Toxicokinetics Flashcards

1
Q

Most common route of exposure in toxicology

A

oral

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2
Q

____ route important in toxic gases and insecticides

A

inhalation

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3
Q

____ route important in insecticides

A

dermal

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4
Q

____ is where a metabolite is more toxic/important than the parent compound

A

Lethal synthesis

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5
Q

The transfer of the toxin from site of administration to systemic circulation is the

A

absorption

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6
Q

T/F: the smaller the molecular size, the faster the penetration through cell membrane pores

A

true

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7
Q

T/F: increased lipid solubility decreases absorption

A

false, it increases it

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8
Q

T/F: the more non-ionized, the greater the absorption

A

true

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9
Q

T/f: the lower the concentration of the drug at absorptive site, the faster the absorption

A

False

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10
Q

What is first pass effect?

A

drugs absorbed from GIT –> liver for metabolism
some drugs metabolized before distribution to other tissues
drugs with high first-pass metabolism have less distribution

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11
Q

The transport of drugs from plasma to tissues is

A

distribution

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12
Q

Factors that affect distribution

A
physicochemical properties (lipid solubility, degree of ionization)
concentration gradient
plasma protein binding
blood flow
tissue barriers
affinity to certain tissues
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13
Q

what protein do acidic compounds bind to?

A

albumin

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14
Q

what proteins do basic compounds bind to?

A

a1-glycoproteins and lipoproteins

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15
Q

T/F: plasma protein binding shortens a compounds half life

A

false, it prolongs it

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16
Q

T/F: a plasma protein bound compound is inactive

A

true

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17
Q

highly perfused tissues

A

brain, liver, kidney, endocrine glands

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18
Q

poorly perfused tissues

A

bone, adipose

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19
Q

moderately perfused tissues

A

muscle, skin

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20
Q

tissue barriers

A

BBB, eye, testicles, placenta, mammary gland

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21
Q

the chemical alteration of the drug molecule by the cells of the animal

A

biotransformation

22
Q

main site of biotransformation

A

liver

23
Q

phase 1 biotransformation reactions

A

oxidation, reduction, hydrolysis

24
Q

phase II biotransformation reactions

A

conjugation (synthetic)

25
Q

most common form of biotransformation reaction

A

oxidation

26
Q

most common conjugation reaction

A

to glucuronic acid

27
Q

T/F: neonates have a lot of conjugation activity

A

false it is deficient

28
Q

what species is deficient in glucuronyl transferases?

A

cats

29
Q

what species is deficient in hydroxylation and dealkylation?

A

cats

30
Q

what species lack acetylating enzymes?

A

dogs

31
Q

_____ have high levels of oxidative enzymes

A

ruminants and horses

32
Q

which species is deficient in methylates?

A

horses

33
Q

___ lack oxidative enzymes

A

birdss

34
Q

___ have low levels of drug metabolizing enzymes

A

fish

35
Q

List some enzyme inducers

A

phenobarbital, phenylbutazone, griseofulvin, rifampin, chlorinated hydrocarbon insecticides

36
Q

T/F: all enzymes are inducible by drugs

A

False - only microsomal enzymes are

37
Q

List some enzyme inhibitors

A

chloramphenicol, cimetidine, ketoconazole

38
Q

T/F: biotransformation continues to increase with age

A

False, both newborns and geriatrics may have less biotransformation than adults

39
Q

T/F: grapefruit juice is an enzyme inhibitor

A

True

40
Q

Plasma protein binding ______ biotransformation

A

decreases

41
Q

Effect of hypothermia on biotransformation

A

decreases it

42
Q

removal of drug from the body

A

excretion

43
Q

3 aspects of renal excretion

A

glomerular filtration
active tubular secretion
tubular reabsorption

44
Q

4 factors that affect glomerular filtration

A

GFR, molecular size, molecular charge, protein binding

45
Q

T/F: negative charged particles pass through the glomerulus easier than positive

A

false - they’re inhibited by negatively charged proteins in capillary wall

46
Q

T/F only unbound drugs can be filtered by the glomerulus

A

true

47
Q

OCTs transport bases and OATs transport acids in active tubular secretion

A

true

48
Q

4 factors affecting tubular reabsorption

A

physicochemical properties of the drugs
degree of ionization
GFR
active tubular reabsorption

49
Q
The second most important organ for drug excretion (kidney is first) is:
A) sweat glands
B) spleen
C) liver
D) tears
A

liver

50
Q

T/F: enterohepatic circulation shortens the half life of a drug

A

false, it prolongs it