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P1 Spring - Pharm Sci > Test 2 - definitions > Flashcards

Test 2 - definitions Flashcards

1
Q

3 major physiologic factors that affect drug distribution

A

blood flow, body composition, protein binding

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2
Q

3 major drug factors that affect drug distribution

A

lipophiliicity, size, ionization

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3
Q

2 major plasma protiens

A

albumin & alpha 1 glycoprotien

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4
Q

albumin

A

prefers acidic binding & hydrophobic; typically constant levels

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5
Q

alpha 1 acidic glycoprotien

A

binds to basic drugs; stressed induced

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6
Q

plasma protein binding is ___ & ___

A

saturable and reversible

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7
Q

amount of drug bound to a plasma protein is determined by

A

drug concentration, # of available binding sites, affinity of drug for protein

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8
Q

what causes pharmacological effect

A

free drug

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9
Q

ion trapping

A

when an ionized species of drug accumulates in a specific tissue or organ, more drug ionized on one side than the other, accumulation of drug in a specific tissue that doesn’t reflect the plasma concentration

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10
Q

Vd

A

hypothetical volume; apparent volume of distribution

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11
Q

Vd ___ describes _____

A

indirectly; the extend to which a drug distributes outside of the plasma compartment which is one of the water compartments within the body; proportionally constant related to the amount of drug in the body to the plasma concentration

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12
Q

Vd is a ____ pharmacokinetic paramater

A

independent; it is dictated by the characteristics of the DRUG such as ionization, lipophilicity, size, etc

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13
Q

Vd is always a ___ divided by ___

A

mass over volume

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14
Q

C0 must be assumed to be

A

instantaneous distribution

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15
Q

total body water = __ X body weight

A

.6

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16
Q

ECF = __ X body weight

A

.2

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17
Q

ICF = ___ X body weight

A

.4

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18
Q

ECF = ___(3/4) & ___(1/4)

A

Interstital fluid / Plasma

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19
Q

Vd (once divided by kg): less than .6 = drug in ___ more than .6 = drug in ___

A

plasma tissues

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20
Q

smaller Vd means more drug is in the

A

plasma bc of protein binding

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21
Q

pericytes

A

have tight junctions between cells to limit diffusion of drug into CNS

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22
Q

PgP also work to

A

pump out toxins and drugs from the brain

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23
Q

what could hinder a drug from passing through BBB

A

large, charged, hydrophillic

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24
Q

metabolism

A

refers to the process by which the administered drug is biochemically altered producing a metabolite

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25
Q

metabolites typically have ___ activation

A

little but some can have significant

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26
Q

pro-drug

A

inactive but upon metabolism release or form active drug

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27
Q

excretion

A

removal of drug from body

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28
Q

___ is the primary organ for excretion

A

kidney, but some drug can be eliminated through bile

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29
Q

when a drug is renally excreted, we mean that ____ is eliminated

A

unchanged parent drug

30
Q

the purpose of drug metabolism is to

A

increase water solubility, increase polarity, and increase H-bonding partners

31
Q

hepatocytes work through what 2 functions

A

passive diffusion & carrier transporters

32
Q

OATP enzymes

A

shuttle drug across membrane into hepatocye taken from GI tract

33
Q

MRP1 / P3 / P4 ABCC1 / C3 / C4

A

work to shuttle drug out of hepatocyte into the blood stream

34
Q

MDR3 / R1 / P2 ABCB4 / B1 / C2

A

filter blood into bile canaliculus for excretion

35
Q

what are the two types of hepatic metabolism

A

Phase 1 and phase 2

36
Q

phase 1

A

introducing or exposing a functional group to increase polarity; these can be redox, hydroxylation, hydrolysis typically removing methyl and adding NH or OH to prepare metabolite for phase 2

37
Q

phase 2

A

conjugating reactions, adding a molecule or large functional group, hydrophilic

38
Q

CYP450 are examples of phase 1 or 2

A

1

39
Q

UGT are examples of phase 1 or 2

A

2

40
Q

CYP450 enzymes

A

involved in many biochemical reactions involving endogenous substrates, including steroids, fatty acids, prostaglandins, and bile acids. they are critically involved in the removal of drugs, carcinogens, insecticides, plant toxins, and environmental pollutants

41
Q

CYP2D6 2 represents ___ & what percent homology D represents ___ & what percent homology 6 represents ___ & what percent homology

A

family (40%) subfamily (55%) gene product (different unless identical)

42
Q

CYP1, CYP2, CYP3 substrates?

A

drugs, other xenobiotics

43
Q

CYP4, CYP5, CYP8 substrates?

A

fatty acids, prostaglandins, thromboxanes

44
Q

CYP7, CYP11, CYP17, CYP21, CYP24, CYP27 substrates?

A

steroid hormones

45
Q

what CYP accounts for 34% in drug metabolization

A

3A4/5

46
Q

1A1, 1A2, 2E1, 3A3, 3A4,5

A

nutrition

47
Q

1A1, 1A2

A

smoking

48
Q

2E1

A

alcohol

49
Q

1A1, 1A2, 2A6, 2B6, 2C, 2D6, 3A3, 3A4,5

A

drugs

50
Q

1A1, 1A2, 2A6, 1B, 2E1, 3A3, 3A4,5

A

environment

51
Q

1A, 2A6, 2C9,19; 2D6, 2E1

A

genetic polymorphism

52
Q

phase 2 relationship to CYP

A

phase 2 occurs after CYP450 has metabolized drug but can also work independently of phase 1

53
Q

phase 2 almost always

A

inactivated the parent drug molecule, but there are some instances where a phase 2 metabolite could still have activity

54
Q

excretion by the kidney is determined by what 3 factors

A

filtration reabsorption secretion

55
Q

filtration

A

occurs in glomerular capillary; cut off point is 5000 daltons

56
Q

reabsorption

A

from filtrate back into the blood happens in the peritubular capillaries (works against drug removal!!!)

57
Q

properties that assist reabsorption

A

nonionized & lipophilic

58
Q

secretion

A

from peritubular capillaries into the tubular space

59
Q

properties that assist secretion

A

lipophilic; transporters

60
Q

amount excreted by kidney =

A

amount filtered - amount reabsorbed + amount secreted

61
Q

what percent of blood actually gets filtered

A

20%

62
Q

amount

A

X, amount given to the patient at the start time of dosing, dose is frequently called X0, mass amount gms, mgs, etc

63
Q

concentrations

A

C; always amount divided by a volume; mg/L, mcg/mL

64
Q

rate

A

a change is something per unit time; can be first or zero order

65
Q

rate constant

A

k, constant rates, do not change with time, determined by slope

66
Q

K for zero order rate is

A

constant

67
Q

elimination rate in zero order is

A

constant

68
Q

zero order characteristics

A

concentration independent elimination; high substrate concentrations

69
Q

K for a first order is

A

a rate constant

70
Q

elimination rate of drug removal is

A

variable

71
Q

first order characteristics

A

concentration dependent elimination; low substrate concentrations

P1 Spring - Pharm Sci (9 decks)

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