Neuro-Intro to Pharmodynamics Flashcards
What is an inert binding site
Part of the biological system where a drug can bind without any changes in the function
What are the characteristics of the covalent binding of a ligand to a receptor
Irreversible, so synthesis of a new receptor or enzymatic cleavage
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
What are the characteristics of the ionic bonds
Interactions between positive and negatively charged ions
What are the characteristics of the hydrogen bonds
Electrostatic between the positive charged hydrogen with eh negative charge of other ions
What are the characteristics of the hydrophobic interactions
Hydrophobic regions between the drugs and the receptors
What are the characteristics of the Van Derek Waals forces
Weak electrostatic between the dipoles in the functional group
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
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)
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
What are the characteristics of the cumulative quantal curve
Number of individuals who are at the dose, and all doses under that value
How is therapeutic Index calculated
TD50/ED50
What is the general trend of the therapeutic index in a safe drug
A higher TI, because the ED50 is lower
What is the therapeutic window
Range of doses of a drug in a bodily system that provides safe and effective therapy
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
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
When you plot a drug dose arithmeticially, what does the curve look like
Hyperbolic
When you plot a dose response curve logarithmically, what does the curve look like
Sigmoidal curve
What does TD50 mean
Mean toxic dose
What the rank in order of affinity for the mu opioid receptor
1) Fentanyl >
2) Morphine >
3) Meperidine
What is the another name for the x axis
Abscissa
What is another name for the y axis
Ordinate
Where in the quantal dose response curve is the low dose responders
The lower plateau phase of the bell curve
Where in the quantal dose response curve is the high dose responders
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
