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Pharmacology- Test 1 Material > 01- Intro to Pharmacology > Flashcards

01- Intro to Pharmacology Flashcards

1
Q

Henderson-Hasselbalch equation of Weak Base

A

pH= pKa + log ([non-ionized]/[ionized])

pH= pKa + log ([B]/[BH+])

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2
Q

Pharmacology

A

study of how drugs (medications) affect biological systems

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3
Q

Pharmacy

A

production, compounding, and distribution of drugs (medications)

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4
Q

Toxicology

A

study of toxic effects of drugs and other chemicals on biological systems

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5
Q

Therapeutics

A

treatment of disease

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6
Q

Pharmacotherapeutics

A

treatment of disease with a drug

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7
Q

Pure Food and Drug Act- 1906

A

Required manufacturers to put active ingredients on drug labels
-first pharma law passed

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8
Q

Harrison Narcotic Act- 1914

A

Made it illegal to sell drugs of abuse over the counter but were made available with a perscription

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9
Q

Food, Drug, and Cosmetic Act- 1938

A

Had to demonstrate product was safe before you could market it and had to label both active and inactive ingredients on content labels

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10
Q

Durham-Humphrey Amendments to Food, Drug, and Cosmetic Act- 1951

A

Created two drug categories:
Legend Drugs- prohibited from dispensing without a prescription (drugs that can cause significant side effects
OTC Drugs- drugs can be received over the counter and considered relatively safe

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11
Q

Kefauver-Harris Amendments to Food, Drug, and Cosmetic Act- 1962

A

Required manufacturers to demonstrate that product had to be as effective or more effective than any current drug on the market

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12
Q

Controlled Substances Act- 1970

A
  • Created strict outlines for distribution of drugs with addictive potential
  • created DEA in dept. of justice
  • required prescribers to be licensed
  • required prescription limits
  • Schedules (I- no medical use, II- highest addictive potential, on down)
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13
Q

Dietary Supplement Health & Education Act- 1994

A

Removed vitamins, minerals, herbals, botanicals, etc. from FDA control

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14
Q

pH Partition Hypothesis

A

For Weak Organic Acids or Weak Organic Bases, the Non-Ionized, more lipid-soluble form crosses biomembranes much more readily than does the Ionized, more Water-Soluble form

HA H+ + A- (weak acid) BH+ B + H+ (weak base)

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15
Q

ABC Transporters

A

Primary active transporters with ATPase activity

-MRPs (MDR, P-Glycoproteins)

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16
Q

SLC Transporters

A

Secondary active transport

  • Co-transporters using indirect energy, usually anti-porters
  • Organic Anion transporters- wide variety of organic acids
  • organic cation transporters- wide variety of organic bases
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17
Q

Receptor Mediated

A

most drugs act via interactions with receptors

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18
Q

Non-Receptor Mediated

A

Drugs that do not act by interaction with receptors.

  • usually produce direct chemical effect or binds a molecule
  • produces a direct effect
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19
Q

Quantal Response

A

all or none response

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20
Q

Graded Response

A

Continually increasing or decreasing

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21
Q

ED50

A

amount of drug that produces a response in 50% of the population

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22
Q

TD50

A

amount of drug that is toxic to 50% of population

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23
Q

LD50

A

amount of drug that is lethal to 50% of the population

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24
Q

Efficacy

A

refers to how big of a response you can produce with a particular drug

  • change in Emax (y-axis)
  • ED50 remains the same (x-axis)
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25
Q

Potency

A

how much drug does it take to produce a response

  • ED50 will change (x-axis)
  • Emax will remain the same (y-axis)
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26
Q

Potency Ratio

A

reflects the difference in potencies of two drugs and is used to measure how much of one drug would you need to get the same effect as the other drug
Potency Ratio= ED50 Drug A/ ED50 Drug B

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27
Q

Therapeutic Index

A

-unitless number that characterizes the safety of a drug by describing the difference between the ED50 and TD50
-drugs with high T.I. will produce therapeutic effects with low risk of toxicity
T.I.= TD50/ED50

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28
Q

Agonist

A

a drug that, by itself, produces a response

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29
Q

Antagonist

A

a drug that, by itself, produces no response but prevents the agonist response

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30
Q

Full Agonist

A

drugs that produce the highest response in a drug class (highest Emax)

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31
Q

Partial Agonist

A

Agonist that produces a response lower then full agonist

-will never have as high of an Emax because doesn’t stimulate receptors as effectively

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32
Q

Inverse Agonist

A

by itself is producing a response but the response is inhibitory
-need some sort of basal response for this to suppress

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33
Q

Competitive Antagonists

A

interferes with the agonist response by competitively binding to a receptor

  • simple competition so is not permanent and can be competed off by giving more agonist
  • will see change in ED50 but not in Emax
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34
Q

Non-Competitive Antagonist

A

covalently bind to receptor irreversibly

  • will see change in Emax but not ED50
  • cannot be reversed by giving more agonist
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35
Q

Chemical Antagonists

A

inhibit agonist by chemically interacting with it which neutralizes its ability to bind to a receptor and produce a response

36
Q

Physiological Antagonist

A

two agonists that act at their own receptor and produce opposite physiological responses
-ACh and Epi

37
Q

Receptor SPECIFIC Drug

A

interacts with only a single receptor sub-type

38
Q

Receptor SELECTIVE Drug

A

interacts with several receptor sub-types but has a preference for one of them

39
Q

Additive Response

A

response of two drugs together is sum of response to each

40
Q

Synergistic Response

A

response to two drugs together is greater than the sum of response to each

41
Q

Idiosyncratic Drug Response

A

unusual or atypical response in small % of individuals

42
Q

Hypersensitivity

A

allergic response

43
Q

Tolerance

A

decreased response (takes hours to develop)

44
Q

Tachyphylaxis

A

decreased response that develops in minutes

45
Q

Refractoriness

A

decreased response to no response

46
Q

Biotransformation

A

metabolism of drugs

  • usually converts to more hydrophilic compound for excretion
  • usually converts substances to less pharmacologically active compound
47
Q

Phase I Reaction

A

introduction or unmasking of a functional group (-OH, -NH2, -SH)

  • oxidations (CYPs, MAOs), reductions, hydrolysis
  • product usually more polar
48
Q

Phase II Reaction

A

conjugation of endogenous polar substance to functional group on substrate

  • transferases
  • products usually very polar
49
Q

Probenecid

A

competitive inhibitor of organic anion transporter

50
Q

Cimetidine

A

an Imidazole that acts as competitive inhibitor of organic cation transporter and also contributes to decrease drug metabolism which leads to higher drug plasma levels

51
Q

Henderson-Hasselbalch Equation of Weak Acid

A

pH= pKa + log (ionized/non-ionized)

pH= pKa + log ([A-]/[HA])

52
Q

Active Metabolite

A

drug metabolite that has significantly activity (sometimes greater than parent compound)

53
Q

Reactive Metabolite

A

very toxic compound (e.g. carcinogen) produced by biotransformation of a relatively inert substance

54
Q

Prodrug

A

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

55
Q

Detoxification

A

conversion of an active or toxic compound to a much less active, or inactive compound

56
Q

Active secretion

A

secretion of a drug through use of active transporters

-requires energy and transporters can be saturated resulting in a maximal rate of secretion

57
Q

Enterohepatic Circulation

A

when a drug travels from liver to bile duct to intestine and then is either reabsorbed back into blood stream or excreted
-some drugs can maintain therapeutic levels by being continuously reabsorbed from intestine

58
Q

Side effects

A

minor, undesired effects of a drug that are not medically serious

59
Q

Adverse effects

A

undesired effects of a drug that are major, and have serious medical consequences

60
Q

Toxic Effects

A

very serious adverse effects produced by a drug

61
Q

Hyperreactive

A

greater then expected response to a drug

62
Q

Hyporeactive

A

less then expected response to a drug

63
Q

Intrinsic Efficacy

A

the ability of a drug to interact with and stimulate the receptor

64
Q

Protein Binding

A

Drugs may bind to plasma proteins

  • protein binding sites are saturable
  • drugs may competitively bind proteins leading to dangerous Drug-Drug interactions (one may become excessively free in plasma and cause toxicity)
  • FROM REVIEW: will not generally effect the absorption of a drug
65
Q

Enteral

A

oral, sublingual, rectal routes of admin

66
Q

Paranteral

A

subQ, IM, IV, IA, intraspinal routes of admin

-usually any route involving a needle

67
Q

Pulmonary Route

A

inhalation routes

68
Q

Dermal

A

topical, transdermal routes

69
Q

Blood-Brain Barrier

A

tight junctions between endothelial cells of brain capillaries

  • lack aqueous channels so drugs must transit cells
  • lipophilic drugs much more permeable then hydrophilic
70
Q

Drug Receptors

A

normal endogenous components of cells that are present to recognize normal endogenous molecules but also happen to recognize and bind specific drugs.
-once activated, receptor produces observed effect of the drug

71
Q

CYPs

A

P450 mixed function oxidases that metabolize a wide variety of endo and xenobiotics

72
Q

SLC Transporter

A

sub-set of active transporters that uses an indirect energy source
-usually functions as co-transporter that transports Ion along with drug (usually anti-porters)

73
Q

OAT Transporter

A

organic anion transporter

-transports a wide variety of weak acids

74
Q

OCT Transporter

A

organic cation transporter

-transports a variety of weak bases

75
Q

MRP Transporter

A

Sub-family of ABC transporters (MDR, P-glycoproteins) that uses active transport molecules (generally out of cell)
-FROM REVIEW: inhibition may cause SLC transporter to function poorly (pump drug into cell) and lead to higher plasma concentrations of drug

76
Q

a1-acid glycoprotein

A

plasma binding protein located in blood plasma that can bind to plasma free drug

77
Q

Redistribution

A

drug becomes inactive because it redistributes from an area containing receptors for the drug to an area that does not contain receptors for the drug

78
Q

Monoamine Oxidase

A

enzymes that performs Phase I reactions by oxidizing agents, usually to expose functional group and create more polar compound

79
Q

Acetylcholinesterase

A

enzyme that performs Phase 1 reaction (usually break down of ACh)
-found at

80
Q

Plasma Cholinesterase

A

enzyme that performs Phase 1 reaction

81
Q

Bioflavonoids

A

inhibitors of drug metabolism that lead to inc. levels of drug in the plasma
-common site of drug-drug interaction

82
Q

Pharmacogenetics

A

genetic polymorphisms to specific enzymes that affect drug metabolism
-variants that decrease level or activity of enzyme so drug is metabolized more slowly

83
Q

Excretion

A

a primary means of reducing drug concentration in tissues, and, thus, in terminating drug action

  • drugs primarily excreted by one route
  • deficiency in route will lead to inc. plasma concentration of a drug unless frequency or dose reduced
84
Q

Filtration

A

a mechanism of drug excretion where drug is filtered out of blood and eliminated
-that takes place primarily in kidney but also in liver

85
Q

ethanol

A

activator of drug metabolism that decreases plasma levels of a drug (can cause toxicity of reactive intermediates formed)
-common site of drug-drug interaction

86
Q

erythromycin

A

macrolide antibiotic that acts as inhibitor of drug metabolism that lead to inc. levels of drug in the plasma
-common site of drug-drug interaction

87
Q

phenobarbital

A

activator of drug metabolism that decreases plasma levels of a drug (can cause toxicity of reactive intermediates formed)
-common site of drug-drug interaction

Pharmacology- Test 1 Material (8 decks)

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