General Principles of Pharacology Flashcards

1
Q

name 3 physiochemical properties of drugs

A

molecular size
fat/water solubility
ionic charge

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2
Q

what determines the degree of fat and water solubility of drug

A

polarity of drug

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3
Q

what determines ionic charge of drug

A

acidic basic neutral nature of drug

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4
Q

how is molecular size determined

A

number and type of atoms in molecule

arrangement of molecules (sterochemistry)

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5
Q

Why is molecular size important for drug

A

determine whether it passes through pores or between cells

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6
Q

Adding what type of element makes molecules bigger

A

halogens

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7
Q

why is solubility important for a drug

A

determines if drug stays in plasma or penetrates tissue

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8
Q

what type of molecule makes a drug polar

A

ionizing

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9
Q

how is solubility measured

A

partition coefficient (P.C.)

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10
Q

formula for partition coefficient (P.C.)

A

[drug]fat/[drug]water

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11
Q

what does P.C. >1 mean

A

lipophilic

hydrophobic

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12
Q

P.C. Less than 1

A

hydrophillic

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13
Q

define acids ( weak/strong)

A

proton donor

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14
Q

for weakly acidic drugs, what are characteristics of its conjugate base

A

polar hydrophilic in plasma

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15
Q

characteristics of weakly acid drug

A

lipophillic in tissue

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16
Q

define base

A

proton acceptor

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17
Q

characteristics of weakly basic drugs

A

lipophillic in tissue

many amines

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18
Q

for weakly basic drugs, what are characteristics of its conjugate acid

A

stay in plasma

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19
Q

define neutral compounds

A

neither donates or accepts protons

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20
Q

what are two categories of neutral durgs

A

charged and uncharged

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21
Q

neuromuscular blocking drugs are what type of drugs

A

neutral charged

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22
Q

neuromuscular blocking drugs characteristics and how is it usually adminstered

A

IV

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23
Q

quaternary ammonium is what type of drug

A

neutral charge

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24
Q

carboxylic acid contributes to becoming what type of drug

A

acidic groups

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25
Q

amines contributes to becoming what type of durg

A

basic groups

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26
Q

what is so special about categorizing amino acids

A

they have both amine and carboxylic acid

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27
Q

alcohols, aldehydes, amides, esters are in what group

A

neutral uncharged

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28
Q

Henderson-Hasselbach equation determines what in drug

A

if drug is going to be ionized or unionized in its form

-whether it not it crosses barrier

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29
Q

equation for Henderson-Hasselback for weak acid

A

pH = pKa + log (base)/(acid)

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30
Q

A-

A

base form of weakly acidic drug

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31
Q

HA

A

acid form of weakly acidic drug

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32
Q

equation Henderson-Hasselback for weak base

A

pH = pKb + log (acid)/(base)

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33
Q

B

A

base form of weakly base drug

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34
Q

BH+

A

acid form of weakly basic drug

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35
Q

Name 4 ways drugs cross biological membranes

A

filtration through pores
passive diffusion
active transport
endocystosis

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36
Q

name 2 types of passive difusion

A

simple

carrier

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37
Q

how do most uncharged drugs cross the membrane

A

passive diffusion

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38
Q

how do most charged drugs cross the membrane

A

active transport

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39
Q

driving force for filtration through pores

A

pressure gradient

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40
Q

what is the rate of filtration through pores dependent on

A

pressure gradient

size of particle

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41
Q

what provides the pressure gradient for filtration through pores

A

heart contraction

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42
Q

active transport requires what

A

cellular energy

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43
Q

active transport can transport across what gradient

A

low to high

against [] gradient

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44
Q

what determines the rate of drug transport by active transportation? what does this cause?

A
  1. binding capacity of drug species with carrier
  2. limited availability of drug
    - causes competition
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45
Q

drug molecule must have what characteristic in order to move by active transport

A

full positive or full negative charge

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46
Q

passive (non-ionic) diffusion occurs in what direction?

A

high to low

proportion to physical force provided

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47
Q

when drugs cross membrane with passive (non-ionic) diffusion what characteristics must the drug have

A

dissolve in aq. solution

dissolve in lipid membrane

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48
Q

how do neutral uncharged drugs go though membrane

A

maybe pores
no active transport
maybe passively diffuse

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49
Q

how do neutral charged drugs go though membrane

A

maybe pores
maybe active transport ( permanent cations)
no passive difusion

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50
Q

how do acid form of weakly acid drugs pass

A

maybe pores
no active transport
maybe passive diffusion

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51
Q

how does base form of weakly acid drug pass

A
maybe pores 
active transport (anionic)
no passive
52
Q

base form of weak base how does it pass membrane

A

maybe pores
no active
maybe passive

53
Q

acid form of weak base, how does it cross membrane

A

maybe pores
maybe active (cationic)
little or no diffusion

54
Q

name 3 routes of enteral administration

A

oral (p.o)
sublingual
rectal

55
Q

define absorption

A

getting drug into blood stream

56
Q

define distribution

A

getting blood out of blood stream and into tissue

57
Q

define excretion

A

get drug out of body

58
Q

define elimination

A

drug biologically inactive, but does not leave the body

59
Q

what are the 3 main routes for administartion

A

enteral
parenteral
topical

60
Q

enteral administration

A

placement of drugs into GI tract

61
Q

parenteral adminstration

A

place drug into body other than GI tract

62
Q

topical administration

A

place drug on surface of tissue

63
Q

where does absorption occur for oral adminstation

A

stomach

small intestines

64
Q

during oral administration, absorption occurs primarily through what type of diffusion

A

passive

65
Q

during oral administration, rate of absorption depends on

A

rate of dissolution
PC of drug
chemical nature

66
Q

during oral administration, drugs stay longer in what part of the GI tract, why

A

small intestines

larger surface area

67
Q

where do drugs go after GI tract via?

A

liver

portal system

68
Q

first pass elimination effect

A

extensive hepatic clearance via biotransformation

69
Q

sublingual

A

drugs go under tongue

70
Q

sublingual transmission, how are drugs diffused

A

passive

71
Q

what type of drug usually uses sublingual administration

A

nitroglycerine

72
Q

during sublingual administration, where does drug enter

A

general circulation then liver

73
Q

what limits the use for sublingual adminstration

A

bad taste

74
Q

during rectal administration, how is drug diffused

A

passive

75
Q

during rectal administration, where does drug enter

A

general circulation then liver

76
Q

rectal administration is good for what type of patients

A

unconscious or vomiting patients

77
Q

diffusion form GI to blood, neutral uncharged drugs, rate of diffusion depends on

A

partition coefficient

78
Q

diffusion form GI to blood, neutral charged drug

A

low partition coefficient

little or no diffusion

79
Q

diffusion form GI to blood, weakly acidic drugs

A

uncharged most likely to diffuse

80
Q

diffusion form GI to blood, weakly basic drugs

A

uncharged most likely to diffuse

not readily absorbed in stomach, increase pH in small intestines–> absorbed

81
Q

ion trapping, give example

A

inject drug IV,

drug will be found in stomach

82
Q

name 6 ways parenteral administration is done

A
subcutaneous 
intramuscluar 
intravenous
intraarterial
inhalation
intrathecal
83
Q

where are drugs placed for subcutaneous

A

directly under skin

84
Q

what type of absorption for subcutaneos

A

passive diffusion though capillary membrane

85
Q

subcutaneous, rate of absorption

A

blood flow at injection site

86
Q

intramuscular as same characteristics as what other administration

A

subcutaneous

87
Q

what is the difference between intramuscular and subcutaneous

A

intramuscluar: uses larger volume

can use more irritating drugs

88
Q

intramuscular is good for what type of drugs?

example

A
orally labile ( easily changed) drugs 
insulin
89
Q

intramscular injections have depot preparations?

A

drug releases its active compound in a consistent way over a long period of time.

90
Q

for intravenous, where does drug go directly into

A

blood

91
Q

what is the advantage for intravanous administration

A

rapid onset
known amount of drug delivered
good for emergency situations

92
Q

what is the disadvantage for intravenous administration

A

cannot redraw drug

cannot retard absorption

93
Q

intraaterial , where is drug directly placed

A

into artery leading to specific organ or tissue

94
Q

what is a benefit for using intraaterial

A

high [drug] into one body site

95
Q

intraarterial is used with what patients

A

cancer chemotherapy

96
Q

inhalation is primarily used for

A

anesthetic/analgesic gases

97
Q

inhalation h as what type of absoprtion

A

passive

98
Q

for intrathecal where does injection occur into

A

spinal subarachnoid space

99
Q

what is intrathecal used for

A

spinal anesthesia

CNS chemotherapy

100
Q

what are 3 topical administration types

A

patches
dermatological and opthalmic
intravaginal

101
Q

dermatological and ophthalmic application ….

intravaginal application deals with what

A

not absorption but deals with infection on surface

102
Q

the first critical step for drugs is absorption, what is the second critical step

A

getting drug out of blood stream to sight of action

103
Q

name 5 factors that influence drug distrubution

A
physiochemical 
biological membranes
protein binding 
blood perfusing 
disease states
104
Q

what is the first barrier of drug distrubtion

A

capillary endothelial membrane

105
Q

name 2 locations for special capillary beds

A

kidney: glomerulus
liver: lack complete endothelial cell lining

106
Q

what is the difference between water soluble and lipid soluble drugs entering cell

A

only lipid soluble enters

107
Q

how do drugs cross the BBB

A

passive diffusion

108
Q

BBB have what type of barrier

A

tight junctions between brain capillary endothelial cells

109
Q

how and where do drugs enter CSF

A

passive diffusion - ventricles

active transport - choroid plexus

110
Q

fetal barrier - placenta have similar characteristics to what

A

capillary beds

111
Q

do drugs enter the placenta

A

most drugs yes

112
Q

what is pH of prostate fluid

A

acidic 6.4 compared to plasma

113
Q

how do drugs enter prostate, what happens to them

A

passive diffusion

protonated (ionized), ionic form of basic drug can’t diffuse out, ion trapping

114
Q

what is the blood supply to prostate gland compared to other organs

A

low

115
Q

where does protein occur

A

plasma

tissue

116
Q

what is the strongest bond type for protein binding

A

covalent, may be irreversible

117
Q

compared to proteins, drugs are pharmacologically active when

A

free in plasma, not bound to protein

118
Q

what is therapeutic index

A

more likely the drug is free in plasma

119
Q

common protein drugs attach to

A

albumin

120
Q

lipid soluble drugs can be stored where

A

fat

121
Q

what is the blood supply to fat

A

poor

122
Q

what drug and metal gets stored in bones

A

tetracycline

lead

123
Q

where can drugs get stored in non-target tissue

A

kidney

124
Q

what can redistribution of drugs do

A

terminate pharmacological action of drugs, especially lipophilic drugs

125
Q

initial distribution of drug depends on

A

blood flow to a body region

126
Q

what does redistribution depend on

A

other factors other than blood flow