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POM Exam II > Pharmacology I > Flashcards

Pharmacology I Flashcards

1
Q

pharmacokinetics

A

movement of a drug through the body to the target site and then out of the body 4 step process 1. absorption 2. distribution 3. metabolism 4. clearance

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2
Q

Total % body weight that is water

A

60%

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3
Q

Total % body weight water that is extracellular

A

20%

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4
Q

Total % body weight water and ml/kg that is intracellular

A

40%; 0.4 L/kg

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5
Q

Total % body water weight and ml/kg that is interstitial

A

16%; 0.16 L/kg

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6
Q

Total % body weight water that is located in the plasma and ml/kg

A

4%; 0.04 L/kg

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7
Q

Most drugs reach their target site by traveling through the _____ and then transversing out

A

blood

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8
Q

Once in the circulatory system, a drug will distribute into the three body water compartments. List those compartments

A

Plasma (seperated by the epithelial layer) Interstitial (separated by the endothelial layer) Intracellular

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9
Q

Except for target IV drugs the amount of drug reaching the target is never _____

A

100%

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10
Q

Vd

A

Volume of distribution is the volume of total body water into which a drug will partition Vd= Q (dosage in mg)/Cp (plasma concentration (mg/l)

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11
Q

About how many liters of water are in a 75 kg adult

A

45 L

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12
Q

Many drugs bind/do not bind to plasma proteins, retaining them in the plasma and increasing/reducing their Vd

A

bind; decreasing

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13
Q

serum protein that and acidic drug would bind to

A

albumin ex. warfarin

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14
Q

serum protein that and basic drug would bind to

A

alpah1- acid glycoprotein

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15
Q

serum protein that and hydrophobic drug would bind to

A

lipoproteins

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16
Q

serum protein that and steroid hormone would bind to

A

globulins

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17
Q

Rank in order from highest water weight to lowest to highest water weight for brain, adipose tissue, and muscle

A
  1. adipose 2. brain (0.75l/kg) 3. Muscle (0.76 l/kg)
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18
Q

total body water content varies based on ______ and ______

A

age; total body fat content

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19
Q

older people tend to have less/more water weight

A

less

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20
Q

children tend to have less/more water weight

A

more

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21
Q

How does increased fat content affect total water weight

A

less water weight because increased water weight correlates with muscle

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22
Q

lipophilic

A

sometimes the Vd can be greater than the total volume of water in the body ex. propofol

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23
Q

Three reasons why Vd can be greater than the total volume of water int he body

A
  1. possible because Vd and Cp are inversely related 2. hydrophobicity 3. weak base drug concentrating in lysosomes due to ph trapping
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24
Q

Tissues whose cells have high levels of lysosomes

A

lungs, liver, muscle, and brain

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25
Q

An example of drug class that participates in ph trapping in cellular lysosomes

A

selective serotonin reuptake inhibitor antidepressants (SSRIs)

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26
Q

plasma protein binding drug will increase/decrease Vd

A

decrease

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27
Q

tissue binding drug and drugs that participate in ph trapping will increase/decrease Vd

A

increase

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28
Q

all drugs that are intended to reach general circulation must at least pass through ______ layer of ________ cells

A

one; epithelial

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29
Q

hydrophobic/hydrophilic drugs are absorbed through the lipid bilayers of epithelial and endothelial cells

A

hydrophobic

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30
Q

many drugs are weak/strong acids and weak/strong bases

A

weak; weak

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31
Q

protonated/un-protonated form of a weak acid can be absorbed

A

protonated because it will be uncharged and therefore will be hydrophobic

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32
Q

pka below pH

A

deprotonated form persists

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33
Q

pka above pH

A

protonated for persists

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34
Q

protonated/un-protonated form of a weak base can be absorbed

A

un-protonated because it will be uncharged and therefore will be hydrophobic

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35
Q

a weak base tends to become charged/uncharged at lower pHs

A

charged

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36
Q

example of a weak base drug

A

lidocaine

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37
Q

a weak acid tends to become charged/uncharged at higher pHs

A

charged

38
Q

example of weak acid drug

A

ibuprofen

39
Q

Henderson-Hasselbalch equation

A

allows you to calculate the ratio of charged to uncharged of a drug at a given pH; de-protonated/ protonated [A-]/[HA] = 10 ^ (pH-pka) [B]/[HB+] = 10 6 (pH-pka)

40
Q

Weak acid equation

A

HA –> H+ + A-

41
Q

Weak base equation

A

HB+ –> H+ + B

42
Q

ph < pKa for a weak acid

A

more absorbable

43
Q

ph > pka for a weak base

A

more absorbable

44
Q

pka value does/does not tell you whether the drug is a weak acid or base

A

does not; only the molecular shape

45
Q

T/F some drugs are both weak acids and weak bases depending on pKa value

A

true

46
Q

pharmacodynamics

A

(PD) how a drug molecule affects its target to produce the desired physiological effect

47
Q

absorption

A

the first pharmacokinetic phase: How does a druge get into the body?

48
Q

distribution

A

second phase of pharmacokinetics; how does the drug get to the target site?

49
Q

metabolic

A

third stage of pharacokinetic; how is a drug molecule chemically altered by the body?

50
Q

clearance

A

Fourth phase of pharmacokinetics; how does the drug get cleared/removed from the body?

51
Q

three factors that affect absorption

A
  1. surface area
  2. drug transit time (how long the drug spends in the area)
  3. pH of the lumen
52
Q

Which organ is the primary site of absoprtion and why?

A

small intestine

because

increased surface are

slow transit time

neutral pH

53
Q

What is the best organ for absorbing acidic drugs?

A

stomach

54
Q

T/F Drugs must pass through four layers of lipid bilayers if they are going to pass through epithelial and enotheilial cells

A

T

55
Q

the rates of ________ and ________ are limited by the amount of transport protein present meaning they can become _______

A

facilitated diffusion

active transport

saturated/saturable

56
Q

two types of passive transport

A
  1. Diffusion
  2. Facilitated diffusion

do not require energy

57
Q

the type of absorption that is non-saturable

A

diffusion - passive transport

58
Q

weak bases/weak acids will be better absorbed in the stomach

A

weak acids

59
Q

weak bases/weak acids will be better absorbed in the small intestine

A

weak bases

60
Q

bioavailability definition

A

the fraction of drug dose that reaches the systemic circulation (plasma)

61
Q

bioavailability of IV drug

A

100%

62
Q

T/F Bioavailability of a drug differs depending on the route of administration

A

T

63
Q

bioavailability equation

A

Area under the curve (AUC)

= (AUC(oral))/(AUC(IV))

64
Q

the bioavailabilty is measured after what effect

A

“first pass effect” = metabolic reactions in the liver

65
Q

some oral drugs may be degraded by intestinal bacteria which would decrease/increase absorption and bioavailability

A

decrease

66
Q

most drugs must reach the ______ in order to be distributed effectively

A

circulation system/ blood/plasma

67
Q

oral drugs are subject to the first pass effect that increases/decreases the drugs bioavailabilty

A

decreases

68
Q

drug binding to serum proteins affects which two phases of pharmacokinetics

A

distribution and clearance

69
Q

If Vd is 0.6 L/kg where is the drug located

A

all compartments ex. ethanol

70
Q

Vd or volume of distribution is important for calculating

A

drug half life

loading dose

rate of drug clearance

71
Q

xenobiotics

A

toxin or drugs

72
Q

which liver enzymes are largely responsible for chemical degradation /modifcation of xenobiotics via Phase I and Phase II

A

cytochrome p450

73
Q

drugs are usually metabolized in order to active/inactive them, and to facilitate their elimination via urine or feces

A

inactivate

74
Q

two phases of clearance

A

Phase I : functional phase

Phase II: congucational phase

75
Q

through the phases the drug molecule becomes more nonpolar/polar and smaller/larger

A

polar and larger

76
Q

Phase I Clearance Reactions

A

Functional Phase

can be oxidation, reduction, hydrolysis

77
Q

Phase II Clearance Reactions

A

Conjugation Phase

Glucuronidation, acetylation, methylation, sulfation, glycine, glutathione

78
Q

What class of enzyme is responsible for functional phase metabolism of xenobiotics?

A

cytochrome p450 (CYP families 1, 2, and 3

79
Q

What type of enzyme is responsible for phase II metabolism of clinically realted drugs?

A

transferases

ex. UDP-glucouronosyltrnsferase

N-acetyl- p- aminophenol

80
Q

What happens when a drug is metabolized via multiple mechanisms?

A

different percentages will be processed via each pathway

81
Q

In some cases, phase I reactions are necessary to convert a pro-drug to its ACTIVE form… provide one example.

A

Clopidogrel (plavix)

82
Q

enterohepatic circulation

A

allows metabolized drugs to be reabsorbed

83
Q

antibiotics role in enterohepatic circulation

A

antibiotics can block this effect

84
Q

how does enterohepatic circulation affect half-life of some drugs?

A

increases the half-life becuase some drugs will become reabsorbed after being metabolized

85
Q

example of a drug interaction that affects absorption

A

ex. omeprazole and cefpodoxime
ex. digoxin and antibiotics

86
Q

example of drug interactions that involve changes in distribution

A

ex. NSAIDS and Warfarin

87
Q

Drug- drug interactions that involve changes in metabolism

A

many drugs inhibit or induce the CYP enzyme systems therefore many drugs interact with each other through their effects on CYP enzymes

ex. omeprazole inhibits CYP enzyme that acts on clopidogrel

88
Q

drug-drug interactions that invovle changes in clearance

A
89
Q

four patient categories that affect pharmacokinetic

A
  1. age
  2. body composition
  3. health status
  4. genetic profile
90
Q

Polymorphisms (genetic variation) among individuals can greatly affect a drug’s pharmocokinetics. Provide and example.

A

p-glycoprotein (transmembrane protein that pumps drugs out of cells)

91
Q

polymorphisms in CYP genes lead to individual variations in _____

A

drug metabolism

92
Q
A

POM Exam II (11 decks)

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