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pharmacology > drug metabolism and elimination > Flashcards

drug metabolism and elimination Flashcards

1
Q

true or false. only drugs that are free and unbound from plasma protiens can be absorbed

A

true

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2
Q

albumin binds to what

A

warfarin and aspirin

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3
Q

albumin binding to aspirin is an example of what

A

a drug drug interaction

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4
Q

blood flow, organ size affect what

A

distribution - more blood flow into the organ, the more medication, the bigger the organ , the more blood flow there is, thus more meducation

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5
Q

blood brain barrier

A

possesses p-glycoprotiens which prevent some drugs from crossing biological membranes

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6
Q

what do p-glycoprotiens do?

A

they adhere to drugs stopping them from crossing biological membranes

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7
Q

fetal placental barrier

A

prevents drugs from affecting the fetus

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8
Q

what mechanical barriers have p-glycoprotiens

A

BBB, fetal-placenta, liver, epithelial

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9
Q

parenteral route distribution

A

bloodstream –> tissue

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10
Q

oral administration distribution

A

liver - hepatic portal –> systemic circulation

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11
Q

first pass effect

A

this means that always the forst part of a drug is going to be metabolized in the liver and is no longer available

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12
Q

how is to bioavilablilty of a drug affected by the metabolism of the liver?

A

the bioavailability of the drug is reduced

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13
Q

what routes of administration are affected by the first pass affect

A

oral and rectal

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14
Q

what is metabolism

A

process by which drugs are biotransformed into water soluble compounds that are easily secreted by the kidneys

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15
Q

the water-soluble metabolites from the liver are what?

A

inactive

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16
Q

hepatic drug metabolism is crucial for what

A

terminating the drug action and facilitates the elimination of drug molecules from the body

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17
Q

what converts lipid soluble drugs into water soluble metabolites

A

metabolism

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18
Q

the kidneys can only excrete what substances

A

water soluble

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19
Q

what are phase one reactions

A

theses reactions are hydrolysis, oxidation, reduction

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20
Q

how do phase one reactions work?

A

they convert non-polar molecules into polar molcules via the addition of a polar funcitonal group

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21
Q

most important phase one reaction

A

oxidation

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22
Q

cytochrome p-450 enzymes do what

A

replace a -CH or -NH group in a molecule with an -OH

23
Q

what enzymes replace a -ch or -nh group in a molecule with an -oh group

A

cytochrome p450 enzymes

24
Q

cytochrome p448 enzymes

A

insert an oxygen atom between two carbons that are connected by a double bond

25
Q

what enzymes insert an oxygen atom between two carbons that are connected by a double bond

A

cytochrome p448

26
Q

what can activites can inhibit cytochrome enzymes

A

smoking and grapefruit juice

27
Q

what drugs can induce or inhibit the synthesis of oxidation enzymes - CYP - 450

A

rifampin and erythromyocin

28
Q

rifampin

A

increases the synthesis of CYP enzymes, effecting the metabolism of the medications

29
Q

what drug causes the increased metabolism and decreased plasma concentration of co-administered drugs

A

rifampin

30
Q

what drug can make things like birth control, antidepessants less effective?

A

rifampin

31
Q

erythromycin

A

inhibits the activity of CYP enzymes

32
Q

what inhibits the activity of the CYP enzymes

A

erytromycin

33
Q

aldehyde oxidase and liver alcohol dehydrogenase

A

can oxidize alcohol

34
Q

monoamine oxidase

A

metabolize things like dopamine and serotonin

35
Q

phase two reactions do what?

A

they form a highly water soluble metabolite

36
Q

what drug isnt rendered inactive after phase two conjugation

A

morphine

37
Q

glucuronyl transferase

A

replaces an -oh or -sh group with glucuronic acid

38
Q

n- acetyltrasnferase

A

replaces an -oh, -sh, -nh2 group with acetate

39
Q

sulfotrasnferase

A

adds a sulfate group replacing -oh

40
Q

glutathione s-transferase

A

forms an adduct between the drug and glutathione

41
Q

forming an adduct means

A

you are almost adding a molecule onto another

42
Q

where do the reactions occur in acetaminophen?

A

sulfation, oxidation, glucuronidation

43
Q

the oxidation of acetaminophen causes what

A

it causes the molecule to be unstable resulting in a spontaneous reaction

44
Q

what does the spontaneous reaction of acetaminophen result in

A

another phase two reaction of glutathione s-transferase

45
Q

in the situation of an acetaminophen overdose, what enzyme stops irreversible damage to the liver?

A

glutathione

46
Q

NAPQI combined with sulfahydryl causes what

A

causes cell death

47
Q

what is administered in acetaminophen overdose

A

acetylcysteine

48
Q

what is acetylcysteine

A

this is a compound that works just like glutathione, it binds to NAPQI and prevents damage to hepatocytes

49
Q

excretion is done by

A

kidneys

50
Q

in order for drugs to be excreted what must the drugs be

A

must be ionized and polar

51
Q

true or false, polarity of drugs can be manipulated by shifting pH of urine

A

true

52
Q

where do drugs that are more fat soluble excreted through

A

the intestines

53
Q

what drugs can experience intra-hepatic absorption

A

fat soluble

pharmacology (26 decks)

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