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Pharmacology Class > Neuro-Intro to Pharmodynamics > Flashcards

Neuro-Intro to Pharmodynamics Flashcards

1
Q

What is an inert binding site

A

Part of the biological system where a drug can bind without any changes in the function

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2
Q

What are the characteristics of the covalent binding of a ligand to a receptor

A

Irreversible, so synthesis of a new receptor or enzymatic cleavage

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3
Q

List the type of bonds from the strongest to the weakest

A

1 ) Ionic Bonds

2) Hydrogen bonds
3) Hydrophobic interactions
4) Van Derek Waals Forces

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4
Q

What are the characteristics of the ionic bonds

A

Interactions between positive and negatively charged ions

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5
Q

What are the characteristics of the hydrogen bonds

A

Electrostatic between the positive charged hydrogen with eh negative charge of other ions

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6
Q

What are the characteristics of the hydrophobic interactions

A

Hydrophobic regions between the drugs and the receptors

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7
Q

What are the characteristics of the Van Derek Waals forces

A

Weak electrostatic between the dipoles in the functional group

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8
Q

What are the characteristics if a graded response

A

Answers “how much”, so the response will vary, but usually represents the mean value of a population

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9
Q

What are the characteristics of the a quantal response

A

All or none, usually yea no binary response. Can also be a predefined response (death, falling asleep, 10% reduction in BP, etc)

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10
Q

What are the characteristics of the non-cumulative dose response curves

A

Quantal dose curve, with eh number of individuals responding to a certain dose and only that dose

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11
Q

What are the characteristics of the cumulative quantal curve

A

Number of individuals who are at the dose, and all doses under that value

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12
Q

How is therapeutic Index calculated

A

TD50/ED50

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13
Q

What is the general trend of the therapeutic index in a safe drug

A

A higher TI, because the ED50 is lower

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14
Q

What is the therapeutic window

A

Range of doses of a drug in a bodily system that provides safe and effective therapy

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15
Q

What is the determining factor in the quantitative relationship between a drug and its effects

A

Receptors determine it and its effect will be proportional to the degree of interaction

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16
Q

What is the level of intrinsic activity in agonists and antagonists

A

Agonists-has intrinsic activity

Antagonists-No intrinsic activity, no change in function of receptor upon binding

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17
Q

When you plot a drug dose arithmeticially, what does the curve look like

A

Hyperbolic

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18
Q

When you plot a dose response curve logarithmically, what does the curve look like

A

Sigmoidal curve

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19
Q

What does TD50 mean

A

Mean toxic dose

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20
Q

What the rank in order of affinity for the mu opioid receptor

A

1) Fentanyl >
2) Morphine >
3) Meperidine

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21
Q

What is the another name for the x axis

A

Abscissa

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22
Q

What is another name for the y axis

A

Ordinate

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23
Q

Where in the quantal dose response curve is the low dose responders

A

The lower plateau phase of the bell curve

24
Q

Where in the quantal dose response curve is the high dose responders

A

The upper plateau phase in the bel curve

25
Q

What will the graph of a non cumulative quantal dose response curve look like

A

A bell shape curved, because it is only talking about one dose of drug

26
Q

What will the cumulative quantal dose response curve look like

A

Sigmoidal

27
Q

What is meant by a wide therapeutic window

A

The location of the therapeutic sigmoidal curve and how far it is from the adverse reaction sigmoidal curve

28
Q

Which type of drug as intrinsic activity

A

Agonists ( whether partial, full, or inverse)

29
Q

What is a full agonists

A

Produce Emax, meaning maximal pharmacological effects at full receptor occupancy

30
Q

What is a partial agonist

A

Produces sub Emax pharmalogical effects at full receptor occupancy (this is the case for most drugs)

31
Q

What is an inverse agonist

A

Produces an effect opposite to a full or partial agonist

32
Q

What is a pharmalogic (receptor) antagonist

A

Action at the same receptor as the endogenous ligand or agonist drug

33
Q

What is a chemical antagonist

A

When the chemical antagonist makes the other drug unavailable

34
Q

What is a physiological antagonist

A

Occurs between endogenous pathways regulated by a different receptor

35
Q

What type of antagonist is a receptor antagonis that binds to the agonist site reversibly

A

Competitive antagonist

36
Q

What type of antagonist is an agonist site binding binding in an irreversible manner

A

Noncompetitive agonist site antagonist

37
Q

What is a characteristic of a full agonist

A

Drug or chemical that mimics the actions of the endogenous chemicals at the receptors

38
Q

What is an example of a situation of a full agonist

A

The use of pain killers to activated the mu opioid receptors Via codeine, morphine, and meperidine

39
Q

What is the overall characteristic of antagonists, partial and inverse agonist

A

Blocking the action of endogenous ligands at the receptors

40
Q

What is the example for antagonists, partial, and inverse agonists

A

Blockade of the alpha 1 adrenoceptors by an antihypertensive drug

41
Q

What does the drug Prozosin work by

A

Blocking of the alpha 1 adrenoceptor from binding norepinephrine (leads to decrease in blood pressure)

42
Q

What is the relation of pathways between the beneficial and adverse effects of a drug

A

Mediated by the same receptors/signal transduction pathway in the same type of cells or via different pathways

43
Q

Via administration of insulin, what is the type of relationship between beneficial and toxic effects

A

They work via the same receptors and signal transduction pathways

44
Q

Via beta 2 administration, what is the relationship between beneficial and toxic effects

A

Work via the same receptors and signal transduction pathways

45
Q

What is the general characteristics of relation between beneficial and toxic effects of more selective drugs

A

More selective drugs are more likely to have more therapeutic effect per adverse effects

46
Q

What does lower selectivity tend to lead to

A

Increased incidences of side effects

47
Q

What are pharmodynamics

A

How the drugs effect the body

48
Q

What does a dose response curve look like when it is plotted arithmetically

A

Hyperbolic curve

49
Q

What does a dose response curve look like when it is plotted logarithmically

A

Sigmoidal curve

50
Q

Which does response curve is used to look at the frequency of responses within a large population

A

Quantal

51
Q

What are the parameters describing drug receptor interactions

A
  • Affinity
  • Selectivity
  • Intrinsic activity
52
Q

What is intrinsic activity

A

Ability of a drug to change a function of a receptor to produce a physiological response upon its binding

53
Q

In the case of partial agonists, what is the mechanism that it produces less than the maximum result

A

The ligand/drug not only binds to the activating receptor, but also binds to the inhibiting receptor that can lower the effect seen

54
Q

What is the characteristic of an antagonist that binds to an allosteric binding site in an irreversible manner

A

Noncompetitive allosteric antagonist

55
Q

What is the characteristic of an antagonist that binds to an allosteric binding site in a reversible manner

A

Noncompetitive allosteric antagonist

Pharmacology Class (7 decks)

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