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Pharmacology > Block 1 > Flashcards

Block 1 Flashcards

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
Q

non-ionized forms of drugs are lipid soluble or water soluble and are easier or harder to absorb

A

lipid
better

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26
Q

ionized drugs are poorly absorbed so they are eliminated in what way

A

renally excreted

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27
Q

weakly acidic drugs are best absorbed in the ___, while weakly basic drugs are best absorbed in the ___

A

stomach
intestine

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28
Q

milk reduces the activity of what drug

A

tetracycline

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29
Q

food reduces the activity of what drug

A

ampicillin

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30
Q

fatty foods increase the absorbance of what drug

A

griseifulvin

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31
Q

does first pass metabolism increase or decrease bioavailability

A

decrease

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32
Q

what 3 factors delay rate of drug absorption

A

increased speed though GIT
delayed transport from stomach to intestines
presence of food in the stomach

33
Q

what is the effect of P-glycoprotein on rate of drug absorption

A

decreases
(pumps drugs out of cell)

34
Q

what is the definition of drug distribution

A

drug reversibly leaves the bloodstream and enters interstitium/tissues

35
Q

what makes up the central compartment for drug distribution

A

highly blood perfused compartments (blood, heart, lungs, liver, kidneys)

36
Q

what makes up the peripheral compartment for drug distribution

A

lower blood flow, less vascularized (fat tissues, muscle, CSF)

37
Q

what does a high volume of distribution tell us

A

more of the drug is in tissue than in plasma

38
Q

what is the equation for volume of ditribution

A

amount of drug in the body/plasma concentration at time 0

39
Q

what does a low volume of distribution tell us

A

the drug mostly remains in the blood

40
Q

A drug with a volume of distribution of __ L is low Vd drug

A

4-8L

41
Q

A drug with a volume of distribution of __ L is medium Vd drug

A

14-16

42
Q

A drug with a volume of distribution of greater than__ L is high Vd drug

A

42

43
Q

what are 3 characteristics of low Vd drugs

A

only in blood/plasma
large weight/charged
bound to plasma proteins (hydrophilic)

44
Q

what are 4 characteristics of medium Vd drugs

A

distribute to interstitial fluid/intravascular
small weight
hydrophilic
not bound to plasma proteins

45
Q

what are 2 characteristics of high Vd drugs

A

drugs distributes to all tissues
small, uncharged (hydrophobic or lipophilic)

46
Q

lipophilic or lipophobic drugs have a greater drug distribution

A

lipophilic

47
Q

the greater the plasma protein binding, the greater or lower drug distribution

A

lower

48
Q

the greater the blood flow, the greater or lower drug distribution

A

greater

49
Q

the greater the capillary permeability the greater or lower drug distribution

A

greater

50
Q

highly protein bound drugs have a longer or shorter duration of action

A

longer

51
Q

what increases the risk of drug toxicity

A

if 2 highly plasma bound drugs are given together and both drugs bind to the same site

52
Q

the blood brain barrier restricts __ soluble drugs while __ soluble drugs cross more easily
(lipid or water)

A

water
lipid

53
Q

do liver and kidney disease increase or decrease Vd

A

increase
(less protein binding in plasma)

54
Q

does heart failure increase or decrease Vd

A

decrease
(less distribution to organs)

55
Q

does obesity increase or decrease Vd

A

increases
(highly lipid soluble drugs get distributed to the adipose tissue)

56
Q

does pregnancy increase of decrease Vd

A

increase
(increase body weight/adipose)

57
Q

what is redistribution

A

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
Q

the greater the lipid solubility the drug, the slower or faster redistribution

A

faster

59
Q

what is an example of a drug that is terminated by drug redistribution

A

anesthetic effect of thiopental

60
Q

what are 3 possible effects of drug metabolism

A

inactivation
conversion to an active metabolite to lengthen drug action
activation

61
Q

what is the definition of a pro-drug

A

a drug needs to go through metabolism to become active

62
Q

microsomal enzymes such as cytochrome P-450 and oxidases are primarily associated with what location

A

ER of liver

63
Q

nonmicrosomal enzymes such as monoamine oxidase, esterases, amidases, and transferases are primarily associated with what 3 main locations

A

cytoplasm
mitochondria of liver cells
plasma

64
Q

characteristics of microsomal enzymes (4)

A

mostly catalyze phase I reactions
non-specific
can be induced or inhibited
metabolize only lipid soluble drugs

65
Q

in the nomenclature of cytochrome P450:
ex: CYP3A4
3= __
A=__
4=__

A

family name
subfamily
isozyme

66
Q

what are the 3 most important cytochrome Ps for drug metabolism

A

CYP3A, CYP2D, and CYP2C

67
Q

2 characteristics of nonmicrosomal enzymes

A

non-inducible
phase II reactions

68
Q

what is the difference between the types of reactions involved in phase I vs II reactions

A

phase I- nonsynthetic
phase II- synthetic/conjugation

69
Q

phase I and II metabolism is used to metabolize __ soluble agents into more polar substances because the kidneys can’t effectively secrete __ drugs

A

lipid
lipophilic

70
Q

phase I reactions are mostly catalyzed by ___ system

A

cytochrome P450

71
Q

phase I reactions convert the drug to a __ soluble metabolite

A

water

72
Q

the reactions involved in phase I reactions are __, __, and __

A

oxidation
reduction
hydrolysis

73
Q

the drug metabolite after phase II is mostly __, __ soluble, and __

A

polar
water
inactive

74
Q

can phase II metabolism occur before phase I

A

yes

75
Q

what are the 6 reactions of phase II metabolism

A

glucuronidation
glutathionylation
glycination
acetylation
methylation
sulfation

76
Q

enterohepatic recycling is between what 3 organs

A

GIT
liver
kidneys

77
Q

what is the effect of enterohepatic recycling

A

prolong half-life

78
Q

what classification of drugs interfere with enterohepatic recycling

A

antibiotics

79
Q

antibiotics that interfere with enterohepatic circulation have what affect on contraceptives

A

failure

Pharmacology (16 decks)

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