Block 1 Flashcards

(79 cards)

1
Q

what are relative contradictions

A

caution should be taken

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2
Q

what are absolute contradictions

A

drug should not be used

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3
Q

what is the national formulary

A

information on the product available to prescribers

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4
Q

what is the pharmacopoeia

A

contains a list of drugs with all there chemical information

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5
Q

what is another name for brand name of a drug

A

proprietary

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6
Q

aspirin is an example of it’s chemical name, non-proprietary name, or proprietary name

A

non-proprietary

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7
Q

what are the 7 stages of drug development

A
  1. discovery
  2. animal studies
  3. IND application
  4. clinical studies
  5. submission of NDA
  6. approval of NDA
  7. post-marketing surveillance
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8
Q

what are the 3 purposes
of animal studies

A

beneficial/harmful effects on organs
mechanism of action
pharmokinetics

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9
Q

what is the dosage for acute toxicity

A

single dose

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10
Q

what is the dose for sub-acute toxicity

A

3 doses, 2 weeks to 3 months

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11
Q

what is the dose for chronic toxicity

A

more than 6 moths (2 species)

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12
Q

what is involved in phase I of a clinical trial

A

evaluation of safety
healthy volunteers
both investigator and subjects know what drug is being administered

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13
Q

what is involved in phase II of a clinical trial

A

patients with the disease
single or double blind
“does the drug work in patients with the targeted condition”

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14
Q

what is involved in phase III of a clinal trial

A

large group of patients with the disease
double blind
“does it work, how safe is it”

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15
Q

what is off-label drug use

A

medication is being used for something other than what is was originally approved for

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16
Q

in what schedule of drugs can medication not be refilled

A

II

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17
Q

in what schedule of drugs are they not accepted for medical use

A

I

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18
Q

schedule III, IV, and V drugs can be refilled but only for a maximum of __ times

A

5

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19
Q

what is first pass metabolism

A

the drug is metabolized before it has reached systemic circulation
(absorption through intestinal mucosa to liver portal system for processing before reaching systemic circulation)

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20
Q

what 2 type of drug administration have no first class metabolism, therefor have a greater bioavailability

A

IV
sublingual/buccal

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21
Q

what drugs move by way of simple or passive diffusion

A

lipid soluble
non-ionized

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22
Q

what is the equation for oral bioavailability if equal dose is given

A

AUCoral/AUCiv
AUC= area under curve

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23
Q

what is the equation for intramuscular bioavailability if equal dosage is given

A

AUCim/AUCiv

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24
Q

what equation is used to calculate bioavailability if an equal dosage is not given

A

(AUCoral x Doseiv)/(AUCiv x Doseoral)

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25
non-ionized forms of drugs are lipid soluble or water soluble and are easier or harder to absorb
lipid better
26
ionized drugs are poorly absorbed so they are eliminated in what way
renally excreted
27
weakly acidic drugs are best absorbed in the ___, while weakly basic drugs are best absorbed in the ___
stomach intestine
28
milk reduces the activity of what drug
tetracycline
29
food reduces the activity of what drug
ampicillin
30
fatty foods increase the absorbance of what drug
griseifulvin
31
does first pass metabolism increase or decrease bioavailability
decrease
32
what 3 factors delay rate of drug absorption
increased speed though GIT delayed transport from stomach to intestines presence of food in the stomach
33
what is the effect of P-glycoprotein on rate of drug absorption
decreases (pumps drugs out of cell)
34
what is the definition of drug distribution
drug reversibly leaves the bloodstream and enters interstitium/tissues
35
what makes up the central compartment for drug distribution
highly blood perfused compartments (blood, heart, lungs, liver, kidneys)
36
what makes up the peripheral compartment for drug distribution
lower blood flow, less vascularized (fat tissues, muscle, CSF)
37
what does a high volume of distribution tell us
more of the drug is in tissue than in plasma
38
what is the equation for volume of ditribution
amount of drug in the body/plasma concentration at time 0
39
what does a low volume of distribution tell us
the drug mostly remains in the blood
40
A drug with a volume of distribution of __ L is low Vd drug
4-8L
41
A drug with a volume of distribution of __ L is medium Vd drug
14-16
42
A drug with a volume of distribution of greater than__ L is high Vd drug
42
43
what are 3 characteristics of low Vd drugs
only in blood/plasma large weight/charged bound to plasma proteins (hydrophilic)
44
what are 4 characteristics of medium Vd drugs
distribute to interstitial fluid/intravascular small weight hydrophilic not bound to plasma proteins
45
what are 2 characteristics of high Vd drugs
drugs distributes to all tissues small, uncharged (hydrophobic or lipophilic)
46
lipophilic or lipophobic drugs have a greater drug distribution
lipophilic
47
the greater the plasma protein binding, the greater or lower drug distribution
lower
48
the greater the blood flow, the greater or lower drug distribution
greater
49
the greater the capillary permeability the greater or lower drug distribution
greater
50
highly protein bound drugs have a longer or shorter duration of action
longer
51
what increases the risk of drug toxicity
if 2 highly plasma bound drugs are given together and both drugs bind to the same site
52
the blood brain barrier restricts __ soluble drugs while __ soluble drugs cross more easily (lipid or water)
water lipid
53
do liver and kidney disease increase or decrease Vd
increase (less protein binding in plasma)
54
does heart failure increase or decrease Vd
decrease (less distribution to organs)
55
does obesity increase or decrease Vd
increases (highly lipid soluble drugs get distributed to the adipose tissue)
56
does pregnancy increase of decrease Vd
increase (increase body weight/adipose)
57
what is redistribution
highly lipid soluble drugs are rapidly distributed to highly blood perfused tissues (brain, heart, kidney) but get redistributed into less vascularized tissues at the end of the drug action
58
the greater the lipid solubility the drug, the slower or faster redistribution
faster
59
what is an example of a drug that is terminated by drug redistribution
anesthetic effect of thiopental
60
what are 3 possible effects of drug metabolism
inactivation conversion to an active metabolite to lengthen drug action activation
61
what is the definition of a pro-drug
a drug needs to go through metabolism to become active
62
microsomal enzymes such as cytochrome P-450 and oxidases are primarily associated with what location
ER of liver
63
nonmicrosomal enzymes such as monoamine oxidase, esterases, amidases, and transferases are primarily associated with what 3 main locations
cytoplasm mitochondria of liver cells plasma
64
characteristics of microsomal enzymes (4)
mostly catalyze phase I reactions non-specific can be induced or inhibited metabolize only lipid soluble drugs
65
in the nomenclature of cytochrome P450: ex: CYP3A4 3= __ A=__ 4=__
family name subfamily isozyme
66
what are the 3 most important cytochrome Ps for drug metabolism
CYP3A, CYP2D, and CYP2C
67
2 characteristics of nonmicrosomal enzymes
non-inducible phase II reactions
68
what is the difference between the types of reactions involved in phase I vs II reactions
phase I- nonsynthetic phase II- synthetic/conjugation
69
phase I and II metabolism is used to metabolize __ soluble agents into more polar substances because the kidneys can't effectively secrete __ drugs
lipid lipophilic
70
phase I reactions are mostly catalyzed by ___ system
cytochrome P450
71
phase I reactions convert the drug to a __ soluble metabolite
water
72
the reactions involved in phase I reactions are __, __, and __
oxidation reduction hydrolysis
73
the drug metabolite after phase II is mostly __, __ soluble, and __
polar water inactive
74
can phase II metabolism occur before phase I
yes
75
what are the 6 reactions of phase II metabolism
glucuronidation glutathionylation glycination acetylation methylation sulfation
76
enterohepatic recycling is between what 3 organs
GIT liver kidneys
77
what is the effect of enterohepatic recycling
prolong half-life
78
what classification of drugs interfere with enterohepatic recycling
antibiotics
79
antibiotics that interfere with enterohepatic circulation have what affect on contraceptives
failure