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Pre-pharmacology > Chapter 4 (the drug cycle) > Flashcards

Chapter 4 (the drug cycle) Flashcards

1
Q

pharmacodynamics

A

drug-receptor binding, transduction of intracellular effects, production of a pharmacological response

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2
Q

rc

A

receptor

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3
Q

most drugs work by

A

binding to a specific receptor

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4
Q

agonist

A

excites the rc

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5
Q

antagonist

A

inactivates the rc; still binds but does not have positive effect so it gets in the way so another chemical that will produce an effect can’t bind
take away effect from molecules activating the receptor

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6
Q

mu receptor

A

rc for opiods

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7
Q

opioid overdose receptor example

A

Heroin is agonist that exerts specific effect (analgesia and respiratory failure in high doses), but Narcan (naloxone) given in ED as antagonist to reverse the effects of the overdose

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8
Q

pt.

A

patient

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9
Q

smelling salts

A

not antagonists; they activate basically all other excitatory neurons to wake someone up, not block inhibitory effects of other molecules

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10
Q

partial agonists

A

bind to receptors but do not yield full effect that a normal full agonist would

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11
Q

synergistic interaction

A

positive drug-drug interaction where synergism is reached: A+B effect is an exaggerated effect greater than the sum of A and B by themselves (whole is greater than sum of parts)

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12
Q

Septra

A

formulation of two antibiotics (a sulfa drug and trimethoprim and together they work better even better than the sum should)
treats bladder infections

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13
Q

tylenol and codeine

A

synergism between two analgesics to give great pain relief

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14
Q

alcohol and tranquilizers

A

synergism even though effect is deleterious; huge depressive effect

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15
Q

propofol and Valium

A

synergism producing a large CNS depressive state

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16
Q

negative drug interactions

A

effect of one drug (or food) interferes or alters effects of another
A given in presence of B leads to diminished A effect

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17
Q

tetracycline and milk

A

negative effect from calcium in milk binding to tetracycline antibiotic

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18
Q

ADME (steps of the drug cycle)

A

basics of pharmacokinetics: absorption, distribution, metabolism, and excretion

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19
Q

pharmacodynamic effects

A

mechanism of action of how drugs produce their effects

what the drug does to the body

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20
Q

pharmacokinetic effects

A

measured response to time and dose (absorption, blood levels, mode of inactivation, etc.)
what the body does to the drug

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21
Q

baking soda pharmacokinetic concern

A

causes rebound acid 3-4 hours later

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22
Q

absorption

A

fraction of admin dose that reaches systemic circulation

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23
Q

distribution

A

where drug goes in body

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24
Q

rate

A

speed at which drug action begins

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25
Q

duration of effect

A

half life (usually)

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26
Q

metabolism

A

way drug is broken down

27
Q

excretion

A

way drug is cleared from body

28
Q

drug cycle

A

deals with pharmacokinetic variables:
how much of admin dose is absorbed, which body fluids its distributed to, how long ti stays in blood before being metabolized, and when and where it is excreted

29
Q

metabolism and excretion

A

elimination

30
Q

percent of admin dose that is actually absorbed (unchanged)

A

is the bioavailability

31
Q

dosage form and bioavailability

A

changing dosage form changes the amount of drug that reaches systemic circulation

32
Q

IV bioavailability

A

100% b/c drug is given directly to blood

33
Q

topicals bioavailability

A

very low b/c almost none gets into blood

34
Q

B

A

bioavailability

35
Q

oral preparations B

A

2/3 of parenteral B so normally higher doses are given or more potent form of drug so medicine given in oral will be as effective as IV even though it has a lower B

36
Q

central compartment with smaller subcompartments

A

systemic circulation with smaller areas where drugs can accumulate (adipose tissue)

37
Q

albumin

A

most abundant blood protein; globular; excellent binder of drugs in blood so must take this into account when administering drug dosages
different drugs bind to albumin to different extents
albumin is also key for remaining osmotic pressure of blood

38
Q

females hormones and albumin

A

bind extensively (such as the estrogens)

39
Q

BBB

A

blood brain barrier: stops many drugs from entering the CNS, but also stops infectious agents too

40
Q

meningitis and crossing the BBB with antibiotics

A

if infection is super bad then may not be able to wait to admin large dose of antibiotic only to have some of it reach CNS through BBB so may give antibiotic intrathecally so it does not have to pass the BBB

41
Q

antihistamines

A

first gen (like benadryl) crossed the BBB and made people sleepy (why benadryl is a good OTC sleep med), but 2 and 3 generation antihistamines were developed to not cross the BBB so only have H1 antag and no drowsy

42
Q

metabolism

A

biotransformation: drug is transformed from initial, usually active form, to a different form (usually less active)

43
Q

liver

A

main organ for metabolism; makes drugs more water soluble so they can be excreted by the kidneys

44
Q

enterohepatic circulation

A

b/c portal veins deliver blood from intestines to liver before any other organ

45
Q

first pass effect

A

microsomal liver enzymes conjugate drugs b/c liver is filled with peroxisomes and lysozymes that break down things that enter the body

46
Q

drugs quickly destroyed by the liver

A

barbiturates, NTG, and opiods (among others)

47
Q

variance in drug metabolism

A

not all drugs are metabolized the same way in the liver
not every person metabolizes the same drugs in the same way
the same person does not metabolize the same drug in the same way from day to day
*Liver function changes based on what is supplied to it

48
Q

first pass effect

A

often must give drugs orally in much higher doses than parenterally b/c much of the drug is lost from liver metabolism

49
Q

Chloral-hydrate

A

the metabolite is the more active form; it does not induce sleep until it is metabolized to a more active form

50
Q

patients that are very young, very old, or have liver disease…

A

may have unpredictable blood levels of a drug because drug metabolism is going to be abnormal
liver makes fat soluble drugs water soluble for elimination so if liver is impaired then drug levels will be higher since it can’t be eliminated and there will be greater drug effect

51
Q

drug tolerance

A

increased exposure to drug leads to increased metabolism of the drug (or naturally higher metabolism of that drug) so it takes more drug to produce same effect
*sometimes altered drug effect is offset by another factor such as change in binding of drug

52
Q

blanket statement of drugs…

A

rarely are true because people metabolize and respond to drugs differently
almost anything with CNS effects affects people very differently like alcohol, opiods, barbiturates, etc.

53
Q

drug elimination

A

most drugs are excreted from body by kidney; thus kidney function is extremely important in the duration of the effect of many drugs

54
Q

drug excretion methods

A

Bile, lungs (breathe), mother’s milk, saliva, sweat, tears, kidney

55
Q

what determines 1/2 life of drug

A

liver accounts for 1/2 life b/c it conjugates it to make it something else so its blood levels decrease as such

56
Q

adjusting drug dosage

A

many times drug dosage must be decreased; only rarely increased like if someone was a fast metabolizer of a drug

57
Q

elderly or young people liver and kidney function

A

significant decrease in kidney and liver function which decreases drug metabolism and excretion; so decrease dose or increase time between doses

58
Q

neonates liver function

A

almost none so huge reduction in dose is needed

59
Q

prodrug

A

biologically inactive compound which can be metabolized into an active drug

60
Q

half life

A

influenced by metabolism and excretion

61
Q

Vd

A

volume of distribution; ratio of dose present in body/ plasma concentration. Info about drug distribution
High Vd means drug is accumulating in tissues and not very much is in blood
Low Vd means drug is basically confined to intravascular fluid

62
Q

drug-receptor model

A

explains most of drugs therapeutic effect

63
Q

natural hormones

A

natural agonists in body

64
Q

basis for drug effect

A

drug binding to a rc

Pre-pharmacology (27 decks)

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