Lecture 1 -
Definition & Classification
Definition
● Pharmacology → Knowledge about drugs or medicines; The art of preparing
medication
○ The science that deals with studying the reciprocal actions, or interactions,
between pharmacological substances and psychological processes
● Pharmacon → medicine / pharmaceutical product
Definition ‘Drug’
● English → Pharmacologically active substance
○ Medication or other substance with a physiological effect
○ Psychoactive substance for abuse, narcotic or stimulating
● Dutch → Psychoactive substance for abuse
○ Drug / stimulant with a more or less ‘drugging’ effect, which can lead to
dependence (addiction)
Classification
● Possible grounds include
○ Chemical structure
■ Interesting, but the same structure can have different effects
○ Working mechanism
■ Ideal, bit working mechanism
○ Behavioral effects
■ Easiest, linked to discord being treated
● However, there are other classifications
○
ATC NbN
Anatomical Therapeutic Chemical Neuroscience-based Nomenclature
Behavioral effects → indication Working mechanism →
based pharmacologically driven
Older (1976) Newer (2018)
Gold standard (WHO) Taskforce 5 organizations
Cons: Cons:
● Use for other than primary ● New, not acknowledged by
disorder WHO / scientific community
● Stigma/patient adherence ● Lack of sufficient evidence
● Differences in nomenclature ATC versus NbN
○
ATC NbN
Antipsychotics Serotonin/Dopamine antagonists
, with antipsychotic actions
Antidepressants Monoamine reuptake inhibitors with
antidepressant action
ATC
● Psychotropic drug main classes
○ Antipsychotics
■ Conventional antipsychotic (e.g. Haloperidol)
■ Atypical (e.g. Risperidone)
○ Antidepressants
■ Tricyclic (e.g. Imipramine)
■ Selective Serotonin Reuptake Inhibitors / SSRI (e.g. Prozac)
■ MonoAmine Oxidase Inhibitors / MAOI (e.g. Nardil)
○ Anxiolytics (anti-anxiety medication)
■ Benzodiazepines (e.g. Valium)
■ Non-Benzodiazepines (e.g. Buspiron)
○ Mood stabilizers
■ Lithium
○ Hypnotics
● Other relevant drug classes
○ Anti-epileptics
■ Benzodiazepines, Clonazepam, Clorazepaat
○ Stimulants
■ Cocaine, Amphetamine, Methylphenidate, Caffeine, Nicotine
○ Narcotic pain killers
■ Opioids, Morphine, Codeine, Heroin
○ Central Nervous System suppressors
○ Psychedelics & Hallucinogens
■ LSD, Marijuana, Hashish, Mescaline, Psylocybin
Administration
● Includes four important stages
1. Absorption → from site of administration to blood
2. Distribution → throughout body
3. Metabolism → conversion by body
4. Excretion → elimination from body
Absorption
● Oral
● Rectal
● Topical
○ Skin
○ Oral mucosa → sublingual, buccal
● Parenteral
○ Intravenous
○ Intramuscular
, ○ Subcutaneously
● Inhalation
Distribution
● In blood (albumin)
● Extracellular → blood plasma
● Intracellular → water in body cells
● Speed of distribution depends on lipid solubility (= the ability to dissolve through the
lipid (fat) portion of a membrane)
○ Through membranes → passive diffusion following concentration gradient
○ Higher lipid solubility → faster distribution
Important processes
● Pharmacokinetics
○ How does the body process the medication?
● Pharmacodynamics
○ How does the body respond to the medication?
Pharmacokinetics
● Change over time in terms of serum concentration of medication and metabolites
● Entire blood circulation takes +/- 1 minute
● Capillaries (= haarvaten)
○ 10 billion
○ 200 m^2
Pharmacodynamics
● Time - Concentration relation
○ To (Time o)
■ First: Large peak ik medication concentration in plasma → medication
administered
■ Then: Large decrease medication concentration in plasma → leaves
bloodstream, enters body
● Half-lives → Time for the medication to halve in concentration
○ Distribution half-live
■ Alpha phase
■ To → 50%
■ First half-live = important → onset action
○ Elimination half-live
■ Beta phase
■ Degradation (liver) and 50% excretion (kidneys)
■ Sixth half-live = important → eliminated / Stop action
○ Distribution half-live → How fast absorbed?
○ Elimination half-live → How fast eliminated?
Neurotransmission - Anatomy
Neurons
● Global structure
, ○ Cell body = soma
○ Dendrites
■ With spines
■ Without spines
○ Axon
● Synapses (anterograde)
○ Axodendritic → receiver = dendritic spine
○ Axosomatic → receiver = soma
○ Axoaxonic → receiver = axon
Synapses
● Axonal ending forms synapse with postsynaptic neuron
○ Mitochondria provide energy
○ Neurotransmitter in vesicle
○ Receptors both sides of synaptic cleft
Special Neurons
● Pyramidal
○ Triangular cell body
○ Apical dendrite
○ One axon
○ Stimulating
○ Prefrontal cortex, hippocampus, entorinal cortex → EF, memory
● Chandelier
○ Axoaxonic
○ Inhibitory → inhibits/stops pyramid cells
○ Cortex
● Spiny
○ Dendrites shaped like spikes
○ Long axons
○ Striatum
● Purkinje
○ Dendrites shaped like a tree
○ One axon
○ Cerebellum
● Interneurons
○ Mainly brain and spinal cord (= CNS)
○ Provide neural circuit
○ Sensory ←→ motor
○ Local
■ Short axons
■ Analyze small pieces of information
○ Relay
■ Long axons
■ Over brain regions
● Basket
○ Dendrites shaped like a basket
○ Inhibitory interneuron
Definition & Classification
Definition
● Pharmacology → Knowledge about drugs or medicines; The art of preparing
medication
○ The science that deals with studying the reciprocal actions, or interactions,
between pharmacological substances and psychological processes
● Pharmacon → medicine / pharmaceutical product
Definition ‘Drug’
● English → Pharmacologically active substance
○ Medication or other substance with a physiological effect
○ Psychoactive substance for abuse, narcotic or stimulating
● Dutch → Psychoactive substance for abuse
○ Drug / stimulant with a more or less ‘drugging’ effect, which can lead to
dependence (addiction)
Classification
● Possible grounds include
○ Chemical structure
■ Interesting, but the same structure can have different effects
○ Working mechanism
■ Ideal, bit working mechanism
○ Behavioral effects
■ Easiest, linked to discord being treated
● However, there are other classifications
○
ATC NbN
Anatomical Therapeutic Chemical Neuroscience-based Nomenclature
Behavioral effects → indication Working mechanism →
based pharmacologically driven
Older (1976) Newer (2018)
Gold standard (WHO) Taskforce 5 organizations
Cons: Cons:
● Use for other than primary ● New, not acknowledged by
disorder WHO / scientific community
● Stigma/patient adherence ● Lack of sufficient evidence
● Differences in nomenclature ATC versus NbN
○
ATC NbN
Antipsychotics Serotonin/Dopamine antagonists
, with antipsychotic actions
Antidepressants Monoamine reuptake inhibitors with
antidepressant action
ATC
● Psychotropic drug main classes
○ Antipsychotics
■ Conventional antipsychotic (e.g. Haloperidol)
■ Atypical (e.g. Risperidone)
○ Antidepressants
■ Tricyclic (e.g. Imipramine)
■ Selective Serotonin Reuptake Inhibitors / SSRI (e.g. Prozac)
■ MonoAmine Oxidase Inhibitors / MAOI (e.g. Nardil)
○ Anxiolytics (anti-anxiety medication)
■ Benzodiazepines (e.g. Valium)
■ Non-Benzodiazepines (e.g. Buspiron)
○ Mood stabilizers
■ Lithium
○ Hypnotics
● Other relevant drug classes
○ Anti-epileptics
■ Benzodiazepines, Clonazepam, Clorazepaat
○ Stimulants
■ Cocaine, Amphetamine, Methylphenidate, Caffeine, Nicotine
○ Narcotic pain killers
■ Opioids, Morphine, Codeine, Heroin
○ Central Nervous System suppressors
○ Psychedelics & Hallucinogens
■ LSD, Marijuana, Hashish, Mescaline, Psylocybin
Administration
● Includes four important stages
1. Absorption → from site of administration to blood
2. Distribution → throughout body
3. Metabolism → conversion by body
4. Excretion → elimination from body
Absorption
● Oral
● Rectal
● Topical
○ Skin
○ Oral mucosa → sublingual, buccal
● Parenteral
○ Intravenous
○ Intramuscular
, ○ Subcutaneously
● Inhalation
Distribution
● In blood (albumin)
● Extracellular → blood plasma
● Intracellular → water in body cells
● Speed of distribution depends on lipid solubility (= the ability to dissolve through the
lipid (fat) portion of a membrane)
○ Through membranes → passive diffusion following concentration gradient
○ Higher lipid solubility → faster distribution
Important processes
● Pharmacokinetics
○ How does the body process the medication?
● Pharmacodynamics
○ How does the body respond to the medication?
Pharmacokinetics
● Change over time in terms of serum concentration of medication and metabolites
● Entire blood circulation takes +/- 1 minute
● Capillaries (= haarvaten)
○ 10 billion
○ 200 m^2
Pharmacodynamics
● Time - Concentration relation
○ To (Time o)
■ First: Large peak ik medication concentration in plasma → medication
administered
■ Then: Large decrease medication concentration in plasma → leaves
bloodstream, enters body
● Half-lives → Time for the medication to halve in concentration
○ Distribution half-live
■ Alpha phase
■ To → 50%
■ First half-live = important → onset action
○ Elimination half-live
■ Beta phase
■ Degradation (liver) and 50% excretion (kidneys)
■ Sixth half-live = important → eliminated / Stop action
○ Distribution half-live → How fast absorbed?
○ Elimination half-live → How fast eliminated?
Neurotransmission - Anatomy
Neurons
● Global structure
, ○ Cell body = soma
○ Dendrites
■ With spines
■ Without spines
○ Axon
● Synapses (anterograde)
○ Axodendritic → receiver = dendritic spine
○ Axosomatic → receiver = soma
○ Axoaxonic → receiver = axon
Synapses
● Axonal ending forms synapse with postsynaptic neuron
○ Mitochondria provide energy
○ Neurotransmitter in vesicle
○ Receptors both sides of synaptic cleft
Special Neurons
● Pyramidal
○ Triangular cell body
○ Apical dendrite
○ One axon
○ Stimulating
○ Prefrontal cortex, hippocampus, entorinal cortex → EF, memory
● Chandelier
○ Axoaxonic
○ Inhibitory → inhibits/stops pyramid cells
○ Cortex
● Spiny
○ Dendrites shaped like spikes
○ Long axons
○ Striatum
● Purkinje
○ Dendrites shaped like a tree
○ One axon
○ Cerebellum
● Interneurons
○ Mainly brain and spinal cord (= CNS)
○ Provide neural circuit
○ Sensory ←→ motor
○ Local
■ Short axons
■ Analyze small pieces of information
○ Relay
■ Long axons
■ Over brain regions
● Basket
○ Dendrites shaped like a basket
○ Inhibitory interneuron
