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PHRM 5221 > exam 1 tophat > Flashcards

exam 1 tophat Flashcards

1
Q

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

A

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

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2
Q

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

A

reverse turn

literally looks like a letter-U

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3
Q

Select the hydrophobic amino acid

A

hydrophobic (nonpolar) have an alkyl or aromatic group

r group has no +/-

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4
Q

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?

A

tertiary

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5
Q

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?

A

GPCR - function is to transduce extracellular stimuli into intracellular signals

essentially an on-off switch

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6
Q

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

A

nuclear receptors
-directly bind to DNA

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7
Q

Tachyphylaxis is

A

rapid decrease in drug response following initial administration

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8
Q

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

A

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

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9
Q

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)?

A

Sodium (Na+) and Calcium (Ca2+)

drugs that open Na+ and Ca2+ channels are excitatory

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10
Q

Drugs that open K+ or Cl- channels are

A

inhibitory

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11
Q

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

A

Receptor Tyrosine Kinase

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12
Q

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

A

efficacy

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

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13
Q

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?

A

Kd = EC50

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14
Q

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

A

TI = 10

lower TI more unsafe, higher TI more safe drug

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15
Q

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

A

high

low kd = high affinity
high kd = low affinity

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16
Q

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

A

efficacy

noncompetitive antagonist reduces agonist efficacy

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17
Q

Competitive antagonist reduces agonist ________?

A

potency

competitive antagonist reduces agonist potency

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18
Q

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?

A

potentiation

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19
Q

additive/summation

A

final effect equal to sum of the effect of two drugs

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20
Q

potentiation

A

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

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21
Q

Which of the following is the orthosteric site?

A

the active binding site

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22
Q

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

A

inverse agonist

23
Q

antagonist

A

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

24
Q

agonist

A

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

25
Q

Full agonist

A

binds and has full response

26
Q

Partial agonist

A

50% response

may be more potent than a full agonist

27
Q

Partial agonist

A

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

28
Q

Inverse agonist

A

ligand that binds to receptor eliminating basal activity or constitute activity

29
Q

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?

A

Active Transport

30
Q

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

A

Intravenous

31
Q

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.

A

blood, heart, skeletal muscle, adipose tissue

32
Q

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?

A

clearance

Css x Cl

33
Q

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?

A

Total Body Water (Intracellular + Extracellular)

34
Q

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

A

increases

decreased clearance = increased half life

35
Q

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

A

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

36
Q

Zero order kinetics relates to constant _________ of a drug overtime

A

amount

takes longer to get drug out of body

37
Q

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

A

Vd = 18,000

extremely large Vd means adipose tissue

38
Q

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

A

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

39
Q

Efflux transporters

A

inhibition results in INCREASE in bioavailability for drug substrates

40
Q

Uptake transporters

A

inhibition results in DECREASE in bioavailability

41
Q

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

A

ABC transporters

42
Q

SLC transporters

A

uptake (into cell)

facilitated diffusion

secondary/tertiary active transport

bi-directional

43
Q

ABC transporters

A

A= atp

efflux (out of cell)

primary active transport

uni-directional

44
Q

Which Glucose Transporter (GLUT) is insulin-sensitive?

A

GLUT-4

glut-1-3 are insulin INSENSITIVE

45
Q

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?

A

on-target

46
Q

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?

A

Urinary Alkalinization

47
Q

gastric emptying

A

most effective when used within one hour of ingestion

48
Q

activated charcoal

A

oral poisonings

49
Q

WBI

A

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

50
Q

Urinary alkalinization

A

decontaminates drug once it has been absorbed into bloodstream

51
Q

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

A

Type A - Augmented (dose-related ADRs)

52
Q

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

A

higher

look at graph lecture 10

53
Q
A

PHRM 5221 (6 decks)

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