Neuro-Intro to Pharmodynamics Flashcards by Michael Dennis

What is an inert binding site

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

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

Irreversible, so synthesis of a new receptor or enzymatic cleavage

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List the type of bonds from the strongest to the weakest

1 ) Ionic Bonds

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

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What are the characteristics of the ionic bonds

Interactions between positive and negatively charged ions

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What are the characteristics of the hydrogen bonds

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

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What are the characteristics of the hydrophobic interactions

Hydrophobic regions between the drugs and the receptors

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What are the characteristics of the Van Derek Waals forces

Weak electrostatic between the dipoles in the functional group

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What are the characteristics if a graded response

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

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What are the characteristics of the a quantal response

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

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

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What are the characteristics of the cumulative quantal curve

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

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How is therapeutic Index calculated

TD50/ED50

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

A higher TI, because the ED50 is lower

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What is the therapeutic window

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

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

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

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What is the level of intrinsic activity in agonists and antagonists

Agonists-has intrinsic activity

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

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

Hyperbolic

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

Sigmoidal curve

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What does TD50 mean

Mean toxic dose

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

1) Fentanyl >
2) Morphine >
3) Meperidine

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What is the another name for the x axis

Abscissa

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What is another name for the y axis

Ordinate

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

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The lower plateau phase of the bell curve

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

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The upper plateau phase in the bel curve

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

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

What will the cumulative quantal dose response curve look like

Sigmoidal

What is meant by a wide therapeutic window

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

Which type of drug as intrinsic activity

Agonists ( whether partial, full, or inverse)

What is a full agonists

Produce Emax, meaning maximal pharmacological effects at full receptor occupancy

What is a partial agonist

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

What is an inverse agonist

Produces an effect opposite to a full or partial agonist

What is a pharmalogic (receptor) antagonist

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

What is a chemical antagonist

When the chemical antagonist makes the other drug unavailable

What is a physiological antagonist

Occurs between endogenous pathways regulated by a different receptor

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

Competitive antagonist

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

Noncompetitive agonist site antagonist

What is a characteristic of a full agonist

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

What is an example of a situation of a full agonist

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

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

Blocking the action of endogenous ligands at the receptors

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

Blockade of the alpha 1 adrenoceptors by an antihypertensive drug

What does the drug Prozosin work by

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

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

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

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

They work via the same receptors and signal transduction pathways

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

Work via the same receptors and signal transduction pathways

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

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

What does lower selectivity tend to lead to

Increased incidences of side effects

What are pharmodynamics

How the drugs effect the body

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

Hyperbolic curve

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

Sigmoidal curve

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

Quantal

What are the parameters describing drug receptor interactions

- Affinity - Selectivity - Intrinsic activity

What is intrinsic activity

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

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

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

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

Noncompetitive allosteric antagonist

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

Noncompetitive allosteric antagonist

Neuro-Intro to Pharmodynamics Flashcards

(55 cards)