exam 1 tophat

Question 1

Which of the following is the correct order of interactions in terms of strength (from strongest to weakest)?

Answer 1

Covalent Bonds, Ionic Charge-Charge Interactions, Hydrogen Bonds, Van der Waals forces

Question 2

Which of the following secondary protein structures is best described as a u-shaped four residue segment stabilized by hydrogen bonds?

Answer 2

reverse turn

literally looks like a letter-U

Question 3

Select the hydrophobic amino acid

Answer 3

hydrophobic (nonpolar) have an alkyl or aromatic group

r group has no +/-

Question 4

Which of the these four stages that result in the formation of a protein structure occurs due to interactions between amino acid R groups from the same polypeptide chain?

Answer 4

tertiary

Question 5

The binding of an agonist to which of the following transmembrane receptors does not result in the opening of a pore and an alteration in ion conductance?

Answer 5

GPCR - function is to transduce extracellular stimuli into intracellular signals

essentially an on-off switch

Question 6

Which of the following types of receptor interacts directly with DNA?

Answer 6

nuclear receptors
-directly bind to DNA

Question 7

Tachyphylaxis is

Answer 7

rapid decrease in drug response following initial administration

Question 8

In order for an action potential to be generated, the _____ must first be reached through the activation of a ligand-gated ion channel.

Answer 8

threshold

in order for an action potential to be generated, the THRESHOLD must first be reached through the activation of a ligand-gated ion channel

Question 9

In an excitatory cell, such as a neuron, an antagonist of which of the following voltage-gated ion channels would result in hyperpolarization and therefore an inhibitory effect (select the two that apply)?

Answer 9

Sodium (Na+) and Calcium (Ca2+)

drugs that open Na+ and Ca2+ channels are excitatory

Question 10

Drugs that open K+ or Cl- channels are

Answer 10

inhibitory

Question 11

Which of the following receptors has it’s own intrinsic enzymatic activity?

Answer 11

Receptor Tyrosine Kinase

Question 12

In regards to an agonist, which of the following parameters is the most important clinically?

Answer 12

efficacy

In regards to an AGONIST, which of the following parameters is the most important clinically

Question 13

Assuming that the maximal biological response is achieved when all receptors are occupied and that biological response is proportional to the amount of receptors bound to a drug, which of the following is true?

Answer 13

Kd = EC50

Question 14

Based on the therapeutic index (TI) values, which of the following drugs would most likely require constant patient monitoring.

Answer 14

TI = 10

lower TI more unsafe, higher TI more safe drug

Question 15

A drug that has a low Kd value for a particular receptor has a ___________ affinity

Answer 15

high

low kd = high affinity
high kd = low affinity

Question 16

Assuming that there are no spare receptors, a non-competitive antagonist will reduce the ___________ of an agonist for a particular receptor

Answer 16

efficacy

noncompetitive antagonist reduces agonist efficacy

Question 17

Competitive antagonist reduces agonist ________?

Answer 17

potency

competitive antagonist reduces agonist potency

Question 18

If Drug A has no effect at Receptor X but enhances the effect of Drug B at Receptor X we consider this type of interaction to be which of the following?

Answer 18

potentiation

Question 19

additive/summation

Answer 19

final effect equal to sum of the effect of two drugs

Question 20

potentiation

Answer 20

drug with no or little effect on its own enhances effect of 1st drug

Question 21

Which of the following is the orthosteric site?

Answer 21

the active binding site

Question 22

Which of the following types of ligand requires a receptor to have basal activity in order to alter a receptors response.

Answer 22

inverse agonist

Question 23

antagonist

Answer 23

inhibit action of an agonist but have no effect in absence of the agonist

Question 24

agonist

Answer 24

a ligand that binds to and activates a receptor eliciting a physiological response

Question 25

Full agonist

Answer 25

binds and has full response

Question 26

Partial agonist

Answer 26

50% response may be more potent than a full agonist

Question 27

Partial agonist

Answer 27

binds to receptor at active site but produces only a partial response (even when all receptors occupied) even if it occupies 100% of its receptors, it can't exert 100% of maximal response occurs at 50% of max possible response can be more/less potent than full agonist

Question 28

Inverse agonist

Answer 28

ligand that binds to receptor eliminating basal activity or constitute activity

Question 29

Which of the following mechanisms of transportation of a drug molecule across a cell membrane requires energy to move a drug against it's chemical concentration gradient?

Answer 29

Active Transport

Question 30

Which of route of administration results in the greatest bioavailability for a drug?

Answer 30

Intravenous

Question 31

Sort the following compartments from first to last in terms of when a drug will be distributed into that part of the body after it has been administered.

Answer 31

blood, heart, skeletal muscle, adipose tissue

Question 32

Assuming that your drug is administered intravenously, when calculating your maintenance dose you multiply the steady-state plasma concentration by which of the following parameters?

Answer 32

clearance Css x Cl

Question 33

Drug X has a volume of distribution value of 43 L. Which of the following areas of the body has it most likely been distributed?

Answer 33

Total Body Water (Intracellular + Extracellular)

Question 34

Assuming that the volume of distribution is unaltered, what happens to the half-life of a drug if it's clearance rate slows down?

Answer 34

increases decreased clearance = increased half life

Question 35

First-order kinetics relates to the elimination of a constant _______ of drug for each half-life of the compound.

Answer 35

fraction First order kinetics relates to the elimination of a constant FRACTION of drug for each half-life of the compound gets drug out quicker than zero order

Question 36

Zero order kinetics relates to constant _________ of a drug overtime

Answer 36

amount takes longer to get drug out of body

Question 37

Which of the following drugs is mostly likely to accumulate in adipose tissue?

Answer 37

Vd = 18,000 extremely large Vd means adipose tissue

Question 38

Inhibition of which of the following drug transporters will NOT increase drug bioavailability?

Answer 38

Uptake transporter on the luminal apical membrane of a small intestine enterocyte

Question 39

Efflux transporters

Answer 39

inhibition results in INCREASE in bioavailability for drug substrates

Question 40

Uptake transporters

Answer 40

inhibition results in DECREASE in bioavailability

Question 41

Which of the following drug transporter subfamilies only consist of unidirectional, efflux primary active transporters?

Answer 41

ABC transporters

Question 42

SLC transporters

Answer 42

uptake (into cell) facilitated diffusion secondary/tertiary active transport bi-directional

Question 43

ABC transporters

Answer 43

A= atp efflux (out of cell) primary active transport uni-directional

Question 44

Which Glucose Transporter (GLUT) is insulin-sensitive?

Answer 44

GLUT-4 glut-1-3 are insulin INSENSITIVE

Question 45

An adverse effect that occurs as a result of a drug metabolite binding to the intended receptor in an unintended tissue would be considered to be an ___________ effect?

Answer 45

on-target

Question 46

Which of the following mechanisms of decontaminating a patient after a drug overdose would be the most appropriate if all of the drug has been absorbed into the bloodstream?

Answer 46

Urinary Alkalinization

Question 47

gastric emptying

Answer 47

most effective when used within one hour of ingestion

Question 48

activated charcoal

Answer 48

oral poisonings

Question 49

WBI

Answer 49

flushes and cleanses bowel most useful for substances that are not well-absorbed by activated charcoal.... aids in passing of poison before absorption takes place

Question 50

Urinary alkalinization

Answer 50

decontaminates drug once it has been absorbed into bloodstream

Question 51

Which of the following type of adverse drug reactions is most commonly observed?

Answer 51

Type A - Augmented (dose-related ADRs)

Question 52

If an individual is an ultrarapid CYP2D6 metabolizer they may require a __________ dose of a drug metabolized through that enzyme compared to the average recommended dose

Answer 52

higher look at graph lecture 10