Pharmocokinetics - ADME

Descripción

Test sobre Pharmocokinetics - ADME , creado por MPusey el 08/01/2015.
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Resumen del Recurso

Pregunta 1

Pregunta
What is pharmocokinetics?
Respuesta
  • What the body does to the drug
  • What the drug does to the body
  • Mechanism of actions of the drug
  • An method of calculating what the dose of the drug should be
  • How the drug is excreted from the body

Pregunta 2

Pregunta
Which of the following are included in pharmocokinetics?
Respuesta
  • Absorption
  • Distribution
  • Metabolism
  • Excretion
  • Mechanism of Action

Pregunta 3

Pregunta
Which of the following describes absorption in terms of pharmocokintetics?
Respuesta
  • How quickly and by what means the unchanged drug gets into the body
  • How and where the drug moves among fluids and tissues
  • Transformation of the drug into daughter compounds
  • Removal of a drug or metabolite from the body

Pregunta 4

Pregunta
What best describes the term distribution in relation to pharmocokinetics?
Respuesta
  • How quickly and by what means the unchanged drug gets into the body
  • How and where the drug moves among fluids and tissues
  • Transformation of a drug into daughter compounds
  • Removal of a drug or metabolite from the body

Pregunta 5

Pregunta
What description best describes the term metabolism in relation to pharmocokintetics?
Respuesta
  • How quickly and by what means the unchanged drug gets into the body
  • How and where the drug moves among fluids and tissues
  • Transformation of a drug into daughter compounds
  • Removal of a drug or metabolite from the body

Pregunta 6

Pregunta
Which description best describes the term excretion in relation to pharmocokinetics?
Respuesta
  • How quickly and by what means the unchanged drug gets into the body
  • How and where the drug moves among fluids and tissues
  • Transformation of a drug into daughter compounds
  • Removal of a drug or metabolite from the body

Pregunta 7

Pregunta
Why is pharmocokinetics important?
Respuesta
  • Safe use of medicines by doctors
  • Designing dosing regimes
  • Monitoring treatment compliance
  • Substance abuse monitoring
  • Medicine licensing requirements
  • Ensuring the medicine has the correct mechanism of action

Pregunta 8

Pregunta
What is the main reason that drugs are withdrawn from development?
Respuesta
  • Pharmocokinetics (undesirable effects on the body)
  • Commercial reasons
  • Lack of efficacy
  • Animal toxicity

Pregunta 9

Pregunta
In what circumstance do drugs not need to be absorbed into the body?
Respuesta
  • When they are injected straight into the blood
  • When they act on the stomach or intestines
  • When they act on where they are excreted
  • When they are only being used for clinical trials
  • When the dose of the drug needs to be really small

Pregunta 10

Pregunta
What is bio-availability?
Respuesta
  • The percentage of administered drug that enters the circulation
  • The proportion of cells within the body that the drug will affect
  • The proportion of cells within the body that the drug will enter
  • The percentage of administered drug that is absorbed in the stomach
  • The percentage of administered drug that is absorbed in the intestines

Pregunta 11

Pregunta
Which route of administration has the highest bio-availability?
Respuesta
  • Intravenous injection
  • Oral
  • Inhalation
  • Subcutaneous injection
  • Intramuscular injection

Pregunta 12

Pregunta
What is the bio-availability of a drug that is administered intravenously?
Respuesta
  • 100%
  • 99%
  • 75%
  • 90%
  • 82%

Pregunta 13

Pregunta
Why aren't all drugs given by intravenous injection?
Respuesta
  • It's inconvenient
  • It requires a hospital setting
  • It's more expensive
  • It causes more side effects
  • The high bio-availability can cause toxicity when using some drugs

Pregunta 14

Pregunta
Why is the inhalation of a drug a good route of administration in conditions like asthma?
Respuesta
  • Because the drug goes straight to the site of action
  • Because it decreases the side effects
  • Because it is non-invasive
  • Because it prevents the drug being metabolized by the liver prior to reaching the tissues

Pregunta 15

Pregunta
What are some disadvantages of giving drugs orally?
Respuesta
  • They may metabolized by the liver before they reach the target tissue
  • The bio-availability is unlikely to be 100%
  • They cannot be absorbed in the stomach
  • It makes the drug harder to excrete
  • It leads to more side effects

Pregunta 16

Pregunta
What will increase the diffuse of drugs into the bloodstream?
Respuesta
  • Increased surface area to diffuse across
  • Increased concentration of the drug
  • Decreased surface area to diffuse across
  • Decreased concentration of the drug

Pregunta 17

Pregunta
Which type of absorption is most common?
Respuesta
  • Transcellular absorption
  • Paracellular absorption

Pregunta 18

Pregunta
What will be a problem if a drug is too lipophilic?
Respuesta
  • It will remain within the cell membrane instead of passing through it
  • It will not pass through the cell membrane
  • It will have more side effects
  • It is likely to have animal toxicity

Pregunta 19

Pregunta
What is permeability determined by?
Respuesta
  • How lipophilic the solute is
  • The size of the solute
  • Whether or not the solute is charged
  • The pH of the particle when it dissolves in the solution
  • The surface area available for diffusion to take place across

Pregunta 20

Pregunta
Where are acidic drugs most likely to be absorbed?
Respuesta
  • Stomach
  • Intestines
  • Liver

Pregunta 21

Pregunta
Where are basic drugs most likely to be absorbed?
Respuesta
  • Stomach
  • Intestines
  • Liver

Pregunta 22

Pregunta
Why are drugs often weak acids or weak bases?
Respuesta
  • It allows ion trapping
  • It allows them to be water soluble and lipophilic
  • It means they have a higher efficacy
  • It means they will have less side effects
  • It allows them to pass through cell membranes more easily

Pregunta 23

Pregunta
What state are acidic or basic drugs in when they pass through cell membranes?
Respuesta
  • Ionized
  • Unionized
  • Metabolized

Pregunta 24

Pregunta
Why are acidic drugs more likely to be absorbed in the stomach?
Respuesta
  • Because the stomach is acidic and they will be unionized so can move through the cell membrane
  • Because the stomach is basic and they will be unionized so can move through the cell membrane
  • Because the stomach is acidic and they will be ionized so can move through the cell membrane
  • Because the stomach is basic and they will ionized so can move through the cell membrane

Pregunta 25

Pregunta
What is ion trapping?
Respuesta
  • The prevention of ions leaving the bloodstream once they have been absorbed
  • The prevention of ions leaving the stomach or intestines because they are unable to be absorbed
  • The trapping of ions within the liver because they may be harmful to the body

Pregunta 26

Pregunta
What allows ion trapping to occur?
Respuesta
  • The pH of the stomach being ~1 and the bloodstream being ~7.4
  • The pH of the stomach being ~7.4 and the bloodstream being ~1
  • The stomach having a higher concentration of potassium than the bloodstream
  • The bloodstream having a higher concentration of potassium than the stomach

Pregunta 27

Pregunta
Which drugs are likely to be absorbed most quickly?
Respuesta
  • Acidic drugs
  • Basic drugs
  • Drugs that are neither acidic or basic

Pregunta 28

Pregunta
What makes up for the fact that basic drugs cannot be absorbed in the stomach?
Respuesta
  • The high surface area in the intestines
  • They have a higher efficacy than acidic drugs
  • They have a higher bio-availability than acidic drugs

Pregunta 29

Pregunta
Where will aspirin be absorbed?
Respuesta
  • Stomach
  • Intestines

Pregunta 30

Pregunta
What is the Lipinski rule?
Respuesta
  • A method of predicting the likelihood of a successful development of a drug
  • A method of predicting where a drug is most likely to be absorbed
  • A method of predicting the efficacy of a drug
  • A method of predicting the side effects of a drug
  • A method of calculating the appropriate dose of a drug

Pregunta 31

Pregunta
What are the Lipinski rules?
Respuesta
  • Molecular weight > 500
  • No more than 5 H-bond donors
  • No less than 10 H-bond acceptors
  • Log(partition coefficient) < 5

Pregunta 32

Pregunta
What is a partition coefficient?
Respuesta
  • How lipophilic a drugs is
  • How likely a drug is likely to be absorbed
  • How toxic a drug is
  • Another term for the bio-availability of a drug

Pregunta 33

Pregunta
Where will a drug move to most quickly?
Respuesta
  • A well-perfused muscle
  • A poorly-perfused area of adipose tissue

Pregunta 34

Pregunta
We assume the concentration of a drug is proportional to the concentration at the site of action. True or false?
Respuesta
  • True
  • False

Pregunta 35

Pregunta
Most drugs follow...
Respuesta
  • First order kinetics
  • Zero order kinetics
  • Second order kinetics

Pregunta 36

Pregunta
Which of the following describe first order kinetics?
Respuesta
  • The half life of the drug is constant
  • When the dose of the drug is increased the same fraction of the drug is removed
  • A constant volume of the drug is removed
  • The bigger the dose the longer it takes to remove it

Pregunta 37

Pregunta
Which is most desirable for clinically used drugs?
Respuesta
  • First order kinetics
  • Zero order kinetics
  • Second order kinetics

Pregunta 38

Pregunta
Which of the following are true about zero order drugs?
Respuesta
  • The half-life of the drug is constant
  • If you increase the drug dose the same fraction of drug is removed
  • A constant volume of the drug is removed
  • The larger the dose of the drug the longer it will take to remove it
  • If there is only a small dose it will follow first order kinetics
  • If there is only a small dose of a drug it will follow second order kinetics

Pregunta 39

Pregunta
Alcohol is a zero order drug. True or false?
Respuesta
  • True
  • False

Pregunta 40

Pregunta
Why are zero order drugs dangerous?
Respuesta
  • Because there is saturation of the metabolic pathways
  • Because the drug has a lower efficacy
  • Because the drug will be more slowly removed
  • Because there will be more side effects

Pregunta 41

Pregunta
What is volume of distribution?
Respuesta
  • The volume of plasma that would be necessary to account for the total amount of drug in the patients body, if the drug was were present throughout the body at the same concentration as in the plasma
  • The concentration of the drug in the plasma, which is used to estimate the concentration of the drug at it's site of action
  • The volume of plasma required to dilute the drug to the necessary concentration to have the desired pharmacological effect on the body

Pregunta 42

Pregunta
What is the formula for volume of distribution (Vd)?
Respuesta
  • Vd = total amount of drug/concentration of drug in plasma
  • Vd = concentration of drug in plasma/total amount of drug
  • Vd = concentration of drug in bloodstream/total amount of drug
  • Vd = total amount of drug/concentration of drug at site of action

Pregunta 43

Pregunta
What is volume of distribution useful for?
Respuesta
  • Calculating the loading dose required for desired blood concentration
  • Estimating blood concentration in the treatment of overdose
  • Calculating the amount of time required between each dose of the drug
  • Estimating the percentage of the drug that is at the site of action

Pregunta 44

Pregunta
What is plasma clearance?
Respuesta
  • The volume of plasma cleared of the drug per unit of time
  • The percentage of drug cleared from the plasma per unit time
  • The percentage of plasma cleared of the drug per unit time

Pregunta 45

Pregunta
What is the equation for the plasma clearance of drugs?
Respuesta
  • Clearance = rate of elimination/concentration of drug in plasma
  • Clearance = concentration of drug in plasma/rate of elimination
  • Clearance = rate of elimination x concentration of drug in plasma

Pregunta 46

Pregunta
Which drugs will have a constant plasma clearance?
Respuesta
  • First order drugs
  • Zero order drugs
  • Second order drugs

Pregunta 47

Pregunta
How is bio-availability measured?
Respuesta
  • The fraction of drug in circulation compared to the dose
  • The volume of drug in circulation
  • The percentage of drug that is absorbed in the stomach
  • The percentage of drug that reaches the desired site of action

Pregunta 48

Pregunta
Which method of administration is used to calculate the bio-availability of a drug using a different method of administration?
Respuesta
  • Intravenous injection
  • Intramuscular injection
  • Oral
  • Inhalation
  • Subcutaneous injection

Pregunta 49

Pregunta
What might cause poor bio-availability?
Respuesta
  • Poor absorption
  • Chemical reactions at the site of delivery
  • First pass metabolism
  • Chemical reaction at the site of action
  • The drug being acidic

Pregunta 50

Pregunta
What is first pass metabolism?
Respuesta
  • When the concentration of the drug is greatly reduced before it reaches the systemic circulation
  • When the concentration of the drug is greatly reduced before it reaches the pulmonary circulation
  • When the half-life of the drug is very short the very little drug reaches the site of action

Pregunta 51

Pregunta
Which route of administration will lead to the lowest concentration of drug in the circulation?
Respuesta
  • Oral
  • Intravenous
  • Subcutaneous
  • Intramuscular

Pregunta 52

Pregunta
What is multiple dosing designed to achieve?
Respuesta
  • A "steady state"
  • The least side effects
  • The highest bio-availability
  • The highest efficacy

Pregunta 53

Pregunta
There a no fluctuations in the concentration of drug once it has reached its "steady state" following multiple doses. True or false?
Respuesta
  • True
  • False

Pregunta 54

Pregunta
When using multiple dosing, when should the next dose of the drug be given to ensure a "steady state" is reached?
Respuesta
  • Before the concentration of the drug falls to zero
  • After the concentration of the drug has fallen to zero
  • After the first half life
  • After two half lives

Pregunta 55

Pregunta
What does the time taken for the drug to reach a "steady state" depend on?
Respuesta
  • The drugs half life
  • The drugs efficacy
  • The drugs bio-availability

Pregunta 56

Pregunta
How long does it typically take for the "steady state" to be achieved?
Respuesta
  • 4-5 half lives
  • 1 half life
  • 1-2 half lives
  • A variable amount of half lives

Pregunta 57

Pregunta
Where can drug metabolism occur?
Respuesta
  • Site of administration
  • Site of action
  • Bloodstream

Pregunta 58

Pregunta
When does drug metabolism and excretion begin to occur?
Respuesta
  • Immediately
  • After one half life
  • It is impossible to tell

Pregunta 59

Pregunta
What is metabolism typically designed to do?
Respuesta
  • Make the drug easier to excrete
  • Reduce the side effects of the drug
  • Increase the amount of time the drug remains in the body
  • Prevent the drugs from being absorbed in the stomach

Pregunta 60

Pregunta
Give an example of a drug that is eliminated by the body without being metabolized?
Respuesta
  • Digoxin
  • Enalapril
  • Paracetamol
  • Alcohol

Pregunta 61

Pregunta
All drug metabolites are inactive. True or false?
Respuesta
  • True
  • False

Pregunta 62

Pregunta
How many phases are there to drug metabolism?
Respuesta
  • 2
  • 3
  • 4
  • 5

Pregunta 63

Pregunta
What happens during phase 1 of drug metabolism?
Respuesta
  • Introduction of chemically reactive groups
  • A increase in the water solubility of the drug for excretion
  • Removal of reactive groups from the drug
  • Ionization of the drug to prevent it from crossing cell memebranes

Pregunta 64

Pregunta
Where does phase 1 of drug metabolism usually take place?
Respuesta
  • In the liver
  • In the bloodstream
  • In the kidneys
  • At the site of action

Pregunta 65

Pregunta
What enzyme is usually involved in phase 1 of drug metabolism?
Respuesta
  • Cytochrome P450
  • Lipases
  • DNA polymerases
  • Amylase

Pregunta 66

Pregunta
What usually occurs during phase 2 of drug metabolism?
Respuesta
  • Conjugation of the drug with endogenous compounds
  • Addition of reactive groups to the molecule
  • Oxidation of the molecule
  • Hydrolysis of any hydrogen bonds within the molecule

Pregunta 67

Pregunta
Which drug is metabolised with phase 2 taking place before phase 1?
Respuesta
  • Paracetamol
  • Alcohol
  • Digoxin
  • Enalapril

Pregunta 68

Pregunta
Which phase of paracetamol metabolism produces a toxic compound?
Respuesta
  • Phase 1
  • Phase 2

Pregunta 69

Pregunta
Why is paracetamol more likely to cause problems in alcoholics than in the general population?
Respuesta
  • Because alcoholics have more cytochrome P450 so phase 1 is more likely to occur
  • Because alcoholics have no cytochrome P450 so the toxic compound is readily produced
  • Because alcoholics lack thyamine which is a co-enzyme for the phase 2 part of paracetamol metabolism

Pregunta 70

Pregunta
Only unbound drugs can be excreted. True or false?
Respuesta
  • True
  • False

Pregunta 71

Pregunta
Which drugs are likely to be excreted more slowly?
Respuesta
  • Lipophilic drugs
  • Hydrophilic drugs

Pregunta 72

Pregunta
Why are lipophilic drugs likely to excreted more slowly?
Respuesta
  • Because they are likely to be reabsorbed
  • Because they cannot be filtered through the glomerulus
  • Because they are usually bigger
  • Because they are not secreted into the tubules

Pregunta 73

Pregunta
All drugs can be secreted into the renal tubules from the bloodstream. True or false?
Respuesta
  • True
  • False

Pregunta 74

Pregunta
What sort of process is tubular secretion in terms of drug elimination?
Respuesta
  • Active process requiring a carrier molecule
  • Passive process requiring an activated protein channel
  • Active process without a carrier molecule
  • Passive diffusion through the membrane

Pregunta 75

Pregunta
If renal clearance is slow, the plasma half-life of the drug will be...?
Respuesta
  • Longer
  • Shorter
  • Unchanged

Pregunta 76

Pregunta
Why can age affect drug metabolism and excretion?
Respuesta
  • Cytochrome P450 is less efficient in neonates
  • GFR is increased in elderly people
  • Increased percentage of fat in elderly people decreases excretion of lipophilic drugs
  • Cytochrome P450 is less efficient in elderly people

Pregunta 77

Pregunta
What disease is most likely to affect the pharmocokinetics of a drug?
Respuesta
  • Renal disease
  • Heart disease
  • Parkinson's disease
  • Learning difficulties

Pregunta 78

Pregunta
Which is the most common type of adverse drug reaction?
Respuesta
  • Type A
  • Type B

Pregunta 79

Pregunta
Which of the following describe type A drug reactions?
Respuesta
  • Reaction related to known drug mechanisms
  • Predictable
  • Unavoidable

Pregunta 80

Pregunta
Which of the following may cause type A drug reactions?
Respuesta
  • Wrong dose administered
  • Drug interactions
  • High therapeutic index of the drug
  • Immunological mechanisms

Pregunta 81

Pregunta
Which of the following describe a type 2 drug reaction?
Respuesta
  • Related to unknown mechanisms of the drug
  • Predictable
  • Unexpected
  • Related to patient individuality

Pregunta 82

Pregunta
What is a drawback of the yellow form for monitoring adverse drug reactions?
Respuesta
  • It relies on doctors and patients self-reporting
  • It is only accessible to doctors
  • It only reports on one drug at a time
  • It does not monitor drugs throughout their whole lifetime

Pregunta 83

Pregunta
What is usually added to the yellow form when more information is required about a drug?
Respuesta
  • Black triangle
  • Green form
  • A priority index number
  • A warning about the drug from the BNF

Pregunta 84

Pregunta
What is a benefit of the green form?
Respuesta
  • It is used to record all significant events, not just adverse effects of a drug
  • It is easily accessible by all
  • It is compulsory to fill it in when an adverse reaction occurs
  • It is clearly visible in a copy of every BNF
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