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52 Cards in this Set

  • Front
  • Back
Volume of distribution increase as body weight increases for a lipophilic drug.
true
Creatinine clearance is based on body weight.
true
An obese subject is more likely to receive an overdose than a patient with an ideal body weight for a weakly lipophilic drug given mg/kg.
true
Changes in drug distribution in obese subject can be the result of increased cardiac output, blood volume, and plasma or tissue binding
true
Oral bioavailability increases with increasing body weight
false
Adults have more extracellular body water than children.
false
How will an increase in tissue binding affect the AUC, Cmax, and half-life (t1/2) of a high-extraction drug?
A: High extraction drug: ↑ AUC, ↓ Cmax, ↓ t1/2
B: High extraction drug : ↔ AUC, ↑ Cmax, ↔ t1/2
C: High extraction drug : ↔ AUC, ↓ Cmax, ↑ t1/2
D: High extraction drug : ↓ AUC, ↔ Cmax, ↑ t1/2
E: High extraction drug: ↑ AUC, ↑ Cmax, ↓ t1/2
C: High extraction drug : ↔ AUC, ↓ Cmax, ↑ t1/2
Bioavailability is defined as the rate and extent to which the active ingredient is absorbed from a drug product
true
Bioequivalence is the presence of a significant difference in rate and extent to which the active ingredient from a pharmaceutical alternative becomes available
false
Bioequivalent products are therapeutically interchangeable
true
Bioequivalence studies are required for all strengths of a pharmaceutical alternative
false
Which combination of the following factors makes the serum creatinine level a good choice to estimate renal function? (choose all that are true)
1) Creatinine is endogenous
2) Creatinine is only eliminated by kidney
3) Creatinine is not bound to protein in plasma
4) Creatinine urinary excretion rate is not affected by diseases
5) Creatinine is constantly formed by muscle
1, 2, 3, & 5
Propranolol is a high-extraction drug and only undergoes liver metabolism. It is combined with phenobarbital. Phenobarbital is a known enzyme inducer. How would you change the dose of propranolol to account for this. Choose the best choice.
A) Increase the dose because the clearance is decreased.
B) Leave the dose the same because clearance does not significantly change.
C) Decrease the dose because clearance is increased.
D) Increase the dose because clearance is significantly increased.
B) Leave the dose the same because clearance does not significantly change.
What is the minimum extraction ratio for renal filtration if neither active reabsorption nor active secretion takes place? Assume renal blood flow 1200 ml/min, glomerular filtration rate (GFR) 120 ml/min, the urine flow rate 1.2 ml/min.
A) Eren = 1
B) Eren = GFR/(renal blood flow)
C) Eren = (urine flow)/(renal blood flow)
D) Eren = (urine flow)/GFR
E) Not enough information to determine.
E) Not enough information to determine.
A longer half-life of a drug will cause
A) a larger total body clearance.
B) more fluctuation can be expected at steady state.
C) a shorter dosing interval to maintain a certain fluctuation.
D) a longer time to reach steady state.
E) a larger volume of distribution.
D) a longer time to reach steady state.
Vancomycin exhibits time-dependent bacterial killing rather than concentration-dependent killing (as in aminoglycosides)
true
Monitor peak plasma concentrations for vancomycin efficacy rather than trough concentrations
false

Monitor trough plasma concentrations for vancomycin efficacy. Vancomycin has slow distribution into peripheral tissues making it difficult to identify the true peak
Vancomycin has poor absorption from GI tract
true
Vancomycin is 80-90% eliminated by liver
false

Vancomycin is 80-90% eliminated by kidneys
Vancomycin has good tissue penetration except bile, eye, noninflamed meninges
true
Which of the following statements on bioavailability is correct?
A) Bioavailability reflects rate and extent of absorption.
B) The FDA requires the relative bioavailability is determined from steady-state plasma levels.
C) Differences in bioavailability always lead to difference in therapeutic activity.
D) In case of chronic dosing two tablets with equal rates of bioavailability should be considered bioequivalent.
E) In case of first order kinetics comparison of the amount of unchanged drug in the urine is a proper way to determine relative bioavailability.
A) Bioavailability reflects rate and extent of absorption.
With aminoglycosides usally Cmax and Cmin are calculated using IV infusion equations. However, with vancomycin it is acceptable to use IV bolus equations to calculate Cmax and Cmin instead of IV infusion equations. Why is it justified to use these equations with vancomycin compared to aminoglycosides?
A) Vancomycin has a lower clearance which results in a smaller fluctuation.
B) Vancomycin has a smaller volume of distribution which results in a larger flucutation.
C) Vancomycin has a higher clearance which results in a larger half-life.
D) Vancomycin has a smaller half-life which results in a smaller fluctuation.
E) Vancomycin has a longer half-life which results in a smaller fluctuation.
E) Vancomycin has a longer half-life which results in a smaller fluctuation.
Which combination of the following pharmacokinetic changes best describes the elderly and neonates? (choose all that are true)

1. Low renal clearance
2. Longer half-lives
3. Low metabolic clearance
4. Decreased protein binding
5. Relatively less body water
1, 2, 3 & 4
Which of the following statements is FALSE based on the volume of distribution in obese patients.
A) Hydrophilic drugs display little change in the volume of distribution.
B) The volume of distribution is based on the lipophilicity of the drug.
C) Lipophilic drugs display an increase in the volume of distribution.
D) Hydrophilic drugs display a decrease in the volume of distribution per kilogram.
E) Lipophilic drugs display a decrease in the volume of distribution per kilogram.
E) Lipophilic drugs display a decrease in the volume of distribution per kilogram.
How will an increase in tissue binding affect the following properties of a high-extraction drug administrated through an intravenous injection?
A) ↑ AUC, ↓ Cmax, ↓ t1/2
B) ↔ AUC, ↑ Cmax, ↔ t1/2
C) ↔ AUC, ↓ Cmax, ↑ t1/2
D) ↓ AUC, ↔ Cmax, ↑ t1/2
E) ↑ AUC, ↑ Cmax, ↓ t1/2
C) ↔ AUC, ↓ Cmax, ↑ t1/2
Which combination of the following factors makes the serum creatinine level a good choice to estimate renal function? (choose all that are true)
1) Creatinine is endogenous
2) Creatinine is only eliminated by kidney
3) Creatinine is not binding to protein in plasma
4) Creatinine urinary excretion rate is not affected by diseases
5) Creatinine is constantly formed by muscle
1, 2, 3, & 5
Which statement is wrong?
A) Creatinine clearance is a measurement for kidney function.
B) Bioavailability of high extraction drugs is dependent on plasma protein binding.
C) Clearance and volume of distribution determine the half-life of a drug.
D) A multi-compartment-body model has only one volume of distribution.
E) Clearance determines steady-state plasma levels
D) A multi-compartment-body model has only one volume of distribution.
Which statement is wrong?
A) Renal clearance can vary with age.
B) Heart failure can have an impact on clearance.
C) Aminoglycosides are used to treat infections with both gram-positive and gram-negative pathogens.
D) Given linear pharmacokinetics, a plot of average steady-state concentration vs. dose results in a straight line.
E) AUC, Cmax and tmax are used to evaluate bioequivalence.
E) AUC, Cmax and tmax are used to evaluate bioequivalence.
How will an increase in tissue binding affect the clearance, bioavailability and half-life of a high-extraction drug? (5 pts)
A. Clearance is decreased, bioavailability is not changed, Half-life is increased
B. Clearance is decreased, bioavailability is not changed, Half-life is not changed
C. Clearance is not changed, bioavailability is not changed, Half-life is not changed
D. Clearance is decreased, bioavailability is increased, Half-life is increased
E. Clearance is not changed, bioavailability is not changed, Half-life is increased
E. Clearance is not changed, bioavailability is not changed, Half-life is increased
The dosing interval (τ ) can be greater than drug half-life if:
A) the therapeutic index of the drug is high
B) pharmacologically active metabolites of the drug have
longer half lives than the drug
C) the therapeutic effect of the drug is unrelated to plasma
concentrations
D) both A and B
E) all of the above
E) all of the above
What is the pharmacokinetic parameter that should be monitored for vancomycin
therapy to achieve the desired efficacy?
A. Clearance
B. AUC
C. Peak concentration
D. Trough concentration
E. Vd
D. Trough concentration
For bioequivalence the 90% confidence limit for AUC and Cmax must fall between 90-125%.
false

80-125%.
The extent to which a drug is absorbed partially determines its:
A: elimination rate
B: clearance
C: half-life
D: volume of distribution
E: bioavailability
E: bioavailability
Which of the following statements about body weight in pharmacokinetics are correct? (choose all that are true)
1) We can roughly assume liver and kidney function are proportional to body weight.
2) Effects of obesity on volume of distribution depend on the lipophilicity of the drug.
3) Physical and chemical properties of drugs determine the impact of body weight on pharmacokinetics.
4) In general, we should always use IBW for drug recommendations.
5) Weakly or moderately lipophilic drugs are poorly distributed in obese patients.
1, 2, 3, & 5
How will an increase in tissue binding affect the clearance (CL), bioavailability (F), and half-life (t1/2) of a low-extraction drug?
A: ↑ CL, ↓F, ↓ t1/2
B: ↔ CL, ↑F, ↔ t1/2
C: ↔CL, ↔ F, ↑ t1/2
D: ↓ CL, ↔ F, ↑ t1/2
E: ↑ CL, ↑ F, ↓ t1/2
C: ↔CL, ↔ F, ↑ t1/2
What are the two pharmacokinetic parameters that are evaluated in a bioequivalance study whose log-transformed ratios (test:reference) must pass the two one-sided test about the 90% confidence intervals?
A: Clearance and Volume of distribution
B: Clearance and AUC
C: Cmax and AUC
D: Tmax and AUC
E: AUC and half-life
C: Cmax and AUC
The total body water (in % of body weight) in neonates is usually smaller than in adults
FALSE
The glomerular filtration rate (GFR) in neonates is usually smaller than in adults
TRUE
Patients with an increased body weight tend to have a larger volume of distribution
TRUE
The effect of body weight on volume of distribution does not depend on the lipophilicity of the drug
FALSE
Drugs with a high octanol/water lipid partition coefficient (LPD) usually show a larger volume of distribution in obese patients
TRUE
The allometric body weight model can be used to convert body surface area (BSA) into total body weight (TBW)
FALSE
The terminal half-life of aminoglycosides is approximately 2 hours
FALSE
Aminoglycosides cannot pass membranes very well because of their low protein binding
FALSE
Regarding an aminoglycoside, an obese patient will have a higher Vd than a normal weight person, but it is not proportional to weight.
true
The loading dose of drugs with polar characteristics is based on TBW.
FALSE

(based on IBW)
Doses of compounds with high lipid partition coefficients are based on TBW.
TRUE
For an oral drug, it is possible that the metabolite has a shorter terminal half-life than the parent drug.
FALSE
In general, in bioequivalence studies blood is collected for 3 or more terminal half lives.
TRUE
In general, a multiple dose BE study for modified release dosage forms is not recommended.
TRUE
The AUC extrapolated to time infinity for the first dose is equal to steady-state AUC values over a single dosing day at steady state.
TRUE
In general, bioequivalence study is required for all strengths if the strengths are proportionally similar and meet dissolution profile comparison criteria.
FALSE