Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Biomedical Lab III > Lab 8 > Flashcards

Lab 8 Flashcards

1
Q

drug-receptor interactions occur via which bonds

A

ionic
hydrogen
van der Waals
covalent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

drugs with a ____ duration of action generally have WEAKER bonds

A

short

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what kind of drug-receptor interactions may have stronger bonds?

A

long duration or irreversible interactions (such as covalent)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

define drug receptors

A

generally proteins that bind endogenous molecules to elicit physiological effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

define an agonist

A

a chemical that activates a receptor to produce a biological response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

define a full agonist

A

activates a receptor with the maximum response that an agonist can elicit at the receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

define a partial agonist

A

binds and activates a given receptor, but only has PARTIAL EFFICACY at the receptor (relative to a full agonist)

EVEN AT MAXIMAL RECEPTOR OCCUPANCY

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

define an inverse agonist

A

binds to a receptor and produces the opposite of its normal response (agonist response)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

define an antagonist

A

blocks or dampens a biological response by binding to and blocking a receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

pharmacodynamics relates to what properties of the drug?

pharmacokinetics relates to what properties of a drug?

A

pharmacodynamics relates to drug EFFECT and CONCENTRATION

pharmacokinetics is related to concentration and time

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

TOGETHER, pharmaodynamics and pharmacokinetics provides…..

A

the relationship of a drug’s effects over time

called the TIME COURSE OF EFFECT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

“Time course of drug action” is a function of…..

A

drug absorption, distribution, metabolism, excretion (pharmacokinetics)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

the INTENSITY of a response elicited by a drug is a function of…

A

the dose administered and the concentration of the drug at the site where the action-effect sequence is initiated

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

the proportion of the dose that actually contributes to the concentration at the site of action is the NET RESULT OF THE RATE AND EXTENT OF—–

A

absorption - distribution - metabolism - excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

define absorption

A

the rate at which a drug leaves its site of administration and becomes BIOAVAILABLE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

name 5 factors that affect transport across membranes and influence absorption

A

-solubility
-concentration
-circulation to the site of -absorption
-surface area of absorption
-route of administration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

binding to plasma proteins will _____ the rate of passive absorption.
how?

A

increase

by maintaining the concentration gradient of free drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

after a drug is absorbed or injected into the bloodstream, what may happen

A

may be distributed into interstitial and cellular fluids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

what organs receive most of the drug during the first few minutes after absorption?

A

heart
liver
kidney
brain
other well-perfused organs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

deliver (distribution) to what parts of the body is slower?

A

to muscle and most other viscera
skin
fat

may require several minutes to several hours before a steady state is attained

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

binding to plasma proteins will _____ the distribution of drugs to other tissues

A

decrease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

binding to plasma proteins will _______ the rate of metabolism

A

decrease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

usually, the body transforms drugs into what kind of compounds?
does the opposite ever occur?

A

usually - more polar hydrophilic inactive compounds for elimination

SOMETIMES – the opposite occurs and metabolism activates a drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

what is the primary organ where most biotransformation/metabolism reactions take place?
explain the mechanism

A

liver

phase 1 and phase 2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

explain phase 1 metabolism reactions

give an example

A

biotransformation generally results in the loss of pharmaceutical activity by the ADDITION OF A FUNCTIONAL GROUP

cyt-p450 oxidizes up to 80% of all drugs

26
Q

explain phase 2 metabolism reactions

A

biotransformation is the CONJUGATION of the parent compound/phase 1 metabolite to glutathione, amino acid, sulfate, and glucuronic acid

generally results in the complete inactivation of the drug

27
Q

how can drugs be excreted?

A

excreted from the body either unchanged or as metabolites

28
Q

what is the most important organ for the excretion of water-soluble drugs and metabolites

A

kidney

29
Q

renal excretion of drugs is dependent on several factors:
name 4

A

-protein binding
-GFR (glomerular filtration rate)
-tubular secretion and reabsorption
-blood flow

30
Q

oral drugs that are not absorbed by the GI tract are excreted where

A

in the feces

31
Q

some drugs and their metabolites are excreted where?

A

in the bile

this is the case for drugs absorbed in the GI

32
Q

what 4 things are time course relationships?

A

latency
time of onset
time of peak effect
duration of action

33
Q

what 4 things are dose-response relationships?

A

affinity
potency
efficacy
dose-response curve

34
Q

define latency

A

the time between the administration and the first measurable signs of a response

35
Q

define time of onset

A

the time of the first measurable response

36
Q

define time of peak effect

A

peak effect usually occurs when the drug concentration at the site of action has reached its maximal level

37
Q

define the duration of action

A

from the time of onset to the time when the response is no longer perceptible.(OFFSET)

38
Q

duration of action depends on what 2 things

A

the dose
the rate of drug removal from the site of action

39
Q

what is offset

A

the time when the response is no longer perceptible

40
Q

define the dose response curve

A

analyzes the magnitude of a drug effect by plotting the magnitude of the response as a function of dose of the drug

41
Q

the MAXIMUM EFFECT is when….

A

the dose response curve reaches a plateau

42
Q

define affinity

A

the ability of a given drug to bind with a specific receptor

43
Q

define potency

A

the dose needed to produce a response of a given intensity

44
Q

a shift to the right in the dose response curve means a _______ in potency, while a shift to the left indicates a ____ in potency

A

to the right = decrease in potency

to the left = increase in potency

45
Q

define efficacy

A

the ability of the drug to produce the desired response/effect upon binding to the receptor

46
Q

efficacy describes the…….

A

maximal response that can be created by the drug

47
Q

explain ED50

A

50% effective dose

the dose of a drug that produces an effect in 50% of the population (quantal)

graded - the dose that causes 50% of maximal effect

48
Q

ED50 is a convenient way to do what

A

characterize a drugs and a useful way to compare DRUG POTENCY

49
Q

what is LD50

A

the dose that kills 50% of an exposed population

50
Q

what is therapeutic index

A

a measure of the drug’s safety

= LD50/ED50

higher value = safer drug

51
Q

barbiturates bind to what?
this increases what?
what is the result?

A

barbiturates bind to GABA A receptors

this increases GABA-induced chloride currents

results in CNS depressant effects

52
Q

barbiturates are used as what kind of drugs

A

sedatives
hypnotics
anesthetics
anticonvulsants

53
Q

how are barbiturates classified?

A

on the basis of their duratiokn of actions

ultra short
short
intermediate
long acting

54
Q

barbiturates are schedule —– depressants under what act?

A

schedule II, III, and IV

DEA Controlled Substances Act

55
Q

explain the duration of all of the classes of barbiturates and give an example of each

A

Long acting - over 6 hours - PHENOBARBITAL

Intermediate acting - 3-6 hours - AMOBARBITAL

Short acting - under 3 hours - PENTOBARBITAL

ultra short acting (30 mins) - THIOPENTAL

56
Q

the onset and duration of a drug are dependent on what?

A

ADME

57
Q

the onset of thiopental CNS effects is equal to what

A

the time required to reach the CNS after IV injection

58
Q

how does thiopental have such a short duration of action

A

thiopental is highly lipophilic and the brain is highly perfused and lipophilic.

thus, thiopental rapidly reaches effective blood levels.

HOWEVER, due to its high lipophilicity it also rapidly re-distributes into adipose and other tissues, so the blood levels decrease rapidly to subtherapeutic levels.

as a result, its duration of action is ULTRA SHORT

59
Q

explain how phenoparbital and pentobarbital have a longer duration of action than thiopental

A

they are less lipophilic and thus cross the brain barrier less rapidly, and at the same time the drug is being distributed to other tissues

takes longer to reach effective CNS levels

60
Q
A

Biomedical Lab III (10 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions