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Exam 2 Flashcards

1
Q

Three areas that control drug performance in patients?

A

physiochemical properties, composition of formula (excipients/formulation), physiological barriers

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2
Q

What is drug performance?

A

therapeutic response, not toxic, drug/formulation/body

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3
Q

excipients

A

key ingredient for controlling drug delivery

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4
Q

coatings can be applied to

A

control diffusion rates / modify release properties

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5
Q

disintegrates can be used to

A

control regions of release based on physiochemical properties

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6
Q

lubricants can

A

slow dissolution based on properties

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7
Q

internal excipients can

A

modify release rates

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8
Q

three internal excipients

A

swellable matrices, non-swelling matrices, inert plastics

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9
Q

what can coatings accomplish

A

protect from air/humidity, mask taste, special drug release, asthetics, prevent inadvertent contact

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10
Q

aqueous film coatings contain

A

film forming polymer, plasticizer to produce flexibility, colarant/opafier, vehicle

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11
Q

enteric coating

A

prevent early release of API in region

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12
Q

sustained release

A

slow release so plasma profile is sustained

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13
Q

controlled release

A

implies reproducibility and predictability, allows us to maintain a narrow drug plasma concentration steady state

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14
Q

examples of controlled release

A

beads/granules/microspheres, multitablet, microencapsulated, drug embedding in hydrophillic matrix

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15
Q

steady state

A

rate going in body = disposition (rate being metabolized/excreted)

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16
Q

characteristics of good controlled release formulation

A

not too slow or fast absorbed/excreted, uniformly absorbed GI, small doses, good therapeutic window, chronic therapy

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17
Q

whats permeability/perfusion

A

functional and molecular characteristics of transporters and metabolism

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18
Q

epithelia

A

external surfaces, sit on extracellular proteins, polarized w directional transport

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19
Q

types of epithelia

A

simple squamous, simple columnar, translational, stratified squamous

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20
Q

simple squamous

A

thin layer of flattened cells that are permeable, lines most blood vessels-placenta

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21
Q

simple columnar

A

found in GI tract

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22
Q

translational

A

several layers with different shapes, stretch

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23
Q

stratified squamous

A

multiple layers of squamous that cover areas subject to wear and tear, comes from keratinization

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24
Q

cellular lipid composition is ______ and intracellular membrane lipids are different than extracellular lipids

A

polarized

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25
What does cholesterol provide at low levels?
fluidity
26
passive transport can be
paracellular (around) and transcellular (through)
27
carrier mediated transport can be
active (energy dep) and facilitated diffusion (energy indep)
28
PAMPA >> CACO2
efflux of pgp
29
PAMPA << CACO2
influx or paracellular transport
30
solute carrier (SLC)
43 subfamilies, >300 members, influx or efflux transporters, PepT1/OATs/OATPs
31
ATP binding cassette (ABC)
7 subfamilies, 50 members, efflux (multidrug resistant), Pgp/MRP
32
passive paracellular
hydrophillicity, molecular shape/size, pKa, can open tight junctions and increase transport
33
active transcellular
affinity (Km), capacity (Vmax), concentration dependent, expression level
34
passive transcellular
lipophillicity, molecule shape/size, pKa, increase with increasing concentration
35
oral cavity
stratified squamous
36
sublingual
simple squamous
37
esophagus
stratified squamous
38
trachea
pseudostratified squamous
39
stomach
columnar, goblet, parietal, enterochromaffin like
40
rectum
upper = simple columnar, lower = stratified squamous non keratinized to keratinized near anal sphincter
41
small and large intestines
columnar
42
fasted pH
less than 3
43
fed pH
5 to 7
44
time to gastric empty
30 mins
45
fundus (top)
gas and contractions
46
body (middle)
ingested food and fluids
47
antrum (lower)
pyloric and flow to small intestine
48
cold carbonated drinks will
induce gastric emptying
49
big mac will
slow gastric motility
50
mouth to anus transit time
24 to 32 hours
51
small intestine transit time
3 hours
52
small intestine pH
5 to 6.5
53
columnar epithelium
crypt region (goblet cells = mucus secreting, paneth cells = regulate microflora argentaffin cells = secrete mucus) villus region (absorptive enterocytes, few goblet cells and M cells) crypt migrate to villus tip
54
colon length
125 cm and slow
55
colon is responsible for
water and electrolyte absorption, prevents dehydration and leads to solid poop
56
bile salt content nM in jejunum
2.88 +/- 1.8
57
bioavailability
rate and extent of drug absorption
58
absolute bioavailability
AUC given dosage vs AUC intravenously
59
relative bioavailability
AUC given dosage vs some standard
60
bioequivalent does not mean
therapeutically equivalent
61
dose covers which two aspects
amount of chemical in whole organism, local concentration at biological site
62
drug metabolism objectives can be accomplished by
change shape molecule, change to more hydrophillic, increase molecule size, make more recognizable by efflux pumps
63
pharmaceutical equivalent
same active ingredient, dosage form, route of administration, strength, may differ in excipients / color
64
bioequivalence
rate and extension of absorption are same
65
what percent reports generic being different
30%
66
Tmax and Cmax different due to
faster dissolution
67
mimick clinical conditions (mult choice)
consider patient variables, variables not accurately assessed, absorption windows based on physical chemical, better in vitro/in vivo testing for optimizing dosage form design
68
thalidomide
caused malformations
69
Kefauver Harris Drug Amendments
require efficacy and safety demonstration
70
what percent are pediatrically labeled
20-30%
71
classification is based on
solubility, intestinal permeation, dissolution rate

Dosage (1 decks)

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