Pharmacodynamics Flashcards
It is the study of what the drug does to our body
Pharmacodynamics
A study of biochemical and physiological effects of the drug on the body
Pharmacodynamics
These are the macromolecules to where the medication binds to
Drug receptors
What is a drug-receptor
target molecules with which a drug molecule has to combine in order to elicit a response
When a drug binds to a receptor, what most likely to happen?
Ion channel will open or close
Biochemical messengers are activated
A normal cellular function is physically inhibited
a cellular function is “turned on”
types of biochemical messengers
cAMP
cGMP
Ca2+
inositol phosphate
Why must a receptor be selective in its ligand characteristics?
It has to be selective so it could elicit a response to a proper chemical signal and not to meaningless ones
These have a high selective affinity for the drug molecule
receptor site or recognition site
these are best-characterized drug receptors
regulatory proteins
Proteins that are considered as drug-receptor
Regulatory proteins enzymes transport proteins structural proteins nucleic acid
which of the following is an example of a receptor that could be classified as an enzyme?
- Na+ k+ ATPase
- tubulin
- dihydrofolate reductase
- NOTA
Dihydrofolate reductase
Na+ k+ ATPase is for transport proteins
tubulin is for structural proteins
Which of the following is true about noncompetitive antagonists?
a. surmountable
b. interact with receptors at a different site as the agonist
c. reversible
d. produced by antagonists that have the ability to activate receptors
Interact with receptors at a different site
These are components of endogenous molecules that bind drug without initiating events leading to any of the drug’s effect
Inert Binding sites
When albumin binds to a receptor but its interaction does not elicit a drug effect is an example of
inert binding sites
this refers to the strength of binding between a drug and its receptor
affinity
examples of inert binding sites
albumin and orosomucoid
it is the transduction process between occupancy of the receptors and drug response
coupling
Which of the class of receptors mediate the actions of hormones?
a. enzymes
b. structural proteins
c. nucleic acid
d. transport
e. regulatory proteins
Regulatory proteins
The type of drug interaction shown by the harmful effect observed in a person who takes a dose of alcohol and a dose of barbiturate:
a. additive
b. potentiation
c. antagonism
d. synergism
Synergism
This exists if the maximum drug response is obtained at less than the saturation of receptors
Spare receptors
this can fully activate the effector system when it binds to the receptor
agonist
Which of the following is recognized to be the most common type of receptors in the body?
a. receptors that open /close ion channels
b. G-protein-coupled receptors
c. receptor for lipid-soluble agents
G-protein-coupled receptors
A kind of agonist that fails to produce maximal effects even when all the receptors are occupied by the agonist:
a. strong agonist
b. full agonist
c. weak agonist
d. partial agonist
Partial agonist
a kind of agonist that must be bound to many drugs before it can elicit its maximal effect
weak agonist
An agent that can bind to a receptor and inhibit or block responses
antagonist
This type of agonist binds with the receptor at the same site as the agonists
Competitive agonist
True or False
Competitive antagonist binds to a receptor in a reversible way
True
This induces a change in the receptor that resulted to agonist being unable to recognize binding sites
Noncompetitive antagonist
This is similar to a competitive antagonist but the only difference is, this binds with the receptor permanently
Irreversibly antagonist
When a drug binds to a receptor, one of the following actions is likely to occur, except:
a. a cellular function is turned on
b. an ion channel is permanently configured
c. biochemical messengers are activated
d. a normal cellular function is physically inhibited
An ion channel is permanently configured
Which of the following is/are example(s) of physiologic antagonism:
a. protamine and heparin
b. dimercaprol and lead
c. cortisol and insulin
d. pralidoxime and phosphorus
cortisol and insulin
histamine and epinephrine
This type of antagonist involves two agonists which cancel one another
Physiologic antagonist
Which of the following substances works with ligand-activated receptors?
a. insulin
b. corticosteroid
c. epinephrine
d. acetylcholine
acetylcholine
A type of chemical agonist that is a chelator of lead and some other toxic chemicals
Dimercaprol
A positively charged protein that can be used to counteract histamine
Protamine
Molecules that translate the drug-receptor interaction into a change in cellular activity
effectors
The best example of an effector
adenylyl cyclase
Tyrosine Kinase Effector is both
effector and receptor
Which of the following forms of antagonisms does not involve interactions of drugs at a receptor but instead directly interacts with the drug being antagonized?
a. chemical antagonism
b. noncompetitive antagonism
c. physiologic antagonism
d. irreversible antagonism
Chemical antagonism
Example of agents that bind to intercellular receptors
corticosteroids mineralocorticoids sex steroids vitamin d thyroid hormone nitric oxide
Gs protein-coupled receptor that stimulates cAMP
epinephrine and norepinephrine
Gi protein-coupled receptor that inhibits cAMP
acetylcholine and adenosine
Gq protein-coupled receptors that activate the inositol triphosphate pathway
norepinephrine, angiotensin II, and endothelin-1
types of excitatory amino acids
glycine, aspartate, and glutamate
The following receptors are found outside, except:
a. receptor that open/close ion channels
b. g-protein-coupled receptors
c. receptor for lipid-soluble agents
d. enzyme-linked receptors
receptor for lipid-soluble agents
occurs when the drug has little to no effect on a given variable greatly amplifies the effect of another drug on variable
Potentiation
two drugs with the same effect, when given together, produce an effect that is greater in magnitude
synergism
