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WorksheetsPharmacology Exam 1
Total questions: 91
Worksheet time: 49mins
Which of these is defined as: to study the effects of drugs on populations
pharmacoepidemiology
pharmacoeconomics
Which of these is defined as: to study the cost-effectiveness of drug treatments
pharmacoeconomics
pharmacoepidemiology
What the body does to the drug
pharmacokinetics
pharmacogenomics
pharmacodynamics
Pharmacokinetics focuses on ADME which stands for:
Absorption, Distribution, Metabolism, Elimination
Adverse Reactions, Distribution, Molecule Size, Energy
Accumulation, Drug Interactions, Mechanism of Action, Elimination
What the drug does to the body
pharmacokinetics
pharmacodynamics
pharmacogenomics
Involves receptor interactions, dose-response phenomena, and mechanisms of therapeutic and toxic effects
pharmacodynamics
pharmacokinetics
pharmacogenomics
Biochemical and physiological effects of drugs on the body:
determine classification of drug (ex: antidepressant)
determine suitability for therapeutic uses
determine dosing
determine special situation use ie renal failure
True or false: Specific interaction with regards to pharmacodynamics means receptor binding.
true
false
True or false: Specific interaction regarding pharmacodynamics means no receptor binding (chemical reactions, surfactant reactions, etc)
true
false
Area of pharmacology concerned with genetic variations that lead to differences in drug response among individuals or population.
pharmacokinetics
pharmacodynamics
pharmacogenomics
True or false: general toxic effects, allergies, and side effects are responses that are normally not found in the general population
true
false
Variation of drug pathways:
drug usually exerts its effect by interacting with target proteins (receptor)
effectiveness of drug is greatly affected by genetic variation in these targets
increase or decrease in enzyme activity (CYP enzymes)
not due to differences in target proteins or enzyme metabolism
Variation in enzymes that metabolize the drug:
increase or decrease in enzyme activity (CYP enzymes)
not due to differences in target proteins or enzyme metabolism
yield the least predictable effects of genetic variation
G6PD deficiency
Other "idiosyncratic" effects:
not due to differences in target proteins or enzyme metabolism
yield the least predictable effects of genetic variation
G6PD deficiency
drug usually exerts its effect by interacting with target proteins (receptor)
What are the 3 processes involved when drugs are administered?
drug-receptor interactions (binding)
dose-response (effect)
signal transduction (MOA, pathways)
excretion (waste pattern)
True or false: higher Kd= lower affinity
true
false
True or false: less affinity means less response to the drug.
true
false
Chemical agent that uniquely interacts with a specific target (receptor) in the living organism and thereby causes changes in the biological function
drug
toxin
poison
Chemicals/drugs that have almost exclusively harmful effects
agonists
antagonists
poisons
toxins
Poisons of biological origin, synthesized by plants or animals
drugs
poisons
toxins
Stimulates (increases signal transduction)
agonist
antagonist
Inhibits (decreases signal transduction)
agonist
antagonist
A molecule in the biological system to which a ligand/drug binds and that usually plays a regulatory role
receptor
ligand
A molecule binds to the receptor to activate/deactivate/modify it, resulting in the next step in that biological system
receptor
ligand
Endogenous sources of drugs are produced inside the body and by the body. An example of this would be
hormones
xenobiotics
Exogenous sources of drugs are produced outside of the body. An example of this would be
hormones
xenobiotics
Mainly receptor; a drug is designed to bind to and activate/deactivate/modify to alter the biologic system in which the receptor is found
drug target
orphan receptor
Receptors for which no endogenous ligand has been discovered and for which the function is unknown; important for new drug discovery
drug target
orphan receptor
Choose the main points regarding the nature of drugs.
physical nature (form at room temperature, ionic properties)
drug size (generally a MW of 100-1000u)
drug reactivity and drug-receptor bonds
drug shape
Regarding drug size- does the lower (100) or upper (1000) limit achieve specificity for target receptor?
lower
upper
Regarding drug size, which limit (upper or lower) determines the ability of drugs to move throughout the body?
lower (100)
upper (1000)
Drugs above 1000 MW units do NOT diffuse readily between compartments of the body.
true
false
Which type of drug-receptor bond is the strongest and is often irreversible?
covalent
electrostatic (ionic, hydrogen, Van der Waals forces)
hydrophobic
Which type of drug-receptor bond can range in strength from weak to relatively strong and is more common than covalent?
covalent
electrostatic (ionic, hydrogen, Van der Waals forces)
hydrophobic
Which type of drug-receptor bond is the weakest and involves a very precise fit of the drug to its receptor?
covalent
electrostatic (ionic, hydrogen, Van der Waals forces)
hydrophobic
Stronger binding means shorter duration of action.
true
false
________ bonds require a very precise fit (drug/receptor): prove high selectivity.
weak
strong
Orientation of a chemical structure around a bond; same molecular formula but different 3D structure (mirror image is non-superimposable)
chirality (stereoisomerism)
enantiomer
racemic mixture
Mirror image stereoisomers
chirality (stereoisomerism)
enantiomer
racemic mixture
Mix of stereoisomers in a chemical solution or compound (drug)
chirality (stereoisomerism)
enantiomer
racemic mixture
Optical isomers that are NOT enantiomers, NOT mirror images
chirality
diastereomers
racemic mixture
Drug efficacy is based on which 4 principles?
structure
selectivity
delivery
duration
elimination
Drug efficacy, structure: structure can bind and ________, ________, and ___________ its target.
activate
deactivate
modify
partially activate
To encourage drug selectivity and to prevent binding to other receptors the drug must have a unique size, charge, size, and other properties. Increasing drug selectivity usually decreases what?
adverse drug reactions
allergic reactions
Delivery of a drug is important because of
molecule size
first pass metabolism
What do you do if the drug molecule needed is too large to get to the target compartment?
administer the drug directly to the target compartment
come up with an alternative medication
Which is more important?
safety
efficacy
Which phase of testing measures efficacy, selectivity, and mechanism of action?
pre-clinical
clinical
marketing
When is an IND (Investigational New Drug) filed for approval of a new medication for clinical testing?
between pre-clinical and clinical testing phases
once in the clinical testing phase
between clinical testing phase and marketing phase
Which part of testing occurs after an IND has been filed and in phases?
pre-clinical
clinical
marketing
What is phase 1 of clinical testing (20-100 subjects) testing for?
is it safe, pharmacokinetics
does it work in patients
does it work, double blind
What is phase 2 of clinical testing (100-200 subjects) testing for?
is it safe, pharmacokinetics
does it work in patients
does it work, double blind
What is phase 3 of clinical testing (1000-6000) testing for?
is it safe, pharmacokinetics
does it work in patients
does it work, double blind
When is an NDA (New Drug Application) filed?
pre-clinical testing
clinical testing
marketing
between pre-clinical and clinical
between clinical and marketing
Postmarketing surveillance occurs as phase 4 testing carrying over from clinical testing.
true
false
How many years after filing an NDA will the patent expire?
5
10
20
25
In which phase of studying are the following studied? Efficacy and toxicity, selectivity, MOA, in vitro and in vivo animal models (cellular, organ, and whole animal model)
preclinical
clinical
marketing
What does an IND (Investigational New Drug) application contain?
preclinical data collected
detailed proposal for clinical trials
clinical data collected
trade name of medication
What are the limitations of preclinical studies?
toxicity testing is time-consuming and expensive
large numbers of animals may be needed to obtain valid preclinical data
extrapolations of therapeutic index and toxicity data from animals to humans are reasonably predictive for many (not all) toxicities
rare adverse effects are unlikely to be detected in preclinical testing due to statistical reasons
What are the limitations of clinical trials?
pre-existing conditions
subject bias
observer bias
disease state fluctuations
Which drug type does not use animals for preclinical studies?
highly toxic drugs ie AIDS and chemo
narcotics
statins
NSAIDs
Post marketing surveillance, which occurs after the NDA, mainly occurs to monitor drug safety including documentation of incidence and severity of rare adverse reactions, cost-effectiveness, comparative trials, and quality of life studies.
true
false
Upon expiration of a patent, any company may apply to the FDA to get permission to market a generic version. The generic drug molecule must be ____________ to the original.
bioequivalent
identical
chemically equivalent except for filler products
Choose the answers that are considered to be pharmacokinetics
drug concentration at site of action (distribution)
drug in tissues (distribution)
drug metabolized or excreted pharmacologic effect (elimination)
drug concentration in systemic circulation (distribution)
dose of drug administered (IV, IM, PO...) [absorption]
Choose the answers that are considered to be pharmacodynamics
pharmacologic effect
clinical response
toxicity
efficacy
drug concentration in systemic circulation
Select the processes involved in pharmacodynamics (drug to body)
drug
receptor
effector (may be part of the receptor or separate)
cAMP
IP3
_______________: binds and activates the receptor in some fashion for full receptor effect
agonist
antagonist
allosteric binding
_________: binds and inhibits the receptor by competing for receptor site and preventing agonist binding
agonist
antagonist
allosteric binding
_____________: regulation of the receptor (activation or inhibition) by binding to a site different from the active site
agonist
antagonist
allosteric binding
___________: activates the receptor to the maximum extent (morphine)
full agonist
partial agonist
________________: binds and activates the receptor but not to the maximum activity (buprenorphine) **increasing the concentration will not increase the response
full agonist
partial agonist
__________: the receptor is active in the absence of the drug
constitutive activity
inverse agonist
_____________: binds and reduces any constitutive activity
full agonist
partial agonist
inverse agonist
The ability of drug to bind receptor (Kd) is called what?
affinity
potency
efficacy
The measure of the activity of a drug in a biological systemic called what?
affinity
potency
efficacy
______________: the ability of drug-receptor complex to initiate response
affinity
potency
efficacy
Which type of dose-response describes the effect of a drug of a particular individual?
graded dose response
quantal dose-response
_____________: more receptors exist than are necessary to produce maximal effect
spare receptors
orphan receptors
Define competitive antagonist.
blocks agonist binding (competes for the same site)
activates the receptor to the maximum extent
binds and activates the receptor but not to the maximum activity
binds and inhibits the receptor by competing for receptor site and preventing agonist binding
Will having enough extra agonist overcome inhibition in a competitive (reversible) antagonist situation?
yes
no
_____________: an antagonist that binds to a receptor in such a way that it remains bound for the "life" of the receptor
non competitive (irreversible antagonist)
competitive (reversible) antagonist
_________________: adequate dose will minimize number of receptors available for binding ligand such that Emax cannot be reached
competitive irreversible antagonist
non competitive irreversible antagonist
What type of dose-response is characterized by all or none response?
quantal dose-effect curve
graded dose response
A quantal dose-effect curve is used to generate information regarding the margin of safety.
true
false
How do you calculate the therapeutic index?
TD50 (toxic dose)/ ED50 (median effective dose)
it's the range between the minimum toxic dose and the minimum effective dose
What's the therapeutic window?
TD50/ED50
it's the range between the minimum toxic dose and the minimum effective dose
Voltage-gated ion channels do not bind to neurotransmitters.
true
false
Choose two examples of regulating mechanisms for ligand-gated ion channels
phosphorylation
endocytosis
exocytosis
Which receptor type is the most abundant in our bodies?
G-protein coupling & second messengers
ion-gated channels
Approximately what percentage of drugs target G-protein receptors?
40
75
64
22
Which 2nd messengers are used to amplify the effect of G-protein receptors?
cAMP
IP3
Ca++
