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Dosage > Exam 2 > Flashcards

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
Q

What does cholesterol provide at low levels?

A

fluidity

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26
Q

passive transport can be

A

paracellular (around) and transcellular (through)

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27
Q

carrier mediated transport can be

A

active (energy dep) and facilitated diffusion (energy indep)

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28
Q

PAMPA&raquo_space; CACO2

A

efflux of pgp

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29
Q

PAMPA &laquo_space;CACO2

A

influx or paracellular transport

30
Q

solute carrier (SLC)

A

43 subfamilies, >300 members, influx or efflux transporters, PepT1/OATs/OATPs

31
Q

ATP binding cassette (ABC)

A

7 subfamilies, 50 members, efflux (multidrug resistant), Pgp/MRP

32
Q

passive paracellular

A

hydrophillicity, molecular shape/size, pKa, can open tight junctions and increase transport

33
Q

active transcellular

A

affinity (Km), capacity (Vmax), concentration dependent, expression level

34
Q

passive transcellular

A

lipophillicity, molecule shape/size, pKa, increase with increasing concentration

35
Q

oral cavity

A

stratified squamous

36
Q

sublingual

A

simple squamous

37
Q

esophagus

A

stratified squamous

38
Q

trachea

A

pseudostratified squamous

39
Q

stomach

A

columnar, goblet, parietal, enterochromaffin like

40
Q

rectum

A

upper = simple columnar, lower = stratified squamous non keratinized to keratinized near anal sphincter

41
Q

small and large intestines

A

columnar

42
Q

fasted pH

A

less than 3

43
Q

fed pH

A

5 to 7

44
Q

time to gastric empty

A

30 mins

45
Q

fundus (top)

A

gas and contractions

46
Q

body (middle)

A

ingested food and fluids

47
Q

antrum (lower)

A

pyloric and flow to small intestine

48
Q

cold carbonated drinks will

A

induce gastric emptying

49
Q

big mac will

A

slow gastric motility

50
Q

mouth to anus transit time

A

24 to 32 hours

51
Q

small intestine transit time

A

3 hours

52
Q

small intestine pH

A

5 to 6.5

53
Q

columnar epithelium

A

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
Q

colon length

A

125 cm and slow

55
Q

colon is responsible for

A

water and electrolyte absorption, prevents dehydration and leads to solid poop

56
Q

bile salt content nM in jejunum

A

2.88 +/- 1.8

57
Q

bioavailability

A

rate and extent of drug absorption

58
Q

absolute bioavailability

A

AUC given dosage vs AUC intravenously

59
Q

relative bioavailability

A

AUC given dosage vs some standard

60
Q

bioequivalent does not mean

A

therapeutically equivalent

61
Q

dose covers which two aspects

A

amount of chemical in whole organism, local concentration at biological site

62
Q

drug metabolism objectives can be accomplished by

A

change shape molecule, change to more hydrophillic, increase molecule size, make more recognizable by efflux pumps

63
Q

pharmaceutical equivalent

A

same active ingredient, dosage form, route of administration, strength, may differ in excipients / color

64
Q

bioequivalence

A

rate and extension of absorption are same

65
Q

what percent reports generic being different

A

30%

66
Q

Tmax and Cmax different due to

A

faster dissolution

67
Q

mimick clinical conditions (mult choice)

A

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
Q

thalidomide

A

caused malformations

69
Q

Kefauver Harris Drug Amendments

A

require efficacy and safety demonstration

70
Q

what percent are pediatrically labeled

A

20-30%

71
Q

classification is based on

A

solubility, intestinal permeation, dissolution rate

Dosage (1 decks)

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