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
Q

Which drugs may exhibit increased potency in a patient who frequently drinks grapefruit juice?

A

Fentanyl and midozalam 

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26
Q

which local anesthetic is least likely to accumulate in a hypoxic fetus?

A

Chloroprocaine

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27
Q

What molecular bond is strongest?

A

Covalent

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28
Q

Which bond keeps liquids together and drugs in medications?

A

Van der Waals forces

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29
Q

Which bonds do we prefer in anesthesia?

A

Non-covalent: vanderwaal/ionic because they are more easily reversed
lipid soluble/volatile anesthetics

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30
Q

What is a stereoisomer?

A

a compound differing only with the spatial arrangement of atoms

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31
Q

Dextrotary:

A

clockwise rotation

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32
Q

Levorotatory:

A

counter clockwise rotation

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33
Q

what is chirality?

A

a mirror image of another atom/molecule that cannot be superimposed

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34
Q

Which inhaled anesthetic is not chiral?

A

Sevoflurane

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35
Q

Enationerism:

A

a pair of molecules existing in two forms mirror image of each other/classified by rotation

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36
Q

pharmacokinetics:

A

what your body does to the drug- metabolism, clearance

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37
Q

Pharmacodynamics:

A

what drug does to body - receptor interactions, potency

38
Q

Which receptor requires an enzyme to activate?

A

G-protein coupled receptors

39
Q

Which medications used G-protein coupled receptors?

A

haloperidol, morphine, losartan, plavix

40
Q

Example of enatiomers that make a racemic mixture:

A

ropivicaine and bupivicaine

41
Q

racemic mixture:

A

50%/50% enatomer mixture

42
Q

Ligand-gated ion channel:

A

ligand (signaling molecule) binds to receptor to open gate to initiate cellular response/gate closes when ligand moves

43
Q

which channels are activated by neuromuscular blocking agents?

A

Ligand-gated channels

44
Q

What type of drugs move across the cell membrane, BBB, and placenta?

A

Non-ionized

45
Q

Active transport against the gradient requires _____

A

ATP

46
Q

4 parts of pharmacokinetics

A
  1. Absorption
  2. Distribution
  3. Metabolism
  4. Excretion
47
Q

Cmax =

A

peak plasma concentration

48
Q

Tmax =

A

time when Cmax is observed

49
Q

Bioavailability is:

A

how much drug is absorbed

50
Q

What medication rate has the highest bioavailability?

A

Intravenous route

51
Q

What three things affect absorption rate?

A

site of administration, drug formulation, clinical effectiveness of a drug

52
Q

What is down regulation?

A

When you’re on a medication for a long time, desensitizes/enzyme removal of protein molecule

53
Q

what is efficacy?

A

the ability to produce an intended effect

54
Q

What is potency?

A

the power of something to influence or make an impression

55
Q

What is included in the Vessel rich group?

A

Brain, Heart, Kidneys, Liver, Endocrine tissues, Gi tract

56
Q

Why is the Vdss larger than Vdcc?

A

at Vdss you have equal concentrations throughout all the compartment/tissues vs in Vdcc your drug is to the vessel rich group only

57
Q

What are the three phases of the multi compartment model?

A

Rapid distribution
Slow distribution
Terminal phase

58
Q

Why is fentanyl long acting?

A

because its highly fat soluble, which increases its VD and it is extensively redistributed

59
Q

What is the therapeutic index?

A

Safety profile of the drug

60
Q

what is metabolism?

A

conversion of parent drug into active metabolites to be excreted

61
Q

which organ has the largest metabolic capacity?

A

Liver

62
Q

what are the four processes that occur in phase 1 metabolism?

A

oxidation, reduction, hydrolysis, de-methylation

63
Q

what is the goal of phase 2 metabolism?

A

Conjugation, and to become more water soluble

64
Q

What are the four types of conjugation reactions?

A

Sulfonic acid
glutathione
glucuronic acid
acetylation

65
Q

What liver enzyme is MOST important?

A

CYP 450

66
Q

what three things effect enzyme induction?

A

Acute alcohol ingestion, chronic alcohol ingestion, cigarette smoking

67
Q

What is the bioavailability of topical medications?

A

100% IF target tissue is localized

68
Q

Which drugs undergo first pass in the lungs?

A

lidocaine, propranolol, fentanyl

69
Q

What are the two ways medications are excreted?

A

kidneys into urine, bile into stool

70
Q

What is a half-life?

A

Time it takes for half of drug to be removed

71
Q

Which receptors are most frequently used in anesthesia?

A

G-coupled protein receptors

72
Q

Which medications are metabolized by zero order effects?

A

Aspirin, ethanol, phenytoin

73
Q

what is the curve for medications of high efficacy?

A

Up and to the LEFT

74
Q

what is an inverse agonist?

A

binds to a receptor and causes the opposite effect to that of a full agonist

75
Q

What is Rocuronium?

A

competitive antagonist

76
Q

define ED50

A

dose that produces clinical response in 50% of population

77
Q

Define therapeutic index

A

measurement of drug safety. ration of the LD50 to the ED50

78
Q

What is aspirins pharmacodynamic action?

A

non-competitive antagonism

79
Q

What does the slope tell us in the dose-response curve?

A

number of receptors that are occupied to produce a clinical effect

80
Q

What is up-regulation?

A

producing more receptors

81
Q

What drug routes bypass the first pass effect?

A

Intravenous, intramuscular, sublingual, inhalation, and Intradermal (if dermis is target tissue)

82
Q

Continuous administration of an agonist may cause ______ of the target receptors

A

down regulation

83
Q

______ is the tetrahedral bonding of carbon (carbon binding to 4 different atoms)

A

Chirality

84
Q

what factor could cause a drug to be avidly taken up in the first pass through the lungs?

A

being highly fat soluble

85
Q

What occurs in Phase 2 metabolism?

A

covalent linkage of drug/metabolite to high polar molecule

86
Q

Where in the body does metabolism occur?

A

Liver: hepatic microsomes enzymes which are located in hepatic smooth endoplasmic reticulum

87
Q

what are the three parts of renal clearance?

A
  1. glomerular filtration
  2. active tubular secretion
  3. passive tubular reabsorption
88
Q

what type of drug is normally reabsorbed during renal clearance?

A

lipid soluble deugs

89
Q

what are the two factors that influence the rate of reabsorption?

A

pH and rate of urine flow

90
Q

clearance =

A

elimination/plasma concentration