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824 > ADME tutorials > Flashcards

ADME tutorials Flashcards

1
Q

Percentage of drugs that fail in clinical trials due to ADME

A

10%

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2
Q

Route with most rapid onset

A

intravenous

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3
Q

Morphine is a metabolite of codeine and this metabolite is responsible for the
analgesic effect when codeine is administered. In a patient who has a genetic
defect such that they cannot metabolize codeine, the magnitude of pain relief
would be expect to be _____________ compared to normal patients

A

Decreased

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4
Q

Slowing gastric emptying would be expected to have what effect on the absorption
of a drug absorbed by passive diffusion?

A

It will take longer to achieve peak concentration

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5
Q

Which mechanisms move drug down a concentration gradient?

A

Paracellular, transcellular, facilitated diffusion

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6
Q

Which mechanism goes against concentration gradient?

A

Active transport

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7
Q

Co-administration of an inhibitor of the efflux protein p-glycoprotein (pgp) would be
expected to have what effect on the oral absorption of a drug that is a substrate
for pgp?

A

Increase amount of drug absorbed

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8
Q

Which of the following modifications would be not expected to increase the
transcellular permeability of a drug molecule?
Removing ionized groups
Decreasing lipophilicity
reducing molecular size

A

Decreasing lipophilicity

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9
Q

A drug that is only distributed into vascular space will exhibit a monoexponential
blood concentration versus time curve after intravenous administration. True or
False?

A

False

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10
Q

Which of the following drugs is most likely to undergo transvascular transport via
convection?
a. Aspirin (MW 180 g/mole)
b. Cimetidine (MW 252 g/mole)
c. Vancomycin (MW 143 g/mole)
d. Idarucizumab (MW 47,766 Daltons)

A

Idarucizumab

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11
Q

A decrease in the plasma protein binding of a drug would be expected to have
what effect on the distribution of drug into tissue?

A

Increase amount of drug in tissue

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12
Q

A change in the structure of a drug molecule such that it is no longer transported
by pgp (MDR1) would be expected to have what effect on the CNS concentration
of drug compared to the original drug?

A

The new drug would have a higher concentration in the CNS

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13
Q

Which of the following renal excretory processes for drugs is most likely subject to
competitive drug-drug interactions?

A

tubular secretion

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14
Q

In examining the renal elimination of a series of chemically related compounds, as
molecular weight increases, the extent of filtration will ______________

A

Decrease

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15
Q

%in bile vs mw plot relationship

A

direct

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16
Q

What is the effect of enterohepatic recirculation (EHR) on the half-life of a drug?

A

Increases the half life

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17
Q

For a drug that is eliminated solely by glomerular filtration, a decrease in plasma
protein binding will result in a(n) ____________ in the renal elimination of the drug

A

Increase

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18
Q

Which of the following undergoes bioactivation in the kidney?

A

Vitamin D

19
Q

Which pathway of metabolism is most likely to result in a significant increase in the
molecular weight of a drug?

A

Phase II

20
Q

Which pathway of metabolism is most likely to result in a metabolite eliminated in
the bile?

A

Phase II

21
Q

Which type of inhibitor of CYP450 would produce the longest lasting inhibition?

A

Mechanism base inhibition

22
Q

In general, inducers of CYP450 are selective for one specific enzyme or enzyme
family

A

False

23
Q

The fate of a drug once it enters the systemic circulation.

A

Disposition

24
Q

The study of the absorption, distribution, biotransformation, and
elimination of xenobiotics.

A

Pharmacokinetics

25
Q

The study of the molecular, biochemical, and physiological effects
of xenobiotics and their mechanisms of actions.

A

Pharmacodynamics

26
Q

A chemical that is normally foreign to the body. This includes drugs,
occupational chemicals, environmental compounds, etc.

A

Xenobiotics

27
Q

The passive movement of drug through lipid membranes. This
movement is driven by concentration gradient

A

Transcellular diffusion

28
Q

The passive movement of drug between cells via tight junctions.
This movement is driven by concentration gradient.

A

Paracellular diffusion

29
Q

A carrier-mediated process that involves a transport protein which
moves drug with a concentration gradient.

A

Facilitated diffusion

30
Q

A carrier-mediated process that requires energy and can move drug
against a concentration gradient

A

Active transport

31
Q

A process by which a cell engulfs and internalized a particle

A

Endocytosis

32
Q

The movement of drug molecules across biological membranes into various
tissues in the body.

A

Distribution

33
Q

The movement of drug molecules cross vascular endothelial
cells and into tissue interstitial space

A

Transvascular transport

34
Q

A transvascular transport process that is driven by pressure.

A

Convection

35
Q

A transvascular transport process that is driven by a concentration gradient.

A

Diffusion

36
Q

The concentration of drug within a tissue due to pH differences that lead
to ionization of the drug in the tissue environment

A

Drug trapping

37
Q

The initial movement of drug from highly perfused tissues to poorly
perfused tissues

A

Redistribution

38
Q

Biotransformation of xenobiotics (a compound foreign to the body)
that includes oxidation, hydroxylation, and related changes that either introduce or expose
a functional group

A

Phase i Metabolism

39
Q

Biotransformation of xenobiotics that involves conjugation with a
polar group (e.g., sulfate, glucuronic acid) yielding a polar metabolite that can be more
readily excreted in the bile or urine. These pathways are sometimes referred to as
conjugation reactions and can be influenced by the availability of the co-substrate (e.g.,
sulfate or activated sulfate).

A

Phase II Metabolism

40
Q

The active transport of drug from blood into the renal tubule,
occurring primarily in the proximal tubule.

A

Active tubular secretion

41
Q

The movement of solute from inside the renal tubule back into
the blood. This is primarily a passive process for drugs and is driven by the high
concentration effect that occurs as a result of the large fraction of filtrate that is
reabsorbed

A

Tubular reabsorption

42
Q

The reabsorption of drug from the small intestine after drug
has been excreted through the bile into the intestine.

A

Enterohepatic recirculation

43
Q

The process by which food stimulates release of bile, and drug contained
therein, into the small intestine, followed by reabsorption of the drug. This occurs because
release of bile into the small intestine in man is periodic, allowing drug to accumulate in
the gall bladder

A

Dose dumping

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