Drug Action Exam 1 Flashcards
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drug
any substance intended for human exposure capable of producing a change in a living system
Modern Definition of Pharmacology
the study of the interactions between drugs and living systems
Paracelsus
Grandfather of pharmacology
1540
concept- body is made up of chemicals, pathology is a result of chemical imbalance, use chemicals to treat
Felix Fontana
1790
chemicals have an active principle and act on a specific site
Friedrich Serturner
1806
isolates morphine- first active principle
C. Bernard
1850-1855
found specific site using curarine in frogs
Oswald Schmiedeberg
father of pharmacology
1870
magnitude and duration of a drugs action is dependent upon the dynamic equilibrium between the ability if the drug to reach its site of action and the ability of the body to remove it
John Abel
started ASPET and JPET
action
the result of combining of molecules of substance with molecules of living system
effect
the consequences at higher levels of integration of a drugs action
occupancy theory
Langley, Clark, and Gaddum
the magnitude of effect is directly proportional to the percent of total receptors occupied by that drug at that time
Rate theory
Paton
not only the quantity of receptors occupied but the rate at which they are being occupied that determines effect
Induced Fit theory
the amount of effect observed depends on the amount of conformational twisting of the receptor when it is occupied by the drug
agonist
a substance that combines with a receptor and produces an effect that we have designated in advance
antagonist
combines with a receptor and produces no effect itself, but blocks the effect of the agonist
affinity
how well is it attracted to receptor; a measure of action
intrinsic activity/efficacy
once bound how much effect is produced; a measure of effect
homergic
2 substances that produce same effect
heterergic
2 substances that produce different effects
addition
homergic, same MOA, effect seen is that expected by adding together individual effect of drugs
summation
same as addition but different or unknown MOA
potentiation
homergic, different MOA, effect is greater than expected by adding individual effects
synergism
one drug that does not produce an effect itself enhances the effect of a different drug, heterergic
competitive antagonism
drug 2 blocks effect of drug 1 by competing for receptor; can be overcome by increasing concentration of drug 1
non competitive antagonism
drug 2 permanently binds blocking drug 1 can only be overcome by getting more receptors
pharmacologic antagonism
at molecular level; competitive and non-competitive antagonism
physiologic antagonism
antagonism at level of effect
G-alpha S
beta-1 & beta-2
G-alpha I
muscarinic type 2
GABA type B
alpha-2
opioid
IP3 & DAG stimulators
alpha-1
muscarinic type 1
serotonin type 1
thesh-hold dose reflects
relative affinity
graded data
Emax reflects
relative efficacy
graded data
distance from y-axis reflects
relative potency
graded and quantal data
quantal data look at
potency
slope
variability
confidence
therapeutic index
TD50/ED50
margin of safety
TD5 - ED95
safety index
TD5/ED95
litchfield-wilson
least squares method for best-fit line
2 major variables for magnitude of effect
dose
time
inherent factors
factors that are a function of living system
toxicology
study of deleterious effects of chemicals and physical agents on living systems
toxic or toxicity
the ability of an agent to cause injury; qualitative (yes or no)
Gleason chart
measure of how toxic
specific
molecular; refers to drug/receptor relationship
selective
refers to subsequent effects; how many effect does it have
acceptors/silent receptors
combining points in a living system that produce no effect
hazard
the likelihood that a deleterious or injurious situation will occur in the context of the present situation; measured as low, medium, high
risk
the expected frequency of occurrence of undesirable effects from exposure setting; fractional or %; expectations based on past data
direct effects
are the direct result of drug action at a particular site
Gleason #1
practically nontoxic
practically non-toxic
above 15 g/kg
lethal dose: more than 1 quart
gleason #2
slightly toxic
slightly toxic
5-15 g/kg
lethal dose: 1 pint - 1 quart
Gleason #3
moderately toxic
moderately toxic
500 mg - 5 g/kg
lethal dose: 1 ounce - 1 pint (or 1 lb)
Gleason #4
very toxic
very toxic
50-500 mg/kg
lethal dose: 1 tsp - 1 ounce
gleason #5
extremely toxic
extremely toxic
5-50 mg/kg
lethal dose: 7 drops - 1 tsp
Gleason #6
super toxic
super toxic
less than 5 mg
lethal dose: a taste (<7 drops)
indirect effects
allergic reactions
idiosyncratic reactions
mutagenicity/carcinogenicity reactions
teratogenicity reactions
teratogenicity reaction
birth defects
acute exposure
a single discrete exposure or many exposures over a relatively short period of time
subacute exposure
several discrete exposures over a somewhat intermediate period of time
chronic exposure
continuous exposure over a longer period of time
acute toxicity spectrum
symptoms of acute toxicity
chronic (cumulative) toxicity spectrum
symptoms of chronic exposure due to accumulation of toxic substance or toxic injury
toxic injury
repetitive injury to kidney or liver
immediate/emergency treatment
stabilization/support
removal from exposure situation
sustained treatment
continued support
hastening elimination
antidotes
acidic diuresis
make urine more acidic to remove basic toxicant
alkaline diuresis
make urine more basic to remove acidic toxicant
neutral diuresis
osmotic
peritoneal dialysis
filter blood using the peritoneal membrane as the dialyzing membrane
hemodialysis
run blood through external membrane from artery to vein
hemoperfusion
trickle blood over adsorbing substance
