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pharmacology > Pharmacodynamics - Mechanism of drug action > Flashcards

Pharmacodynamics - Mechanism of drug action Flashcards

1
Q

what two factors determine how quickly a drug initiates an effect and how long the effect lasts

A

strength and length

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2
Q

penicillin binds to what enzyme on bacterial cell wall to prevent cross linking

A

transpeptidase
this means if the bacterial load is high a higher dose of penicillin must be given to completely eliminate the bacteria from the body

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3
Q

factors that can affect the pharmacodynamics of a drug include

A

change in receptor binding
alteration in level of binding protein
decrease receptor sensitivity
genetic mutation
selectivity
malnutrition
aging
effects of other drugs

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4
Q

All drugs only alter the pace of ongoing activity and do not impart new functions on any system or organ
T or F

A

F
the only exception to this rule is gene based drugs

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5
Q

stimulation and depression is applied to specialized cells while irritation is applied to non specialized cells and is non selective
T or F

A

T

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6
Q

activated charcoal binds with poisons in stomach is an example of what mechanism of drug action

A

physical mechanism
in physical mechanism there is no change to cells in the body and the drug effect is strictly physical
other examples include
mannitol as an osmotic diuretic
bulk laxatives e.g ispaghula

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7
Q

example of chemical mechanism of drug action include

A

antacids e.g NaHCO3
acetylcholineesterase reactivator e.g pralidoxime
cholestyramine for bile and cholesterol sequestration
Chelating agents e.g dimecaprol, penicilamine, desferroxiamine

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8
Q

angiotensin converting enzyme inhibitors use what kind of inhibition

A

e.g captopril
competitive inhibition

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9
Q

reversible cholinesterase e.g neostigmine
and xanthine oxidase inhibitor e.g allopurinol
are all examples of competitive inhibitors
T or F

A

T

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10
Q

the action of allopurinol on xanthine oxidase enzyme is what kind of antagonism

A

competitive inhibition

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11
Q

the effect of aspirin on cyclooxygenase is what kind of inhibition

A

non competitive inhibition

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12
Q

omeprazole deactivates proton pump in stomach via what mechanism

A

non competitive inhibition

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13
Q

irreversible anticholinesterase like organophosphate and insecticide act via what mechanism

A

non competitive inhibition

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14
Q

monamine oxidase inhibitors e.g imipramine act via what mechanism

A

non competitive inhibition

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15
Q

list 2 examples each of channel blockers of these ions
1. Na
2. K
3. Ca
4. Cl

A
  1. Procainamide, quinidine, local anesthetic (
  2. Amiodarone, sulfonylurea
  3. nifedipine, verapamil, diltiazem
  4. benzodiazepens
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16
Q

list 2 uses each of channel blockers of these ions
1. Na
2. K
3. Ca
4. Cl

A
  1. Arrhythmia and anesthetic
  2. Arrhythmia(blockage causes prolonged refractory period)
  3. Arrhythmia and hypertension
  4. the slide explanation just dey somehow man
    if you see it in incourse skip it
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17
Q

list the inhibitors of these carriers
1.noradrenaline vessicular uptake
2.neuronal reuptake of noradrenaline
3.neuronal reuptake of serotonin
4.weak acid(e.g uric acid) carriers

A

1.reserpine
2.desipramine
3.fluoxetin
4.probenecid (thus prevents uric acid reabsorption and facilitate excretion)

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18
Q

The specific chemical constituent of the cell with which drugs interact with to produce it’s pharmacological effect is the

A

Receptor

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19
Q

drug receptors are regulatory micromolecules
T or F

A

F
macromolecules

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20
Q

list the 4 characteristics of receptors

A

The 4 S
sensitivity
specificity
selectivity
saturability

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21
Q

list 4 molecules that can serve as a receptor

A

Enzymes
membrane proteins
nucleic acid
complex polysaccharides

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22
Q

an agent which activates a receptor to produce submaximal effect but antagonizes the agonist is called

A

a partial agonist

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23
Q

an agent which activates a receptor to produce an effect opposite to that of an agonist is called

A

inverse agonist
e.g Beta Carboline

24
Q

the capacity to induce functional changes in the receptor in a way that produces an effect is called

A

Intrinsic activity / efficacy

25
Q

irreversible anticholinesterase e.g organophosphates form what kind of bond

A

covalent bond

26
Q

most drugs employ what kind of bond to receptors

A

ionic bond

27
Q

a receptor would produce a response only when it is occupied by an appropriate ligand with the response directly proportional to the fraction of occupied receptors

This theory is called

A

Occupancy Theory

this means maximal respones will only occur when all the receptors are occupied

28
Q

response is proportional to rate of onset and offset of drug binding to receptor
response is proportional to rate of drug-receptor Complex dissociation

The above statement describes what Receptor theory

A

Rate theory

29
Q

according to rate theory ______ determines whether a ligand is an agonist, antagonist or partial agonist

A

the duration of drug-receptor Complex dissociation

30
Q

response is directly proportional to intrinsic activity and fraction of occupied receptors

the receptor theory above is called

A

Stephenson Theory

31
Q

Response is a function of affinity, maximum response can be produced without 100% occupancy

A

Ariens theory

32
Q

binding of ligand to receptor is based on plastic modeling with receptor and ligand both undergoing a dynamic process
with agonist inducing conformational change in the receptor

the receptor theory above is the

A

induced fit theory

33
Q

when a drug receptor interaction occurs either a specific conformational pertubation(by agonist) which leads to a biological response or a nonspecific conformational pertubation(by antagonist) which leads to no response

This receptor theory is called

A

Macromolecular conformational theory

34
Q

List 6 the receptor theory

A
  1. Occupancy theory
  2. Rate theory
  3. Stephenson theory
  4. Ariens theory
  5. Induced fit theory
  6. Macromolecule Pertubation theory
35
Q

Receptors have 2 domain which are

A

Ligand binding domain
Effector domain
it is the effector domain that undergoes conformational change

36
Q

the basis for designating receptor subtypes is the

A

relative tissue distribution of receptor

37
Q

receptor subtypes such as serotonin(5-HT) where delineated from each other based ____

A

high affinity and displacement by various selective agonist/antagonist

38
Q

receptors without a known ligand are called

A

orphan receptors

39
Q

receptors/site which binds specific drugs without eliciting a pharmacological response are known as

A

Silent receptors/Drug acceptors/ Site of loss
e.g plasma proteins

40
Q

the remaining unoccupied receptors in a tissue are called

A

spare receptors

41
Q

in upregulation there is increase in number of receptors with subsequent increase in sensitivity
T or F

A

T

42
Q

list 2 disease in which there is mutations of genes encoding for G protein coupled receptors

A

Cancer
Hypoparathyroidism

43
Q

list the 4 major categories of transducer mechanism

A

GPCR
receptors with intrinsic ion channels
receptors linked with enzymes
transcription factors(receptors for gene expression)

44
Q

GPC-receptor have how many transmembrane domain

A

7

45
Q

GPCR have ___ alpha helical membrane spanning hydrophobic amino acid segments

A

7

46
Q

gpcr have how many loops

A

3 intracellular and 3 extracellular
6

47
Q

ligand gated ion channels open very fast and are thus confined to excitable tissue
T or F

A

T

48
Q

G proteins have how many sub units

A

3
Ga GB GY

49
Q

G proteins are classified into Gi, Gs and Gq based on

A

their Ga subunit

50
Q

list the functions of these G proteins
1.Gi
2.Gs
3.Gq
4.Go

A

1.inhibits adenyl cyclase
2.stimulate adenyl cyclase
3.stimulates phospholipase C
4.inhibits calcium channel

there’s a G12/13 which regulates actin cytoskeletal modeling in migrating cells or cancer cells metastatic

51
Q

list the 3 second messenger system

A

CAMP
CGMP
Calcium and phosphoinositol system

52
Q

in their inactive form G proteins are bound to

A

GDP

53
Q

the G protein is bound to the receptor in its active state
T or F

A

F
in its inactive state
when it the receptor is stimulated it activates the G protein which subsequently detaches from the receptor
this detachment allows the receptor to bind more inactive G proteins and activate them

54
Q

what are the 3 possible targets for G proteins

A

adenyl cyclase (for CAMP formation)
phospholipase c (for Ip3 and DAG formation)
ion channels (particularly Ca and K)

55
Q

the GBY dimer formed (when the G protein is activated and split) function in

A

modulation of signal

pharmacology (8 decks)

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