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PHARMACOLOGY > M1: Ch2 Drug Receptors & Pharmacodynamics > Flashcards

M1: Ch2 Drug Receptors & Pharmacodynamics Flashcards

0
Q

Chemical agent that affects the biological system in a potentially useful way. For prevention, diagnosis & treatment of illnesses.

A

Drug

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1
Q

Science of dealing w/ interactions of chemical agents & living systems

A

Pharmacology

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2
Q

Used for diagnosis of Pheochromocytoma

A

VGA

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3
Q

Chemical agent that produces harmful effects. Especially in high doses.

A

Poison

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4
Q

Drug concentration and its biologic effects. What drugs do to the body.

A

Pharmacodynamics

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5
Q

What the body does to the drug

A

Pharmacokinetics

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6
Q

Four processes occurring in Pharmacokinetics

A

Absorption, Distribution, Metabolism & Elimination

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7
Q

Formulated the latin saying “Corpora non agunt nisi fixata”

A

Paul Ehrlich

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8
Q

Chemical reaction of molecules through their interaction of basic/acidic properties

A

Mechanism of Action

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9
Q

An example of Antacid

A

Aluminum Magnesium Hydroxide

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10
Q

Other name of Aluminum Magnesium Hydroxide

A

Maalox

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11
Q

Used as an antidote in heparin overdose

A

Protamine Sulfate

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12
Q

An example of membrane surfactant which binds with ergosterol. Interferes with synthesis of fungal cell wall then destroys its integrity causing leakage.

A

Amphotericin B

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13
Q

Ability of drugs to denature protein. An example of this is

A

Astringent

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14
Q

Macromolecule component of a cell or organism that interacts with a drug and initiates the chain of biochemical events leading to the drug’s observed effects.

A

Receptor

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15
Q

Drug molecule. May interact with drug receptor & would translate to a positive reaction.

A

Ligands

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16
Q

Ability to bind

A

Affinity

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17
Q

Ultimately leads to a drug effect

A

Transduction of signal

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18
Q

Nonregulatory molecules capable of binding to receptors which will result in no detectable change in function; not completely without significance (used to determine amount of free drug in the circulation). It can be bind but unable to transduce particular signals.

A

Inert binding sites

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19
Q

Examples of Inert binding sites

A

Albumin & A1 Glycoprotein

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20
Q

Receptor Subtypes: example is xanthine oxidase

A

Enzymes

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21
Q

Interferes with action of Xanthine Oxidase. Anti hyperuricemic agent.

A

Allopurinol

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22
Q

Receptor Subtypes: Examples are Calcium channel blockers

A

Ion Channels

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23
Q

Example of Calcium channel blockers

A

Nifedipine, Verapamil & Daltiazem “NVD”

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24
Q

Receptor Subtypes: examples are alpha & beta adrenergic receptors

A

Membrane receptors

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25
Q

Alters the activity of membrane activated enzymes. G proteins.

A

Epinephrine

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26
Q

Perfect compatibility between drug molecule and receptors. Perfect fit.

A

Lock & Key model

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27
Q

Chemical Basis for D-R Interaction: weak but able to interact. More common.

A

Electrostatic Interaction

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28
Q

Examples of Electrostatic Interaction

A

H bonds & vdw

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29
Q

Chemical Basis for D-R Interaction: Important for lipid soluble drugs

A

Hydrophobic Interactions

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30
Q

Chemical Basis for D-R Interaction: Least common but strongest in all chemical reactions.

A

Covalent bond

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31
Q

An example of a drug with covalent bond which interacts with Alpha adrenergic receptors.

A

Phenoxybenzamine

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32
Q

An example of a Stereospecific drug

A

Carvedilol

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33
Q

For Alpha & Beta Adrenergic Receptors

A

S Carvedilol

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34
Q

Only for Alpha Adrenergic Receptors

A

B Carvedilol

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35
Q

Drug agonists act by binding to (occupying) a distinct class of biologic molecules with a characteristic affinity for the drug receptor.

A

Mass action law

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36
Q

Maximal response that can be produce by a drug

A

Emax

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37
Q

Concentration of drug that produces 50% maximal effect

A

EC50

38
Q

Total concentration of receptor sites are occupied already (ex. Sites bound to the drug at infinitely high concentrations).

A

Bmax

39
Q

Concentration of free drug at which half maximal binding has been achieved.

A

Kd

40
Q

If Kd is low, binding affinity is

A

High

41
Q

Dose-Response Relationship: Responses to low doses of the drug usually ______ in direct proportion of the dose.

A

Increase

42
Q

Dose-Response Relationship: As the dose increase, it reaches a point where

A

No further increase in response can be achieved

43
Q

Dose-Response Relationship: At low concentration, effect changes

A

Rapidly

44
Q

Dose-Response Relationship: At higher concentration, effect changes

A

Gradually

45
Q

Transduction process that links drug occupancy of receptors & pharmacologic response

A

Coupling

46
Q

Maximal biologic response at a concentration of agonist that does not result in occupancy of the full complement of available receptors. Full effect was achieved but D-R binding are not fully saturated.

A

Spare receptors

47
Q

In Spare Receptors: Non occupancy of the full complement of available receptors. EC50 is ___________.

A

Less than Km

48
Q

Drugs that bind & activate receptors. They are the key.

A

Agonists

49
Q

Bind and prevent agonist from binding.

A

Classical Antagonist

50
Q

Prevent agonists from activating receptors. Binds to receptors but do not activate them.

A

Receptor Antagonists

51
Q

The tenacity or degree of attraction of a ligand to a receptor. Probability of a molecule to bind to its receptor. Drug gets bound to the receptor.

A

Affinity

52
Q

Quality to determine its ability to produce a biologic effect. Property relating to drug molecule to itself. What happens once the drug is bound.

A

Efficacy

53
Q

Comparative for distinguishing which agonist has higher affinity for a given receptor

A

Potency

54
Q

Drug that produce less than maximal activation of a receptor.

A

Partial Agonist

55
Q

Signal Transduction Mech of Agonist: Drug structurally attach itself to ion channels. Conformational change in receptor complex. Ion channels open w/c results to a flow of permeant ion.

A

Direct Activation of Ion Channel

56
Q

Direct Activation of Ion Channels are commonly found in

A

NMJ, Excitatory receptors & GABA receptors “NEG”

57
Q

Receptors that commonly affects NMJ

A

Nicotinic Receptors

58
Q

Excitatory AAs

A

Glycine, Aspartate & Glutamine “GAG”

59
Q

Signal Transduction Mech of Agonist: Activation of ion channels. Drug attaches to receptor. Activation of G protein. G protein subunits stimulate the channel to open.

A

Activation of G Proteins

60
Q

Example of Activation of G Proteins

A

M2 Cholinergic Receptors

61
Q

Activation of ion channels

A

GS activation

62
Q

Induces B1 Receptor Binding

A

NorEpinephrine

63
Q

Activation of adenylyl cyclic, (+) cAMP, (+) Protein Kinase A which acts as a second messenger.

A

G protein mediated

64
Q

Activation of PKC to IP3 then release of Calcium

A

Phospholipase C

65
Q

Uses second messenger, PK-C. Increases vascular wall.

A

Angiotensis

66
Q

Most hormones utilize this

A

Tyrosine Kinase

67
Q

Long lasting in nature

A

Phosphorylation of Tyrosine Kinase

68
Q

Positive Affinity, Negative Efficacy.

A

Antagonist

69
Q

Binding to a site on the receptor protein separate from the agonist binding site and thereby preventing receptor activation without blocking agonist binding. Actions are irreversible if they do not bind covalently.

A

Noncompetitive Antagonism

70
Q

Bind to a separate site on the receptor protein and alter receptor function without inactivating the receptor.

A

Allosteric modulators

71
Q

Bind to the agonist binding site of a receptor

A

Competitive Antagonism

72
Q

As the degree of antagonism increases with increasing dose of antagonist but can be overcome by increasing the dose of agonist. Agonist concentration-effect curve is shifted to the right.

A

Reversible competitive antagonism

73
Q

By covalent bond with the receptor or by binding so tightly that the receptor is unavailable for binding of agonist. Effect of antagonist is not affected even by the increase dose of drug. Antagonist inactivates the receptor.

A

Irreversible competitive antagonism

74
Q

Other types of Antagonism

A

Chemical, Pharmacokinetic & Physiological “CPP”

75
Q

Effect of two drugs may be combined

A

Additivity

76
Q

Example of Additivity

A

Barbiturates & Tranquilizers

77
Q

Phenomenon of total effect of two or more drugs more than cumulative sum of their individual effects. Barbiturates plus Alcolohol equals ______.

A

Synergism. Coma.

78
Q

Ability of a drug to affect a particular cell type.

A

Selectivity

79
Q

Narrow range of action

A

Increase Selectivity

80
Q

Broad range of action

A

Decrease Selectivity

81
Q

Drug has only one effect on all biological systems

A

Specificity

82
Q

Alpha 2 Selectivity

A

Yohimbine

83
Q

Majority of the drugs are more _________ than __________.

A

Selective than Specific

84
Q

Concentration range which a drug produces its therapeutic effect

A

Therapeutic window

85
Q

Cumulative calculation of the population responding to a particular drug. Depicts the dose of drug and the dose that gives a minimal effect. All or none.

A

Quantal Dose-Response Curve

86
Q

Example of a Quantal Drug-Response Curve Application

A

Use of Anticonvulsants

87
Q

Dose that produces a toxic effect in 50% of population. Median toxic dose.

A

TD50

88
Q

Dose that produces mortality in 50% of population. Median lethal dose.

A

LD50

89
Q

Therapeutic dose. Dose that produces desired response in 50% of population. Median effective dose.

A

ED50

90
Q

Ratio of the TD50 to the ED50. TD50/ED50.

A

Therapeutic Index

91
Q

The Higher the Therapeutic Index

A

The safer the drug would be

92
Q

The lower the EC50

A

The higher the Potency

93
Q

Indicates a more toxic scenario

A

Lower Therapeutic Index

PHARMACOLOGY (8 decks)

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