PHARMACODYNAMICS TERMS Flashcards
study of the time course of drug absorption, distribution, metabolism and elimination
pharmacokinetics
application of PK principles to the safe and effective therapeutic management of drugs in a patient
clinical pharmacokinetics
the events that occur in the body that lead to a drugs effect
mechanism of action
synthesized outside of the body
xenobiotics
synthesized within the body
hormones
produces harmful effects
poisons
poisons of biologic origin
toxins
molecules that binds to another molecule
i.e. drug, hormone, NT
ligands
components of a cell or organism that interact with a drug and initiates the chain of events leading to the drugs observed effects
receptor
agonist or antagonist act as activators
agonists
agonist or antagonist act as inhibitors
antagonists
affects multiple receptors on different cells/tissues
nonselective drugs
exerts more specific binding
selective drugs
components of a cell or organism that interacts with a drug and initials chain of events leading tot he drugs observed effects
receptor
aspirin and sarin have what type of drug-receptor bond
covalent bonds
this drug receptor bond consists of ionic, hydrogen, van Der Waals
nicotine as an example
electrostatic bonds
lipids have what type of drug receptor bond
hydrophobic bonds
bind to the same receptor sites as the endogenous agonist
primary agonists
blind to different regions of the receptor
allosteric agonists
ligand binds only to the active form of the receptor to produce full max effect
full agonist
ligand binds to both active and inactive forms of the receptor but with more affinity for the active form leading to partial effect
partial agonist
blocks the agonist from binding to the receptor
antagonist
produce a lower response that do full agonist (ceding effect) inhibits the response produced by full agonist
buprenorphine
partial agonists
refers to the relative ability of a drug receptor complex to produce a maximum response
intrinsic efficacy
drugs that produce the opposite effect/response of the agonist
a receptor is either active or inactive, what is this activity called?
inverse agonist
constitutive activity
antagonist competes for the same binding spot as the ligand/drug
competitive antagonism
nonselective beta blocker
competes with norepinephrine and epic
reduces resting heart rate
exhibits competitive antagonism
propanolol
one that does not bind drug when the drug concentration is sufficient to produce maximal effect
spare receptor
bind to receptor in an irreversible manner
a noncompetitive antagonist reduces the maximal response that an agonist can produce
increasing the agonist concentration cannot surmount the inhibitory effect
noncompetitive antagonist
drug used to treat hypertension in patients pheochromocytoma
phenoxybenzamine
drugs have both agonistic and antagonistic properties
mixed agonist
a drug may antagonize the actions of a second drug by binding to and inactivating the second drug
heparin reversal with protamine
chemical antagonism
many physiologic functions are controlled by opposing regulatory pathways
glucocorticoids and insulin
physiologic antagonism
mediate actions of endogenous chemical signals
NTs, hormones
regulatory proteins
protein receptors are activated or inactivated by drugs which themselves can be enzymes
enzymes
receptors that regular movement of materials
NTs
transport proteins
structural elements like tubulin
structural proteins
name this effect of receptor regulation:
EGF receptor kinase
ligand binding leads to internalization of receptor
de novo synthesis of receptors rate < receptor degradation
decreased total number of cell surface receptors
downregulation
name this receptor regulation
cells responsiveness to ligand decreases
desensitization
name this receptor regulation
when responsiveness to a drug diminishes rapidly after administration of a drug
i.e. acute tolerance
tachyphylaxis
name this receptor regulation
an increase in the number of receptors on the surface of target cells
upregulation
this the concentration that produces 50% of the maximal response
EC50
the maximal response that can be produced by the drug
-maximal effect of a drug can be seen by the plateau of the dose response curve
Emax
dose at which 50% of the subject exhibits the quantal effect
i.e. therapeutic effect
ED50
dose at which 50% of subjects experienced a toxic event
TD50
dose at which 50% of subjects died
LD50
denotes the amount of drug needed to produce a specified effect
EC50
ED50
potency
the ratio of equivalent-effective doses
used in to compare one drug with another
relative potency
do not equate greater potency of a drug with therapeutic superiority
one can possibly increase the dose of a less potent and get the same clinical response
equipotent dose
a dose response that is defined as either absent or present
all or none
useful for finding the dose required to produce a specified response in each member of the population
quantal dose response
plotting the increment in the percent of the population that responds with a specified effect as the dose is increased
quantal dose response curve
range between the minimum toxic dose and the minimum therapeutic dose
therapeutic range
TD50/ED50
what is this index? increased means?
therapeutic index
greater the margin of safety
drugs that have both agonistic and antagonistic properties?
mixed agonist
doesn’t take any opioids?
opioid naive
has been taking a full agonist like oxycodone for pain
opioid tolerant
