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

Chapter 4 (the drug cycle) Flashcards

(64 cards)

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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
duration of effect
half life (usually)
26
metabolism
way drug is broken down
27
excretion
way drug is cleared from body
28
drug cycle
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
metabolism and excretion
elimination
30
percent of admin dose that is actually absorbed (unchanged)
is the bioavailability
31
dosage form and bioavailability
changing dosage form changes the amount of drug that reaches systemic circulation
32
IV bioavailability
100% b/c drug is given directly to blood
33
topicals bioavailability
very low b/c almost none gets into blood
34
B
bioavailability
35
oral preparations B
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
central compartment with smaller subcompartments
systemic circulation with smaller areas where drugs can accumulate (adipose tissue)
37
albumin
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
females hormones and albumin
bind extensively (such as the estrogens)
39
BBB
blood brain barrier: stops many drugs from entering the CNS, but also stops infectious agents too
40
meningitis and crossing the BBB with antibiotics
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
antihistamines
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
metabolism
biotransformation: drug is transformed from initial, usually active form, to a different form (usually less active)
43
liver
main organ for metabolism; makes drugs more water soluble so they can be excreted by the kidneys
44
enterohepatic circulation
b/c portal veins deliver blood from intestines to liver before any other organ
45
first pass effect
microsomal liver enzymes conjugate drugs b/c liver is filled with peroxisomes and lysozymes that break down things that enter the body
46
drugs quickly destroyed by the liver
barbiturates, NTG, and opiods (among others)
47
variance in drug metabolism
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
first pass effect
often must give drugs orally in much higher doses than parenterally b/c much of the drug is lost from liver metabolism
49
Chloral-hydrate
the metabolite is the more active form; it does not induce sleep until it is metabolized to a more active form
50
patients that are very young, very old, or have liver disease...
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
drug tolerance
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
blanket statement of drugs...
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
drug elimination
most drugs are excreted from body by kidney; thus kidney function is extremely important in the duration of the effect of many drugs
54
drug excretion methods
Bile, lungs (breathe), mother's milk, saliva, sweat, tears, kidney
55
what determines 1/2 life of drug
liver accounts for 1/2 life b/c it conjugates it to make it something else so its blood levels decrease as such
56
adjusting drug dosage
many times drug dosage must be decreased; only rarely increased like if someone was a fast metabolizer of a drug
57
elderly or young people liver and kidney function
significant decrease in kidney and liver function which decreases drug metabolism and excretion; so decrease dose or increase time between doses
58
neonates liver function
almost none so huge reduction in dose is needed
59
prodrug
biologically inactive compound which can be metabolized into an active drug
60
half life
influenced by metabolism and excretion
61
Vd
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
drug-receptor model
explains most of drugs therapeutic effect
63
natural hormones
natural agonists in body
64
basis for drug effect
drug binding to a rc

Pre-pharmacology (27 decks)

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