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Quiz am Phamacodynamics and Pharmacokinetics, erstellt von offersforalice am 01/05/2015.

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Phamacodynamics and Pharmacokinetics

Frage 1 von 122

1

What is pharmacodynamics?

Wähle eine der folgenden:

  • The effects of a drug on the body.

  • What the body does to a drug.

Erklärung

Frage 2 von 122

1

What is pharmacokinetics?

Wähle eine der folgenden:

  • The effects of a drug on the body.

  • What the body does to a drug.

Erklärung

Frage 3 von 122

1

Pharmacodynamics allows us to...

Wähle eine der folgenden:

  • 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.

Erklärung

Frage 4 von 122

1

What does ADME stand for?

Wähle eine oder mehr der folgenden:

  • Administration

  • Affect

  • Absorption

  • Distribution

  • Dissolving

  • Metabolism

  • Modification

  • Excretion

  • Editing

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Frage 5 von 122

1

Absorption is...

Wähle eine der folgenden:

  • 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.

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Frage 6 von 122

1

Distribution is...

Wähle eine der folgenden:

  • 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.

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Frage 7 von 122

1

Metabolism is...

Wähle eine oder mehr der folgenden:

  • how the body inactivates the drug.

  • enzymatic modification.

  • how the drug travels through the body.

  • how the drug passes cell walls.

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Frage 8 von 122

1

Excretion is...

Wähle eine der folgenden:

  • 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.

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Frage 9 von 122

1

From what sources can we create drugs?

Wähle eine oder mehr der folgenden:

  • 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.

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Frage 10 von 122

1

How many types of proteins act as drug targets?

Wähle eine der folgenden:

  • 1

  • 2

  • 3

  • 4

  • 5

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Frage 11 von 122

1

What are the four types of proteins that can act as drug targets?

Wähle eine der folgenden:

  • 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.

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Frage 12 von 122

1

Drug interaction with the target is determined by two factors. What are they?

Wähle eine oder mehr der folgenden:

  • Shape

  • Charge Distribution

  • Colour

  • Name

  • Time

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Frage 13 von 122

1

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.

Wähle eine der folgenden:

  • Shape

  • Charge

  • Colour

  • Mass

Erklärung

Frage 14 von 122

1

This determines the strength of associations between the drug and it's target, because it determines the bonds that the drug can make.

Wähle eine der folgenden:

  • Charge Distribution

  • Shape

  • Colour

  • Mass

Erklärung

Frage 15 von 122

1

Order these forces, weakest to strongest.

Ionic Bonds
Hydrogen Bonds
Van der Waals Forces
Covalent Bonds

Wähle eine der folgenden:

  • 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

Erklärung

Frage 16 von 122

1

Why are antidotes, antacids and laxatives unusual drugs?

Wähle eine der folgenden:

  • 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.

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Frage 17 von 122

1

What is the target of an antidote?

Wähle eine der folgenden:

  • Hormone

  • Ion Channel

  • Enzyme

  • Poison

Erklärung

Frage 18 von 122

1

Drugs that act on receptors...

Wähle eine der folgenden:

  • always activate the receptor.

  • either activate the receptor or stop something else from activating it.

  • block the receptor.

  • denature the receptor.

Erklärung

Frage 19 von 122

1

Drugs that act on ion channels...

Wähle eine oder mehr der folgenden:

  • 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.

Erklärung

Frage 20 von 122

1

Drugs that act on enzymes...

Wähle eine der folgenden:

  • 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.

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Frage 21 von 122

1

Agonists are ligands. Which of these can be examples of ligands?

Wähle eine oder mehr der folgenden:

  • Drugs

  • Hormones

  • Neurotransmitters

  • Enzymes

  • Ion Channels

Erklärung

Frage 22 von 122

1

An antagonist is...

Wähle eine der folgenden:

  • 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.

Erklärung

Frage 23 von 122

1

Receptors within a given family generally occur in several molecular varieties (subtypes). They often have similar structures but very different pharmacological responses.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 24 von 122

1

All drug targets can be considered generally as...

Wähle eine der folgenden:

  • receptors.

  • ion channels.

  • enzymes.

  • carriers.

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Frage 25 von 122

1

Receptor subtypes are identified on the basis of selectivity of agonists and/or antagonists. What technique is used to determine this?

Wähle eine der folgenden:

  • ligand binding assay

  • plaque assay

  • ELISA

  • dose/response curve

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Frage 26 von 122

1

Channel linked (ionotrophic) receptors can be...

Wähle eine oder mehr der folgenden:

  • ligand gated

  • voltage gated

  • temperature gated

  • concentration gated

  • time centred

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Frage 27 von 122

1

Ligand gated ion channels require...

Wähle eine der folgenden:

  • an agonist to open the channel.

  • energy (in the form of ATP) to open the channel.

  • an antagonist to open the channel.

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Frage 28 von 122

1

Voltage gated ion channels are not linked to receptors.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 29 von 122

1

Which of these are true of voltage gated ion channels?

Wähle eine oder mehr der folgenden:

  • 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.

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Frage 30 von 122

1

How many transmembrane helices do G-Protein coupled receptors have?

Wähle eine der folgenden:

  • 1

  • 3

  • 5

  • 7

  • 9

Erklärung

Frage 31 von 122

1

What is another name for G-Protein coupled receptors?

Wähle eine der folgenden:

  • Ionotrophic

  • Metabotrophic

  • Kinase

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Frage 32 von 122

1

How many subunits do G-Protein coupled receptors have?

Wähle eine der folgenden:

  • 1

  • 3

  • 5

  • 7

  • 9

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Frage 33 von 122

1

What are the subunits of a G-Protein coupled receptor?

Wähle eine oder mehr der folgenden:

  • alpha

  • beta

  • gamma

  • theta

  • delta

  • eta

  • zeta

  • omega

Erklärung

Frage 34 von 122

1

Which subunit of a G-Protein receptor alters between different receptors, giving variation?

Wähle eine der folgenden:

  • Alpha

  • Beta

  • Gamma

  • Eta

  • Zeta

Erklärung

Frage 35 von 122

1

What do Gs receptors do?

Wähle eine der folgenden:

  • activate adenyl cyclase and Ca2+ channels

  • inhibit adenyl cyclase and activate K+ channels

  • activate phospholipase C

Erklärung

Frage 36 von 122

1

What do Gi G-Protein receptors do?

Wähle eine der folgenden:

  • activate adenyl cyclase and Ca2+ channels

  • inhibit adenyl cyclase and activate K+ channels

  • activate phospholipase C

Erklärung

Frage 37 von 122

1

What do Gq receptors do?

Wähle eine der folgenden:

  • activate adenyl cyclase and Ca2+ channels

  • inhibit adenyl cyclase and activate K+ channels

  • activate phospholipase C

Erklärung

Frage 38 von 122

1

Another name for enzyme linked receptors is kinase linked receptors.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

Erklärung

Frage 39 von 122

1

How many transmembrane domains do kinase linked receptors have?

Wähle eine der folgenden:

  • 1

  • 3

  • 5

  • 7

  • 9

Erklärung

Frage 40 von 122

1

Guanylyl cyclase-linked and cytokine are types of...

Wähle eine der folgenden:

  • G-Protein linked receptor

  • Kinase linked receptor

  • Ion channel

Erklärung

Frage 41 von 122

1

There are four main types of kinase linked receptor, these are:
receptor tyrosine kinase
serine/threonine kinase
cytokine
guanylyl cyclase - linked

Wähle eins der folgenden:

  • WAHR
  • FALSCH

Erklärung

Frage 42 von 122

1

The mode of action of kinase linked receptors is:

Wähle eine der folgenden:

  • ligand binding ➨ dimerisation ➨ autophosphorylation

  • dimerisation ➨ ligand binding ➨ autophosphorylation

  • ligand binding ➨ autophosphorylation ➨ dimerisation

  • change in membrane potential ➨ autophosphorylation ➨ dimerisation

  • change in membrane potential ➨ dimerisation ➨ autophosphorylation

Erklärung

Frage 43 von 122

1

Nuclear receptors are insoluble receptors.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 44 von 122

1

There are two classes of nuclear receptors. Class 1 receptors...

Wähle eine oder mehr der folgenden:

  • 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

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Frage 45 von 122

1

Nuclear receptors are harder to target with drugs because...

Wähle eine der folgenden:

  • they are intracellular.

  • they are extracellular.

  • they require ATP to be activated.

  • they are millions of different types of them.

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Frage 46 von 122

1

The binding of hormone response elements to nuclear receptors directly initiates changes in what process?

Wähle eine der folgenden:

  • Gene Transcription

  • Gene Translation

  • Protein Degredation

  • Apoptosis

  • Acidosis

Erklärung

Frage 47 von 122

1

Drug binding to nuclear receptors has rapid and dramatic effects.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

Erklärung

Frage 48 von 122

1

Most receptors have multiple binding sites, what are the two kinds of sites that drugs can target?

Wähle eine oder mehr der folgenden:

  • Orthosteric

  • Allosteric

  • Metabotrophic

  • Ionotrophic

  • Left side

  • Primary

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Frage 49 von 122

1

Orthosteric binding sites...

Wähle eine der folgenden:

  • house full and partial agonists, and reversible competitive antagonists.

  • bind positive and negative, non competitive antagonists.

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Frage 50 von 122

1

Allosteric binding sites...

Wähle eine der folgenden:

  • house full and partial agonists, and reversible competitive antagonists.

  • bind positive and negative, non competitive antagonists.

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Frage 51 von 122

1

An agonist is...

Wähle eine der folgenden:

  • 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.

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Frage 52 von 122

1

Dose/response curves are similar to concentration/effect curves.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

Erklärung

Frage 53 von 122

1

Dose/response curves are semi logarithmic. The correct set up of the graph is...

Wähle eine der folgenden:

  • 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

Erklärung

Frage 54 von 122

1

Graded relationships use Concentration/Effect curves and are used to show...

Wähle eine der folgenden:

  • 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.

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Frage 55 von 122

1

Quantal relationships use Dose/Response curves and are used to show...

Wähle eine der folgenden:

  • 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.

Erklärung

Frage 56 von 122

1

Why plot a concentration effect curve?

Wähle eine oder mehr der folgenden:

  • 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

Erklärung

Frage 57 von 122

1

KD is a physiochemical constant and is the same for a drug/receptor combination in any species, anywhere in the universe.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 58 von 122

1

KD can be used to determine an unknown receptor.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 59 von 122

1

KD can be used to quantitatively compare the ___________ of different drugs on the same receptor.

Wähle eine der folgenden:

  • affinity

  • efficacy

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Frage 60 von 122

1

The ________ the KD the greater the potency.

Wähle eine der folgenden:

  • lower

  • higher

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Frage 61 von 122

1

The lower the EC50 the ________ the potency.

Wähle eine der folgenden:

  • greater

  • lower

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Frage 62 von 122

1

Efficacy describes...

Wähle eine der folgenden:

  • 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).

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Frage 63 von 122

1

Full agonists have...

Wähle eine der folgenden:

  • high efficacy (AR* is very likely)

  • low efficacy (AR* is unlikely)

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Frage 64 von 122

1

Partial agonists have...

Wähle eine der folgenden:

  • low efficacy (AR* is less likely).

  • high efficacy (AR* is very likely)

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Frage 65 von 122

1

Antagonists are...

Wähle eine der folgenden:

  • drugs which block the response to an agonist.

  • the same as agonists.

  • endogenous molecules like hormones and neurotransmitters.

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Frage 66 von 122

1

Pure agonists cause a cellular effect by binding to a receptor.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 67 von 122

1

There three classes of antagonist. What are they?

Wähle eine oder mehr der folgenden:

  • chemical

  • physiological

  • pharmacological

  • enterohepatic

  • primary

  • active site

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Frage 68 von 122

1

Pharmacological antagonists are also known as "receptor antagonists".

Wähle eins der folgenden:

  • WAHR
  • FALSCH

Erklärung

Frage 69 von 122

1

Which class of antagonists are also known as "chelating agents"?

Wähle eine der folgenden:

  • chemical

  • physiological

  • pharmacological

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Frage 70 von 122

1

Competitive antagonists bind to the ____________ site of a receptor.

Wähle eine der folgenden:

  • active

  • allosteric

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Frage 71 von 122

1

Non competitive antagonists bind to the ___________ site of receptors.

Wähle eine der folgenden:

  • allosteric

  • active

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Frage 72 von 122

1

Reversible competitive antagonists...

Wähle eine der folgenden:

  • 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.

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Frage 73 von 122

1

Irreversible competitive antagonists...

Wähle eine der folgenden:

  • 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.

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Frage 74 von 122

1

Non competitive reversible antagonists...

Wähle eine der folgenden:

  • 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.

Erklärung

Frage 75 von 122

1

Irreversible non competitive antagonists...

Wähle eine der folgenden:

  • 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.

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Frage 76 von 122

1

Antagonists have no efficacy.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 77 von 122

1

The effect of reversible competitive antagonists...

Wähle eine oder mehr der folgenden:

  • 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.

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Frage 78 von 122

1

The effect of irreversible competitive antagonists...

Wähle eine oder mehr der folgenden:

  • 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.

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Frage 79 von 122

1

Non-competitive antagonist effects...

Wähle eine oder mehr der folgenden:

  • 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.

Erklärung

Frage 80 von 122

1

Water soluble molecules cross membranes easier so are more rapidly absorbed than their lipid soluble counterparts.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 81 von 122

1

Uncharged molecules are absorbed easier than charged molecules.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

Erklärung

Frage 82 von 122

1

The route of administration of a drug is determined by...

Wähle eine oder mehr der folgenden:

  • physiochemical/pharmacokinetic properties of the drug

  • therapeutic objectives

  • patient preference

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Frage 83 von 122

1

The parenteral route of administration (injected) is used for...

Wähle eine oder mehr der folgenden:

  • 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.

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Frage 84 von 122

1

Select the correct definitions:

Wähle eine oder mehr der folgenden:

  • bolus: all at once

  • infusion: over time

  • depot: solid/oil

  • bolus: over time

  • bolus: solid/oil

  • infusion: solid/oil

  • infusion: all at once

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Frage 85 von 122

1

Sub routes of the parenteral route include...

Wähle eine oder mehr der folgenden:

  • intravenous

  • intramuscular

  • subcutaneous

  • submuscular

  • thyroidal

  • femural

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Frage 86 von 122

1

What is the most important site of absorption in the body?

Wähle eine der folgenden:

  • Stomach

  • Small Intestine

  • Large Intestine

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Frage 87 von 122

1

Which of the following are properties of the small intestine that help it to absorb drugs?

Wähle eine oder mehr der folgenden:

  • 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

Erklärung

Frage 88 von 122

1

The rectal route of administration is used when...

Wähle eine oder mehr der folgenden:

  • the drug causes vomiting

  • the patient is vomiting

  • the drug is excreted in the urine

  • the patient has a low blood count

Erklärung

Frage 89 von 122

1

Which of these is true of the vaginal route of drug administration?

Wähle eine oder mehr der folgenden:

  • 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.

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Frage 90 von 122

1

Which of these is true of the transdermal route of drug administration?

Wähle eine oder mehr der folgenden:

  • 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.

Erklärung

Frage 91 von 122

1

Drugs given as an inhaled substance are generally intended to be distributed via the systemic circulation.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

Erklärung

Frage 92 von 122

1

How well a drug is absorbed when it is inhaled, depends strongly on particle size.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

Erklärung

Frage 93 von 122

1

First pass metabolism occurs in both the _________ and ___________ . It occurs when a drug is metabolised before entering the ________________ .

Wähle eine oder mehr der folgenden:

  • liver

  • intestine

  • systemic circulation

  • pulmonary circulation

  • heart

  • kidneys

Erklärung

Frage 94 von 122

1

Factors affecting absorption include:

Wähle eine oder mehr der folgenden:

  • 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

Erklärung

Frage 95 von 122

1

Which of the correct description of this pharmacokinetic parameter?

Cmax

Wähle eine der folgenden:

  • 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

Erklärung

Frage 96 von 122

1

Which of the correct description of this pharmacokinetic parameter?

Tmax

Wähle eine der folgenden:

  • 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)

Erklärung

Frage 97 von 122

1

Which of the correct description of this pharmacokinetic parameter?

AUC

Wähle eine der folgenden:

  • 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)

Erklärung

Frage 98 von 122

1

Which of the correct description of this pharmacokinetic parameter?

F (Bioavailability)

Wähle eine der folgenden:

  • 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)

Erklärung

Frage 99 von 122

1

Which of the correct description of this pharmacokinetic parameter?

Ka

Wähle eine der folgenden:

  • 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)

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Frage 100 von 122

1

What is the correct equation for calculating Bioavailability?

Wähle eine der folgenden:

  • F = (AUC oral/AUC IV) x (dose IV/dose oral)

  • F = (AUC IV/AUC oral) x (dose oral/dose IV)

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Frage 101 von 122

1

A drugs ability to distribute around the body depends on...

Wähle eine oder mehr der folgenden:

  • 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

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Frage 102 von 122

1

Drugs with a high molecular weight and/or high degree of binding to plasma proteins will...

Wähle eine der folgenden:

  • distribute quickly into tissues and organs.

  • tend to stay in the systemic circulation rather than distribute into tissues and organs.

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Frage 103 von 122

1

Albumin...

Wähle eine oder mehr der folgenden:

  • 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

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Frage 104 von 122

1

Alpha 1 acid glycoprotein...

Wähle eine oder mehr der folgenden:

  • 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

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Frage 105 von 122

1

Albumin is also known as HSA.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 106 von 122

1

Only unbound (free) fraction of drug in the plasma is free to partition into cells.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 107 von 122

1

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.

Wähle eine der folgenden:

  • Volume of Distribution (VD)

  • Clearance (CL)

  • Cmax

  • Tmax

  • AUC

  • F

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Frage 108 von 122

1

Volatile gases are eliminated...

Wähle eine der folgenden:

  • by exhalation

  • in the urine

  • in faeces

  • after metabolism forming water soluble metabolites

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Frage 109 von 122

1

Water soluble compounds are...

Wähle eine der folgenden:

  • 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.

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Frage 110 von 122

1

Lipid soluble compounds...

Wähle eine der folgenden:

  • 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.

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Frage 111 von 122

1

The best measure of the ability of eliminating organs to remove a drug from the body is...

Wähle eine der folgenden:

  • Clearance (CL)

  • Elimination Rate Constant (Ke)

  • Half-life

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Frage 112 von 122

1

Clearance can be defined as...

Wähle eine der folgenden:

  • 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.

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Frage 113 von 122

1

The elimination rate constant...

Wähle eine oder mehr der folgenden:

  • 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.

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Frage 114 von 122

1

Half-life is...

Wähle eine der folgenden:

  • 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.

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Frage 115 von 122

1

Cytochrome P450 enzymes...

Wähle eine oder mehr der folgenden:

  • 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.

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Frage 116 von 122

1

CYPs are only found in the endoplasmic reticulum of cells.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 117 von 122

1

The largest concentration of CYPs in the human body is in the liver, in hepatocytes.

Wähle eins der folgenden:

  • WAHR
  • FALSCH

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Frage 118 von 122

1

In phase 1 drug metabolism...

Wähle eine der folgenden:

  • 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.

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Frage 119 von 122

1

Inhibition of CYPs causes:

Wähle eine oder mehr der folgenden:

  • reduced metabolism of substrate drug

  • increased metabolism of substrate drug

  • increased drug exposure

  • reduced drug exposure

  • risk of toxicity

  • risk of lacking therapeutic effect

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Frage 120 von 122

1

Induction of CYPs causes:

Wähle eine oder mehr der folgenden:

  • 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

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Frage 121 von 122

1

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?

Wähle eine der folgenden:

  • Conjugation

  • Acid/Base

  • Esterification

  • Elimination

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Frage 122 von 122

1

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?

Wähle eine oder mehr der folgenden:

  • sulphuric acid

  • amino acids

  • glucuronic acid

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