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Pharm > 01a: Pharmacokinetics > Flashcards

01a: Pharmacokinetics Flashcards

1
Q

List the pharmacologic phenomena that describe time course of drug in body.

A
  1. Absorption
  2. Distribution
  3. Elimination
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2
Q

Passive diffusion follows (0/1/2)-order kinetics. Thus, rate of transport depends on (X).

A

1

X = conc gradient

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3
Q

List the physicochemical features of drug molecules that affect drug transport.

A
  1. MW
  2. Lipophilicity (oil:water partition coeff)
  3. pKa (ionizable groups)
  4. Physical form (solid/liquid/gas)
  5. Stability in aqueous soln
  6. Affinity for proteins
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4
Q

Active transport follows (0/1/2)-order kinetics. Thus, (X) is constant.

A

0

X = rate of transport

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5
Q

(X) method of drug transport is especially important for high MW compounds, such as protein therapeutics.

A

X = endocytosis

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6
Q

Ionization markedly increases (X), thus (increasing/decreasing) lipophilicity.

A

X = hydrophilicity

Decreasing

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7
Q

Drugs with (X) groups act as acids and become (pos/neg)-charged as pH (increases/decreases).

A

X = carboxylate
Neg
Increases

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8
Q

Drugs with (X) groups act as bases and become (pos/neg)-charged as pH (increases/decreases).

A

X = amine
pos;
Decreases

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9
Q

A drug that’s a weak base is able to cross cell membrane via diffusion at (high/low) pH.

A

High (loses H, becomes neutral)

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10
Q

Aspirin is a (strong/weak) (acid/base) with pKa of 3.5. At physiological pH, can it cross membrane via diffusion?

A

Weak acid;

No - neg charged (lost H)

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11
Q

(X) is the transport of small molecule drugs in bulk flow of aqueous fluid. What does the rate of this transport depend on?

A

X = filtration

  1. Hydrostatic P
  2. Drug properties (MW, size, charge, binding)
  3. Tissue porosity
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12
Q

List some organs/structures that use filtration as method of drug transport.

A

Glomerulus, liver sinusoids, choroid plexus

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13
Q

(X) transport is an important mechanism for mAb transport. In the body, mAb are transported from (Y) into (Z) spaces.

A 
X = convective
Y = lymph or blood
Z = tissue spaces
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14
Q

Convective transport depends on:

A
  1. Fluid flow rate (into tissue)
  2. Sieving effect of paracellular pores
  3. Hydrostatic P gradient
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15
Q

The sieving effect in (X) transport depends on:

A

X = convective

  1. Size/shape of pores
  2. Size/shape/charge of Ab
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16
Q

P-glycoprotein1 (Pgp) is a drug transporter belonging to (X) family. Which types of substrates does it transport?

A

X = ABC

Neutral, cationic, and amphipathic substrates (multidrug/variable)

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17
Q

OAT1, aka (X), is a drug transporter belonging to (Y) family.

A 
X = Organic anion transporter;
Y = solute carrier
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18
Q

Rate of receptor-mediated endocytosis is dependent on:

A
  1. Receptor expression

2. Membrane insertion of receptor

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19
Q

T/F: All transport of Ab via endocytosis involves specific binding.

A

False - fluid phase endocytosis is nonspecific (no ligand binding)

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20
Q

Fluid-phase endocytosis is a process driven by (X). It’s responsible for entrance of which drugs into (Y) tissues?

A

X = mAb concentration on extracellular side
mAb
Y = endothelial and peripheral

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21
Q

Absorption kinetics: how long it takes for….

A

Transport of drug from site of admin to systemic circulation

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22
Q

Absorption kinetics are characterized by:

A
  1. Absorption half-life

2. Bioavailability

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23
Q

Define bioavailability.

A

Percent of the administered dose that’s absorbed (reaches circulation in SAME molecular form)

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24
Q

T/F: Fastest possible input rate is seen in oral route of drug administration.

A

False - IV

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25
Q

IV drug administration: in addition to sterility, which two characteristics are important to consider?

A
  1. Lack of particulates

2. Aqueous solubility

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26
Q

IV administration is a good route for (low/high) MW, (polar/nonpolar) molecules.

A

High; polar

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27
Q

T/F: Enteral administration of drugs is simply another way to say “oral” admin.

A

False - enteral can be via mouth or rectum

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28
Q

“First-pass effect” influences (bioavailability/abs half-life) when drugs are administered via (X) route. Briefly describe this effect.

A

Bioavailability;
X = enteral (oral)

Lumenal, mucosal, and/or hepatic biotransformation

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29
Q

Oral administration of drug: absorption half-life affected by which three things?

A
  1. Formulation of drug (dissolution from solid)
  2. Gastric emptying time
  3. Interactions with diet/other drugs in GI lumen
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30
Q

The GI mucosa could serve as a barrier, affecting (bioavailability/abs half-life) of drugs with which characteristics?

A

Bioavailability;

High MW, low lipophilicity, carrier-mediated extrusion (back to lumen)

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31
Q

Parenteral admin of drugs includes which specific method(s)?

A
  1. IV injection

2. Intramuscular or subcutaneous injection

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32
Q

Uptake of high MW compounds into (X), when administered via I.M./S.C. injections, provides (fast/slow) absorption rate.

A

X = lymphatics

Slow

33
Q

Inhalation route of admin provides (fast/slow) absorption of gases/vapors into circulation. Why?

A

Fast;

  1. High pulmonary blood flow
  2. Low diffusional distance from alveolus to blood
34
Q

Distribution kinetics: rate and extent of drug distribution from (X) to (Y).

A 
X = vascular fluid
Y = tissue space
35
Q

Distribution kinetics: the equilibration rate is based on (X).

A

X = blood flow/tissue perfusion rates

36
Q

Distribution kinetics: list some tissue factors that affect equilibrium gradient.

A
  1. Vascular permeability
  2. Macromolecular and plasma protein binding
  3. Dissolution of lipid-soluble drugs in adipose
37
Q

V(d), the apparent volume of distribution, refers to:

A

volume of body into which drug appears to have distributed

38
Q

T/F: Drugs will distribute into their V(d) depending on their chemical characteristics.

A

True

39
Q

TBW (total body water) in 70 kg subject is (X) L and (Y)% body weight.

A 
X = 40-42
Y = 58
40
Q

Majority of total body water, about (X)%, is (Y) fluid compartment.

A 
X = 67
Y = intracellular
41
Q

Extracellular fluid compartment in 70 kg subject is (X) L and (Y)% body weight.

A 
X = 12-14
Y = 17
42
Q

Plasma fluid is part of (intra/extra)-cellular fluid compartment. In 70 kg subject, this is (X) L and (Y)% body weight.

A

Extracellular;
X = 3-4
Y = 4

43
Q

High MW drugs (ex: therapeutic proteins) will likely have V(d) equal to:

A

Plasma V

44
Q

Low MW, polar drugs will likely have V(d) equal to:

A

Extracellular fluid

45
Q

Low MW, non-polar/lipophilic drugs will likely have V(d) equal to:

A

TBW (or greater; stored in adipose)

46
Q

Patient variability: V(d) is generally (directly/inversely/un)-proportional to body weight.

A

Directly

47
Q

T/F: A drug’s V(d) is always larger in obese patients.

A

False - depends on its characteristics/where it’s distributed (TBW v adipose)

48
Q

Clearance of an organ depends on which two key factors?

A
  1. Plasma flow

2. Extraction ratio (how readily organ extracts drug)

49
Q

Total clearance is the (sum/product) of:

A

Sum;

Renal and non-renal clearances

50
Q

T/F: Renal clearance of drug involves its elimination in an unchanged form.

A

True

51
Q

Fc-mediated elimination pathways is for (endogenous/therapeutic) (X). Which receptors are involved?

A

Either;
X = IgGs or mAbs

FcRn or Fc(gamma)

52
Q

In (X) method of drug elimination, (Y) complex forms in the (acid/neutral/basic) environment of the early endosome.

A

X = FcRn-mediated elimination/recycling
Y =FcRn-mAb
Acid

53
Q

FcRn-mediated elimination/recycling: large fraction of endosomes end up where?

A

Not delivered to lysosome, but sorted to cell surface for Ab recycling

54
Q

Administration of mAb can trigger immune response, generating (X), which then form (Y). How are these eliminated?

A 
X = endogenous Ab (antidrug Ab/ADA)
Y = immune complexes

Via RES (reticuloendothelial system, predominantly phagocytes)

55
Q

Non-renal clearance via (X) system(s) involves excretion of the unchanged drug.

A

X = lungs or bile

56
Q

Non-renal clearance: biotransformation of drug involves Phase I, which involves (X) processes.

A

X = ox, red, or hydrolysis

57
Q

Non-renal clearance: biotransformation of drug involves Phase II, which involves (X) processes.

A

X = conjugation

58
Q

Mechanisms of renal clearance of drugs, (same/different) as clearance of endogenous substances.

A

Same;

  1. Glomerular filtration
  2. Prox tubule carrier-mediated/active secretion
  3. Passive reabsorption
59
Q

Glomerular filtration: (X)% renal blood flow is filtered.

A

X = 20

60
Q

T/F: Protein-bound drugs of any size are not filtered at the glomerulus.

A

True

61
Q

Acid drugs excreted into urine via (X) process in (Y) part of renal clearance.

A 
X = active transport (via organic anion transporter);
Y = proximal tubule secretion
62
Q

T/F: Protein-bound drugs of any size are not secreted at the proximal tubule.

A

False - protein binding doesn’t affect secretion

63
Q

T/F: Renal clearance: distal tubule reabsorption is passive and involves lipophilic, unionized drugs.

A

True

64
Q

Acid drug in alkaline urine has (increase/decrease) excretion.

A

Increase (ionized at high pH, so not passively reabsorbed at distal tubule)

65
Q

Renal clearance, Cl(R), is determined by: (equation)

A

Urine excretion rate/Cp

66
Q

When calculating renal clearance, the plasma conc (Cp) is taken at (beginning/middle/end) of time interval during which urine excretion is measured.

A

Middle

67
Q

Renal clearance (increases/decreases) with body weight and (increases/decrease) with age.

A

Increases; decreases

68
Q

(X)-mediated recycling results in long elimination half-life of IgG and many mAbs.

A

X = FcRn

69
Q

Elimination in first-order kinetics: the plot of Cp v time has which shape?

A

Curvilinear

70
Q

Elimination kinetics: in first-order kinetics, therapeutic drug levels tend to be (higher/equal/lower) than Km. List some exceptions.

A

Much lower;

Aspirin, Acetaminophen, EtOH

71
Q

Elimination kinetics: in first-order kinetics, rate of biotransformation is proportional to:

A

Concentration

72
Q

Why do elimination kinetics of EtOH and aspirin follow (X)-order?

A

X = zero

Effective drug conc is much higher than Km of enzyme of biotransformation

73
Q

Biotransformation (for elimination): Drug becomes (X) after phase 1 and (Y) after phase 2. (Y) is typically (more/less) active and (more/less) polar than parent compound.

A 
X = metabolite
Y = conjugated metabolite

Inactive and more polar

74
Q

T/F: Absorption and elimination half-lives are typically first-order, meaning a constant amount of dose eliminated/absorbed per unit time.

A

False - constant FRACTION (first-order)

75
Q

Phase 1 biotransformation carried out by (X) enzymes, which catalyze (Y) process. These are most typically located where?

A 
X = cytochrome p450
Y = addition of molecular oxygen

sER membrane (with highest activity in liver)

76
Q

Phase 2 biotransformation involves (X) process. List some moieties involved.

A

X = conjugation

  1. Glucaronic acid
  2. Sulfate
  3. Methyl groups
  4. Glutathione
  5. Acetyl groups
  6. Glycine
77
Q

T/F: Renal clearance of drugs would be reduced by renal disease.

A

True

78
Q

SC/IM drug administration: more
extensive absorption of (high/low) molecular weight, (polar/nonpolar) molecules than by
p.o. route.

A

High; polar

79
Q

(X) is an enzyme that hydrolyzes
succinylcholine. Rare gene mutation in this enzyme results in markedly (faster/slower)
clearance and (longer/shorter) elimination half-life.

A

X = Pseudocholinesterase
Slower;
Longer

Pharm (16 decks)

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