Pharm week 1 Flashcards

1
Q

The volume of distribution (Vd) is the relationship between:

A

Administered dose and plasma concentration

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2
Q

Vd =

A

amount of drug/plasma concentration

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3
Q

__________ is a measurement of an amount of drug in a given volume

A

concentration

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4
Q

a drug that is lipophilic has a ______ volume of distribution, requiring a ______ dose

A

larger, higher

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5
Q

a drug that is hydrophilic has a ______ volume of distribution, requiring a ______ dose

A

smaller, smaller

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6
Q

clearance is the _______ that is cleared of drug per unit time

A

volume of plasma

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7
Q

CL is directly proportionate to:

A

blood flow to clearing organ
extraction ratio
drug dose

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8
Q

CL is indirectly proportional to:

A

half-life
drug concentration in central compartment

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9
Q

to maintain “steady state in plasma the ______ must equal the rate of clearance

A

infusion rate/interval dosing

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10
Q

how many half-times are required to reach a steady state? what can decrease this?

A

5, administering a loading dose

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11
Q

Define steady state

A

steady state is when the amount of drug entering the body is equivalent to the amount of drug being eliminated from the body

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12
Q

the alpha phase of the plasma concentration curve represents

A

distribution into the peripheral compartment (tissues)

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13
Q

The beta phase of the plasma concentration curve represents:

A

elimination from the central compartment

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14
Q

most drugs we administer follow a ______ model

A

multi-compartment model

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15
Q

The slope of line A (plasma concentration curve) is influenced by the drugs _______

A

volume of distribution

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16
Q

The more _______ the drug, the larger the Vd, the ________ the slope

A

lipophilic, steeper

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17
Q

which kinetic model describes the process that metabolizes a constant amount of drug per unit time

A

Zero order

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18
Q

which kinetic model describes the process that metabolizes a constant fraction of a drug per unit time?

A

first order

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19
Q

what occurs in phase II?

A

Conjugation

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20
Q

what occurs in phase 1?

A

Modification: oxidation, reduction, hydrolysis, de methylation

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21
Q

what occurs in phase 3?

A

Excretion

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22
Q

drugs with ester linkage are MOST susceptible to which type of metabolism

A

Hydrolysis

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23
Q

The clearance of which drug is best categorized by perfusion dependent elimination

A

Ketamine

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24
Q

which drugs accelerate methadone metabolism

A

ethanol and phenobarbital

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25
Which drugs may exhibit increased potency in a patient who frequently drinks grapefruit juice?
Fentanyl and midozalam 
26
which local anesthetic is least likely to accumulate in a hypoxic fetus?
Chloroprocaine
27
What molecular bond is strongest?
Covalent
28
Which bond keeps liquids together and drugs in medications?
Van der Waals forces
29
Which bonds do we prefer in anesthesia?
Non-covalent: vanderwaal/ionic because they are more easily reversed lipid soluble/volatile anesthetics
30
What is a stereoisomer?
a compound differing only with the spatial arrangement of atoms
31
Dextrotary:
clockwise rotation
32
Levorotatory:
counter clockwise rotation
33
what is chirality?
a mirror image of another atom/molecule that cannot be superimposed
34
Which inhaled anesthetic is not chiral?
Sevoflurane
35
Enationerism:
a pair of molecules existing in two forms mirror image of each other/classified by rotation
36
pharmacokinetics:
what your body does to the drug- metabolism, clearance
37
Pharmacodynamics:
what drug does to body - receptor interactions, potency
38
Which receptor requires an enzyme to activate?
G-protein coupled receptors
39
Which medications used G-protein coupled receptors?
haloperidol, morphine, losartan, plavix
40
Example of enatiomers that make a racemic mixture:
ropivicaine and bupivicaine
41
racemic mixture:
50%/50% enatomer mixture
42
Ligand-gated ion channel:
ligand (signaling molecule) binds to receptor to open gate to initiate cellular response/gate closes when ligand moves
43
which channels are activated by neuromuscular blocking agents?
Ligand-gated channels
44
What type of drugs move across the cell membrane, BBB, and placenta?
Non-ionized
45
Active transport against the gradient requires _____
ATP
46
4 parts of pharmacokinetics
1. Absorption 2. Distribution 3. Metabolism 4. Excretion
47
Cmax =
peak plasma concentration
48
Tmax =
time when Cmax is observed
49
Bioavailability is:
how much drug is absorbed
50
What medication rate has the highest bioavailability?
Intravenous route
51
What three things affect absorption rate?
site of administration, drug formulation, clinical effectiveness of a drug
52
What is down regulation?
When you're on a medication for a long time, desensitizes/enzyme removal of protein molecule
53
what is efficacy?
the ability to produce an intended effect
54
What is potency?
the power of something to influence or make an impression
55
What is included in the Vessel rich group?
Brain, Heart, Kidneys, Liver, Endocrine tissues, Gi tract
56
Why is the Vdss larger than Vdcc?
at Vdss you have equal concentrations throughout all the compartment/tissues vs in Vdcc your drug is to the vessel rich group only
57
What are the three phases of the multi compartment model?
Rapid distribution Slow distribution Terminal phase
58
Why is fentanyl long acting?
because its highly fat soluble, which increases its VD and it is extensively redistributed
59
What is the therapeutic index?
Safety profile of the drug
60
what is metabolism?
conversion of parent drug into active metabolites to be excreted
61
which organ has the largest metabolic capacity?
Liver
62
what are the four processes that occur in phase 1 metabolism?
oxidation, reduction, hydrolysis, de-methylation
63
what is the goal of phase 2 metabolism?
Conjugation, and to become more water soluble
64
What are the four types of conjugation reactions?
Sulfonic acid glutathione glucuronic acid acetylation
65
What liver enzyme is MOST important?
CYP 450
66
what three things effect enzyme induction?
Acute alcohol ingestion, chronic alcohol ingestion, cigarette smoking
67
What is the bioavailability of topical medications?
100% IF target tissue is localized
68
Which drugs undergo first pass in the lungs?
lidocaine, propranolol, fentanyl
69
What are the two ways medications are excreted?
kidneys into urine, bile into stool
70
What is a half-life?
Time it takes for half of drug to be removed
71
Which receptors are most frequently used in anesthesia?
G-coupled protein receptors
72
Which medications are metabolized by zero order effects?
Aspirin, ethanol, phenytoin
73
what is the curve for medications of high efficacy?
Up and to the LEFT
74
what is an inverse agonist?
binds to a receptor and causes the opposite effect to that of a full agonist
75
What is Rocuronium?
competitive antagonist
76
define ED50
dose that produces clinical response in 50% of population
77
Define therapeutic index
measurement of drug safety. ration of the LD50 to the ED50
78
What is aspirins pharmacodynamic action?
non-competitive antagonism
79
What does the slope tell us in the dose-response curve?
number of receptors that are occupied to produce a clinical effect
80
What is up-regulation?
producing more receptors
81
What drug routes bypass the first pass effect?
Intravenous, intramuscular, sublingual, inhalation, and Intradermal (if dermis is target tissue)
82
Continuous administration of an agonist may cause ______ of the target receptors
down regulation
83
______ is the tetrahedral bonding of carbon (carbon binding to 4 different atoms)
Chirality
84
what factor could cause a drug to be avidly taken up in the first pass through the lungs?
being highly fat soluble
85
What occurs in Phase 2 metabolism?
covalent linkage of drug/metabolite to high polar molecule
86
Where in the body does metabolism occur?
Liver: hepatic microsomes enzymes which are located in hepatic smooth endoplasmic reticulum
87
what are the three parts of renal clearance?
1. glomerular filtration 2. active tubular secretion 3. passive tubular reabsorption
88
what type of drug is normally reabsorbed during renal clearance?
lipid soluble deugs
89
what are the two factors that influence the rate of reabsorption?
pH and rate of urine flow
90
clearance =
elimination/plasma concentration