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Fundies Second test > pharmacokinetics > Flashcards

pharmacokinetics Flashcards

1
Q

parmacokinetics = ADME

A 
ADME
Absorption
Distribution
Metabolism
Excretion
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2
Q

ratio of molar mass to the molar mass constant

A

molecular weight MW

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3
Q

Molecular weight – why important for drugs

A

g/mol
most drugs in range of 250-450
* passage through pores

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4
Q

solubility goes up as _____ goes up

A

temperature – usually

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5
Q

the maximum concentration of a substance that may be completely dissolved in a given solvent at a given temp/ pressure

A

solubility

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6
Q

the only form of an aqueous solution that a drug can be absorved into the gen circulation to exert a therapeutic effect

A

aqueous solubility

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7
Q

factors that affect drug solubility 4

A
  1. temp
  2. multiple solutes
  3. solute/solvent polarities
  4. pH
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8
Q

drug must be soluble in _______ to pass through membrane and soluble in ____ to be disolved. conundrum

A

lipid-

water

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9
Q

solvents may be ______, _______, or _______

A

polar, semi-polar, non-polar

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10
Q

like dissolves _____

A

like

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11
Q

semi-polar solvent ex.

A

alcohols and ketones–may be added to improve solubility of polar and non-polar liquids

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12
Q

molecular state=

ionic state=

A

undissociated states -

dissociated states

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13
Q

altering the pH of solution or using the ____ form of the compound may ^ or v solubility

A

salt–

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14
Q

Form a solvent system of optimum polarity or mix solvents of dif polarities to form a solvent system of optimum polarity to dissolve the solute

A

solvent blending or cosolvency

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15
Q

most drugs exist as weak _________; either weak ______ or weak _______

A

electrolyte-

acid or base

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16
Q

molecule that takes on (-) by giving H+

A

acid– HA = A- + H+

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17
Q

molecule that accept proton and become + charge molecule

A

cation- anion

BH+ = B + H+

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18
Q

salt form

A

A- or BH+

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19
Q

the pH at which 50% of the molecules are ionized and 50% are unionized

A

pKa

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20
Q

pKa

A

pH at which 50% of the molecuels are ionized and 50% are unionized

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21
Q

if has + or - sign

A

soluble in water

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22
Q

unionized form of acid or base (respectively)

A

HA or B

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23
Q

more soluble salt form:

biologically active acid or base:

A

A- or BH+
HA or B
In biological systems drug will move back and forth

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24
Q

henderson-Hasselbalch equation

A

pH = pKa + log study pic on page 6 of notes

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25
Q

in acidic environment if pH < pKa

A

more HA and BH+

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26
Q

in basic environment if pH >pKa

A

more A- and B

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27
Q

a weakly acidic drug will accumulate on the more ____ side of membrane

A

basic

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28
Q

weakly basic drug will accumulate on the more _____ side

A

acidic

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29
Q

for our purposes HA=

A

nonpolar so well move through GI wall –HA will be made in highly H+ environment of stomach–trapped out of stomach

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30
Q

in stomach HA will be made preferentially from A- + H+ then

A

move out of stomach and be turned back to A- + H+ and be trapped in blood

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31
Q

interplay of ionized and unionized form leads to

A

trapping–as in kidneys–> body can alkalized urine to “trap” drugs wo we can get rid of them

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32
Q

some drugs are weak base liquids naturally but can be _____ with another ____ to make it a _____

A

pairing-
ion-
salt

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33
Q

second name in generic drug name

A

salt molecule that drug is paired to– i.e. fluiticasone PROPRIONATE

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34
Q

pairing can be through ____ or _____ bonds

A

covalent or ionic

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35
Q

zonula occludens aka

A

tight junctions (protected tissues)–limit membrane permeability to ion channels

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36
Q

protected tissues

A

BBB

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37
Q

movement into area through GAP between cells

A

paracellular pathway–some leaky for small solutes and ions

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38
Q

paracellular pathway vs.

A

transcellular pathway (BBB’s only path)

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39
Q

no energy needed aside from concentration gradient

A

passive diffusion

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40
Q

key method for drug distribution to unrestricted tisues

A

paracellular pathways

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41
Q

key driving force for paracellular pathway

A

hydrostatic pressure (also influenced by oncotic pressure and drug concentration gradient)

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42
Q

requires energy

A

active transport

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43
Q

Rate of diffusion=

A

concentration grade X surface area X diffusion coefficent/ Membrane thickness

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44
Q

diffusion coefficent =

A

permeability/ molecular weight

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45
Q

Diffusion rate increased by:

A
  1. ^ concentration gradient (large dif inside and out)
  2. ^ surface area
  3. ^ diffusion coefficent (^ perm membrane & v MW)
  4. small membrane thickness
  5. ^ lipid/water partition coefficient (lipophilic solutes have larger coefficients)
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46
Q

Active transport is: 2

A
  • Primary active transport (protein directly uses energy 2 transport
  • Secondary active transport uses electrochemical potential difference to fuel transport (coupled transport = symporters/antiporters)
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47
Q

process of engulfing particles or dissolved materials by cell

A
  1. endocytosis

2. exocytosis

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48
Q

connected to absorption is the _____ __ _______

A

route of administration–formulated w/ this in mind

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49
Q

why would DISSOLUTION/ ABSORPTION rate need to be changed?

A

to prolong the duration of action (“controlled release” “extended release”)

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50
Q

step 2 of drug absorption

A

dissolution–usually takes place in stomach but can be coated for later release

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51
Q

How is dissolution rate slowed

A
  1. water-insoluble coating
  2. drug embedded in matrix
  3. etc.
    Mostly absorbed in L intestines
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52
Q

if absorption slowed too much

A

active drug will be excreted

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53
Q

drug in
Stomach:
Small intestines
Large intestines

A

2-4 hrs (depends on acidity–more food=^acidity–> ^ dissolu.)
4-10 hrs
12-15 hrs

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54
Q

oral drug must cross _____ ____ lining GI tract before entering circ system

A

epithelial cells

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55
Q

time drug given

A

zero time

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56
Q

the extent and rate at which the active moity (drug or metabolite) enters systemic sirculation

A

bioavailability

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57
Q

bioavailability of IV drug admin

A

100%

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58
Q

moity

A

drug or metabolite

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59
Q

causes for low bioavailability

A
  1. insufficient absorption (insufficient time, reduced absorption)
  2. first-pass metabolism
  3. age, sex, physical activity, genetics, stress, GI problems, surg, etc.
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60
Q

Bioavailability assessed by AUC

A

area under the curve–
X axis: time
Y axis: plasma drug concentration

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61
Q

AUC of IV admin at zero time

A

100%

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62
Q

biovailability (AUC) measured with

A

frequent drug draws after drug administration

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63
Q

time when maximum plasma drug concentration occurs

A

peak time (most widely used general index of absorption rate)

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64
Q

Tmax

A

time it took to reach Cmax (peak drug concentration in plasma)

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65
Q

process of the delivery of a drug from systemic circulation to tissues

A

distribution

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66
Q

distribution to –>

A

extravascular fluid vs.

site of action

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67
Q

ECF and ICF in __________ equilibrium

A

osmotic–solute concentration on each side are balanced) i.e. no osmosis

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68
Q

fluid component of blood

A

plasma (intravascular compartment) of ECF

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69
Q

kidney has speciealized cells that detect the ________ ______ gradients–> signal to either ^orv pressure

A

hydrostatic pressure

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70
Q

cond. too much fluid in interstitial compartment

A

edema

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71
Q

interstitial compartment supplied and collected by

A

lymph vessels

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72
Q

space where there is no physiological functions for that fluid

A

“third space”

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73
Q

TBW raises as we get ______

A

older

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74
Q

Two phases of distribution

A
  1. cardiac output and regional blood flow

2. total equilibrium of blood

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75
Q

Vd –pg 28 in packet

A

apparent volume of distribution–refers to the space in the body into which the drug apears to disseminate

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76
Q

Vd

A

over time: plasma => plasma+interstial fluid=>plasma+interstitial fluid+intracellular

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77
Q

just in plasma:

A

low Vd- (mostly likely bound to plasma proteins cant escape)

large concentration

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78
Q

distributed to all compartments

A

high Vd-

small concentration

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79
Q

Vd tells us _____ drug is distributed but not ______

A

where-

why

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80
Q

proteins in general are weakly ____

A

basic – likes to bind to acids–so acidic drugs will bind to albumin and stay in blood plasma

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81
Q

basic drugs tend to want to bind to ____ ______

A

tissue proteins (vs. plasma)–thus high Vd

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82
Q

most common protein in whole body

A

albumin in plasma–made in liver

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83
Q

drug able to have physiological effect

A

unbound and ionized–non-depot bound

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84
Q

alpha1- acid glycoprotein and lipoprotiens

A

binds weak bases in plasma–low CAPACITY high AFFINITY

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85
Q

lipoprotein types

May bind drugs when albumin saturated

A

low density lipoproteins LDL
very low density lipoproteins VLDL
High density lipoproteins HDL

86
Q

lipoproteins bind

A

basic drugs

87
Q

drugs can also bind too _______

A

erythrocytes–45% of plasma volume–

88
Q

*protein binding is considered when drugs designed, thus problems arise when _____ blood proteins produced

A

less–

less albumin w/ liver disease, protein catabolism, protein distribution, ^ renal excretion

89
Q

adjustments in dosing based on protein binding must be made considering:

A
  1. pt health (renal disease hypoalbuminemia, liver disease, age, sex, edema, BMI, relative blood flow, capillary permeability
90
Q

sexual dimorphism in relation to drug dosing

A

physiological and hormonal

91
Q

age differences in relation to drug dosing

A

aging affects every organ–^ toxicity due to v excretion

92
Q

BMI range in drug studies important due to

A

lipophilic drugs can alter drug concentration/distribution-

may see: “dose using ideal body weigt” –same for fat/thin ppl

93
Q

“dose using adjusted body weight” on label means

A

estimate the proportion of adipose tissue that distributes medication

94
Q

“dose using total body weight” on label means

A

more drug given to obese pt

95
Q

imp for drug dosing in relation to circulatory system

A
  1. relative blood flow
  2. cardiac output
  3. specific tissue perfusion rates
96
Q

distribution slow in

A

poorly perfused tissues (muscle, fat)

97
Q

^ perfusion rate

A

^ drug concentration

98
Q

the rate of blood flow through capillaries per unit mass of tissue

A

perfusion rate (depends on amount of blood flow & size of tissue)

99
Q

capillary permeability

A

drug gets out mainly using pericellular pathway: greater->less permiable
liver>kidney>muscle = fetus > Brain

100
Q

lipid solubility most important when trying to get drugs to _____ ______

A

restricted spaces

101
Q

ion trapping

wealy acidic drugs are _______ in _____ ________

A

trapped in basic environments

102
Q

wealy basic drugs are trapped in _______ ______

A

acidic environments

103
Q

water soluble drugs (dissolve in water) tend to stay in

A

blood and the interstitial space (DRUG RESERVOIR)

104
Q

tetracyclin loves

A

calcium–accumulates in teeth (yellow)

105
Q

resevoir for lipid soluble drugs

A

adipose tissue

106
Q

tissue reservoir ex.s

A

Bone
GI tract
Thyroid

107
Q

Astrocyte foot processes secrete _____ to promote tight junction formation

A

paracrines

108
Q

epithelial cells of the _____ ____ also contain ____ ______–contributing to BBB along w/ astrocytes

A

choroid plexus
tight junctions
inflamation can break down barrier

109
Q

acid in acidic environment will be in _____ form

A

bound–HA

because much free H+

110
Q
  • placental barrier somewhat like ____

- fetal plasma is slightly more _____ than mothers, thus ion trapping of ____ drugs

A
  • BBB

- acidic, basic

111
Q

the irreversible removal of drug from the body by all routes

A

drug clearance

112
Q

____ and _____ clearance mechanisms

A

simple and complicated

113
Q

MAJOR organs for drug clearance

A

liver & kidney

114
Q

liver cells

A

hepatocytes

115
Q

minor drug clearance systems

A
  1. sweat glands
  2. lungs
  3. GI tract
  4. breast milk
116
Q

two drug clearance components

A

metabolism and excretion

117
Q

metabolism aka

A

biotransformation (enzymatic process)

118
Q

conjugation makes drug more

A

water soluble–ionic

119
Q

reduced as opposed to

A

oxidized

120
Q

product of biotransformation

A

metabolite

121
Q

Highest concentration of enzymes

A

GI tract– liver>small intestines>large intestines

122
Q

liver wants to _______ drug and make it more ______ _______

A 
inactivate,
water soluble (inhibit movement through lipid bilayer)
123
Q

inactive drug or less active drug–pre-activated by liver metabolism

A

pro-drug (longer half-life or more potent)

124
Q

drugs carried to liver from GI tract via the

A

portal vein “first pass metabolism”

125
Q

metabolite types

A

active vs inactive

126
Q

phase I rxn

A

(redox) does little to change the water solubility of the drug but does significantly alter the biologic properties of the drug–altered pharmacodynamics

127
Q

Phase II rxn’s

A

(synthetic rxn) increases drug polarity and water solubility.

128
Q

phase II rxn’s involve

A

conjugation with an endogenous substance (i.e. glycine, sulfate)

129
Q

phase I vs. phase II rxn’s

A

oxidation vs. conjugation

130
Q

if drug goes through phase I red/ox rxn’s and is still too neutral for excretion

A

will go for second pass through liver

131
Q

if you want to make something polar

A

conjugate it

132
Q

no drug has ____% protein binding

A

zero–given by manufacturer in %

133
Q

enzymatic system for Phase I rxn’s

A

cytochrome P450 system (CYP450)–6 isoenzymes metabolize 90% of drugs

134
Q

CYP450

A

catalyzes the oxidation of many drugs

135
Q

*metabolizes 50% of drugs

A

CYP3A4–CYP450 isoenzyme

136
Q

CYP450 enzymes located in

A

smooth ER particularly in hepatocytes (also in small intestine, lungs, placenta, kidneys)

137
Q
  • metabolizes 30% of drugs
A

CYP2D6

138
Q

redox is

A

protons changing molecule

139
Q

electrons supplied during oxydation by

A

NADPH –> NADP+

140
Q

functional groups for redox ex’s

functional groups unmasked or introduced

A

OH
NH2
SH
COO-

141
Q

reduced means

A

it can receive proton

142
Q

CYP450 drug-drug interaction considerations

A

Inhibition –> slows metabolism
Induction –> speeds metabolism
So, if drug “inhibits” CYP450 system (particularly CYP3A4)–will get ^ interactions

143
Q

CYP450 genetic polymorphisms–responsible for variations in drug metabolism

A 
ppl may be:
1. "extensive" metabolizer
2. normal
3. "poor" metabolizer
Checked through plasm concentrations
144
Q

Phase II rxn–named for functional group added

A

phase II enzyme

Drug ______________> Drug Conjugation

145
Q

Phase II functional groups added–essentially makes new molecule and very polar

A
  1. Glucuronide
  2. amino acids
  3. acetyl group
  4. sulfate ester
  5. methyl group
    come from diet–rate limiting step
146
Q

drugs may need to go through phase ___ rxn before able to go through phase ___ rxn

A

I, II

147
Q

Glucuronidated molecules secreted in ____ and eliminated in ______

A

bile-

urine

148
Q

amino acid conjugation with

A

glutamine or glycine – readily excreted in urine

149
Q

upper limit in the metabolism rate in any given pathway

A

capacity limitation of Rate of Metabolism

150
Q

half-life will be prolonged if

A

the metabolizing sites are at capacity

151
Q

*if liver damage/ disease

A

need to make dose adjustment

152
Q

Protein poor/ rich diet will ____/_____ drug metabolism

A

slow/speed

153
Q

intestinal microflora (anaerobic microbes which colonize gut) are rich in ______

A

reductases (similar to liver metabolic processes) –may metabolize drugs before their absorbed

154
Q

principle mechanism of eliminating drug from body

A

renal excretion–

155
Q

*( read excretion portion in packet before exam)

excretion=

A

flitration - reabsorption +secretion

156
Q

first step in urine production

A

glomerular filtration–

157
Q

_______ ______ (arterial blood pressure) drives filtrate into glomerulus of kidney

A

hydrostatic pressure

158
Q

allows recovery of drugs filtered by glomerulus

A

active tubular reabsorption–2nd step

159
Q

the transfer of materials from the peritubular capillaries into the renal tubular lumen

A

active tubular secretion

160
Q

liver secreation of 1 L of bile/ day contributes to

A

biliary excretion

161
Q

volatile drugs primarly excreted by

A

pulmonary excretion (breathed out)–passive diffusion into lungs

162
Q

extremely _____ soluble drugs, penetrate milk in higher concentration almost without exception

A

lipid

163
Q

Milk is _____ acidic than blood

A

more–will trap weak bases

164
Q

how long before drug is half concentration from time-point

A

T1/2

half-life

165
Q

half-life important for determining

A

frequency of administration

166
Q

adjusting dosage according to T1/2, physiological marker, or toxicity

A

“dosing for effect”

167
Q

time it would take for a drug to lose half of its effectiveness or efficacy

A

efficacy half-life–less precise than plasma CO

168
Q

concentration at which a pharmacologic response first occures

A

minimum effective concentration MEC

169
Q

Cmax

A

peak concentration

170
Q

maximum amount of drug when ADRs occure at a high enough rate to make it intolerable or dangerous for pt

A

“upper limit of drug concentration”

171
Q

dosing the same druge at teh same dose multiple times at regular intervals to build up in body

A

drug accumulation

172
Q

time it take to reach the peak concentration

A

Tmax – time to peak concentration

173
Q

drug in = drug out

plasma levels stay consistant–use “loading dose”

A

“steady state” – peaks and troughs
formula used
CL= renal clearance

174
Q

goal of dosing regimen

A

one where steady-state conentration is reached as quickly as possible while maximizing benefit and minimizing harm to the pt.

175
Q

how often a pt needs to take the drug in order to reach a steady state concentration

A

Css

176
Q

Tylenol–not NSAID

A

acetominophen–MAO

177
Q

acetaminophen and NSAIDs both

A

inhibit COX-2

178
Q

Cyclooxygenae COX enzymes convert _____ ____ to _________

A

arachidonic acid,

prostaglandins

179
Q

key role in pain, inflammation, cell proliveration, mucus production, fever

A

prostaglandins

180
Q

COX1 roles

A

“housekeeper”

  1. gastric (^ mucus prod) and renal protection
  2. COX1 platelets aid in clotting
  3. kidney profusion
181
Q

COX1

A

constitutive

182
Q

COX2

A

inducible

183
Q

increased in response to inflammation

A

COX2

184
Q

inflammation symptoms 4–mediated by prostaglandins

A

pain, swelling, redness, and warmth

185
Q

inhibiting COX2 will decrease

A

pain, swelling, redness, and warmth

186
Q

COX2 in the kidney

A

helps regulate water and Na excretion–inhibition–>fluid retention

187
Q

COX 1,2, and 3 involved in _________ synthesis

A

prostaglandin

188
Q

unlike NSAIDS, ________ doesn’t inhibit COX in peripheral tissues thus no peripheral ____-_____ affects

A

acetaminophen-

anti-inflammatory

189
Q

acetominophen’s blackage of COX is ineffective in presence of ________

A

peroxides (high in platelets and immune system)

190
Q

antipyretic properties of acetominophen due to

A

effects on the heat-regulating center of the hypothalamus –> peripheral vasodilation, sweating –> heat dissipation

191
Q

only analgesic approved for infants <6 months

A

acetaminophen

192
Q

acetaminophen highly metabolized through _____ __ rxns in _____

A

Phase II,
liver
(toxic metabolite when phase I–hepatotoxic) so need to ask pt what OTCs taking

193
Q

alcohol is

A

conjugated–thus drug-drug interactions but not many others for acetamenophen

194
Q

Know:

A

drug list

195
Q

ibuprofen is ________ COX inhibitor

A

NONSELECTIVE–pain, fever, swelling, inflammation

196
Q

ibuprofen inhibits

A

prostaglandin synthesis

197
Q

ibuprofen more potent than

A

acetaminophen

198
Q

onset of action for ibuprofen for pain and fever

A

30 min–first time dose vs. inflammation (higher dose needed)

199
Q

ibuprofen ______ binds to albumin (_______%)

A

avidly,

90-99%

200
Q

ibuprofen metabolism

A

extensive and rapid metabolism by liver (CYP450 & v phase II)

201
Q

ibuprofen should be taken w/ food due to

A

COX1 inhibition–> ulcers, upset stomach, dyspepsia,

202
Q

highest cause of gastric ulcer

A

ibuprofin–discontinue use

203
Q

strong FDA warning

A

“black box” warning

204
Q

prostaglandins important for renal __________, so for vulnerable populations (those with kidney disease)

A

ibuprofin limit blood flow through kidney–very dangerous–not for normal people

205
Q

COX in afferent arteriales in kidney

A

keeps arterial open–disrupted by ibuprofen–> stops blood flow

206
Q

acetamenophen inhibits only

A

CENTRAL COX2

207
Q

cardiovascular risk of ibuprofen

A

black box warning– ^ risk of thrombotic event from COX II inhibition

208
Q

2 things to remember w/ ibuprophen–too many ADRs to remember or list

A
  1. any drug can cause any symptom

2. any pt can have an allergic rxn to any drug

209
Q

imp Ibuprophen ADRs

A

GI tract
kidneys
heart

210
Q

2 main enzyme systems

A

3A4

2D6

211
Q

(2) more acidic than blood–will trap ___ drugs

A

Breast milk,

amniotic fluid

212
Q

Principle means of phase II reaction

A

Conjugation– GLUCURONIDATION

Fundies Second test (8 decks)

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