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Flashcards in Basic Principles 3 Deck (31)
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1
Q

occurs following frequent or continuous exposure of the receptor to the agonist over a short period of time (seconds to minutes)

A

densensitization

2
Q

desensitization is a rapid and _______ process that desensitizes the tissue to further receptor-agonist interaction for only a few minutes

A

reversible

3
Q

of receptor molecules occurs following frequent or continuous exposure of the receptor to the agonist over a relatively short period of tie (minutes to hours)

A

internalization

4
Q

during internalization, receptor molecules are _______ intact to the plasma membrane via endocytic vesicles.

A

recycled

5
Q

process that regulates receptor-mediated repsonses. it occurs only after prolonged or repeated exposure of cells to the agonist over a long period of time (hours to days)

A

down-regulation

6
Q

down-regulation _____ the number of receptor molecules present in the cell or tissue

A

decreases

7
Q

down-regulation involves ________ of receptor molecules present in the cell and requires the biosynthesis of new receptor molecules for recovery

A

degradation

8
Q

down-regulation may cause relative _________ to the effects of a drug agonist int he some patients

A

tolerance

9
Q

refers to a decrease in the intensity of the response to a given dose of a drug as a consequence of continued drug administration over an extended period of time

A

tolerance

10
Q

tolerance may also occur as a result of _________ of essential substrates required for downstream effects in the signal transduction pathway following continuous activation of the receptor-effector system

A

depletion

11
Q

of the receptor occurs when receptor activation is blocked for prolonged periods of time (usually several days) by pharmacologic antagonists or by denervation.

A

up-regulation

12
Q

refers to the ability of the drug to accomplish a specified effect

A

efficacy

13
Q

reflects the amount of drug required to cause an effect (EC50)

A

potency

14
Q

a drug may have ____ efficacy but _____ potency or vice versa

A

high;low

15
Q

refers to the concentration (EC50) or dose (ED50) of the drug required to produce 50% of its maximal therapeutic efficacy

A

potency

16
Q

potency of a drug depends on the ______ (KD) of the drug for binding tot he receptor and the efficiency of the occupancy-response coupling process

A

affinity

17
Q

of a drug depends on its maximal therapeutic efficacy (Emax) and its ability to reach its site of action (not on its pharmacologic potency)

A

clinical effectiveness

18
Q

in selecting on of two drugs to administer to a patient, one must make that selection based on the relative ______ rather than the relative ______ of the two drugs

A

effectiveness;potency

19
Q

pharmacologic potency is going to largely determine the administered ______ of the selected drug.

A

dose

20
Q

is the upper limit of the dose-response relationship on the response axis of the graph

A

maximal efficacy

21
Q

in a patient may be determined by the mode of interactions of the drug with the receptor or by the characteristics of the receptor-effector system

A

drug efficacy

22
Q

in a patient also depends on a host of other factors

A

therapeutic efficacy

23
Q

the practical clinical efficacy of drug of a drug may in some cases be limited by the drug’s tendency to cause a _______ effect, even if the drug can otherwise exert a greater therapeutic effect

A

toxic

24
Q

a quantal dose response curve represents the _____ of individuals under study who exhibit a specified drug effect plotted as a function of drug

A

percentage

25
Q

illustrates the potential variability of responsiveness to the drug among individuals in a given human population

A

quantal dose response curve

26
Q

the drug dose at which 50% of individuals exhibit the specified quantal effect

A

median effictive dose (ED50)

27
Q

drug dose required to produce a particular toxic effect in 50% of individuals or lab animals

A

median toxic dose (TD50)

28
Q

if the toxic effect is death it is defined as ______

A

median lethal dose (LD50)

29
Q

of a drug relates the dose of the drug required to produce a desired effect to the dose of the drug which produces an undesirable effect

A

therapeutic index TD50/ED50

30
Q

represents an estimate of the safety of a drug

A

therapeutic index TD50/ED50

31
Q

of a drug is a more clinically useful index of safety

A

therapeutic window (therapeutic range)