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P1 Spring - Pharm Sci > Test 3 > Flashcards

Test 3 Flashcards

1
Q

clearance

A

volume of blood that has drug completely removed from it

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2
Q

ROE units

A

mass/time

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3
Q

concentration units

A

mass/volume

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4
Q

clearance units

A

volume/time

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5
Q

Q

A

blood flow same on both sides

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6
Q

extractor

A

organ removing drug / liver kidney etc

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7
Q

E

A

extraction ratio
whats coming in / whats coming out
.1 = 10% each time = 1st order removal always

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8
Q

ROP

A

Cin x Q

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9
Q

ROE

A

Q x (Cin - Cout)

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10
Q

E

A

ROE/ROP

(Cin - Cout)/ Cin

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11
Q

ways you could impact the ability of the extractor to remove drug

A 
blood flow
heart failure = lower Q
liver failure
- any change in Q or E
enzyme inhibitors
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12
Q

ROE is concentration independent or dependent

A

dependent / 1st order

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13
Q

clearance is a constant or variable

A

constant

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14
Q

CL =

A

vol/time

Q x E

flow rate x extraction ratio

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15
Q

ROE =

A

Cin x Q x E

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16
Q

k =

A

CL/VD

volume/time
——————- = time^-1
volume

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17
Q

inactive metabolite

A

devoid of pharmacological activity; results in termination of a drug, chemical properties are changed affecting how a drug interacts with target or changes in distribution

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18
Q

active metabolite

A

has pharmacological activity; similar to the desired activity, new activity not observed with the parent drug

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19
Q

drug bioactivation

A

parent has no activity; must be activated

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20
Q

phase 1 reactions

A

add or reveal polar functional group, generally increase H2O solubility and facilitate excretion; does not always terminate; may undergo phase 1

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21
Q

phase 2 reactions

A

conjugation; add biomolecule to a functional group or phase 1 metabolite; increase water solubility; increase molecular weight; high energy cofactors; usually terminate

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22
Q

5 types of reactions catalyzed by CYP

A 
N/S oxidation
alkene oxidation
O/N dealkylation
aromatic, acyclic, aliphatic hydroxylation
deamination
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23
Q

other phase 1 reactions

A 
epoxide hydrolase
ADH/ALDH
esterase
nitro reduction
keto reduction
azo reduction
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24
Q

most common phase 2

A

glucronidation

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25
Q

high capacity system

A

glucuronidation

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26
Q

low capacity system

A

sulfation

27
Q

protects from electrophiles, conc. usually is high but can be depleted rapidly

A

glutathione

28
Q

phase 2 reaction co substrates are rate limiting meaning

A

if one pathway becomes saturated alternative metabolic pathways can be used

29
Q

object drug

A

drug being effected; E

30
Q

precipitant drug

A

drug doing the inhibition or induction; Q

31
Q

inhibition

A

reduces activity
major issue with CYPs
rapid onset
decreases CL, increase pharm affect, decreases metabolite toxicity

32
Q

induction

A

induces activity
slow onset
less common
increases CL, decrease pharm affect, increases metabolite toxicity, increases pharm affect if prodrug

33
Q

strong inhibitors

A

greater than 80% reduction in clearance, 5 fold increase in AUC

34
Q

weak inhibitors

A

greater than 50-80% reduction in clearance, 3-5 fold increase in AUC

35
Q

cigs & charcoal broiled food

A

induces CYP1A2

36
Q

cruciferous veggies

A

induces CYP1A2

37
Q

ethanol consuption

A

induces CYP2E1; reduces GSH

38
Q

piperine

A

inhibits CYP3A4

39
Q

herbal products

A

induce / inhibit various transporters

40
Q

fruit juices

A

inhibit CYP3A4 transporters

41
Q

gene

A

the basic physical and functional unit of heredity transferred from parent to offspring that codes for a specific characteristic; it is a distinct sequence of nucleotides forming part of a chromosome, the order which determines the order of monomers in a polypeptide or nucleic acid molecule which a cell or virus may synthesize

42
Q

allele

A

a particular form or variant of a gene that can affect phenotypic expression of traits

43
Q

homozygous

A

describes an organism that possesses two identical alleles for a particular trait

44
Q

heterozygous

A

describes an organism that possess two different alleles for a particular trait

45
Q

wild type

A

a characteristic that prevails among individuals in natural conditions; the product of the normal allele

46
Q

mutation

A

a change in the nucleotide sequence of the genome of an organism that is either a result of mistakes made when DNA is copied or due to exposure to environmental factors that cause irreparable damage

47
Q

polymorphism

A

the presence of genetic variation within a population due to multiple alleles that occupy the same locus on a chromosome

48
Q

promotor

A

a region of DNA that initiates the transcription of a particular gene; a promotor is located upstream on the same strand near the transcription start site of a gene

49
Q

untranscribed regions

A

genomic sequences that are not transcribed to the primary transcript; untranscribed regions may contain important regulatory elements such as promotors

50
Q

3’

A

refers to the carbon number in DNA backbone that has a hydroxyl group attached to it

51
Q

5’

A

refers to the carbon number that has a phosphate group attached to it

52
Q

intron

A

any nucleotide sequence within a gene that is removed by RNA splicing during maturation of the final RNA product

53
Q

exon

A

any part of a gene that will encode a part of the final mature RNA produced by that gene after introns have been removed by RNA splicing

54
Q

stop codon

A

nucleotide triplet within messenger RNA that signals a termination of translation into proteins; 3 stop codons are UGA, UAA, UAG

55
Q

transcript

A

a single stranded RNA product synthesized by transcription of DNA and processed to yield various mature RNA products such as mRNAs, tRNAs, rRNAs

56
Q

gene product

A

the biochemical material, either RNA or protein, resulting rom expression of a gene

57
Q

single nucleotide polymorphism

A

SNPs; most common genetic variation among people, each SNP represents a difference in a single nucleotide; SNPs do not always cause a change in gene products activity or expression

58
Q

synonymous SNP

A

results in no change to the AA sequence

59
Q

nonsynonymous SNP

A

results in a different AA put into the gene product

60
Q

TA repreats

A

TATA box is a DNA sequence consisting of repeating thymine and adenine that indicates where a genetic sequence can be read and decoded; if TA are inserted or deleted, phenotypic changes can occur in the gene product that the TATA box precedes

61
Q

insertion

A

occurs when one or more nucleotides are added to an AA sequence

62
Q

deletion

A

occurs when one or more nucleotides are removed from an AA sequence

63
Q

nonsense mutation

A

occurs when a SNP results in a premature stop codon in protein translation, truncating the protein and most likely rendering it nonfunctional; stop codon is TAG

P1 Spring - Pharm Sci (9 decks)

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