MCQ Questions Flashcards
A company has discovered a candidate compound that is highly selective and potent H1 receptor inhibitor. The drug is rapidly absorbed in the gut but is also rapidly excreted in the urine, and so it need to be taken every 30 minutes to be effective. Which of the following statements is most correct:
A) This drug has a poor pharmacodynamic profile
B)This drug has significant on-target side effects
C)This drug has a poor pharmacokinetic profile
D)This drug is likely a prodrug
E)This drug causes activation of the H1 receptor
This drug has a poor pharmacokinetic profile
Terfenadine is best described as a prodrug because it:
A)promotes H1 receptor activation
B)is a pro-inflammatory compound
C)is processed by the liver when it is targeted for excretion
D)is inactive but is metabolized in body to generate its active form
E)is a higher quality formulation than the generic drug
is inactive but is metabolized in body to generate its active form
A common class of anti-epileptic drugs acts by targeting GABAA receptors in the brain, and has the benefit of suppressing seizures. Activation of GABAA receptors can also cause drowsiness and sedation. This is an example of a:
A)Off-target side effect
B)Pharmacogenomic profile
C)On-target side effect
D)Highly potent drug interaction
E)Pharmacokinetic consideration
On-target side effect
Which of the following statements describes a potentially relevant drug interaction that could affect the desired effects of a therapeutic drug?
A)Inhibition of H1 receptors by fexofenadine
B)Taking fexofenadine along with a substance that inhibits metabolism of terfenadine to fexofenadine
C)Conversion of terfenadine to fexofenadine in the liver
D)Taking terfenadine along with a substance that inhibits metabolism of terfenadine to fexofenadine
E)Inhibition of H1 receptors by terfenadine, leading to potentially fatal cardiac arrhythmias
Taking terfenadine along with a substance that inhibits metabolism of terfenadine to fexofenadine
Why are pharmacokinetic principles important in drug development?
A)Pharmacokinetics refer to specific interactions of drugs with their receptors
B)Pharmacokinetics affect the specificity of a drug:receptor interaction
C)Pharmacokinetics are used to determine how much and how frequently a drug should be taken for maximum effectiveness
D)A poor pharmacokinetic profile likely means that a drug has off-target side effects
E)Pharmacokinetic properties of a drug cannot be improved or altered.
Pharmacokinetics are used to determine how much and how frequently a drug should be taken for maximum effectiveness
The mechanism of action of an intracellular steroid hormone receptor involves:
A. Activation of the Gq signaling cascade
B. Binding to DNA leading to altered transcription of target genes
C. GTP hydrolysis to terminate the signal
D. Enzymatic modification of the hormone by the receptor
E. Processing of the steroid to its active form
Binding to DNA leading to altered transcription of target genes
Which of the following best describes the relative speed required for responses from these receptor types (slowest to fastest)?
A. Voltage-gated ion channel < G-protein coupled receptor < intracellular steroid hormone receptor
B. G-protein coupled receptor < ligand-gated ion channel < intracellular steroid hormone receptor
C. G-protein coupled receptor < intracellular steroid hormone receptor < ligand-gated ion channel
D. Intracellular steroid hormone receptor < G-protein coupled receptor < ligand-gated ion channel
E. Ligand-gated ion channel < voltage-gated ion channel < G-protein coupled receptor
Intracellular steroid hormone receptor < G-protein coupled receptor < ligand-gated ion channel
Given the accompanying set of concentration response curves showing the response of a receptor system to four different drugs, which of the following statements is true:
A. Drug A has the highest efficacy and strongest potency
B. Drug D has the highest efficacy and strongest potency
C. Drug A has the highest efficacy but drug D has the strongest potency
D. Drugs C and D have equal potency.
E. Drugs A and C have equal potency.
Drug A has the highest efficacy and strongest potency
When generating concentration response curves such as those above, which of the following would not be an appropriate parameter to describe as Emax?
A. Heart rate
B. Losartan (anti-hypertensive drug) concentration
C. Blood pressure
D. Force of muscle contraction
E. Breathing rate
Losartan (anti-hypertensive drug) concentration
Activation of a GPCR that is coupled to the Gq signaling pathway may lead to:
A. Hydrolysis of a membrane phospholipid, leading to the generation of IP3 and diacylglycerol (DAG).
B. Activation of Gq by hydrolysis of GTP
C. Activation of protein kinase A
D. Translocation of the activated Gq protein to the nucleus.
E. Steroid hormone receptor dimerization
Hydrolysis of a membrane phospholipid, leading to the generation of IP3 and diacylglycerol (DAG).
Ion channel proteins generate signals by:
A. Activation of signaling cascades.
B. Activation of transcription of target genes.
C. Affecting the concentration of ions in the bloodstream.
D. Enabling movement of ions from one side of the membrane to the other.
E. Calmodulin binding to effector proteins
Enabling movement of ions from one side of the membrane to the other.