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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
SYNAPSE
* Area between two neurons that ensures the transmission of information * Interesting target for many psychotropic drugs
26
NEUROTRANSMISSION
``` RECEPTION INTEGRATION / CHEMICAL ENCODING ELECTRICAL ENCODING SIGNAL PROPAGATION SIGNAL TRANSDUCTION ```
27
RECEPTION
``` STIMULATION OF A PRESYNAPTIC NEURON VIA : o Hormone o Neurotransmitter o Drug o Nerve impulse ```
28
ENCODING
o Chemical signal converted to electrical signal
29
SIGNAL PROPAGATION
o Electrical signal spreads to the terminal axon
30
SIGNAL TRANSDUCTION
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
NEUROTRANSMITTERS | SYNTHESIS BY
By the neuron
32
NEUROTRANSMITTERS | RELEASE By
the axonal termination
33
NEUROTRANSMITTERS | EFFECT
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
NEUROTRANSMITTERS | ACTION ARE TERMINATED BY :
1. Recapture by receptors | 2. Degradation by an enzyme
35
SEROTONIN (5-HT) | SYNTHESIS
* By the neuron | * Tryptophan is the precursor to 5-HT
36
SEROTONIN (5-HT) | RECEPTORS
• 5-HT1 to 5-HT7 | Ø Many have subtypes (e.g. 5-HT1A)
37
SEROTONIN (5-HT) | ACTION ARE TERMINATED BY :
1. Recapture by SERT receptors 2. Degradation by an enzyme, monoamime oxidase (MAO)
38
SEROTONIN (5-HT) | IMPLICATIONS
``` o Mood o Sleep o Appetite o Pain o Temperature o Cognition o Psychomotor agitation / retardation ```
39
NOREPINEPHRINE (NE) | SYNTHESIS
* By the neuron | * Tyrosine is the precursor to NE
40
NOREPINEPHRINE (NE) | RECEPTORS
• Alpha or beta receptors
41
NOREPINEPHRINE (NE) | ACTION ARE TERMINATED BY :
1. Recapture by NET receptors 2. Degradation by an enzyme, monoamime oxidase (MAO)
42
NOREPINEPHRINE (NE) | IMPLICATIONS
``` o Awakening/sleep o Mood o Agitation/ psychomotor delay o Attention o Heart rate o Blood circulation ```
43
DOPAMINE (DA) | SYNTHESIS
* By the neuron | * Tyrosine is the precursor to DA
44
DOPAMINE (DA) | RECEPTORS
• D1 to D5
45
DOPAMINE (DA) | ACTION ARE TERMINATED BY :
1. Recaptured by DAT receptors 2. Degradation by an enzyme, monoamime oxidase (MAO)
46
DOPAMINE (DA) | IMPLICATIONS
``` o Movement o Posture o Pleasure o Emotional response o Pain ```
47
GLUTAMATE, receptors, implications
• Excitatory neurotransmitter • Receptors (examples): Ø NMDA, AMPA • Implications : memory, energy
48
GABA, receptors, implications
* Inhibitory neurotransmitter * Receptor : GABA * Implications : stress, anxiety
49
ACETYLCHOLINE (ACH) | SYNTHESIS
* By the neuron | * Choline and acetyl coenzyme A are the precursors of ACh
50
ACETYLCHOLINE (ACH) | RECEPTORS
* Muscarinic (M1 to M5) | * Nicotinic
51
ACETYLCHOLINE (ACH) | ACTION ARE TERMINATED BY :
1. Degradation by acetylcholinesera (AChE) | 2. Degradation by butyrylcholineseterase (BuChE)
52
ACETYLCHOLINE (ACH) | IMPLICATIONS
``` o Memory o Learning o Cognition o Awakening o Muscle contraction ```
53
MAIN TARGETS FOR PSYCHOTROPIC DRUGS
TRANSPORTERS G PROTEIN-COUPLED RECEPTORS ENZYMES ION CHANNELS
54
MONOAMINES TRANSPORTERS
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
DRUGS THAT TARGET MONOAMINE TRANSPORTERS
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
G PROTEIN-COUPLED RECEPTORS
Neurotransmitter binds to a receptor The receptor changes its conformation to Médicament bind to the G protein
57
ROLE OF THE ENZYME
Converts the substrate into a different molecule (product)
58
DRUGS THAT TARGET ENZYMES
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
ION CHANNELS
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
VARIATIONS IN PHARMACOLOGICAL RESPONSE
o Receptor desensitization o Tolerance o Dependence o Placebo effect
61
Receptor desensitization
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
Tolerance
- ↓ pharmacological response following chronic administration of a drug (loss of efficacy) - Higher plasma concentrations required to replicate initial pharmacological effect
63
Dependence
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
Placebo effect
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
Define what synergy is in pharmacology.
amplified effects
66
What is the enzyme that degrades monoamines? Why is this enzyme an interesting target for some psychotropic drugs?
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
What happens when a ligand binds to a receptor coupled to a G protein? Give examples of drugs that are antagonists to these receptors.
Neurotransmitter binds to a receptor The receptor changes its conformation to Médicament bind to the G protein activates secondary messenger, makes a response
68
Drugs that target serotonin acts on what targets? Give examples for each target.
SSRIs: transporter MAOI: enzymes Mirtazapine: g protein
69
What is the effect of an agonist, partial agonist or antagonist on intrinsic activity?
Agonist: generates intrinsic activity Partial agonist: generates lower intrinsic activity than agonist 0-99% ex: abilify Antagonist: no intrinsic activity
70
What neurotransmitters are used for during neurotransmission?
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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