Exam one add-ons Flashcards
During phase 1 of clinical drug trials, potential uses and effects are determined by what action?
a. Giving doses to healthy volunteers
b. Giving doses to people with the disease
c. Utilizing double blind studies
d. Utilizing crossover studies
a. Giving doses to healthy volunteers
Pharmacodynamics involves the biological effects of a drug that is exerted on a living system. This occurs by ligand complexes with all of the following except
a. Membrane receptors
b. Enzymes
c. Albumin
d. Intracellular receptors
c. Albumin
What is an example of a drug that has affinity for a receptor but does not elicit a response?
a. Albuterol
b. Lisinopril
c. Metoprolol
d .morphine
c. Metoprolol
Anaphylactic shock is a:
a. Type I reaction called immediate hypersensitivity reaction.
b. Type II reaction, called cytotoxic hypersensitivity reaction
c. Type III allergic reaction, call the noon complex hypersensitivity
d. Type IV reaction, called delayed hypersensitivity reaction.
a. Type I reaction called immediate hypersensitivity reaction.
Which receptor type acts as a binding site for many hormones, adrenoreceptors and chemokines?
a. Transmembrane G protein coupled receptor
b. Transmembrane ligand gated ion channels
c. Enzyme linked receptors
d. nuclear receptor
a. Transmembrane G protein coupled receptor
What is the effect of drug antagonism?
a. There is an increased physiological response of endogenous hormones.
b. The drug is modified by the concurrent administration of another drug
c. The drug cannot be metabolize before another dose is administered
d. There is a decreased physiological response when combined with another drug.
d. There is a decreased physiological response when combined with another drug.
Which of the following is a true statement about drug A that reaches maximum effect at 10 mg as opposed to drug B that requires 100 mg to produce the same effect?
a. Drug A is more efficacious
b. Drug B has a lower affinity
c. Drug A is more potent
d. Drug A is more selective
c. Drug A is more potent
Lock and key
Specificity
Greater affinity for certain receptor subtypes
Selectivity
Dose of a drug required to produce a specific effect
Potency
Determines what happens at a receptor
Efficacy
Attraction to the receptor
Affinity
In general, the effect of a drug is limited by which one of the following?
a. All available receptors are saturated
b. There are not enough receptors present.
c. The drug dose is too small
d. The receptor is allosteric in structure
a. All available receptors are saturated
These respond to peptide ligands
Cytokine receptors
These require second messengers
G protein linked receptors
these ligands bind to ion channels
ligand gated ion channel receptors
Protein that interacts with the ligand, typically on the plasma membrane
Receptor
ligand receptor binding process
1) ligand binding
2) Signal transduction; produces the biological effect
3) Cellular response - through first or second messengers
What individual characteristics of a person can affect pharmacodynamics
Age, sex, ethnicity
Any drug or chemical that has an opposite effect but through different physiological pathways
Physiologic antagonist
binds to the agonist (not the receptor) via ionic binding and deactivates the agonist
Chemical antagonist
Defined as the ratio of the median effective dose ED50 to the medium toxic dose TD50?
Therapeutic index
A high degree of plasma protein binding can result in restricted drug distribution?
True or false?
True. When medications are highly protein-bound, it is only the unbound portion of the drug that is distributed and active. For example, if the medication is 99% protein-bound, then only one 1 % is unbound an active in the system to cause pharmacologic effects.
When drugs have been metabolized & reach the kidney tubule, if the drug is ionized and lipophobic, the drug will tend to
a. Be passively illuminated in the urine
b. Be actively reabsorbed through the tubular lumen
a. Be passively illuminated in the urine
(the drug that is ionized also cannot easily pass through the lipid bilayer, so will not be reabsorbed and rather will be passively eliminated in the urine)
Rifampin is a nonspecific CYP450 inducer. How might this impact metabolism of another drug that is metabolized by the CYP450 enzymes that is co-administered?
a. This leads to toxic levels of Rifampin
b. This leads to toxic levels of both drugs
c. This could lead to therapeutic failure of the second drug.
d. This would cause nonspecific changes in drug metabolism
c. This could lead to therapeutic failure of the second drug.
If the patient is a poor metabolism phenotype, what do you need to consider as a prescriber?
a. There may be slow metabolism of a pro drug into an active drug
b. There maybe an accumulation of inactive metabolites of drugs
c. You may need to increase dosages of the medication
d. There may be increased metabolism of a pro drug into an active drug
a. There may be slow metabolism of a pro drug into an active drug
If the patient has an ultra rapid metabolism phenotype, what do you need to consider as a prescriber?
a. Decrease dosages of drugs to prevent drug accumulation
b. Increase metabolism of a Prodrug into an active drug, leading to therapeutic failure
c. Increase elimination of active, non-metabolized drug
d. Slowed metabolism of a prodrug into an active drug, leading to an accumulation of prodrug
b. Increase metabolism of a Prodrug into an active drug, leading to therapeutic failure
Which variable is a factor in drug absorption?
A. the smaller the surface area for absorption, the more rapidly the drug is absorbed
b. A rich blood supply to the area of absorption leads to better absorption
c. The less soluble the drug the more easily it is absorbed
d. ionized drugs are easily worked across the cell membrane
b. A rich blood supply to the area of absorption leads to better absorption
What is an advantage of prescribing sublingual medications?
a. Excreted rapidly
b. Less side effects
c. Distributed equally
d. avoids first past metabolism effect
d. avoids first past metabolism effect
What may occur when drug A uses the CYP3A4 isoenzyme for metabolism?
a. Induces the metabolism of drug B that also uses that pathway for metabolism
b. Inhibits the metabolism of drug B that also uses the pathway for metabolism
c. Both A and B
d. Neither A nor B
c. Both A and B
The difference between the effective dose and the lethal dose is referred to as
a. Dose response algorithm
b. ED50
c. Serum concentration
d. Therapeutic index
d. Therapeutic index
(You have learned that during drug development, concepts like selectivity, specificity, and others are considered. It is known that a specific plasma concentration of a drug must be achieved in order for that drug to be effective and to be therapeutic. For some of the drugs, the range of plasma concentration of a drug is quite large between effective and lethal dose. In some cases, this range can be quite narrow and produce a potentially dangerous situation for our patients. Therapeutic index is the difference between ED50, or the Effective Dose for 50% of the study population, and LD50, which is the Lethal Dose for 50% of the study population. Mind you, it’s an animal population, not human.)
If an NP abruptly terminates an antihypertensive agent like a beta blocker, what is the predictable receptor adaptation called?
a. Upregulation
b. Tolerance
c. Downregulation
d. Reversible agonism
a. Upregulation
(The longterm exposure of this antagonist drug at the receptor site has essentially increased the receptor affinity and responsiveness to the naturally occurring, or endogenous, agonist. In this case, abrupt withdrawal of the antihypertensive antagonist causes upregulation of the receptors. And now your patient is at great risk for a hypertensive crisis)
True or false?
A high degree of plasma protein binding can result in restricted drug distribution.
true
(When medications are highly protein bound, it is only the unbound portion of the drug that is distributed and active. For example, if a medication is 99% protein bound then only 1% is unbound and active in the system to cause pharmacologic effects)
