
Pregunta
How many transmembrane helices do G-Protein coupled receptors have?
Respuesta
-
1
-
3
-
5
-
7
-
9
Pregunta 31
Pregunta
What is another name for G-Protein coupled receptors?
Respuesta
-
Ionotrophic
-
Metabotrophic
-
Kinase
Pregunta 32
Pregunta
How many subunits do G-Protein coupled receptors have?
Respuesta
-
1
-
3
-
5
-
7
-
9
Pregunta 33
Pregunta
What are the subunits of a G-Protein coupled receptor?
Respuesta
-
alpha
-
beta
-
gamma
-
theta
-
delta
-
eta
-
zeta
-
omega
Pregunta 34
Pregunta
Which subunit of a G-Protein receptor alters between different receptors, giving variation?
Respuesta
-
Alpha
-
Beta
-
Gamma
-
Eta
-
Zeta
Pregunta 35
Pregunta
What do Gs receptors do?
Respuesta
-
activate adenyl cyclase and Ca2+ channels
-
inhibit adenyl cyclase and activate K+ channels
-
activate phospholipase C
Pregunta 36
Pregunta
What do Gi G-Protein receptors do?
Respuesta
-
activate adenyl cyclase and Ca2+ channels
-
inhibit adenyl cyclase and activate K+ channels
-
activate phospholipase C
Pregunta 37
Pregunta
What do Gq receptors do?
Respuesta
-
activate adenyl cyclase and Ca2+ channels
-
inhibit adenyl cyclase and activate K+ channels
-
activate phospholipase C
Pregunta 38
Pregunta
Another name for enzyme linked receptors is kinase linked receptors.
Respuesta
- True
- False
Pregunta 39
Pregunta
How many transmembrane domains do kinase linked receptors have?
Respuesta
-
1
-
3
-
5
-
7
-
9
Pregunta 40
Pregunta
Guanylyl cyclase-linked and cytokine are types of...
Respuesta
-
G-Protein linked receptor
-
Kinase linked receptor
-
Ion channel
Pregunta 41
Pregunta
There are four main types of kinase linked receptor, these are:
receptor tyrosine kinase
serine/threonine kinase
cytokine
guanylyl cyclase - linked
Respuesta
- True
- False
Pregunta 42
Pregunta
The mode of action of kinase linked receptors is:
Respuesta
-
ligand binding ➨ dimerisation ➨ autophosphorylation
-
dimerisation ➨ ligand binding ➨ autophosphorylation
-
ligand binding ➨ autophosphorylation ➨ dimerisation
-
change in membrane potential ➨ autophosphorylation ➨ dimerisation
-
change in membrane potential ➨ dimerisation ➨ autophosphorylation
Pregunta 43
Pregunta
Nuclear receptors are insoluble receptors.
Respuesta
- True
- False
Pregunta 44
Pregunta
There are two classes of nuclear receptors. Class 1 receptors...
Respuesta
-
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
Pregunta 45
Pregunta
Nuclear receptors are harder to target with drugs because...
Respuesta
-
they are intracellular.
-
they are extracellular.
-
they require ATP to be activated.
-
they are millions of different types of them.
Pregunta 46
Pregunta
The binding of hormone response elements to nuclear receptors directly initiates changes in what process?
Respuesta
-
Gene Transcription
-
Gene Translation
-
Protein Degredation
-
Apoptosis
-
Acidosis
Pregunta 47
Pregunta
Drug binding to nuclear receptors has rapid and dramatic effects.
Respuesta
- True
- False
Pregunta 48
Pregunta
Most receptors have multiple binding sites, what are the two kinds of sites that drugs can target?
Respuesta
-
Orthosteric
-
Allosteric
-
Metabotrophic
-
Ionotrophic
-
Left side
-
Primary
Pregunta 49
Pregunta
Orthosteric binding sites...
Respuesta
-
house full and partial agonists, and reversible competitive antagonists.
-
bind positive and negative, non competitive antagonists.
Pregunta 50
Pregunta
Allosteric binding sites...
Respuesta
-
house full and partial agonists, and reversible competitive antagonists.
-
bind positive and negative, non competitive antagonists.
Pregunta 51
Pregunta
An agonist is...
Respuesta
-
a ligand that combines with receptors to elicit a cellular response.
-
a ligand that served to block the effect of other ligands which combine with receptors to elicit a cellular response.
Pregunta 52
Pregunta
Dose/response curves are similar to concentration/effect curves.
Respuesta
- True
- False
Pregunta 53
Pregunta
Dose/response curves are semi logarithmic. The correct set up of the graph is...
Respuesta
-
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
Pregunta 54
Pregunta
Graded relationships use Concentration/Effect curves and are used to show...
Respuesta
-
the response of a particular system to a drug at varying concentrations.
-
the drug dose required to produce a specified response in each member of a population.
Pregunta 55
Pregunta
Quantal relationships use Dose/Response curves and are used to show...
Respuesta
-
the drug dose required to produce a specified response in each member of a population.
-
the response of a particular system to varying concentrations of an agonist.
Pregunta 56
Pregunta
Why plot a concentration effect curve?
Respuesta
-
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
Pregunta 57
Pregunta
KD is a physiochemical constant and is the same for a drug/receptor combination in any species, anywhere in the universe.
Respuesta
- True
- False
Pregunta 58
Pregunta
KD can be used to determine an unknown receptor.
Respuesta
- True
- False
Pregunta 59
Pregunta
KD can be used to quantitatively compare the ___________ of different drugs on the same receptor.
Respuesta
-
affinity
-
efficacy
Pregunta 60
Pregunta
The ________ the KD the greater the potency.
Respuesta
-
lower
-
higher
Pregunta 61
Pregunta
The lower the EC50 the ________ the potency.
Respuesta
-
greater
-
lower
Pregunta 62
Pregunta
Efficacy describes...
Respuesta
-
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).
Pregunta 63
Pregunta
Full agonists have...
Respuesta
-
high efficacy (AR* is very likely)
-
low efficacy (AR* is unlikely)
Pregunta 64
Pregunta
Partial agonists have...
Respuesta
-
low efficacy (AR* is less likely).
-
high efficacy (AR* is very likely)
Pregunta 65
Pregunta
Antagonists are...
Respuesta
-
drugs which block the response to an agonist.
-
the same as agonists.
-
endogenous molecules like hormones and neurotransmitters.
Pregunta 66
Pregunta
Pure agonists cause a cellular effect by binding to a receptor.
Respuesta
- True
- False
Pregunta 67
Pregunta
There three classes of antagonist. What are they?
Respuesta
-
chemical
-
physiological
-
pharmacological
-
enterohepatic
-
primary
-
active site
Pregunta 68
Pregunta
Pharmacological antagonists are also known as "receptor antagonists".
Respuesta
- True
- False
Pregunta 69
Pregunta
Which class of antagonists are also known as "chelating agents"?
Respuesta
-
chemical
-
physiological
-
pharmacological
Pregunta 70
Pregunta
Competitive antagonists bind to the ____________ site of a receptor.
Respuesta
-
active
-
allosteric
Pregunta 71
Pregunta
Non competitive antagonists bind to the ___________ site of receptors.
Respuesta
-
allosteric
-
active
Pregunta 72
Pregunta
Reversible competitive antagonists...
Respuesta
-
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.
Pregunta 73
Pregunta
Irreversible competitive antagonists...
Respuesta
-
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.
Pregunta 74
Pregunta
Non competitive reversible antagonists...
Respuesta
-
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.
Pregunta 75
Pregunta
Irreversible non competitive antagonists...
Respuesta
-
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.
Pregunta 76
Pregunta
Antagonists have no efficacy.
Respuesta
- True
- False
Pregunta 77
Pregunta
The effect of reversible competitive antagonists...
Respuesta
-
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.
Pregunta 78
Pregunta
The effect of irreversible competitive antagonists...
Respuesta
-
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.
Pregunta 79
Pregunta
Non-competitive antagonist effects...
Respuesta
-
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.
Pregunta 80
Pregunta
Water soluble molecules cross membranes easier so are more rapidly absorbed than their lipid soluble counterparts.
Respuesta
- True
- False
Pregunta 81
Pregunta
Uncharged molecules are absorbed easier than charged molecules.
Respuesta
- True
- False
Pregunta 82
Pregunta
The route of administration of a drug is determined by...
Respuesta
-
physiochemical/pharmacokinetic properties of the drug
-
therapeutic objectives
-
patient preference
Pregunta 83
Pregunta
The parenteral route of administration (injected) is used for...
Respuesta
-
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.
Pregunta 84
Pregunta
Select the correct definitions:
Respuesta
-
bolus: all at once
-
infusion: over time
-
depot: solid/oil
-
bolus: over time
-
bolus: solid/oil
-
infusion: solid/oil
-
infusion: all at once
Pregunta 85
Pregunta
Sub routes of the parenteral route include...
Respuesta
-
intravenous
-
intramuscular
-
subcutaneous
-
submuscular
-
thyroidal
-
femural
Pregunta 86
Pregunta
What is the most important site of absorption in the body?
Respuesta
-
Stomach
-
Small Intestine
-
Large Intestine
Pregunta 87
Pregunta
Which of the following are properties of the small intestine that help it to absorb drugs?
Respuesta
-
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
Pregunta 88
Pregunta
The rectal route of administration is used when...
Respuesta
-
the drug causes vomiting
-
the patient is vomiting
-
the drug is excreted in the urine
-
the patient has a low blood count
Pregunta 89
Pregunta
Which of these is true of the vaginal route of drug administration?
Respuesta
-
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.
Pregunta 90
Pregunta
Which of these is true of the transdermal route of drug administration?
Respuesta
-
It has very slow absorption giving a continuous slow release of drug.
-
It has very fast local absorption giving a rapid release of the drug to a small area.
Pregunta 91
Pregunta
Drugs given as an inhaled substance are generally intended to be distributed via the systemic circulation.
Respuesta
- True
- False
Pregunta 92
Pregunta
How well a drug is absorbed when it is inhaled, depends strongly on particle size.
Respuesta
- True
- False
Pregunta 93
Pregunta
First pass metabolism occurs in both the _________ and ___________ . It occurs when a drug is metabolised before entering the ________________ .
Respuesta
-
liver
-
intestine
-
systemic circulation
-
pulmonary circulation
-
heart
-
kidneys
Pregunta 94
Pregunta
Factors affecting absorption include:
Respuesta
-
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
Pregunta 95
Pregunta
Which of the correct description of this pharmacokinetic parameter?
Cmax
Respuesta
-
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
Pregunta 96
Pregunta
Which of the correct description of this pharmacokinetic parameter?
Tmax
Respuesta
-
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)
Pregunta 97
Pregunta
Which of the correct description of this pharmacokinetic parameter?
AUC
Respuesta
-
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)
Pregunta 98
Pregunta
Which of the correct description of this pharmacokinetic parameter?
F (Bioavailability)
Respuesta
-
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)
Pregunta 99
Pregunta
Which of the correct description of this pharmacokinetic parameter?
Ka
Respuesta
-
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)
Pregunta 100
Pregunta
What is the correct equation for calculating Bioavailability?
Respuesta
-
F = (AUC oral/AUC IV) x (dose IV/dose oral)
-
F = (AUC IV/AUC oral) x (dose oral/dose IV)
Pregunta 101
Pregunta
A drugs ability to distribute around the body depends on...
Respuesta
-
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
Pregunta 102
Pregunta
Drugs with a high molecular weight and/or high degree of binding to plasma proteins will...
Respuesta
-
distribute quickly into tissues and organs.
-
tend to stay in the systemic circulation rather than distribute into tissues and organs.
Pregunta 103
Pregunta
Albumin...
Respuesta
-
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
Pregunta 104
Pregunta
Alpha 1 acid glycoprotein...
Respuesta
-
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
Pregunta 105
Pregunta
Albumin is also known as HSA.
Respuesta
- True
- False
Pregunta 106
Pregunta
Only unbound (free) fraction of drug in the plasma is free to partition into cells.
Respuesta
- True
- False
Pregunta 107
Pregunta
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.
Respuesta
-
Volume of Distribution (VD)
-
Clearance (CL)
-
Cmax
-
Tmax
-
AUC
-
F
Pregunta 108
Pregunta
Volatile gases are eliminated...
Respuesta
-
by exhalation
-
in the urine
-
in faeces
-
after metabolism forming water soluble metabolites
Pregunta 109
Pregunta
Water soluble compounds are...
Respuesta
-
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.
Pregunta 110
Pregunta
Lipid soluble compounds...
Respuesta
-
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.
Pregunta 111
Pregunta
The best measure of the ability of eliminating organs to remove a drug from the body is...
Respuesta
-
Clearance (CL)
-
Elimination Rate Constant (Ke)
-
Half-life
Pregunta 112
Pregunta
Clearance can be defined as...
Respuesta
-
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.
Pregunta 113
Pregunta
The elimination rate constant...
Respuesta
-
is known as Ke.
-
is the slope of the logged concentration-time graph.
-
has units of 1/time.
-
is linked to Ka.
-
is not relevant in humans.
Pregunta 114
Pregunta
Half-life is...
Respuesta
-
the time it takes for the concentration of active drug to reach half its current value.
-
half the time taken for all of the drug to be eliminated.
Pregunta 115
Pregunta
Cytochrome P450 enzymes...
Respuesta
-
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.
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are found in the cytoplasm of cells.
Pregunta 116
Pregunta
CYPs are only found in the endoplasmic reticulum of cells.
Respuesta
- True
- False
Pregunta 117
Pregunta
The largest concentration of CYPs in the human body is in the liver, in hepatocytes.
Respuesta
- True
- False
Pregunta 118
Pregunta
In phase 1 drug metabolism...
Respuesta
-
CYPs add a reactive functional group (e.g. -OH) to the active drug compound.
-
CYPs cleave active drug compounds to make them unreactive.
-
CYPs are not involved.
Pregunta 119
Pregunta
Inhibition of CYPs causes:
Respuesta
-
reduced metabolism of substrate drug
-
increased metabolism of substrate drug
-
increased drug exposure
-
reduced drug exposure
-
risk of toxicity
-
risk of lacking therapeutic effect
Pregunta 120
Pregunta
Induction of CYPs causes:
Respuesta
-
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
Pregunta 121
Pregunta
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?
Respuesta
-
Conjugation
-
Acid/Base
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Esterification
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Elimination
Pregunta 122
Pregunta
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?
Respuesta
-
sulphuric acid
-
amino acids
-
glucuronic acid
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