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Pharmaco > Class 2-Pharmacodynamics > Flashcards

Class 2-Pharmacodynamics Flashcards

1
Q

PHARMACODYNAMCS

A

« WHAT THE DRUG DOES TO THE BODY »
• Relationship between drug concentration and response
• Drug activity at the receptor

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2
Q

RECEPTOR

A

o Mainly made up of proteins
o Specific conformation
Ø Receptor only interacts with ligands that have a compatible structure

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3
Q

LIGAND

A

o Any substance capable of binding to a receptor
Ø Neurotransmitters
Ø Hormones (natural ligands)
Ø Drugs

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4
Q

« RECEPTOR BINDING » CHARACTERIZED BY 4 CRITERIA

A
  1. Affinity
  2. Saturability
  3. Reversibility
  4. Specificity
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5
Q

Affinity

A

Probability of a drug occupying a receptor at any given time. how much the drug loves to bind to the receptor
Expressed by a constant : Ki
- Ki = dose of a drug needed to occupy 50 % of receptors
- Ki is inversely proportional to affinity
high number = low affinity

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6
Q

Saturability

A

« Receptor binding » is sometimes limited by the number of receptors
available

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7
Q

Reversibility

A

« Receptor binding » can be reversible or irreversible

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8
Q

Specificity

A
  • Specific = binds only to its receptor

- Non specific = binds to other receptors

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9
Q

EC50

A

Concentration needed to achieve 50% of the maximum effect

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10
Q

POSSIBLE EFFECTS OF A DRUG / SUBSTANCE ON A RECEPTOR

A 
o Complete agonist
o Partial Agonist
o Antagonist
Ø Competitive
Ø Non competitive
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11
Q

INTRINSIC ACTIVITY

A

The ability of a substance to initiate a response after binding to a receptor

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12
Q

COMPLETE AGONIST

A

o Generates intrinsic activity

o May be endogenous (e.g. neurotransmitter) or exogenous (e.g. medication)

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13
Q

PARTIAL AGONIST

A

o Generates lower intrinsic activity than agonist
ü 0 to 99,9 % of response (Vs an agonists)
o Good affinity for the receptor, just like the agonist

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14
Q

ANTAGONIST

A

o No intrinsic activity
o Binds to the receiver, but does not activate it
o Prevents an agonist from binding to the same receiver

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15
Q

ANTAGONIST-COMPETITIVE

A

o Antagonist effect is surmountable if we increase concentration of the agonist
o If simultaneous administration of an agonist + competitive antagonist : affinity to the receptor and drug concentrations will determine the winner

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16
Q

ANTAGONIST-NON COMPETITIVE

A

o Inhibits an agonist’s response regardless of concentration

o Antagonist effect is insurmountable even if concentrations of the agonist are increased

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17
Q

PHARMACODYNAMIC INTERACTIONS

A

o Additive effect
o Synergistic effect
o Antagonistic effect

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18
Q

Additive effect

A

Drug 1 + Drug 2
- 1 + 1 = 2
- Total effect = sum of the effects of
the two drugs used separately

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19
Q

Synergistic effect

A

Drug 1 + Drug 2

  • 1 + 1 > 2
  • Total effect > sum of the effects of the two drugs used separately
  • Generally when drugs have different mechanisms of action
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20
Q

Antagonistic effect

A

Drug 1 + Drug 2

  • 1 + 1 < 2
  • Administration of drugs with opposite effects
  • Measured effect is less for at least 1 of the drugs
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21
Q

DENDRITES

A

• Extension of the cell body
• Present receptors to detect chemical signals
(neurotransmitters)

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22
Q

AXONE

A

Transmet un signal électrique

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23
Q

CELL BODY

A
  • Includes core

* Protein synthesis and maintaining cellular integrity

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24
Q

AXONAL TERMINATION

A

• The main site of the synthesis and release of neurotransmitters

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25
Q

SYNAPSE

A
  • Area between two neurons that ensures the transmission of information
  • Interesting target for many psychotropic drugs
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26
Q

NEUROTRANSMISSION

A 
RECEPTION
INTEGRATION / CHEMICAL ENCODING
ELECTRICAL ENCODING
SIGNAL PROPAGATION
SIGNAL TRANSDUCTION
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27
Q

RECEPTION

A 
STIMULATION OF A PRESYNAPTIC
NEURON VIA :
o Hormone
o Neurotransmitter
o Drug
o Nerve impulse
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28
Q

ENCODING

A

o Chemical signal converted to electrical signal

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29
Q

SIGNAL PROPAGATION

A

o Electrical signal spreads to the terminal axon

30
Q

SIGNAL TRANSDUCTION

A

o Reconversion to a chemical signal
o Release of a neurotransmitter
o Stimulation of the post-synaptic receptor
Communication between neurons is chemical (not electrical)

31
Q

NEUROTRANSMITTERS

SYNTHESIS BY

A

By the neuron

32
Q

NEUROTRANSMITTERS

RELEASE By

A

the axonal termination

33
Q

NEUROTRANSMITTERS

EFFECT

A

Produce an effect on the post-synaptic neuron
Ø The same effect as that generated by stimulation
of the pre-synaptic neuron
Ø Interact with the post-synaptic receptor in a specific way

34
Q

NEUROTRANSMITTERS

ACTION ARE TERMINATED BY :

A
  1. Recapture by receptors

2. Degradation by an enzyme

35
Q

SEROTONIN (5-HT)

SYNTHESIS

A
  • By the neuron

* Tryptophan is the precursor to 5-HT

36
Q

SEROTONIN (5-HT)

RECEPTORS

A

• 5-HT1 to 5-HT7

Ø Many have subtypes (e.g. 5-HT1A)

37
Q

SEROTONIN (5-HT)

ACTION ARE TERMINATED BY :

A
  1. Recapture by SERT receptors
  2. Degradation by an enzyme, monoamime oxidase
    (MAO)
38
Q

SEROTONIN (5-HT)

IMPLICATIONS

A 
o Mood
o Sleep
o Appetite
o Pain
o Temperature
o Cognition
o Psychomotor agitation / retardation
39
Q

NOREPINEPHRINE (NE)

SYNTHESIS

A
  • By the neuron

* Tyrosine is the precursor to NE

40
Q

NOREPINEPHRINE (NE)

RECEPTORS

A

• Alpha or beta receptors

41
Q

NOREPINEPHRINE (NE)

ACTION ARE TERMINATED BY :

A
  1. Recapture by NET receptors
  2. Degradation by an enzyme, monoamime oxidase
    (MAO)
42
Q

NOREPINEPHRINE (NE)

IMPLICATIONS

A 
o Awakening/sleep
o Mood
o Agitation/ psychomotor delay
o Attention
o Heart rate
o Blood circulation
43
Q

DOPAMINE (DA)

SYNTHESIS

A
  • By the neuron

* Tyrosine is the precursor to DA

44
Q

DOPAMINE (DA)

RECEPTORS

A

• D1 to D5

45
Q

DOPAMINE (DA)

ACTION ARE TERMINATED BY :

A
  1. Recaptured by DAT receptors
  2. Degradation by an enzyme, monoamime oxidase
    (MAO)
46
Q

DOPAMINE (DA)

IMPLICATIONS

A 
o Movement
o Posture
o Pleasure
o Emotional response
o Pain
47
Q

GLUTAMATE, receptors, implications

A

• Excitatory neurotransmitter
• Receptors (examples):
Ø NMDA, AMPA
• Implications : memory, energy

48
Q

GABA, receptors, implications

A
  • Inhibitory neurotransmitter
  • Receptor : GABA
  • Implications : stress, anxiety
49
Q

ACETYLCHOLINE (ACH)

SYNTHESIS

A
  • By the neuron

* Choline and acetyl coenzyme A are the precursors of ACh

50
Q

ACETYLCHOLINE (ACH)

RECEPTORS

A
  • Muscarinic (M1 to M5)

* Nicotinic

51
Q

ACETYLCHOLINE (ACH)

ACTION ARE TERMINATED BY :

A
  1. Degradation by acetylcholinesera (AChE)

2. Degradation by butyrylcholineseterase (BuChE)

52
Q

ACETYLCHOLINE (ACH)

IMPLICATIONS

A 
o Memory
o Learning
o Cognition
o Awakening
o Muscle contraction
53
Q

MAIN TARGETS FOR PSYCHOTROPIC DRUGS

A

TRANSPORTERS
G PROTEIN-COUPLED RECEPTORS
ENZYMES
ION CHANNELS

54
Q

MONOAMINES TRANSPORTERS

A

PRE-SYNAPTIC REUPTAKE OF NEUROTRANSMITTERS
o Prevents the neurotransmitter from accumulating in the
synapse
o Interesting target to increase the activity of these neurotransmitters

55
Q

DRUGS THAT TARGET MONOAMINE TRANSPORTERS

A

o Antidepressant
Ø Selective serotonin reuptake inhibitors (SSRIs; e.g. citalopram): • Selective inhibition of 5-HT recapture via SERT receptor inhibition
• ↑ amount of serotonin in the synapse
Ø Serotonin and norepinephrine reuptake inhibitors (NSRI; e.g. venlafaxine)
Ø Norepinephrine and dopamine reuptake inhibitors (e.g. bupropion)

56
Q

G PROTEIN-COUPLED RECEPTORS

A

Neurotransmitter binds to a receptor
The receptor changes its conformation to
Médicament bind to the G protein

57
Q

ROLE OF THE ENZYME

A

Converts the substrate into a different molecule (product)

58
Q

DRUGS THAT TARGET ENZYMES

A

o Antidepressant
Ø Monoamine oxydase inhibitors (MAOI; e.g. phenelzinde): • Monoamine oxydase
• Enzyme that degrades monoamines (5-HT, NE, DA)
• ↑ amount of 5-HT, NE and DA in the synapse
o Drug used to treat cognitive impairment
Ø Acetylcholinesera inhibitors (e.g. rivastigmine)

59
Q

ION CHANNELS

A

o Transmembrary proteins with integrated ion channel that activate following a change in membrane voltage
o When the electric current arrives, change of conformation which allows specific ions (e.g. Na, Ca, K) to cross the cell membrane
o Important in the propagation of the action potential in the neurons of the brain

60
Q

VARIATIONS IN PHARMACOLOGICAL RESPONSE

A

o Receptor desensitization
o Tolerance
o Dependence
o Placebo effect

61
Q

Receptor desensitization

A

G protein-coupled receptors trigger adaptive mechanisms to regulate pharmacological response :
- Change in receptor conformation
- Neurotransmitter depletion (tachyphylaxis)
- Loss of receptors (e.g. internalization)
Can gradually lead to the development of tolerance

62
Q

Tolerance

A
  • ↓ pharmacological response following
    chronic administration of a drug (loss of efficacy)
  • Higher plasma concentrations required to replicate initial pharmacological effect
63
Q

Dependence

A

Psychological dependance
- Patient cannot get rid of the need to consume the substance
Physical dependance
- Symptoms of withdrawal if sudden cessation of substance or rapid dose

64
Q

Placebo effect

A

Placebo

  • Placebo effect = the drug’s real beneficial effect, but not related to its mechanism of action, only to the psychological effects of taking the drug
  • Experimental tool to assess the clinical effect of any treatment that has a variable
65
Q

Define what synergy is in pharmacology.

A

amplified effects

66
Q

What is the enzyme that degrades monoamines? Why is this enzyme an interesting target for some psychotropic drugs?

A

Ø Monoamine oxydase inhibitors (MAOI; e.g. phenelzinde): • Monoamine oxydase
• Enzyme that degrades monoamines (5-HT, NE, DA)
• ↑ amount of 5-HT, NE and DA in the synapse
Interesting for psychotropic drugs because if we block enzyme, monoamines won’t be degraded = more monoamines = treat depression, for example

67
Q

What happens when a ligand binds to a receptor coupled to a G protein? Give examples of drugs that are antagonists to these receptors.

A

Neurotransmitter binds to a receptor
The receptor changes its conformation to
Médicament bind to the G protein
activates secondary messenger, makes a response

68
Q

Drugs that target serotonin acts on what targets? Give examples for each target.

A

SSRIs: transporter
MAOI: enzymes
Mirtazapine: g protein

69
Q

What is the effect of an agonist, partial agonist or antagonist on intrinsic activity?

A

Agonist: generates intrinsic activity
Partial agonist: generates lower intrinsic activity than agonist 0-99% ex: abilify
Antagonist: no intrinsic activity

70
Q

What neurotransmitters are used for during neurotransmission?

A

Produce an effect on the post-synaptic neuron
Ø The same effect as that generated by stimulation
of the pre-synaptic neuron
Ø Interact with the post-synaptic receptor in a specific way

Pharmaco (11 decks)

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