PSYCHOPHARMACOLOGY
Lecture 1.1
DEFINITION Difference in nomenclature (naamgeving) ATC
Pharmacology = Knowledge about drugs or versus NbN
medicines; the art of preparing medication ATC: Antipsychotics
- The science that deals with studying the - NbN: Serotonin/Dopamine antagonists with
reciprocal actions, or interactions, between antipsychotic actions
pharmacological substances and ATC: Antidepressants
physiological processes - NbN: Monoamine reuptake inhibitors with
- Pharmakon = medicine / pharmaceutical antidepressant action
product à NbN is more describing
CLASSIFICATION ATC – PSYCHOTROPIC DRUG MAIN CLASSES
Possible grounds include: - Antipsychotics
- Chemical structure à what does it look like o Conventional antipsychotic, e.g.,
o Interesting, but the same structure Haloperidol
can have different effects o Atypical, e.g., Risperidone
o Doesn’t tell you how the - Antidepressants
medications affect your body o Tricyclic, e.g., Imipramine
- Working mechanism o Selective Serotonin Reuptake
o Ideal, but working mechanism not Inhibitors (SSRI), e.g., Prozac
always known o MonoAmine Oxidase Inhibitors
- Behavioral effects (MAOI), e.g., Nardil
o Easiest, linked to treated disorder - Anxiolytics (anti-anxiety medication)
o Benzodiazepines, e.g., Valium
ATC NbN o Non-Benzodiazepines, e.g.,
Anatomical Therapeutic Neuroscience-based Buspirone
Chemical Nomenclature
- Mood stabilizers
Behavioral effects Working mechanism
- Indication - Pharmacologically o Lithium
based driven - Hypnotics
Older (1976) Newer (2018)
Gold standard (WHO) Taskforce 5 organizations
OTHER RELEVANT DRUG CLASSES
Cons: Cons:
- Anti-epileptics
- Use for other - New, not
than primary acknowledged by o ¢Benzodiazepines (à also used for
disorder (e.g., WHO/scientific anxiety), Clonazepam, Clorazepate
antipsychotics community - Stimulants
for ASD - Lack of sufficient
o ¢Cocaine, Amphetamine, Methyl-
- Stigma/patient evidence
adherence
phenidate, Caffeine, Nicotine, Ritalin
1
, - Narcotic pain killers o Higher lipid solubility à Faster
o ¢Opioids, Morphine, Codeine, Heroin distribution (e.g., heroin vs. morphine)
- Central Nervous System (CNS) suppressors
- Psychedelics & Hallucinogens
o ¢LSD, Marijuana, Mescaline, Psylocibin ADMINISTRATION
Includes 4 important stages:
ADMINISTRATION 1. Absorption
Includes 4 important stages o Site of administration à blood
1. Absorption = from site of administration à 2. Distribution
blood o Throughout body
2. Distribution = throughout body 3. Metabolism
3. Metabolism = conversion by body o Conversion by body
4. Excretion = elimination from body 4. Excretion
o Elimination from body
ABSORPTION
- Oral PHARMACOKINETICS
- Rectal Change over time in terms of serum concentration
- Topical (regional) of medication and metabolites
o Skin - How does the body process the
o Oral mucosa medication?
§ Sublingual Has an effect on:
§ Buccal - Absorption
§ Snorting - Distribution
- Parenteral (through the blood) à fastest - Interaction with receptor
o Intravenous - Elimination
o Intramuscular Entire blood circulation takes +/- 1 minute
o Subcutaneously - Pharmacokinetics = done by bloodstream
à If you want a storage of the medication Capillaries (= small blood vessels)
- Inhalation - 10 billion
- 200 m2
DISTRIBUTION Every cell < 10-30 micron from capillary (micron =
- In blood (albumin) 0,001 millimeter)
- Distribution
o Extracellular (blood plasma) THE DIFFERENCE
o Intracellular (water in body cells) Pharmacokinetics = How does the body process
- Speed of distribution depends on lipid the medication?
solubility Pharmacodynamics = How does the body respond
o Through membranes: passive diffusion to the medication?
following concentration gradient Medication – Receptor interaction
à Spreads evenly so there’s the same amount Determine pharmacological, therapeutic, and toxic
everywhere effect.
2
,PHARMACODYNAMICS TO SUM IT UP
Time – Concentration relation Pharmacokinetics = how does the body process
T0 (time 0) the medication?
- First: Large peak in medication Pharmacodynamics = how does the body respond
concentration in plasma to the medication?
o Medication administered Distribution half-life = how fast absorbed?
- Then: Large decrease medication Elimination half-life = how fast eliminated?
concentration in plasma
o Leaves bloodstream, enters body (cells,
fat, muscles etc.)
Half-lives = time for the medication to halve in NEURONS
concentration Global structure
- Distribution half-live - Cell body = Soma
o ¢Alpha phase Dendrites
o T0 à 50% - With spines
- Elimination half-live - Without spines
o ¢Beta phase Axon
o ¢Degradation (liver) and 50% excretion Synapses (anterograde)
(kidneys) - Axodendritic
o Receiver = dendritic spine
PHARMACODYNAMICS - Axosomatic
# % Eliminated % Present in system o Receiver = soma
0 0 100 - Axoaxonic
1 50 50 o Receiver = axon
2 75 25
3 87,5 12,5 SYNAPSES
4 93,75 6,25 Axonal ending forms synapse with postsynaptic
5 96,875 3,125
neuron
6 98,4375 1,5625
- Mitochondria provide energy
- Neurotransmitter stored in vesicle
Distribution half-life
o If they were floating around, they get
- Alpha phase
broken down and we don’t want that
- T0 à 50%
- Receptors both sides of synaptic cleft
- ¢First half-live = important à Onset action
Elimination half-life
PYRAMIDAL CELLS
- Beta phase
Triangular cell body
- Degradation (liver) and 50% excretion
Apical dendrite
(kidneys)
One axon
- Sixth half-live = important
Stimulating
- Eliminated/Stop action
3
, Located in motor cortex, prefrontal cortex, NEURONS II
hippocampus, entorhinal cortex Subcellular organelles
- EF, Memory Protein synthesis
- ‘Get your hand out of the fire’ Internal transport
CHANDELIER CELLS Functions are zone-dependent (anatomically)
Because it looks like a chandelier
Axo-axonic NEURONAL ANATOMY
Inhibitory Input
- Inhibits/Stops pyramid cells - Signal from another neuron
Cortex - Environment: warmth, darkness, coldness
SPINY CELLS - Chemicals
Dendrites = shaped like spikes - Hormones
Long axons - Medication
Striatum - Integration
o signal cascade to
PURKINJE CELLS genome
Dendrites = shaped like a tree o decoding genome à encoding
One axon chemical signals
Cerebellum Electric coding = Integration incoming electrical
signals
INTERNEURONS Signal transduction = Electr. signal over membrane
Mainly brain & spinal cord Output = Chemical à signal output to next neuron
Provide neural circuit
Sensory ßà motor CYTOPLASM
Local 1. Nucleolus = stores DNA
- Short axons 2. Nucleus = other things happen here
- Analyze small pieces info 3. Ribosome = small dots
Relay 4. Vesicle = contains neurotransmitters
- Long axons 5. Rough ER = because of the ribosomes
- Over brain regions 6. Golgi apparatus = protein synthesis
7. Cytoskeleton
BASKET CELLS 8. Smooth ER = because of NO ribosomes
Dendrites = shaped like a basket 9. Mitochondrion = looks like kidney bean,
Inhibitory interneuron energy
Cortex 10. Vacuole
11. Cytoplasm = the juice
7
DOUBLE BOUQUET CELLS 12. Lysosome
Dendrites = shaped like two bouquets 13. Centrioles/Centrosome = DNA related
Inhibitory interneuron 14. Membrane = lipid solubility
Cortex
4
Lecture 1.1
DEFINITION Difference in nomenclature (naamgeving) ATC
Pharmacology = Knowledge about drugs or versus NbN
medicines; the art of preparing medication ATC: Antipsychotics
- The science that deals with studying the - NbN: Serotonin/Dopamine antagonists with
reciprocal actions, or interactions, between antipsychotic actions
pharmacological substances and ATC: Antidepressants
physiological processes - NbN: Monoamine reuptake inhibitors with
- Pharmakon = medicine / pharmaceutical antidepressant action
product à NbN is more describing
CLASSIFICATION ATC – PSYCHOTROPIC DRUG MAIN CLASSES
Possible grounds include: - Antipsychotics
- Chemical structure à what does it look like o Conventional antipsychotic, e.g.,
o Interesting, but the same structure Haloperidol
can have different effects o Atypical, e.g., Risperidone
o Doesn’t tell you how the - Antidepressants
medications affect your body o Tricyclic, e.g., Imipramine
- Working mechanism o Selective Serotonin Reuptake
o Ideal, but working mechanism not Inhibitors (SSRI), e.g., Prozac
always known o MonoAmine Oxidase Inhibitors
- Behavioral effects (MAOI), e.g., Nardil
o Easiest, linked to treated disorder - Anxiolytics (anti-anxiety medication)
o Benzodiazepines, e.g., Valium
ATC NbN o Non-Benzodiazepines, e.g.,
Anatomical Therapeutic Neuroscience-based Buspirone
Chemical Nomenclature
- Mood stabilizers
Behavioral effects Working mechanism
- Indication - Pharmacologically o Lithium
based driven - Hypnotics
Older (1976) Newer (2018)
Gold standard (WHO) Taskforce 5 organizations
OTHER RELEVANT DRUG CLASSES
Cons: Cons:
- Anti-epileptics
- Use for other - New, not
than primary acknowledged by o ¢Benzodiazepines (à also used for
disorder (e.g., WHO/scientific anxiety), Clonazepam, Clorazepate
antipsychotics community - Stimulants
for ASD - Lack of sufficient
o ¢Cocaine, Amphetamine, Methyl-
- Stigma/patient evidence
adherence
phenidate, Caffeine, Nicotine, Ritalin
1
, - Narcotic pain killers o Higher lipid solubility à Faster
o ¢Opioids, Morphine, Codeine, Heroin distribution (e.g., heroin vs. morphine)
- Central Nervous System (CNS) suppressors
- Psychedelics & Hallucinogens
o ¢LSD, Marijuana, Mescaline, Psylocibin ADMINISTRATION
Includes 4 important stages:
ADMINISTRATION 1. Absorption
Includes 4 important stages o Site of administration à blood
1. Absorption = from site of administration à 2. Distribution
blood o Throughout body
2. Distribution = throughout body 3. Metabolism
3. Metabolism = conversion by body o Conversion by body
4. Excretion = elimination from body 4. Excretion
o Elimination from body
ABSORPTION
- Oral PHARMACOKINETICS
- Rectal Change over time in terms of serum concentration
- Topical (regional) of medication and metabolites
o Skin - How does the body process the
o Oral mucosa medication?
§ Sublingual Has an effect on:
§ Buccal - Absorption
§ Snorting - Distribution
- Parenteral (through the blood) à fastest - Interaction with receptor
o Intravenous - Elimination
o Intramuscular Entire blood circulation takes +/- 1 minute
o Subcutaneously - Pharmacokinetics = done by bloodstream
à If you want a storage of the medication Capillaries (= small blood vessels)
- Inhalation - 10 billion
- 200 m2
DISTRIBUTION Every cell < 10-30 micron from capillary (micron =
- In blood (albumin) 0,001 millimeter)
- Distribution
o Extracellular (blood plasma) THE DIFFERENCE
o Intracellular (water in body cells) Pharmacokinetics = How does the body process
- Speed of distribution depends on lipid the medication?
solubility Pharmacodynamics = How does the body respond
o Through membranes: passive diffusion to the medication?
following concentration gradient Medication – Receptor interaction
à Spreads evenly so there’s the same amount Determine pharmacological, therapeutic, and toxic
everywhere effect.
2
,PHARMACODYNAMICS TO SUM IT UP
Time – Concentration relation Pharmacokinetics = how does the body process
T0 (time 0) the medication?
- First: Large peak in medication Pharmacodynamics = how does the body respond
concentration in plasma to the medication?
o Medication administered Distribution half-life = how fast absorbed?
- Then: Large decrease medication Elimination half-life = how fast eliminated?
concentration in plasma
o Leaves bloodstream, enters body (cells,
fat, muscles etc.)
Half-lives = time for the medication to halve in NEURONS
concentration Global structure
- Distribution half-live - Cell body = Soma
o ¢Alpha phase Dendrites
o T0 à 50% - With spines
- Elimination half-live - Without spines
o ¢Beta phase Axon
o ¢Degradation (liver) and 50% excretion Synapses (anterograde)
(kidneys) - Axodendritic
o Receiver = dendritic spine
PHARMACODYNAMICS - Axosomatic
# % Eliminated % Present in system o Receiver = soma
0 0 100 - Axoaxonic
1 50 50 o Receiver = axon
2 75 25
3 87,5 12,5 SYNAPSES
4 93,75 6,25 Axonal ending forms synapse with postsynaptic
5 96,875 3,125
neuron
6 98,4375 1,5625
- Mitochondria provide energy
- Neurotransmitter stored in vesicle
Distribution half-life
o If they were floating around, they get
- Alpha phase
broken down and we don’t want that
- T0 à 50%
- Receptors both sides of synaptic cleft
- ¢First half-live = important à Onset action
Elimination half-life
PYRAMIDAL CELLS
- Beta phase
Triangular cell body
- Degradation (liver) and 50% excretion
Apical dendrite
(kidneys)
One axon
- Sixth half-live = important
Stimulating
- Eliminated/Stop action
3
, Located in motor cortex, prefrontal cortex, NEURONS II
hippocampus, entorhinal cortex Subcellular organelles
- EF, Memory Protein synthesis
- ‘Get your hand out of the fire’ Internal transport
CHANDELIER CELLS Functions are zone-dependent (anatomically)
Because it looks like a chandelier
Axo-axonic NEURONAL ANATOMY
Inhibitory Input
- Inhibits/Stops pyramid cells - Signal from another neuron
Cortex - Environment: warmth, darkness, coldness
SPINY CELLS - Chemicals
Dendrites = shaped like spikes - Hormones
Long axons - Medication
Striatum - Integration
o signal cascade to
PURKINJE CELLS genome
Dendrites = shaped like a tree o decoding genome à encoding
One axon chemical signals
Cerebellum Electric coding = Integration incoming electrical
signals
INTERNEURONS Signal transduction = Electr. signal over membrane
Mainly brain & spinal cord Output = Chemical à signal output to next neuron
Provide neural circuit
Sensory ßà motor CYTOPLASM
Local 1. Nucleolus = stores DNA
- Short axons 2. Nucleus = other things happen here
- Analyze small pieces info 3. Ribosome = small dots
Relay 4. Vesicle = contains neurotransmitters
- Long axons 5. Rough ER = because of the ribosomes
- Over brain regions 6. Golgi apparatus = protein synthesis
7. Cytoskeleton
BASKET CELLS 8. Smooth ER = because of NO ribosomes
Dendrites = shaped like a basket 9. Mitochondrion = looks like kidney bean,
Inhibitory interneuron energy
Cortex 10. Vacuole
11. Cytoplasm = the juice
7
DOUBLE BOUQUET CELLS 12. Lysosome
Dendrites = shaped like two bouquets 13. Centrioles/Centrosome = DNA related
Inhibitory interneuron 14. Membrane = lipid solubility
Cortex
4
