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Kinetics > Ex. 2 Practice Questions > Flashcards

Ex. 2 Practice Questions Flashcards

1
Q

L1: T/F: Higher dose is expected to show greater drug accumulation (i.e. higher accumulation index)

A

False - greater not dose dependent

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1
Q

L1: When you switch dosage regimen from 10mg q12h to 10mg 24h, what happens to: Fluctuation?

A

Goes up

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2
Q

L1: When you switch dosage regimen from 10mg q12h to 10mg 24h, what happens to:
Average CSS?

A

Lower

Because CSSave is (dose/T)/CL

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3
Q

L1: When you switch dosage regimen from 10mg q12h to 10mg 24h, what happens to:
TSS

A

Same

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4
Q

L1: When you switch dosage regimen from 10mg q12h to 10mg 24h, what happens to: Accumulation index?

A

Lower

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5
Q

L3: “A” (close to top) is called the distribution phase

A

True

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6
Q

L3: “B” (mid-line) is called the elimination phase

A

True

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7
Q

L3: The data show a drug following a one-compartment model (slight curve at beginning, then linear throughout)

A

False - two compartment

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8
Q

L3: This happens (bi-phasic) because drug distribution to/from tissue is slow

A

True

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9
Q

L4: After IV admin, Drug A and Drug B show MRT values of 1 and 5 hr respectively. Which drug is eliminated faster?

  1. A
  2. B
  3. Not enough info given
A

Drug A

MRT is mean residence time; lower time = faster elimination

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10
Q

L4: After 1 gram of drug C is admin intravenously, the following concentration time profile is obtained:

(Straight line, no curve)

T/F
1: AUC can be estimated
2. AUMC can be estimated
3. MRT can be estimated
4. CL can be estimated
5. Vdss can be estimated

A
  1. True
  2. True
  3. True
  4. True
  5. True
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11
Q

L4: After 1 gram of drug C is admin intravenously, the following concentration time profile is obtained:

(Curvy line)
T/F
1: AUC can be estimated
2. AUMC can be estimated
3. MRT can be estimated
4. CL can be estimated
5. Vdss can be estimated

A
  1. True
  2. True
  3. True
  4. True
  5. True
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12
Q

L5: What is rate-limiting step that determines metabolite amount in the body?

Kf = 0.0.5
K(m) = 1.2

A

Kf = 0.05 formation of metabolite (slower step)

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13
Q

L5: What is the apparent t/12 of parent drug from the body?
Kf = 0.05
k(m) = 1.2

A

T1/2 = 0.693/k

0.693/0.05 = 14 hr

parent drug = Kf

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14
Q

L5: What is the apparent t1/2 of metabolite from the body after administration of the parent drug?
Kf = 0.05
k(m) = 1.2

A

0.693/k
0.693/0.05hr

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15
Q

L5: What would be the true t1/2 of metabolite from the body (i.e., t1/2 obtained by administering the metabolite)
Kf = 0.05
K(m) = 1.2

A

0.693/k= 0.693/1.2 = 0.6 hr

15
Q

L5: What is the rate-limiting step that determines metabolite amount in the body?
Kf = 1.2
K(m) = 0.05

A

Elimination of metabolites (0.05)

15
Q

L5: What is the apparent t1/2 of parent drug from the body?
t1/2 = 0.693/k
Kf = 1.2
K(m) = 0.05

A

t1/2 = 0.693/k

0.693/1.2 = 0.6 hr

16
Q

L5: What is the apparent t1/2 of metabolite from the body after administration of parent drug?:
Kf = 1.2
K(m) = 0.05

A

t1/2= 0.693/k

0.693/0.05 = 14 hr

17
Q

L5: What would be the true t1/2 of metabolite from the body (i.e., t1/2 obtained by administering the metabolite)
Kf = 1.2
K(m) = 0.05

A

t1/2 = 0.693/k

0.693/0.05 = 14 hr

18
Q

L5: Q1 Tolbutamide is a low EH drug, and its fe = 0. What would happen to the half-life of tolbutamide when it is combined with rifampin, an inducer of CYP2C9 expression?

A

Rifampin will increase CYP2C9 level, increase the rate of formation, increase clearance, increase K, =
t1/2 will decrease

19
Q

L5: What would happen to half-life of hydroxytolbutamide when tolbutamide is combined with rifampin, an inducer of CYP2C9 expression?

A

Decreased t1/2
Governed by formation

20
Q

L5: Shown is a graph of formation rate limited

T/F:

1.This is likely represents a kinetic profile of pro-drugs

  1. It demonstrates “metabolite formation rate-limited” kinetics
  2. The “true” t1/2 of metabolite (i.e. the t1/2 obtained after administration of metabolite, assuming its commercial availability) would be much shorter than t1/2 estimated from this graph
  3. This occurs when elimination rate of metabolite is faster than its formation rate
A
  1. False
  2. True
  3. True
  4. True
21
Q

L5: Shown is a graph that is elimination rate limited

T/F:

  1. This likely represents a kinetic profile of pro-drugs
  2. It demonstrates “metabolite formation rate-limited kinetics”

3.The “true” t/2 of metabolite (i.e. the t1/2 obtained after admin of metabolite, assuming its commercial availability) would be much shorter than the t1/2 estimated from this graph

  1. This occurs when elimination rate of metabolite is faster than its formation rate

T/F: Drugs of High EH are associated with low F. A prodrug that has a high EH would exhibit minimal/no pharmacological activity after oral dosing

A
  1. True
  2. False
  3. False
  4. True
  5. False
22
Q

L6: T/F: Inhibition of P-gp in cancer cell is expected to improve anticancer drug efficacy by increasing intracellular drug concentrations

A

True

23
Q

L6: T/F inhibition of Pgp in brain is expected to increase the penetration of Pgp substrates into brain

A

True

24
Q

L6: T/F: HIV-associated Neurocognitive Disorders occur when HIV enters the nervous system and impacts the health of nerve cell. Combining HIV Protease inhibitors (p-gp susbtrates) with P-gp inhibitors will likely increase brain distribution of anti-HIV drugs

A

True

25
Q

L6: T/F: Combining paclitaxel with a P-gp inhibitor will likely decrease biliary excretion of paclitaxel

A

True

Biliary excretion major form of elimination - inhibit pgp

26
Q

L6: T/F: Biliary excretion of paclitaxel is its major elimination route. Combining paclitaxel with a P-gp inhibitor will likely decrease paclitaxel elimination from the body and increase systemic drug concentration

A

True

27
Q

L6: T/F: P-gp inhibitors will likely increase the passage of P-gp substrates across placenta, leading to increased fetal drug levels

A

True

28
Q

L6: T/F: OATP1B1 inhibition will likely decrease the intrahepatic concentration OATP1B1 substrates

A

True

29
Q

L6: Which of the following is NOT the expected biological consequence of a P-gp substrate drug when it is co-administered with a pgp inhibitor?

A. Increased brain distribution
B. Increased biliary excretion
C. Increased intestinal absorption
D. Increased drug transfer to fetus

A

B - increased biliary excretion

30
Q

L6: which one of the following transporters is responsible for increased absorption of valacyclovir as compared to acyclovir?
A. Pgp
B. OATP1B1
C. PEPT1
D. OCT1

A

C - PEPTI

31
Q

L6: Which one of the following transporters is responsible for hepatic uptake of statins?
A. Pgp
B. OATP1B1
C. PEPT1
D. OCT1

A

B. OATP1B1

32
Q

L6: Genetic polymorphisms of OATP1B1 that are associated with nonfunctional transporter activity would lead to:
A. Increased hepatoxicity of statins
B. Decreased efficacy of statins
C. Decreased myopathy of statins
E. None of the above

A

B - decreased efficacy of statins

Kinetics (20 decks)

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