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Flashcards in 1,2,3,4 Deck (147):
1

What is the definition of pharmacology?

study of how drugs affect bio systems

2

Any chemical which affects biological processes is called?

Drug

3

What is the difference between endobiotics and xenobionics?

Endobiotics are normally produced by body and used as therapeutics and xenobiotics are not from the body (this is the majority)

4

What is the production, compounding, and distributions of drugs?

pharmacy

5

T-F--toxicology and pharmacology are roughly the same thing?

False--interrelate, but toxicology looks at the toxic effects of drugs and chemicals on the body.

6

What is pharmacotherapeutics?

treatment of disease with drug (as opposed to regular therapeutics)

7

What are drugs that are USUALLY (not always) specifically used to treat cancer? 2 names he gave us

chemotherapeutic agents or anti-neoplastic

8

What did the pure food and drug act of 1906 start requiring?

labeling of active ingredients

9

What act restricted the sale of addictive substances of abuse?

Harrison Narcotic ACt of 1914

10

What did the food, drug, and cosmetic act of 1938 require?

documentation of safety to the FDA and inactive ingredients to be labelled

11

What act created 2 classifications of drugs?

Durham-Humphrey Amendments-1951 (legend drugs and OTC drugs)

12

What is a legend drug?

federal law prohibits dispensing without a prescription

13

What act or amendment required documentation of EFFICACY?

Kefauver-Harris amendment 1962

14

What act replaced the Harrison Narcotic Act in 1970?

Controlled substances Act 1970

15

What 3 things did the controlled substances Act do?

1. DEA
2. Have to have license as a physician to prescribe
3. Create a schedule of the drugs

16

What is phase I in a clinical trial?

Initial dose range & safety

17

In phase I…do the individuals have the disease?

No

18

What is a phase II clinical trial?

efficacy in disease and effective dose

19

What is a phase III clinical trial?

compare w/best current treatment DOUBLE BLIND

20

What is phase IV of a clinical trial?

post-marketing monitoring--->looking for that potentially harmful effect that only occurs 1/100,000

21

What is category I of OTC drugs?

safe and effective

22

What is Category II of OTC drugs?

not safe, not effective or both

23

What is category III of OTC drugs?

data inconclusive

24

T-F--vitamins, minerals etc. are under control of the FDA? per what act?

False
Dietary Supplement Health & Education Act 1994

25

Who does responsibility of the safety of dietary supplements etc. fall on? effectiveness?

the manufacturer----no responsibility for ensuring effectiveness

26

What are the 3 types of names each drug usually has.

Chemical name--> Generic (official) name---> Trade Names

27

What is the implication of a generic drug with only one trade name?

company still has patent in effect and is the sole producer

28

What is the implication of a generic drug with more than one trade name?

1. Different companies producing same drug
2. Same company, but different amounts or marketing strategy etc.

29

T-F---multiple products containing different generic drugs with the same single trade name exist?

True (according to his slide but he didn't really explain)

30

What are the two main ways drug classes are grouped by?

Therapeutic use and pharmacological class

31

What is the pharmacological class based on?

target of action

32

What are 2 of the sources of drug info from manufacturers?

package inserts
physician desk reference

33

What are sources of technical drug info not from manufacturers---Just review don't memorize.

American Hospital Formulary Service
US Pharmacopeia Dispensing Information
Facts and Comparisons
AMA Drug Evals
Publications
Internet

34

What phase of drug reaction is associated with disintegration of Dosage?

Pharmaceutical phase

35

What phase of drug reaction is associated with absorption, distribution, metabolism and excretion of the drug?

pharmacokinetic phase

36

What phase of drug reaction is associated with drug receptor interaction (effect)?

pharmacodynamic phase

37

What are the 4 general routes of administration

enteral, parenteral, pulmonary, dermal

38

What route of administration has to deal with needles?

parenteral

39

What are the 2 types and their differences of dermal administration?

topical-site of intended use
transdermal-eventually goes systemic

40

There are 5 important considerations in selecting a route of administration. What are they? May just use this card for review.

Convenience
Chemical Nature
Extent of Metabolism
Rate of Absorption
Concentration at site of action

41

What are the 4 main advantages of oral administration?

convenient, economical, relatively safe, slow/prolonged absorption

42

Why isn't oral administration always used?

HAS THE MOST PROBLEMS TOO!
-irritation
-destruction by acids
-formation of complexes in gut
-slow onset
-Uncooperative patients
incomplete absorption
-first pass effect

43

What is the first pass effect?

is a phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation---mainly by the liver

44

What is the advantage of sublingual administration?

eliminates first pass effect- avoids acids, enzymes and liver

45

What is the problem(2) with sublingual administration?

irritation and bad taste

46

What is the advantage of rectal administration?

reduces first pass effect (certain patients might be better i.e.. unconscious)

47

What are the 2 problems with rectal administration?

lack of compliance and inconvenience

48

What are the advantages (2) for subQ/intramuscular injections?

useful for proteins/peptides
can alter rate of absorption in the body

49

What are the 2 problems with subQ/intramuscular injections?

irritation
variable blood flow

50

What are the 3 advantages to intravenous administration?

easily controlled rate of administration
rapid onset of action
entire dose enters blood

51

What are 2 disadvantages of intravenous administration?

sterility
not for self medication

52

What is the advantage of an intra-arterial administration?

high dose to a specific organ

53

What are the 2 disadvantages of intra-arterial administration?

danger of hemorrhage
difficult technique

54

What is the advantage of intraspinal administration? problem?

high level into the CNS past the BBB, problem=difficult technique

55

What is the advantage of inhalation as an administration?

only choice for gases or volatile liquids

56

what are the 2 disadvantages of inhalation administration.

irritation, solids need to be fine particles

57

What is the advantage of dermal administration? problem?

adv= local action with minimum systemic effects
problem= possible absorption and systemic effects

58

What is the advantage of transdermal administration? problem?

adv=convenient and prolonged delivery
problem=irritation

59

T-F--systemic intranasal administration is useful for peptides?

True

60

What is the difference between passive diffusion and facilitated diffusion?

passive has lipid solubility and facilitated need a carrier, but both are down a concentration gradient

61

For an acid-is the ionized form associated with the hydrogen or disassociated? For a base?

ACID=disassociated is ionized
BASE=associated is ionized

62

What is the henderson hasselbalch equation for acids?

pH=pKA+log[ionized]/[non-ionized]

63

What is the henderson hasselbalch equation for bases?

pH=pKA+log[non-ionized]/[ionized]

64

What is the pH partition hypothesis?

Non-ionized more lipid-soluble form of a weak acid/base crosses the biomembrane much more readily than the ionized more water-soluble form does

65

Does charged or non-charged particles move across a membrane easier?

non-charged

66

Are weak acids better absorbed at pHs below or above their pKA?

BELOW

67

Are weak bases better absorbed at pHs below or above their pKa?

ABOVE

68

What is the key difference between facilitated diffusion and active transport?

active transport needs an energy source

69

what is the key difference between an ABC transporter and a SLC transporter?

ABC transport is primary active transport and directly contains an ATPase, whereas SLC has an indirect energy source and works through an anti porter type system down the gradient of a solute.

70

What disease is caused by defect in ABC A1 transporter?

tangier disease (cholesterol)

71

What disease is caused by defect in ABC C2 transporter?

dubin-johnson syndrome (bilirubin)

72

What disease is caused by defect in ABC C7 transporter?

cystic fibrosis (chloride)

73

What disease is caused by defect in glutamate transport?

ALS

74

What disease is caused by folate-thiamine transporter defect?

megaloblastic anemia

75

Are ABC transporters primarily involved in efflux or influx in regards to the cell?

efflux

76

Are SLC transporters primarily involved in efflux or influx in regards to the cell?

influx

77

What are 4 factors that affect absorption of drugs from all sites? (JUST REVIEW IT)

1. blood flow
2. surface of administration site
3. Number of cell layers
4. drug concentration

78

What are 4 factors that affect absorption of drugs in the GI tract? (JUST REVIEW IT)

1. Gastric Emptying Time
2. Intestinal Transit Time
3. Binding to Mucus and food
4. First pass effect

79

Are tissues with receptors or without receptors typically considered storage sites?

without receptors---> no response but drugs usually accumulate here.

80

What are 4 factors that affect distribution of drugs in the body? (Just review)

1. Blood Flow
2. Crossing membrane barriers
3. Polarity of drug
4. Binding to plasma proteins

81

Does a drug bound to plasma proteins get out of the blood well?

No

82

T-F---no matter how much drug is administered for the drug that binds plasma proteins, saturation will not be reached?

False-- administration of additional drug results in a more marked increase in the plasma concentration of free drug.

83

Can certain drugs compete with each other in regards to binding plasma proteins? consequences?

Yes---> can lead to potential dangerous side effects if both are in blood at same time.

84

Generally speaking what does not take place if a drug is bound to plasma proteins? [3]

no effect
no metabolism
no toxic effect
[opposite is true when it is not bound]

85

The blood brain barrier is made up of tight junctions between endothelial cells, what consequence in regards to drugs passing the barrier does this create?

lacks aqueous channels
must cross through diffusion or limited transporters

86

Do most drugs act receptor mediated or non-receptor mediated?

receptor mediated

87

What is the word for an all or none drug response?

quantal

88

What type of drug response is associated with blood pressure, plasma glucose levels, anti diabetic agents etc.?

graded drug response [as opposed to quantal which is all or none]

89

What is ED50?

effective dose to see results in 50% of the population OR effective dose to elicit a 50% proportion to a drug concentration

90

Can you measure quantal dose response in 1 individual?

No, but you can measure graded dose response in 1

91

CAn a lethal dose be graded?

No, must be quantal

92

In a graded response curve- can the curve always go up with more drug?

No- saturates and plateau

93

What are the key differences in regards to efficacy and potency?

efficacy-Emax is different
potency-Emax can be reached but dose amount is different

94

What is the potency ratio?

ED50 of drug that takes a larger dose divided by ED50 of drug that takes a smaller dose to elicit same response

95

That is the therapeutic index ratio?

TD50/ED50
or
LD50/ED50
[it is important to remember that when we are looking at potency, it is the same effect. however, when we are looking at therapeutic index, it is a very different effect]

96

Is a therapeutic index of lower than 10 safe?

No

97

Is a therapeutic index of higher than 500 safe?

Yes- considered very safe

98

What is a drug that by itself produces a response?

agonist

99

What is a drug that produces no response but stops other responses?

antagonist.

100

can the antagonist block an endogenous agonist or only other drugs?

can block both

101

Is an antagonist and an inverse agonist the same?

no--an inverse agonist illicits a response in the effect that it represses. antagonist don't illicit any response by itself

102

What are the 3 main types of antagonists mentioned?

pharmacological
chemical
physiological

103

What are the 2 types of pharmacological antagonists?

competitive and non-competitive

104

Do pharmacological antagonists interact with receptors directly?

yes

105

Can adding more agonist overcome competitive antagonists or non-competitive antagonists?

competitive antagonists-->effects are reversible

106

Are the non-competitive antagonist effects reversible?

No- have to wait for re-synthesis of the receptor

107

Are partial agonists used as antagonists?

yes---they compete with the agonist and because their effects are partial they illicit a smaller effect and therefore antagonize

108

How do chemical antagonists act?

bond with agonist in a way that the receptor can not be activated

109

What type of drug only reacts with a single receptor sub-type?

receptor specific drug

110

What type of drug reacts with multiple receptor subtypes but favors one of them?

receptor selective drug---most drugs

111

What is synergistic effect?

response is greater than the sum of the 2 drugs

112

What is an unusual or atypical response in small % of individuals?

idiosyncratic drug response

113

what is an allergic response to a drug?

hypersensitivity

114

What is a less than expected response?

hyporeactivity

115

what is a greater than expected response?

hyperreactivity

116

what is a decreased response that takes hours to develop?

tolerance

117

What is a decreased response that takes minutes to develop?

tachyphylaxis

118

What is a decreased response to the point that there is not response?

refractoriness

119

What are the four basic sources of side/effects? (just think logically, not that bad)

1. Chemical Properties of the drug
2. Drug that interacts with multiple receptor types (dirty)
3. Interact with single receptor but multiple subtypes
4. Drug that interacts with single receptor but it is on many different tissues.

120

What is the one goal of pharmacology?

eliminate undesirable effects by increasing receptor specificity

121

What are the 3 main ways of terminating drug action?

redistribution, biotransformation, excretion

122

What are the 2 usual major effects of biotransformation?

1. more hydrophilic
2. less pharmacologically active

123

What happens in a phase I reaction?

introduction or unmasking of OH, NH2, SH

124

What are the main metabolizing families for biotransformation oxidation?

CYP1, CYP2, CYP3

125

What are the 3 reaction types of phase I biotransformation?

Oxidation, reduction, hydrolysis

126

What happens in a phase II reaction?

conjugation of an endogenous polar substance [typically these are fairly large moieties]

127

What type of reaction do UGTs, STs, COMT, acetyltransferase, and glutathione transferases fall under?

Phase II

128

What is conversion of an active or toxic compound to a much less active, inactive or non-toxic compound?

detoxification

129

What is a drug metabolite that has significant activity?

active metabolite

130

What is an inactive or relatively inactive precursor that is converted by metabolism to a more active compound?

pro-drug

131

What is a very toxic compound produced by biotransformation of a relatively inert substance?

reactive metabolite

132

What does cimetidine, macrolide antibiotics, grapefruit, and proadifen do?

inhibitors of drug metabolism and therefore increase drug level
[NOTE: THIS IS A VERY COMMON SITE OF WHERE DRUG DRUG INTERACTION OCCURS]

133

What do ethanol, phenobarbital, phenytoin, and DDT do?

activators of drug metabolism and therefore decrease drug levels

134

What are the 4 major routes of drug excretion?

kidney, liver, GI, Lungs

135

What are 4 minor routes of drug excretion? [JUST REVIEW]

mammary glands, sweat glands, salivary glands, tear ducts

136

What is the primary means of terminating drug action?

excretion [mainly urine and feces]

137

T-F---most drugs are able to be excreted through urine and feces.

False--usually one route

138

What are the limitations to kidney filtration in the glomerulus?

size and protein binding

139

How can we alter drug excretion through excretion? [2]

increase urinary volume [diuretics]
increase blood flow to the kidney

140

What types of drugs readily diffuse across membranes so retention in renal tubule is limited as fluid is reabsorbed?

non-ionized, lipophilic drugs

141

What is one benefit of making drugs more polar through biotransformation as it relates to excretion?

Polar molecules won't cross back into the body once in the renal tubules [or it is less likely]

142

How can we alter excretion for weak acids and weak basis for better excretion?

Change pH of plasma or tubule lumen

143

What is a competitive inhibitor of organic anion transporter?

probenecid

144

What is a competitive inhibitor of organic cation transporter?

cimetidine

145

What is the excretion pathway in the liver?

via bile into the intestine [remember same process in the liver as in kidney, but substances <200 MW are only filtered]

146

What is enterohepatic circulation?

reservoir created by recycling drug getting reabsorbed by intestine then going back through liver

147

T-F--our micro biome may take of conjugate of a drug metabolite?

True--then it may get recycled